Selective inhibitorKinase inhibitorProteinSubstrates and inhibitorsEGFRTimes more potentProteaseIrreversible inhibitorProton pump inhibVitroReversibleEnzymeEnzymesErbB2ReceptorMetaboliteIC50SelectivityAnalogsMetabolicCdk4CompoundsInhibitionDephosphorylationMechanism of ActHistonePeptideChemicalMethanolSpecificBiological activityMolecularVinblastineProductsChronicAcidHighlyDualActiveSmall
Selective inhibitor4
- IU1 is a selective inhibitor of Usp14. (adooq.com)
- P005091 is a selective inhibitor of ubiquitin-specific protease (USP) 7 (IC50 = 4.2 uM). (adooq.com)
- BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases. (adooq.com)
- GSK2606414 is a novel, highly selective inhibitor of protein kinase R‑like endoplasmic reticulum kinase (PERK). (spandidos-publications.com)
Kinase inhibitor6
- Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). (adooq.com)
- Butein is a plant polyphenol that acts as a specific protein tyrosine kinase inhibitor. (adooq.com)
- Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). (adooq.com)
- BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. (adooq.com)
- We also describe the rapid discovery of an orally-available ATP-competitive kinase inhibitor that displays high selectivity and potent anti-cancer activity using a dual ligand-based phenotypic strategy. (selectbiosciences.com)
- This trial assessed the preferential Janus kinase 1 (JAK1) inhibitor filgotinib and the spleen tyrosine kinase inhibitor lanraplenib in patients with LMN. (bmj.com)
Protein5
- It is a potent inhibitor of specific protein phosphatases and is known to have a variety of negative effects on cells. (chemspider.com)
- WP1130 (Degrasyn) is a novel selective small molecular deubiquitinase inhibitor and a Bcr/Abl destruction pathway activator that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells. (adooq.com)
- Using a newly developed human neuronal cell model, derived from patient-induced pluripotent stem cells, we find that 2-aminobenzamide histone deacetylase (HDAC) inhibitors increase FXN mRNA levels and frataxin protein in FRDA neuronal cells. (frontiersin.org)
- Free shipping on inhibitor and protein orders over $500. (adooq.com)
- RNase Inhibitor is an acidic, 52 kDa protein that is a potent non-competitive inhibitor of pancreatic-type ribonucleases such as RNase A, RNase B and RNase C. The enzyme is provided as a fusion of the porcine RNase Inhibitor gene with a proprietary 22.5 kDa protein tag. (qiagen.com)
Substrates and inhibitors1
- Previous studies with substrates and inhibitors of ACE suggested that it was a zinc-containing metalloprotein and a carboxypeptidase similar to pancreatic carboxypeptidase A. However ACE releases dipeptides rather than single amino acids from the C-terminus of the peptide substrates. (wikipedia.org)
EGFR2
- Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR. (adooq.com)
- CO-1686 is a novel, oral, targeted covalent (irreversible) inhibitor of the cancer-causing mutant forms of epidermal growth factor receptor (EGFR) currently being studied for the treatment of non-small cell lung cancer (NSCLC). (adooq.com)
Times more potent3
- This yielded a potent inhibitor that was 1000 times more potent than succinyl-L-proline. (wikipedia.org)
- SJB3-019A (IC50 = 0.0781 uM) was 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells. (adooq.com)
- The active metabolite is 10 to 40 times more potent by weight than losartan and appears to be a reversible, non-competitive inhibitor of the AT1 receptor. (nih.gov)
Protease14
- P 22077 is a cell-permeable inhibitor of the ubiquitin-specific protease (IC? (adooq.com)
- HBX 41108 is an inhibitor of ubiquitin-specific protease (USP) 7 activity (IC50 = 424 nM). (adooq.com)
- SJB2-043 is one of analogs/derivatives of C527, which is a novel and potent USP1 (ubiquitin-specific protease 1) inhibitor. (adooq.com)
- NSC 687852 is an inhibitor of ubiquitin-specific-processing protease 14 (USP14) and ubiquitin carboxyl-terminal hydrolase isozyme L5 (UCHL5), two proteasome-associated DUBs. (adooq.com)
- Ritonavir, indinavir, and saquinavir, all human immunodeficiency virus-1 protease inhibitors with a potent antiviral effect during triple therapy, are extensively metabolized by liver cytochrome P450 3A4. (aspetjournals.org)
- As this P450 isoform is involved in the metabolism of about 50% of drugs, coadministration of protease inhibitors with other drugs may lead to serious effects due to enzyme inhibition. (aspetjournals.org)
- In this study, metabolic interactions between these protease inhibitors and methadone or buprenorphine were studied in vitro in a panel of 13 human liver microsomes. (aspetjournals.org)
