ABSTRACT The present study aims to investigate the cytotoxic effect of the major aflatoxins (B1, B2, G2 and G2) and also aflatoxin combination, using a simple, rapid and cheap cytotoxicity test like MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay in three in vitro models (human umbilical vein endothelial cells [HUVEC], human lung fibroblasts [HFL] and A2780 cell line) and to extrapolate the data to in vivo situation using a prediction model. A difference in cell sensitivity has been observed for B1 and B1 + B2, in the following order A2789 > HFL > HUVEC, while for B2, G1, G2, Mix (B1 + B2 + G1 + G2) the order was HFL > A2789 > HUVEC when comparing the IC50 (half maximal inhibitory concentration) values. We confirm that in vitro cytotoxicity test MTT assay is able to predict in vivo toxicity, at least for aflatoxins using the prediction model. The values of LD50 (lethal dose 50%) calculated from experiments are different for each cell line. This fact may indicate that ...
BioAssay record AID 64221 submitted by ChEMBL: In vitro minimum inhibition concentration against Escherichia coli D21f2, LPS mutant; Range is from 25-50.
Cadmium (Cd) is harmful for humans and animals, especially for the reproductive system. However, the mechanism of its toxicity has not been elucidated, and how to alleviate its toxicity is very important. This study aimed to explore the role and mechanism of action of sulforaphane (SFN) in protecting mouse Leydigs (TM3) cells from cadmium (Cd)-induced damage. The half-maximal inhibitory concentration (IC50) of Cd and the safe doses of SFN were determined using a methyl thiazolyl tetrazolium (MTT) assay. The testosterone secretion from TM3 cells was measured using the enzyme-linked immunosorbent assay. The intracellular oxidative stress was evaluated using corresponding kits. The cell apoptosis was detected using flow cytometry. The mRNA expression of genes associated with NF-E2-related factor 2 (Nrf2)/antioxidant response element (ARE) signaling was detected using reverse transcriptionâ »polymerase chain reaction, including Nrf2, heme oxygenase I (HO-1), glutathione peroxidase (GSH-Px), ...
In this study we (i) calculated half-maximal inhibitory concentrations (IC.sub.50) by motility tests against O. felineus adults and newly excysted metacercarie ...
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A8326 AZD-5438 AZD5438 is a potent small molecule inhibitor of cyclin-dependent kinase (CDK) 1, 2 and 9 with half maximal inhibitory concentration IC50 of 16 nmol/L, 6 nmol/L and 20 nmol/L respectively. AZD5438 has also been found to potently inhibit the human cyclin E/CDK2 complex, the cyclin B1/CDK1 complex and the cyclin A/CDK2 complex with IC50 of 0.006 μM, 0.016 μM and 0.045 μM respectively. In previous studies, AZD5438 has exhibited significant anti-proliferative activity in a few human tumor cell lines with IC50 ranging from 0.2 μmol/L to 1.7 μmol/L, in which the phosphorylation of a few proteins, including CDK substrates pRb, nucleolin, protein phosphatase 1a and RNA polymerase II COOH-terminal domain, and cell cycling at G2-M, S and G1 phases were inhibited. ...
Curcumin (1) and ten derivatives (2-11) were synthesized and evaluated as cytotoxic and antioxidant agents. The results of primary screening by Sulforhodamine B assay against five human cancer cell lines (U-251 MG, glioblastoma; PC-3, human prostatic; HCT-15, human colorectal; K562, human chronic myelogenous leukemia; and SKLU-1, non-small cell lung cancer) allowed us to calculate the half maximal inhibitory concentration (IC50) values for the more active compounds against HCT-15 and K562 cell lines. Compounds 2 and 10 were the most active against both cell lines and were more active than curcumin itself. Thiobarbituric acid reactive substances (TBARS) assay showed that 7 has potent activity; even stronger than curcumin, α-tocopherol, and quercetin.
BioAssay record AID 594378 submitted by ChEMBL: Cell cycle arrest in human K562 cells assessed as accumulation at G0-G1 phase at IC100 after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 43.40%).
