Selective inhibit inhibitor protein. Medical search. Frequent questions

Y-27632A, CAS 331752-47-7, is a cell-permeable, reversible, inhibitor of Rho kinases (K i = 140 nM for p160ROCK). (sigmaaldrich.com)
A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinases (K i = 140 nM for p160 ROCK ). (sigmaaldrich.com)
Homeodomain-interacting protein kinases (HIPKs) belong to the CMGC kinase family and are closely related to dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs). (nature.com)
Homeodomain-interacting protein kinases (HIPKs) are an evolutionarily conserved kinase family comprising the members HIPK1, HIPK2, and HIPK3 in vertebrates, and, additionally, HIPK4 in mammals. (nature.com)
Y-27632 is a potent, selective inhibitor of Rho-associated protein kinases (ROCK) with IC50 values of 140-220 nM for ROCK1 and ROCK2. (bioquote.com)
The ROCK family of Rho-associated serine-threonine protein kinases is known to play an important role in Rho-mediated cell adhesion and smooth muscle contraction. (bioquote.com)
These compounds exhibit high selectivity for SFKs over a panel of recombinant protein kinases, excellent pharmacokinetics, and in vivo activity following oral dosing. (rcsb.org)
N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine (AZD0530) inhibits c-Src and Abl enzymes at low nanomolar concentrations and is highly selective over a range of kinases. (rcsb.org)
Reversible inhibitor of EGFR (HER1) and HER2 receptor kinases. (pharmacology2000.com)
JAKs are intracytoplasmic protein tyrosine kinases that bind to the cytoplasmic region of cytokine transmembrane receptors and mediate signalling via type 1 and type 2 cytokine receptors. (jle.com)
[2] Anisomycin can activate stress-activated protein kinases , MAP kinase and other signal transduction pathways. (wikipedia.org)
The Company's pipeline consists of ARQ 621, designed to inhibit the Eg5 kinesin motor protein, and ARQ 736, designed to inhibit the RAF kinases. (aol.com)
Introduction Proteins kinase CK2, a Ser/Thr kinase (also recognized to phosphorylate Tyr residues), one of the most pleiotropic of most protein kinases, has a key function in cell development, differentiation, cell loss of life and survival, and it is a highly powerful suppressor of apoptosis. (bioinbrief.com)

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase. (chemspider.com)
Scientists from Cancer Research Technology Ltd (CRT) presented new findings at the 2009 AACR Meeting, Denver, showing that a potent and selective inhibitor of protein kinase D called CRT0066101, inhibits the growth of pancreatic tumours. (ecancer.org)
We implemented a rational design approach to identify potent and selective ACE2 inhibitors. (acs.org)
Development of Potent and Selective Phosphinic Peptide Inhibitors of Angiotensin-Converting Enzyme 2. (acs.org)
AZ 3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM). (adooq.com)
CC-671 is a potent and selective dual inhibitor of TTK (Mps1) and CLK2. (adooq.com)
BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM. (adooq.com)
Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM. (adooq.com)
Here we have used the novel, potent, and selective mGlu5 inhibitor CTEP to address this issue in the Fmr1 knockout mouse. (autismsciencefoundation.org)

For example, selective inhibitors of BMPR1A and BMPR1B have displayed potential in inhibiting metastasis and tumor growth in preclinical studies. (news-medical.net)
AZD0530 is a potent inhibitor of tumor growth in a c-Src-transfected 3T3-fibroblast xenograft model in vivo and led to a significant increase in survival in a highly aggressive, orthotopic model of human pancreatic cancer when dosed orally once daily. (rcsb.org)
Enzastaurin apparently inhibits tumor growth via multiple mechanisms: suppression of tumor cell proliferation, induction of tumor cell apoptosis and inhibition of tumor-induced angiogenesis. (lclabs.com)
A new study reveals a new genomic approach to screen for compounds that inhibit tumor growth by causing cancer cells to differentiate. (sciencedaily.com)
A study published by Cell Press in the May 23 issue of Chemistry & Biology reveals a new genomic approach to screen for compounds that could inhibit tumor growth by causing cancer cells to differentiate, or convert from immature cells to more specialized cell types. (sciencedaily.com)