- In brief, caution should be advised if human immunodeficiency virus-1 protease inhibitors are coadministered with methadone and buprenorphine. (aspetjournals.org)
- These drugs, namely ritonavir, indinavir, and saquinavir, are potent and specific inhibitors of HIV-1 protease, one of the major enzymes encoded by the retrovirus. (aspetjournals.org)
- Mello and Mendelson, 1980 ), are likely to be coadministered with protease inhibitors to acquired acquired immunodeficiency syndrome (AIDS) patients. (aspetjournals.org)
- 1997a ), these two drugs are potential candidates to interact with protease inhibitors. (aspetjournals.org)
- The aim of this study was to compare the inhibitory potential of the HIV protease inhibitors ritonavir, indinavir, and saquinavir against methadone and buprenorphine N -dealkylations catalyzed by P450 3A4 in a panel of human liver microsomes. (aspetjournals.org)
- As the prediction of in vivo metabolic drug interaction from in vitro data has made significant advances in the last decade ( Bertz and Granneman, 1997 ), in vitro data allow us to estimate the likelihood of metabolic interactions between three protease inhibitors and two opioid substitutes. (aspetjournals.org)
- Stock solutions of protease inhibitors were 1 mM ritonavir in methanol, 1 mM saquinavir, and 1 mM indinavir both in H 2 O/acetonitrile (1/1, v/v). (aspetjournals.org)
Irreversible inhibitor1
- Potent, irreversible inhibitor of PI 3-kinase. (tocris.com)
Proton pump inhib3
- Vonoprazan , an oral potassium-competitive acid blocker (PCAB), provides more potent inhibition of gastric acid than proton pump inhibitors (PPIs) and is seen as a potential alternative. (medscape.com)
- Proton pump inhibitors have replaced H2 blockers in most clinical situations because of efficacy. (msdmanuals.com)
- Data are limited to the use of proton pump inhibitors in children. (msdmanuals.com)
Vitro2
Reversible2
Enzyme7
- The discovery of an orally inactive peptide from snake venom established the important role of angiotensin converting enzyme (ACE) inhibitors in regulating blood pressure. (wikipedia.org)
- Later, the researchers compared a few mercaptoacyl amino acid inhibitors and concluded that the binding of the inhibitor to the enzyme involved a hydrogen bond between a donor site on the enzyme and the oxygen of the amide carbonyl, much like predicted for the substrates. (wikipedia.org)
- DUBs-IN-1 is a potent deubiquitinase enzyme inhibitor with IC50s of 18 uM/0.71 uM for USP7/USP8 respectively. (adooq.com)
- AZ1 is a dual inhibitor of the USP25/28 deubiquitinating enzyme subfamily. (adooq.com)
- Angiotensin II [formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II)], is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. (nih.gov)
- Dilutions of the enzyme were made in 1X RNase Inhibitor Reaction Buffer and added to 1000 μL reactions containing 1mM cytidine 2',3'-cyclic monophosphate, 1μg RNase A in a 1X reaction buffer containing 100mM Tris-Acetate, 1mM EDTA, pH 6.5. (qiagen.com)
- Lisinopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE). (ncats.io)
Enzymes3
- Objectives: The objective of this study was to explore potential drug-drug/food interactions of ciprofloxacin and grapefruit juice, known hepatic cytochrome P450 (CYP) 1A2 inhibitors, on single-dose oral pharmacokinetics of riluzole, a substrate of CYP 1A2 enzymes. (researchgate.net)
- To understand the mechanism of action of these compounds, we probed the kinetic properties of the active and inactive inhibitors, and found that only compounds that target HDACs 1 and 3 exhibited a slow-on/slow-off mechanism of action for the HDAC enzymes. (frontiersin.org)
- Moreover, inhibitors must have a long residence time on their target enzymes for this activity. (frontiersin.org)
ErbB21
- AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling. (adooq.com)
Receptor3
- For these, reasons both leukotriene synthesis inhibitors and leukotriene receptor antagonists have been suggested for inducing beneficial effects at different stages of the atherosclerosis process and may represent a new therapeutic target in the treatment of atherosclerotic vessel diseases, in particular in acute coronary syndrome. (hindawi.com)
- Please refer to our complete listing of receptor tyrosine kinase inhibitors for possible alternatives. (merckmillipore.com)
- CDK4/6 inhibitors combined with endocrine therapy have demonstrated higher antitumor activity than endocrine therapy alone for the treatment of advanced estrogen receptor-positive breast cancer. (bvsalud.org)
Metabolite1