Dengue is a major mosquito-borne disease currently with no effective antiviral or vaccine available. Effort to find antivirals for it has focused on bioflavonoids, a plant-derived polyphenolic compounds with many potential health benefits. In the present study, antiviral activity of four types of bioflavonoid against dengue virus type -2 (DENV-2) in Vero cell was evaluated. Anti-dengue activity of these compounds was determined at different stages of DENV-2 infection and replication cycle. DENV replication was measured by Foci Forming Unit Reduction Assay (FFURA) and quantitative RT-PCR. Selectivity Index value (SI) was determined as the ratio of cytotoxic concentration 50 (CC50) to inhibitory concentration 50 (IC50) for each compound. The half maximal inhibitory concentration (IC50) of quercetin against dengue virus was 35.7 μg mL-1 when it was used after virus adsorption to the cells. The IC50 decreased to 28.9 μg mL-1 when the cells were treated continuously for 5 h before virus infection and up to
The study was carried out to evaluate the antioxidant activity and α-amylase activity inhibitory potential of Sarotherodon galillaeus muscle protein hydrolysates. Sarotherodon galillaeus muscle protein isolate was hydrolysed with three digestive proteases namely trypsin, chymotrypsin and pepsin. Degree of hydrolysis was determined. The antioxidative potential of the hydrolysates was investigated using DPPH radical scavenging, ferric reducing power, hydrogen peroxide scavenging and metal chelating activity. The ability of the hydrolysates to inhibit the activity of sugar-hydrolysing enzyme was also evaluated. Highest degree of hydrolysis was obtained with pepsin (55.86%) followed by trypsin (47.11%) and chymotrypsin (42.36%) after 6 hrs of hydrolysis. The half maximal inhibitory concentration (IC50) of hydrolysates produced by trypsin, chymotrypsin and pepsin for DPPH radical scavenging activity were 1.26 ± 0.95, 0.98 ± 0.07 and 1.18 ± 0.34 mg/ml respectively. Trypsin-produced hydrolysates ...
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity. - Mechanism of Action & Protocol.
InChI=1S/C28H30N6OS/c1-20-5-10-24(16-25(20)31-28-32-26(19-36-28)23-4-3-11-29-17-23)30-27(35)22-8-6-21(7-9-22)18-34-14-12-33(2)13-15-34/h3-11,16-17,19H,12-15,18H2,1-2H3,(H,30,35)(H,31,32) ...
The Quantitative Structure-Activity Relationship of a series of novel Thiazoline derivatives with anticancer activity has been studied by using the density functional theory by B3LYP/ 6-31G. Descriptors of quantum mechanics of 21 thiazoline derivatives with known activity were obtained. Multiple linear regressions were employed to model the relationships between molecular descriptors and biological activity of molecules using stepwise method. The most model shows not only significant statistical quality, but also predictive ability, with the square of adjusted correlation coefficient (R2=0.945) and standard error (SE=0.586). We find that the anticancer activity expressed that as half maximal inhibitory concentration (IC50), closely relates to the highest occupied molecular orbital, dipole moment, softness, hardness, ionization energy, electron affinity. Accordingly can be offered a quantitative model, and interpret the activity of the compounds relying on the multivariate statistical analysis. This
Masitinib is a selective tyrosine kinase inhibitor with potent activity against the juxta membrane domain of c-Kit. Masitinib is also thought to promote survival via modulation of immunostimulation-mediated anticancer effects and modulation of the tumor microenvironment. The objective of this study was to evaluate the efficacy and safety of masitinib with respect to dacarbazine in the treatment of non-resectable or metastatic stage 3 or stage 4 melanoma carrying a mutation in the juxta membrane domain of c-Kit. Following a protocol amendment, the dacarbarzine treatment group was closed and recruitment restricted to masitinib treatment of chemo-naïve (first-line) patients ...
Sapacitabine cancer drug molecule (nucleoside analogue). Stylized skeletal formula (chemical structure): Atoms are shown as color-coded circles: hydrogen (hidden), carbon (grey), nitrogen (blue), oxygen (red). - Stock Image F018/3177
AC220 (Quizartinib) is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56 ± 0.3 nM and >10 mM for MC4-11 and A375, respectively.
Sigma-Aldrich offers abstracts and full-text articles by [Marta Leirós, Eva Alonso, Mostafa E Rateb, Wael E Houssen, Rainer Ebel, Marcel Jaspars, Amparo Alfonso, Luis M Botana].