RN1 inhibits Smad/Id-3 signaling pathway by blocking Gal-3 interaction with BMPRs. (news-medical.net)

It also inhibits PRK2 with an IC50 value of 600 nM. (bioquote.com)
CW069 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 uM, significant selectivity over KSP. (adooq.com)
ARRY-520 R enantiomer is the R form of ARRY-520, which is a synthetic, small molecule kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM. (adooq.com)
Dimethylenastron is an inhibitor of mitotic motor kinesin Eg5 with IC50 value of 200 nM. (adooq.com)
K 858 is a selective ATP-uncompetitive mitotic kinesin Eg5 inhibitor with IC50 value of 1.3 uM. (adooq.com)
Eg5 Inhibitor V, trans-24 is a potent and specific kinesin Eg5 inhibitor with an IC50 of 0.65 μM, and can be used in the research of cancer. (adooq.com)
BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint with an IC50 of 2 nM. (adooq.com)
Empesertib (BAY 1161909) is a potent Mps1 inhibitor, with an IC50 of (adooq.com)
NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM. (adooq.com)
Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1. (adooq.com)
A novel, potent, brain permeant PKC inhibitor with IC50 of 80 nM, without detectable binding to the estrogen receptor (Ki>10 uM). (dcchemicals.com)
Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC). (dcchemicals.com)
Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. (dcchemicals.com)
GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. (dcchemicals.com)
ICA-1 is a potent, specific inhibitor of Protein Kinase C-iota (PKC-ι) with IC50 of 0.1 uM, does not inhibit PKC-ζ, the closely related atypical PKC family member. (dcchemicals.com)
LY-333,531 Hydrochloride is a potent, selective inhibitor of Protein Kinase C isozymes, PKC beta I (IC50 = 4.7 nM) and PKC beta II (IC50 = 5.9 nM). (dcchemicals.com)
Ro 31-8220 mesylate (Bisindolylmaleimide IX) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively. (dcchemicals.com)
ζ(ZETA)-Stat (1,3,6-Naphthalenetrisulfonic acid) is a novel PKC-zeta (PKC-ζ) specific inhibitor with IC50 of 5 uM, showed only 13% inhibition on PKC-I at 20 uM. (dcchemicals.com)
Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. (dcchemicals.com)
Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). (dcchemicals.com)
Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM. (dcchemicals.com)
PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCι (IC50=30 μM). (dcchemicals.com)
iFSP1 (FSP1 inhibitor) is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1, AIFM2) with IC50 of 103 nM. (probechem.com)
Liproxstatin-1 is a specific small molecule ferroptosis inhibitor (IC50=22 nM) via inactivation of the ferroptosis regulator Gpx4 (glutathione peroxidase 4), shows no activity on necroptosis. (probechem.com)
To help expand clarify the function of the average person bromine atoms of 4,5,6,7-tetrabromotriazole (TBBt), a comparatively selective inhibitor of proteins kinase CK2, we've examined the inhibition (IC50) of human CK2 simply by both mono-, the four di-, and both tri- bromobenzotriazoles in accordance with that of TBBt. (bioinbrief.com)

PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 uM for μ-Calpain, about 20-fold selectivity over m-calpain. (adooq.com)
H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. (dcchemicals.com)
To help expand define the function of the average person Br atoms of TBBt, in regards to strength and selectivity as inhibitors of CK2, we've synthesized all of the feasible two mono-, four di-, and two tri- bromobenzotriazoles [22] (Body 1), and herein we model the framework of their complexes with CK2 and look at the relationship between their physico-chemical properties and inhibitory actions CK2. (bioinbrief.com)
However, current commercial Keap1-targeting drugs covalently inhibit Keap1, a mechanism of action that comes with a lack of selectivity, side effects, and other complications during drug development. (lu.se)