【市場調査レポート】タッチパネル用コントローラーICの世界市場2017-2021 | 発行日:2017年4月12日 | 商品コード:IRTNTR12538 | 発行/調査会社:Technavio | Global Touch Controller IC Market 2017-2021 | キーワード:グローバル、電子、タッチパネルコントローラーIC、タッチスクリーン [市場規模/動向/予測など世界の産業分析レポート販売のマーケットレポート.jp]
Masitinib is a selective, oral tyrosine kinase inhibitor with neuroprotective capability demonstrated via numerous preclinical studies. Two of masitinibs main cellular targets are the mast cell and microglia cell. It is well-established that mast cells play a prominent role in neuroinflammatory processes. Microglia, resident immune cells of the central nervous system (CNS), also constitute an important source of neuroinflammatory mediators and may have fundamental roles in numerous neurodegenerative disorders. The development of masitinib in ALS is therefore based on the pharmacological action of masitinib in microglia cells and mast cells, thereby slowing microglial-related disease progression, reducing neuro-inflammation, and modulating the neuronal microenvironment in both central and peripheral nervous systems. This is a multicenter, double-blind, randomized, placebo-controlled, parallel-group (two ascending dose titrations of masitinib and matching placebo), comparative study of oral ...
Class I PI3Ks can form an allosteric or "specificity" pocket (adjacent to the adenine pocket) only in the presence of propeller-like inhibitors (29). The half-maximal inhibitory concentrations (IC50s) for the propeller-like PI3K inhibitors (e.g., PIK-39) (fig. S9) are generally much worse for Vps34 than other PI3Ks. This is probably due to increased rigidity of the Vps34 pocket arising from a bulky residue substituted in the P loop (Phe612-Hs, Phe673-Dm) that packs against the aromatic hinge residue unique to Vps34 (Phe684-Hs, Tyr746-Dm). These differences effectively close off a corner of the adenine-binding pocket, giving it a more constrained appearance.. Currently there is no high-affinity, specific inhibitor of Vps34. We determined the structure of a complex of Vps34 with 3-methyladenine (3-MA) (Fig. 4, B and C), which is often used as a specific inhibitor of autophagy. We also determined the structures of Vps34 in complexes with three multi-targeted inhibitors: (i) PIK-90, (ii) PIK-93, ...
Oxidative damage to the vascular endothelium may play an important role in the pathogenesis of atherosclerosis and aging, and may account in part for reduced vascular prostacyclin (PGI2) synthesis associated with both conditions. Using H2O2 to induce injury, we investigated the effects of oxidative damage on PGI2 synthesis in cultured endothelial cells (EC). Preincubation of EC with H2O2 produced a dose-dependent inhibition (inhibitory concentration [IC50] = 35 microM) of PGI2 formation from arachidonate. The maximum dose-related effect occurred within 1 min after exposure although appreciable H2O2 remained after 30 min (30% of original). In addition, H2O2 produced both a time- and dose-dependent injury leading to cell disruption, lactate dehydrogenase release, and 51Cr release from prelabeled cells. However, in dramatic contrast to H2O2 effects on PGI2 synthesis, loss of cellular integrity required doses in excess of 0.5 mM and incubation times in excess of 1 h. The superoxide-generating ...
Silibinin has limited in vitro antiproliferative activity in 4T1 cells 4T1-luc tumor cells were seeded in triplicates in 96-well plates at a concentration of 10
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ProQinase offers custom-tailored development of cancer related cellular assays. The service portfolio comprises stable cell line generation and phenotypic assays
It was initially hard for me to know how to get started and contribute in this project and I think there are others how feel the same way, so Im describing here how I approached it. Its not the only way or even the correct way but just an experience Ive had so far.. ...
Each year the government adds an addional amount of money to our school budget for children who are eligible for free school meals, for Children in Care and for those who are members of service families. This is know as the Pupil Premium.. With the introduction of Universal Infant Free School Meals, parents who are on certain benefits, such as Income Support, are still encouraged to apply for Free School Meals, to enable their children to qualify for the Pupil Premium.. At Millbrook School, this money is particularly used to in the staffing line of the budget to enable more support to be given to the qualifying children, whether this be in general or specific programmes of study. A more detailed report on the expenditure can be found below along with our policy. ...
TY - JOUR. T1 - A conformational and structure-activity relationship study of cytotoxic 3,5-bis(arylidene)-4-piperidones and related N-acryloyl analogues. AU - Dimmock, J. R.. AU - Padmanilayam, M. P.. AU - Puthucode, R. N.. AU - Nazarali, A. J.. AU - Motaganahalli, N. L.. AU - Zello, G. A.. AU - Quail, J. W.. AU - Oloo, E. O.. AU - Kraatz, H. B.. AU - Prisciak, J. S.. AU - Allen, T. M.. AU - Santos, C. L.. AU - Balzarini, J.. AU - De Clercq, E.. AU - Manavathu, E. K.. PY - 2001/2/15. Y1 - 2001/2/15. N2 - A series of 3,5-bis(arylidene)-4-piperidones 1 and related N-acryloyl analogues 2 were prepared as candidate cytotoxic agents with a view to discerning those structural features which contributed to bioactivity. A number of the compounds were markedly cytotoxic toward murine P388 and L1210 leukemic cells and also to human Molt 4/C8 and CEM neoplasms. Approximately 40% of the IC50 values generated were lower than the figures obtained for melphalan. In virtually all cases, the N-acyl compounds ...
As expected, the soluble CD4 positive control inhibited CXCR4 (50% inhibitory concentration [IC(50)] 3.7 μg/ml) and CCR5 (IC(50) 0.03 μg/ml) tropic HIV-1 infectivity. Free melittin doses ,2 μM were not cytotoxic and were highly effective in reducing HIV-1 infectivity for both CXCR4 and CCR5 strains in TZM-bl reporter cells, while VK2 vaginal cell viability was adversely affected at all free melittin doses tested. However, VK2 cell viability was not affected at any dose of melittin-loaded nanoparticles. Melittin nanoparticles safely and significantly decreased CXCR4 (IC(50) 2.4 μM and IC(90) 6.9 μM) and CCR5 (IC(50) 3.6 μM and IC(90) 11.4 μM) strain infectivity of TZM-bl reporter cells. Furthermore, melittin nanoparticles captured more HIV-1 than blank nanoparticles.. ...
Exploration of Scaffolds from Natural Products with Antiplasmodial Activities, Currently Registered Antimalarial Drugs and Public Malarial Screen Data. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
The present invention relates to a mast cell inhibitor, a pharmaceutical composition and a method for the treatment of patients afflicted with Parkinsons disease, wherein said patients are treated with a tyrosine kinase inhibitor or mast cell inhibitor, in particular masitinib, or a compound selected from imatinib, cromolyn sodium, midostaurin, BLU-285, bosutinib, ibrutinib, LAS189386, DP-2618, fostamatinib, dasatinib, sunitinib, axitinib, pazopanib, and toceranib or a pharmaceutically acceptable salt or solvate thereof, optionally in combination with at least one pharmaceutically active ingredient.
Novel anti-HIV-1 agents derived from betulinic acid have been greatly concerned. 3D-QSAR and molecular docking studies were applied to rationalize the structural requirements responsible for the anti-HIV activity of these compounds. The CoMFA and CoMSIA models resulted from 28 molecules gave rcv² values of 0.599 and 0
Laurie Arliss, professor of speech communication, has worked with the Exploratory Program for more than a dozen years and has taught at IC since 1984. Her...
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e-Dentico - dwumiesięcznik stomatologa praktyka, polsko-angielski poradnik stomatologiczny. MNiSW: 5 pkt, IC: 5,5 pkt., punkty edukacyjne: 30 pkt.
Urtica dioica, Taraxacum officinale, Calea integrifolia and Caesalpinia pulcherrima are widely used all over the world for treatment of different illnesses. In Mexico, these plants are traditionally used to alleviate or counteract rheumatism and inflammatory muscle diseases. In the present study we evaluated the activity of aqueous and methanolic extracts of these four plants, on the replication of dengue virus serotype 2 (DENV2). Extraction process was carried out in a Soxtherm® system at 60, 85 and 120 °C; a chemical fractionation in silica gel chromatography was performed and compounds present in the active fractions were identified by HPLC-DAD-ESI/MSn. The cytotoxic concentration and the inhibitory effect of extracts or fractions on the DENV2 replication were analyzed in the BHK-21 cell line (plaque forming assay). The half maximal inhibitory concentration (IC50) and the selectivity index (SI) were calculated for the extracts and fractions. The methanolic extracts at 60 °C of T. officinale and U.