This library represents a selection of drug-like compounds aimed at modulating protein-protein interaction (PPI) of β-catenin with different proteins involved in significant physiological processes. (chemdiv.com)

they suppress the signaling function of prostaglandins, which are important mediators of pain, fever, and inflammation responses, by inhibiting the cyclooxygenase enzymes and thereby reducing prostaglandin synthesis. (wikipedia.org)
Here, we summarize the different types of epigenetic enzymes which target corresponding protein domains, emphasize DNA methylation , histone modifications, and microRNA-mediated cooperation with epigenetic modification, and highlight recent achievements in developing targets for epigenetic inhibitor therapy. (frontiersin.org)
This article reviews current anticancer small-molecule inhibitors targeting epigenetic modified enzymes and displays their performances in different stages of clinical trials. (frontiersin.org)
PARP enzymes are drug targets: Drugs that inhibit PARP activity are already in use today in treatment of certain forms of cancer. (lu.se)

The phorbol ester-induced stabilization of GAP-43 mRNA was blocked by the protein kinase inhibitor polymyxin B and was partially inhibited by dexamethasone, an agent that blocks GAP-43 expression and neuronal differentiation in PC12 cells. (rupress.org)
Genetic disruption of TrkB-Shc signaling had no effect on severity of SE yet partially inhibited activation of the prosurvival adaptor protein Akt. (jneurosci.org)

Recombinant human protein Gal-3, EGFR, BMPR1A, and BMPR2 were obtained from Sino Biological. (news-medical.net)
Enzastaurin had a synergistic inhibitory effect with the EGFR inhibitor gefitinib on the proliferation of parental and gefitinib-resistant (GR) cancer cells. (lclabs.com)
Enzastaurin inhibits tumours sensitive and resistant to anti-EGFR drugs. (lclabs.com)
Breast cancer therapy has improved following the development of drugs with specific molecular targets, exemplified by inhibitors of human epidermal growth factor receptor-2 (HER2) or epidermal growth factor receptor (EGFR) such as trastuzumab and lapatinib. (jcancer.org)
We investigated the effects of TAK-285, a novel, investigational, dual EGFR/HER2 inhibitor that has been shown to penetrate the CNS and has comparable inhibitory efficacy to lapatinib which is a known Pgp substrate. (jcancer.org)
Exposure of Beas-2B cells to HDE caused EGFR phosphorylation and downstream ERK activation, and both responses were blocked by the EGFR-selective kinase inhibitor AG1478. (cdc.gov)

ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. (adooq.com)
Litronesib is a selective, allosteric inhibitor of kinesin Eg5. (adooq.com)
PS315, a derivative of PS48, is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. (dcchemicals.com)
However, for most allosteric proteins identified to date the mechanistic details of allosteric modulation are not yet well understood. (biomedcentral.com)
This relatively unexplored therapeutic potential and the putative advantages of allosteric drugs over classical active-site inhibitors fuel the attention allosteric-drug research is receiving at present. (biomedcentral.com)
In this article, we describe a simple computational approach, based on the effect allosteric ligands exert on protein flexibility upon binding, to predict the existence and position of allosteric sites on a given protein structure. (biomedcentral.com)
By querying the literature and a recently available database of allosteric sites, we gathered 213 allosteric proteins with structural information that we further filtered into a non-redundant set of 91 proteins. (biomedcentral.com)
We performed normal-mode analysis and observed significant changes in protein flexibility upon allosteric-ligand binding in 70% of the cases. (biomedcentral.com)
These results agree with the current view that allosteric mechanisms are in many cases governed by changes in protein dynamics caused by ligand binding. (biomedcentral.com)
Furthermore, we implemented an approach that achieves 65% positive predictive value in identifying allosteric sites within the set of predicted cavities of a protein (stricter parameters set, 0.22 sensitivity), by combining the current analysis on dynamics with previous results on structural conservation of allosteric sites. (biomedcentral.com)
We introduce a simple computational approach to predict the presence and position of allosteric sites in a protein based on the analysis of changes in protein normal modes upon the binding of a coarse-grained ligand at predicted cavities. (biomedcentral.com)
Its performance has been demonstrated using a newly curated non-redundant set of 91 proteins with reported allosteric properties. (biomedcentral.com)
An important factor fueling interest in allosteric drugs consists in their characteristic advantages compared to traditional active-site inhibitors. (biomedcentral.com)