Aqueous extract of Rabdosia rubescens leaves: forming nanoparticles, targeting P-selectin, and inhibiting thrombosis Yuji Wang,1 Jingcheng Tang,1 Haimei Zhu,1 Xueyun Jiang,1 Jiawang Liu,1 Wenyun Xu,1 Haiping Ma,1 Qiqi Feng,1 Jianhui Wu,1 Ming Zhao,1,2 Shiqi Peng1 1Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, Peoples Republic of China; 2Faculty of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung, Taiwan Abstract: The hot water extract of Rabdosia rubescens was traditionally used as an antithrombotic medicine. To explore its antithrombotic utility and mechanism, we carried out a series of in vitro and in vivo assays in this study. In vitro platelet aggregation assay showed that the half maximal inhibitory concentration values of aqueous
Cyclopeptide alkaloids are polyamidic, macrocyclic compounds, containing a 13-, 14-, or 15-membered ring. The ring system consists of a hydroxystyrylamine moiety, an amino acid, and a β-hydroxy amino acid; attached to the ring is a side chain, comprised of one or two more amino acid moieties. In vitro antiplasmodial activity was shown before for several compounds belonging to this class, and in this paper the antiplasmodial and cytotoxic activities of ten more cyclopeptide alkaloids are reported. Combining these results and the IC50 values that were reported by our group previously, a library consisting of 19 cyclopeptide alkaloids was created. A qualitative SAR (structure-activity relationship) study indicated that a 13-membered macrocyclic ring is preferable over a 14-membered one. Furthermore, the presence of a β-hydroxy proline moiety could correlate with higher antiplasmodial activity, and methoxylation (or, to a lesser extent, hydroxylation) of the styrylamine moiety could be important for
SR9009, also known as Stenabolic, is a research drug that was developed by professor Thomas Burris of the Scripps Research Institute as an agonist of Rev-ErbA (i.e., increases the constitutive repression of genes regulated by Rev-ErbA)[1] with a half-maximum inhibitory concentration (IC50) = 670 nM for Rev-ErbAα and IC50 = 800 nM for Rev-ErbAβ.[2] Activation of Rev-ErbA-α by SR9009 in mice increases exercise capacity by increasing mitochondria counts in skeletal muscle.[3] Abuse of SR9009 has been reported within the bodybuilding community, resulting in SR9009 being placed on the World Anti-Doping Agency list of prohibited drugs. SR9009 and the related SR9011 drug are described as "Hormone and Metabolic Modulators".[4][5] ...
Paris, France, Nov. 12, 2014-- AB Science SA, a pharmaceutical company specialized in research, development and marketing of protein kinase inhibitors, announces that the external Data and Safety Monitoring Board has recommended the continuation of its phase 2 study of masitinib in advanced hepatocellular carcinoma based upon review of the latest safety and...
Determining the antiplasmodial activity of candidate antimalarial drugs in vitro identifies new therapies for drug‐resistant malaria
The goal of this clinical research study is to compare the ability of decitabine given alone versus the combination of sapacitabine and decitabine to control AML. The safety of the drug combination will also be studied.
The investigational tyrosine kinase inhibitor quizartinib is extremely promising as a monotherapy for patients with |em|FLT3-ITD–|/em|positive relapsed acute myeloid leukemia.
The industry is making strides in the development of additional therapeutic options for the treatment of MS, including several new medications in the pipeline. An agent that was granted breakthrough therapy designation, fast track designation, and priority review by the FDA, Ocrevus (ocrelizumab), was approved on March 28, 2017 for the treatment of relapsing forms of MS and PPMS. Ocrevus is the first medication to be approved for the treatment of PPMS. Another advancement in treatment includes agents called sphingosine-1-phosphate receptor immunomodulators (ponesimod, siponimod, ozanimod), which are all in phase 3 trials for the treatment of MS. One of these drugs, siponimod, is being studied for the treatment of SPMS; there is currently only one drug that is specifically approved for SPMS, mitoxantrone. Another agent in a phase 3 trial is masitinib. Masitinib is a tyrosine kinase inhibitor that is being studied for PPMS and relapse-free SPMS. If approved, these agents could offer additional ...
Eyebrows have been raised after Astellas Pharma decided to end its collaboration with Ambit Biosciences Corp to develop the latters acute myeloid leukaemia treatment quizartinib. - News - PharmaTimes
1EET: Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
Results: The amount of extract required to inhibit HIV-I replication by 50 % (IC50) in MT 4 cell culture, and the dose that reduced the viability of uninfected cells by 50 % (CC50) were observed. The ratio of IC50 /CC50 was calculated as selectivity index (SI). One herbal water extract in the concentration of 2000 ug/ml to16 ug/ml was found highly bioactive against HIV in vitro. The plant is abundantly available in Pakistan, whereas, the other sets of extracts obtained from different plant sources, have shown as good, moderate and mild anti-HIV activity (in vitro) in the concentration of 200 ug/ml to 1.6 ug/ml ...
... : Antiproliferative activity of carboxamides 2a-c, imatinib and doxorubicin (positive control) against HL-60, SF-295, HCT-8 tumor cell lines and their cytotoxic activity against primary culture of human lymphocytes ...
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The invention provides novel bicyclic azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
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The Food and Drug Administration (FDA) has warned against the use of Bentonite Me Baby by Alikay Naturals due to a potential lead poisoning risk.
Mahr, měřicí technika. Výrobce kompletního sortimentu měřicí techniky pro výrobu. Dodavatel automobilového průmyslu. Systémy a ruční měřicí prostředky. Optická měřicí technika, kuličková vedení, odstředivá čerpadla.\
Diarylquinolines, synthesis pathways and quantitative structure-activity relationship studies leading to the discovery of TMC207 ...
1918 The antineoplastic activity of a plant powder used in African traditional medicine for treating cancer was investigated by analyzing the activity of various extracts in vitro. The most active, aqueous extract was subsequently subjected to a detailed investigation in a panel of 21 cell lines, showing a median IC50 of 27 mg raw powder /ml medium. The sensitivity of the cell lines varied from 1.7 mg/ml in MCF7 breast cancer cells to 170 mg/ml in AR230 chronic-myeloid leukemia cells. The in vivo antitumor activity was determined in the CC531 rat colorectal liver metastasis model. Treatment started one week after implanting 4x106 tumor cells intra-portally and was administered every second day for three weeks. Significant anticancer activity was found following administration of equitoxic total doses of 1000 (po) and 50 (ip) mg raw powder/kg, indicating reduced activity following intestinal absorption. By sequencing the mitochondrial gene for the large subunit of the ribulose bis-phosphate ...
The CH2Cl2-MeOH (1:1) extract of the aerial parts of Sphaeranthus bullatus, an annual herb native to tropical East Africa, showed activity against chloroquine sensitive D6 (IC50 9.7 μg/mL) and chloroquine resistant W2 (IC50 15.0 μg/mL) strains of Plasmodium falciparum. Seventeen secondary metabolites were isolated from the extract through conventional chromatographic techniques and identified using various spectroscopic methods. The compounds were evaluated for their in vitro antiplasmodial, antileishmanial and anticancer activities revealing activity of four carvotacetone derivatives, namely 3-acetoxy-7-hydroxy-5-tigloyloxycarvotacetone (1), 3,7-dihydroxy-5-tigloyloxycarvotacetone (2), 3-acetoxy-5,7-dihydroxycarvotacetone (3) and 3,5,7- ...
Selective cytotoxicity of oxysterols through structural modulation on rings A and B. Synthesis, in vitro evaluation, and SAR.: Chemically diverse oxysterols wer
Small Molecule Inhibitors of Retinoic Acid 4-Hydroxylase (CYP26): Synthesis and Biological Evaluation of Imidazole Methyl 3-(4-(aryl-2-ylamino)phenyl) ...
What is (s) product (s) / service (s) proposed (s)?. Acobiom is currently under clinical validation of several diagnosis in the treatment of cancer of the pancreas (338,000 new cases per year worldwide).. Diagnostics companions in cancer of the pancreas are able to predict a higher survival of 12 to 15 months for patients with this pathology.. The first sales expected for 2018 are:. -The companion diagnostic associated with Gemcitabine (generic of the Gemzar), with a turnover expected after 5 years of marketing valued at 17 million € / year;. -Associated with the AB science Masitinib, companion Diagnostics with a turnover expected after 5 years of marketing valued at 32 million € / year;. -The diagnosis of cancer of the pancreas with a turnover expected after 5 years of marketing estimated at 6 million € / year.. For Alzheimers disease (7.7 million new cases annually worldwide), the first sales expected for 2020 are:. -A companion associated with Masitinib, diagnostic with a turnover ...
Selleck provides signaling inhibitors, modulators and compound libraries with terrific validation, customer reviews, product citations, tech support and prompt delivery.
An Open Source project like the OLPC thrives on ideas. However, we need to have some order to the ideas because different groups will be working on different aspects of the project. There are already many idea pages in this Wiki and most of them are referenced in one of the following pages. Learn about "Categories" to link up pages that mention or partially deal with the same topic; its a great way to bring/find contributors with a similar interest together. Other interesting Categories: ...
From a Western medical perspective, certain veggies rank high when it comes to serious detox, since they contain potent compounds that can stop cell damage.
New page: Ive been watching OLPC for over two years now. I recently subscribed to the OLPC News RSS feed. Current Projects: * Maintaing this wiki (See TODO) * Testing Sucrose) ...