Single-chain antibodies (scFv) take an important role in the field, because they are less immunogenic than whole antibodies, their smaller size allows faster and deeper penetration into solid tumors, and are by definition recombinant proteins, therefore easier to produce and modify. (biomedcentral.com)

The pharmaceutical industry currently uses cyclin-dependent kinase (CDK) inhibitors to target cell proliferation for cancer chemotherapy. (foxchase.org)
CGP60474 is a potent inhibitor of cyclin-dependent kinase (CDK). (dcchemicals.com)

NU 7026 is an ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK). (tocris.com)

While no NLRP3-targeting drugs have hit the market just yet, "the science is unequivocal," says Kate Schroder, an inflammasome researcher at the University of Queensland in Australia and one of the co-inventors on inflammasome inhibitor patents originally licensed to the Ireland-based company Inflazome (since acquired by Roche). (the-scientist.com)

Veuger et al (2003) Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-I. Cancer Res. (tocris.com)
Remarkably, DYRK1A is inhibited by abemaciclib to the same extent as Cdk4/Cdk6 in vitro, raising the question of whether targeting of DYRK1A contributes to the transcriptional inhibition and therapeutic activity of abemaciclib. (nature.com)
Y-27632 inhibited the kinase activity of both ROCK-I and ROCK-II in vitro, and this inhibition was reversed by ATP in a competitive manner. (bioquote.com)
One of the primary causes of ARF is ischemia/reperfusion (I/R). Inflammatory process and oxidative stress are thought to be the major mechanisms causing I/R. MK-886 is a potent inhibitor of leukotrienes biosynthesis which may have anti-inflammatory and antioxidant effects through inhibition of polymorphonuclear leukocytes (PMNs) infiltration into renal tissues. (biomedcentral.com)
Partial inhibition of DNA synthesis occurs at anisomycin concentrations that effect 95% inhibition of protein synthesis. (wikipedia.org)
The short-term protein trafficking inhibition and long-term effect on plant growth and survival caused by TE1 were fully reversible upon drug washout. (portlandpress.com)
NPD4928 (NPD 4928) is a small molecule that enhances ferroptosis via inhibition of ferroptosis suppressor protein 1 (FSP1). (probechem.com)
Inhibition of vaccinia virus L1 N-myristoylation by the host N-myristoyltransferase inhibitor IMP-1088 generates non-infectious virions defective in cell entry. (cdc.gov)

We believe this is the first orally administered small-molecule inhibitor of PKD with significant biological efficacy in pre-clinical animal models of pancreatic cancer. (ecancer.org)
GSK-923295, is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E, (CENP-E). (adooq.com)

Ispinesib (SB-715992) is a potent inhibitor of kinesin spindle protein, a kinesin motor protein essential for the formation of a bipolar mitotic spindle and cell cycle progression through mitosis. (adooq.com)

Herein, the synthesis of a new scaffold useful for the preparation of peptidyl-AOMKs is reported and it is demonstrated that the new synthetic probes bearing a 4-functionalized 2,6-dimethylbenzoate efficiently inhibit cysteine proteases like cathepsin B. (thieme-connect.com)
Anisomycin , also known as flagecidin , is an antibiotic produced by Streptomyces griseolus which inhibits eukaryotic protein synthesis . (wikipedia.org)
Anisomycin interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system. (wikipedia.org)
Because of anisomycin's wide use as a protein synthesis inhibitor, there have been many studies centered on the biosynthesis of anisomycin. (wikipedia.org)
Acute CTEP treatment corrects elevated hippocampal long-term depression, protein synthesis, and audiogenic seizures. (autismsciencefoundation.org)
Thus, changes in GAP-43 mRNA turnover do not appear to require continuous protein synthesis. (rupress.org)