Tripos Sybyl-X 2.1.1 [center] Tripos Sybyl-X 2.1.1 | 851/616/835 MB Whether you need to find new lead candidates, optimize lead series, or perform other re...
TY - JOUR. T1 - Protective effect of resveratrol against caspase 3 activation in primary mouse fibroblasts. AU - Ulakcsai, Zsófia. AU - Bagaméry, Fruzsina. AU - Vincze, István. AU - Szöko, Éva. AU - Tábi, Tamás. PY - 2015/1/1. Y1 - 2015/1/1. N2 - Aim: To study the effect of resveratrol on survival and caspase 3 activation in non-transformed cells after serum deprivation. Methods: Apoptosis was induced by serum deprivation in primary mouse embryonic fibroblasts. Caspase 3 activation and lactate dehydrogenase release were assayed as cell viability measure by using their fluorogenic substrates. The involvement of PI3K, ERK, JNK, p38, and SIRT1 signaling pathways was also examined. Results: Serum deprivation of primary fibroblasts induced significant activation of caspase 3 within 3 hours and reduced cell viability after 24 hours. Resveratrol dose-dependently prevented caspase activation and improved cell viability with 50% inhibitory concentration (IC50) = 66.3 ± 13.81 μM. It also reduced ...
Plasmodium falciparum, the most deadly agent of malaria, displays a wide variety of resistance mechanisms in the field. The ability of antimalarial compounds in development to overcome these must therefore be carefully evaluated to ensure uncompromised activity against real-life parasites. We report here on the selection and phenotypic as well as genotypic characterization of a panel of sensitive and multidrug-resistant P. falciparum strains that can be used to optimally identify and deconvolute the cross-resistance signals from an extended panel of investigational antimalarials. As a case study, the effectiveness of the selected panel of strains was demonstrated using the 1,2,4-oxadiazole series, a newly identified antimalarial series of compounds with in vitro activity against P. falciparum at nanomolar concentrations. This series of compounds was to be found inactive against several multidrug-resistant strains, and the deconvolution of this signal implicated pfcrt, the genetic determinant of ...
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Neuroblastoma is the most deadly extra-cranial solid childhood tumor. Despite advanced therapies, over 60% of high-risk NB patients have aggressive tumors spreading to bone and bone marrow and die of metastasis-related disease. IL-6 promotes the growth and survival of metastatic NB cells via activation of STAT3 in the BM and is an independent poor-prognosis marker in tumors from high-risk NB patients. This suggests that blockade of IL6/JAK/STAT3 signaling may represent a promising therapeutic strategy. We tested the anti-tumor effect of inhibition IL6/JAK/STAT3 pathway by the JAK1/2 inhibitor AZD1480, which is in Phase II clinical trials in adult tumors, in three highly metastatic pediatric tumor types (Neuroblastoma, Ewing sarcoma and rhabdomyosarcoma). AZD1480 (0.5uM) significantly blocked IL-6-induced P-STAT3-Tyr705 in all tumor types tested. AZD1480 decreased cell viability in the 6 NB, 5 RMS and 2 EWS cell lines tested (median IC50 1.17uM, ranging from 0.42-5.1uM). AZD1480 induced cell ...
Total synthesis and structure-activity relationship studies of cyclic depsipeptide YM-254890, as selective inhibitors of Gq proteins
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提供693种凋亡相关化合物集合,靶向作用于Bcl-2,Caspase,p53,TNF-alpha,Mdm2,survin等,可用于高通量筛选和高内涵筛选。
You are viewing an interactive 3D depiction of the molecule (2R)-2-amino-5-pyrimidin-2-yl-pentanoic acid (C9H13N3O2) from the PQR.
Validation of Cell-based Assays in the GLP Setting provides the professional with an invaluable reference source, featuring key guidelines.
Aim of the Journal is to provide rigorous training in the fundamentals and practice of pathology and epidemiology in molecular field
Neuren Pharmaceuticals is developing trofinetide (NNZ 2566), a proprietary small molecule analogue of Neurens initial lead compound, glycine-proline-glutamate
Elektronische Hochschulschriften; Titel: Development of novel indolyl-derived biologically active compounds, Verfasser: El-Sayed, Mardia El-Dessoky Teleb, 2013 ; Halle, Saale : Universitäts- und Landesbibliothek Sachsen-Anhalt, 2013
श्रीयुत रॉय यांची २० लोकांची एक आयुर्विमा पॉलिसी होती .त्याच्या अवेळी मृत्यूमुळे त्यांच्या कुटुंबाने आयुर्विमा कंपनीकडे दावा केला . परंतु आयुर्विमा कंपनीने तो दावा नामंजूर केला . तेव्हा त्यांनी कोपा जिल्हा स्तरावर न्यायासाठी विनंती केली .कोपच्या निर्णयाने नाखूष होऊन त्यांनी लोकपाल ला निवेदन केले . लोकपाल ह्या प्रकरणाची सुनावणी करेल ?. ...