MG-101 (ALLN) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins. (adooq.com)

SJA6017 is a cell permeable peptide aldehyde which functions as a reversible calpain inhibitor. (adooq.com)
PD 150606 is a cell-permeable, non-competitive, selective, non-peptide Ca2+ dependent calpain inhibitor for calpain-1 and for calpain-2 directed towards the Ca2+ binding sites of calpain. (adooq.com)
Structure-Guided Chemical Optimization of Bicyclic Peptide (Bicycle) Inhibitors of Angiotensin-Converting Enzyme 2. (acs.org)
CIGB-300 is a cell-permeable selective CK2 inhibitor peptide undergoing clinical trials for several cancers. (oncotarget.com)

Z-FA-FMK is an irreversible cysteine protease inhibitor. (adooq.com)
CA-074 methyl ester is a cell-permeable analog of CA-074 that acts as an irreversible cathepsin B inhibitor. (adooq.com)
Peptidyl-acyloxymethyl ketones (AOMKs) belong to a class of selective, irreversible inhibitors (activity-based probes) widely used as chemical tools of investigating proteins, for example, in activity-based protein profiling. (thieme-connect.com)

Also acts as a potent inhibitor of agonist-induced Ca 2+ sensitization of myosin phosphorylation and smooth muscle contractions (IC 50 = 700 nM for phenylephrine-induced contractions in aortic strips). (sigmaaldrich.com)
Also acts as a potent inhibitor of agonist-induced Ca 2+ sensitization of myosin phosphorylation and smooth muscle contraction. (sigmaaldrich.com)
The GSK-3, that is the key enzyme is normally showing its actions by various mechanisms that include its phosphorylation, formation of protein complexes, and other cellular distribution and thus it control and directly affects cellular morphology, its growth, mobility and apoptosis of the cell. (scielo.br)
Phosphorylation of residue Y515 promotes association of TrkB with the adaptor protein Shc and activation of PI3-kinase (PI3K)/Akt, MAPK signaling pathways whereas phosphorylation of residue Y816 promotes association of phospholipase Cγ1 (PLCγ1) and signaling mediated by IP3 and DAG ( Reichardt, 2006 ). (jneurosci.org)

A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinase (Ki = 140 nM for p160 ROCK (ROCK-I). Also inhibits ROCK-II with almost equal potency. (sigmaaldrich.com)

Potent JAK3 inhibitor. (rndsystems.com)

Ritonavir is a potent inhibitor of CYP3A4- and CYP2D6- mediated drug metabolism. (who.int)

Induction of p16 inhibits cell proliferation and thus can help to block the growth of tumors in a specific manner. (foxchase.org)
Downregulation of protein kinase C (PKC) by high doses of phorbol esters or selective PKC inhibitors prevented the induction of this mRNA by NGF, suggesting that NGF and TPA act through a common PKC-dependent pathway. (rupress.org)
In mRNA decay studies, phorbol esters caused a selective 6-fold increase in the half-life of the GAP-43 mRNA, which accounts for most of the induction of this mRNA by TPA. (rupress.org)

Protein kinase C inhibitor enzastaurin induces in vitro and in vivo antitumor activity in Waldenström macroglobulinemia. (lclabs.com)
Litronesib is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity. (adooq.com)

3.The higher the number of " * " is, the more potent the inhibitor or activator is. (adooq.com)
Most likely, tetraamine (70) is a potent activator of G(i) proteins. (inrae.fr)

Entrectinib is a selective tyrosine kinase inhibitor designed to inhibit the kinase activity of the tropomyosin receptor kinase (TRK) A/B/C and ROS1 proteins. (medscape.com)

The protein kinase Cβ-selective inhibitor, enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. (lclabs.com)
Enzastaurin induces apoptosis in multiple myeloma (MM) cell lines by inhibiting signaling through the AKT pathway, which is caspase-independent. (lclabs.com)
Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines. (lclabs.com)
An Active Site Inhibitor Induces Conformational Penalties for ACE2 Recognition by the Spike Protein of SARS-CoV-2. (acs.org)

Inhibitors of protein biosynthesis. (wikipedia.org)

Researchers' collaborative efforts from Denmark and Germany used BioMAX beamline to discover selective, non-covalent inhibitors of Keap1- a common target against oxidative stress and inflammation. (lu.se)
In improving oxidative stress and inflammation treatments, such as sclerosis and various kidney, respiratory, skin, and joint diseases, protein-protein interaction (PPI) between Nrf2 and Keap1 has become a key observation point. (lu.se)
TCDD for every step of the mechanism described for 2,3,7,8-TCDD carcinogenesis in humans including receptor binding, gene expression, protein activity changes, cellular replication, oxidative stress, promotion in initiation-promotion studies and complete carcinogenesis in laboratory animals. (who.int)

Notably, the selective anticancer properties of these REV-ERB agonists impair glioblastoma growth in vivo and improve survival without causing overt toxicity in mice. (investfinancialservices.com)

Does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 µM). (sigmaaldrich.com)
Based on these data and expected tissue concentrations of inhibitors, we predict that a p.o. administered curcuminoid/piperine combination is most likely to inhibit CYP3A, CYP2C9, UGT, and SULT metabolism within the intestinal mucosa. (aspetjournals.org)

Anisomycin is used as a component of Martin Lewis agar, an in vitro diagnostic product which is used extensively in the United States for the selective isolation of Neisseria gonorrhoeae and Neisseria meningitidis . (wikipedia.org)
Triazolam biotransformation by human liver microsomes in vitro: effects of metabolic inhibitors and clinical confirmation of a predicted interaction with ketoconazole. (aspetjournals.org)
CLL cells rely on overexpression and hyperactivation of the ubiquitous serine/threonine protein kinase CK2 for their viability in vitro. (oncotarget.com)

These results show for the first time that an inhibitor of PKD can slow the growth of tumours in pancreatic cancer models. (ecancer.org)
In addition, experiments carried out by CRT have shown that CRT0066101 is also effective at inhibiting the growth of tumours in a lung cancer model. (ecancer.org)

The pathways involved in cellular differentiation or transformation are Smad, Rho proteins, and PI3-kinase. (molvis.org)

Calpeptin is a cell permeable calpain inhibitor. (adooq.com)
Calpain Inhibitor II, ALLM is a cell-permeable inhibitor of calpain I, calpain II, cathepsin L and cathepsin B with Ki values of 120 nM, 230 nM, 0.6 nM and 100 nM, respectively. (adooq.com)
MDL 28170 is a cell permeable selective inhibitor of Calpain 1, a Ca2+-dependent cysteine protease which has been implicated in apoptosis of immune cells as well as neuronal cells. (adooq.com)
Monastrol is a potent, cell permeable non-tubulin-interacting mitosis inhibitor. (adooq.com)

iHPCAL1 is a ferroptosis inhibitor that effectively inhibits RSL3-induced cell death, directly interacts with HPCAL1 and significantly inhibits HPCAL1 protein expression at 1.25-5 uM in HT-1080 and Calu-1 cells. (probechem.com)
Furthermore, a few of them effectively inhibit the NTPase/helicase actions of hepatitis C and related infections [13]. (bioinbrief.com)