Study of the in Vitro Antiplasmodial, Antileishmanial and Antitrypanosomal Activities of Medicinal Plants from Saudi Arabia. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
Background Icaritin (ICT) is a prenylflavonoid derivative from Epimedium brevicornum Maxim. ICT has been shown to have neuroprotective effects. We investigate how ICT affects secretion of amyloid precursor protein (APP). Methods We exposed APP-PS1-HEK293 cells to ICT to investigate its effect on beta-site amyloid cleaving enzyme (BACE)1. Cell viability was evaluated by MTT and lactate dehydrogenase (LDH) assays. The half-maximal inhibitory concentration (IC50) of ICT for BACE1 was measured using fluorescence resonance energy transfer. Effects of ICT on the mRNA expression of APP were assessed by quantitative polymerase chain reaction, and protein expression was measured by western blotting and immunofluorescence. Results Icaritin inhibited BACE1 activity and IC50 was 5.70 ± 1.09 μM. Compared with the control group, at ICT concentrations of 5 μM and 10 μM, the viability increased and LDH leakage decreased in APP-PS1-293 cells. Also, mRNA expression of A disintegrin and metalloproteinase domain
A set of 3 beta-(4-substituted phenyl)-2 beta-heterocyclic tropanes was designed, synthesized, and characterized. We discovered that these compounds can function as bioisosteric replacements for the corresponding WIN 35,065-2 analogs which possess a 2 beta-carbomethoxy group. Several of the compounds showed high affinity and selectivity for the dopamine transporter (DAT)
Gambogic acid has a marked anti-tumor effect for gastric and colorectal cancers in vitro and in vivo. However, recent investigations on gambogic acid have focused mainly on mono-drug therapy, and its potential role in cancer therapy has not been comp
In this article, the in vivo antimalarial activity of novel naphthoquine derivatives is assessed revealing promising candidates for further research.
In this video Simon Sheard, Product Manager at Brooks Life Science Systems, tells SelectScience about the new Brooks Plate Auditor™, which has been specifically designed for the detection and classification of features unique to HTS compound libraries. The Plate Auditor uses vision technology to identify empty wells, wells with insufficient volume of liquid compound sample, wells with colored compounds and wells with compound precipitation. Simon discusses the applications of the Plate Auditor as a quality control tool in compound management and screening. Interview filmed at MipTec 2012 by SelectScience.
Design, Synthesis and Biological Evaluation of Novel 1, 2, 5-Substituted Benzimidazole Derivatives as Gastroprotective Anti-inflammatory and Analgesic Agents Abstract.
The KOMP Repository is located at the University of California Davis and Childrens Hospital Oakland Research Institute. Question? Comments? For Mice, Cells, and germplasm please contact us at [email protected], US 1-888-KOMP-MICE or International +1-530-752-KOMP, or for vectors [email protected] or +1-510-450-7917 ...
The invention relates to a process for producing a carboxamide of the formula ##STR1## which comprises reacting ##STR2## with an excess of urea in water, wherein the variables in the above formulae are as described herein.
At the end of 2012 it appeared that the series was producing diminishing returns but there remained a small number of compounds which needed to be made to complete the campaign - specifically isosters of the troublesome ester in the original GSK hit. Patrick Thompson, a collaborator from the University of Edinburgh built on Matin Deans work on the sulfonamide whilst Murray Robertson and Alice Williamson focused on synthesising further analogues of the near-neighbours, trying to find potent molecules with increased solubility. The near-neighbours were evaluated and a number of potent compounds were discovered, some with lower LogP than the first set of near-neighbour compounds. The OSM project has to date had no luck in securing donations of compounds from commercial suppliers. On considering some structurally similar active compounds from the TCAMS set, the team have also decided to synthesise a few extra compounds plus hybrids, in order to assess their biological activity. What are the ...
For obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months ...
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A reductionist model for optimizing the anticancer property of retinoids. The classical IκB-NFκB signaling cascade proceeds through the sequential phosphoryla
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