Around the same time, a group of scientists at the University of Lausanne in Switzerland found that NALP1/NLRP1, a protein from the same family, forms a large intracellular complex called an inflammasome , which helps generate the IL-1β cytokine, triggering a cascade of inflammation. (the-scientist.com)
Unlike the injected IL-1 receptor blockers that the British man received, which can dampen broader immune responses needed to fight infection, NLRP3 inhibitors could be taken orally and only inhibit NLRP3-mediated inflammation, offering a more practical, more effective, and safer therapy. (the-scientist.com)

Pevonedistat (MLN4924) is a selective small molecule targeting the NEDD8-activating enzyme (NAE) and inhibits an early step in neddylation, resulting in DNA re-replication, cell cycle arrest and death. (nih.gov)
It's been reported to become 635701-59-6 supplier dysregulated and overexpressed in every cancers hitherto analyzed, and is definitely considered an integral target for tumor chemotherapy [1], underlining the need for advancement of low-molecular pounds selective inhibitors of the enzyme, aswell as its two catalytically energetic subunits CK2 and CK2. (bioinbrief.com)

In this review, we summarize the basic principles manipulating the abovementioned epigenetic pathways and highlight the evidence of the promising clinical and preclinical results using small-molecule inhibitors against chromatin regulators for cancer treatment. (frontiersin.org)
SB 743921, a second generation KSP inhibitor, is a highly potent and active therapeutic in preclinical models of cancer. (adooq.com)

Treatment with NMT inhibitor IMP-1088 potently abrogated VACV infection, while VACV gene expression, DNA replication, morphogenesis and EV formation remained unaffected. (cdc.gov)

Background The neddylation pathway conjugates NEDD8 to cullin-RING ligases and controls the proteasomal degradation of specific proteins involved in essential cell processes. (nih.gov)
The National Institute for Health and Care Excellence (NICE) is approving entrectinib ( Rozlytrek , Roche) as a treatment option for ROS1-positive, advanced non-small cell lung cancer (NSCLC) not previously treated with ROS1 inhibitors. (medscape.com)
Phase II study of enzastaurin, a protein kinase C Beta inhibitor, in patients with relapsed or refractory diffuse large B-cell lymphoma. (lclabs.com)
Qin R , Zhu H , Wang F , Song M , Lin P , Xing Y , Zhang W , Zhong M , Wang Z , . Platelet activation in diabetic mice models: the role of vascular endothelial cell-derived protein disulfide isomerase-mediated GP IIb/IIIa receptor activation. (aging-us.com)
The purpose of this study was to investigate the release of Endothelial microparticle (EMP)-associated protein disulfide isomerase (PDI) after endothelial cell injury induced in diabetes and the changes in platelet activation. (aging-us.com)
HDE exposure induced intracellular Ca(2+) mobilization in Beas-2B cells and in primary cell isolates, but this response was neither mimicked by EGF nor inhibited by AG1478. (cdc.gov)
We have recently shown that the replication of rhinovirus, poliovirus and foot-and-mouth disease virus requires the co-translational N-myristoylation of viral proteins by human host cell N-myristoyltransferases (NMTs), and is inhibited by treatment with IMP-1088, an ultrapotent small molecule NMT inhibitor. (cdc.gov)

Strongly inhibits calpain I (Ki = 0.2 nM) and II but does not inhibit papain, trypsin and cathepsin L (Ki = 6 uM). (adooq.com)
Papain breaks down proteins, carbohydrates, and fats. (medlineplus.gov)

Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. (adooq.com)

PKC-412 is a broad spectrum protein kinase inhibitor. (dcchemicals.com)
Given the significant genetic identity between VACV, monkeypox virus and variola virus L1 homologs, our data provides a basis for further investigating the role of N-myristoylation in poxviral infections as well as the potential of selective NMT inhibitors like IMP-1088 as broad-spectrum poxvirus inhibitors. (cdc.gov)

We want to understand enzymatic mechanisms and improve the fit of PARP inhibitors to their enzymatic pockets. (lu.se)

The serotonin2 antagonist antidepressant nefazodone inhibited the alpha-OH and 4-OH pathways (Ki = 0.6 and 1.7 microM, respectively), but with considerably less activity than ketoconazole. (aspetjournals.org)
A beta-2 selective adrenergic antagonist. (lookformedical.com)

Specifically, BRD5529 directly and selectively binds CARD9, disrupts TRIM62 recruitment, inhibits TRIM62-mediated ubiquitinylation and activation of CARD9. (immune-system-research.com)
The newly identified compound works by selectively inhibiting a subset of gene-regulating proteins called histone deacetylases (HDACs). (sciencedaily.com)

Global Supplier of Chemical Probes, Inhibitors & Agonists. (probechem.com)

Y-27632 also inhibited the TGFβ1-induced contraction of seeded collagen gels. (molvis.org)

In co-cultures with K V 10.1-positive cancer cells the fusion protein also induced apoptosis in bystander K V 10.1-negative cancer cells, while normal prostate epithelial cells were not affected when present as bystander. (biomedcentral.com)

Adding chemical groups to the DNA backbone and modifying histone proteins impart distinct characteristics on chromatin architecture. (frontiersin.org)

Acetyl-Calpastatin (184-210) (human), selective calpain inhibitor. (adooq.com)
To explain this briefly, if the pathogen's active site is very well conserved in nature it may share important structural features with the human homologue, which could be then bound and inhibited as well by the antimicrobial drug causing toxic side-effects on the patient. (biomedcentral.com)
icFSP1 is a potent, selective human ferroptosis suppressor protein-1 (hFSP1) inhibitor, promotes ferroptosis and indirectly inhibits FSP1 by inducing condensate formation. (probechem.com)

BMPR family of proteins is a valuable tool for studying ligand-receptor interactions, downstream signaling events, and determining therapeutic targets. (news-medical.net)

Strategies to modulate BMPR signaling consist of the development of small molecule inhibitors, antibodies, and gene therapies. (news-medical.net)

Belongs to the tyr protein kinase family. (lu.se)

KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5) with potential antineoplastic activity. (adooq.com)
Allostery is one of the most powerful and common ways of regulation of protein activity. (biomedcentral.com)
Tight regulation of these processes is fundamental in all kingdoms of life and allostery represents one of the most commmon and powerful means of modulating protein activity[ 1 ]. (biomedcentral.com)
The K V 10.1-specific scFv62 antibody -TRAIL fusion protein was expressed in CHO-K1 cells, purified by chromatography and tested for biological activity. (biomedcentral.com)
This interaction inhibits its tyrosine-kinase activity. (lu.se)

Anatomy14

Organisms8

Diseases1

Chemicals and Drugs79

Analytical, Diagnostic and Therapeutic Techniques and Equipment20

Phenomena and Processes38

Disciplines and Occupations1

Information Science3

Health Care1

Kinases13

Potent and selective9

Tumor growth5

Signaling pathway1

IC5025

Selectivity4

Modulating protein-pro1

Enzymes4

Partially inhibited2

EGFR6

Allosteric13

Recombinant1

Cyclin-depend2

Competitive inhibitor1

Inflammasome Inhibitor1

Inhibition8

Small-molecule inhibitor2

Kinesin motor protein1

Synthesis6

Cysteine proteases1

Peptide4

Irreversible3

Phosphorylation4

Reversible1

JAK31

Drug Metabolism1

Induction3

Antitumor activity2

Activator2

Receptor kinase1

Induces4

Biosynthesis1

Oxidative stress3

Anticancer1

Concentrations2

Vitro3

Tumours2

Smad1

Permeable4

Effectively2

Inflammation2

Enzyme2

Preclinical2

Potently1

Cell7

Papain2

Cathepsin1

Broad spectrum2

Mechanisms1

Antagonist2

Selectively2

Agonists1

Contraction1

Apoptosis1

Histone1

Human3

Targets1

Antibodies1

Kinase family1

Activity5