- For circulating testosterone to exert its stimulatory effects on the hair follicle, it first must be converted into its more potent follicle-active metabolite, dihydrotestosterone. (medscape.com)
IC504
- It is a potent ATP-competitive inhibitor of GSK3alpha and GSK3beta (IC50 values of 0.65 and 0.58 nM, respectively). (mcw.edu)
- IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. (adooq.com)
- GRL0617 is a potent, selective and competitive noncovalent inhibitor of SARS PLPro, with an IC50 of 0.6 μM, and with a Ki of 0.49 μM. (adooq.com)
- BMS 599626 is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50=22, 32 and 190 nM, respectively) with potential antineoplastic activity. (adooq.com)
Selectivity1
- In summary, SR-4835, as an orally bioavailable inhibitor of CDK12/13, it has excellent isoform selectivity and few off-target interactions. (cancer-research-network.com)
Analogs1
- Structural analogs of the active HDAC inhibitors that selectively target either HDAC1 or HDAC3 do not show similar increases in FXN mRNA levels. (frontiersin.org)
Metabolic1
- Several of the synthesized compounds proved to be potent, competitive M(pro) inhibitors with improved metabolic stability profiles. (cdc.gov)
Cdk41
- Based on a database search, we identified abemaciclib, an FDA-approved Cdk4/Cdk6 inhibitor used for the treatment of metastatic breast cancer, as potent inhibitor of HIPK2, HIPK3, and DYRK1A. (nature.com)
Compounds3
- Over 2000 compounds were tested randomly in a guinea pig ileum test and succinyl-L-proline was found to have the properties of a specific ACE inhibitor. (wikipedia.org)
- GNE-6640 enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors. (adooq.com)
- We were inspired by a series of publications emanating from the Jorgensen and Anderson groups describing the design of potent, non-peptidic, competitive SARS-CoV-2 M(pro) inhibitors, and we saw an opportunity to make several design modifications to improve the overall pharmacokinetic profile of these compounds without losing potency. (cdc.gov)
Inhibition1
- The inhibition modes of E7 for MAO−A and MAO−B were competitive with Ki values of 2.65 ± 0.064 and 0.011 ± 0.0011 μM, respectively. (amrita.edu)
Dephosphorylation1
- This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. (sigmaaldrich.com)
Mechanism of Act1
- BAY-598 is a potent SMYD2 inhibitor and acts via a peptide competitive mechanism of action. (thesgc.org)
Histone1
- By interrogating microarray data from neuronal cells treated with inhibitors of different specificity, we selected two genes encoding histone macroH2A ( H2AFY2 ) and Polycomb group ring finger 2 ( PCGF2 ) that were specifically down-regulated by the inhibitors targeting HDACs1 and 3 versus the more selective inhibitors for further investigation. (frontiersin.org)
Peptide1
- A collaboration between Bayer and the SGC has resulted in the discovery of BAY-598 [4], a potent, peptide-competitive chemical probe for SMYD2. (thesgc.org)
Chemical1
- BAY-598 has a unique chemotype relative to the current SMYD2 chemical probe LLY-507 [5] and inhibitors [6,7]. (thesgc.org)
Methanol1
- When the extract was separated on a Cosmosil column, the eluate with 70% methanol showed the most potent ability to increase [ 3 H]vinblastine uptake. (aspetjournals.org)
Specific1
- Then after the discovery of two active sites of ACE: N-domain and C-domain, the development of domain-specific ACE inhibitors began. (wikipedia.org)
Biological activity2
- The PI 3-Kγ Inhibitor, also referenced under CAS 648450-29-7, controls the biological activity of PI 3-Kγ. (sigmaaldrich.com)
- The Aromatase Inhibitor I, also referenced under CAS 331684-05-0, controls the biological activity of Aromatase. (emdmillipore.com)
Molecular2
- The RNase Inhibitor is intended for molecular biology applications. (qiagen.com)
- First of all, in a molecular modeling study, the X-ray structure of CDK12 predicts that SR-4835 is ATP competitive. (cancer-research-network.com)
Vinblastine1
- An ethyl acetate extract of orange juice did not affect the initial uptake rate of [ 3 H]vinblastine but significantly increased the steady-state uptake, as did cyclosporin A (20 μM), an inhibitor of P-gp. (aspetjournals.org)
Products1
- Other ER Stress/UPR Inhibitors " has 9 results in Products. (rndsystems.com)
Chronic1
- The development of targeted therapies has also been followed by resistance, reminiscent of an evolutionary arms race, as exemplified by imatinib and other BCR-ABL inhibitors for the treatment of chronic myelogenous leukaemia. (nature.com)
Acid4
- L-benzylsuccinic acid (2(R)-benzyl-3-carboxypropionic acid) was described to be the most potent inhibitor of carboxypeptidase A in the early 1980s. (wikipedia.org)
- Proline was chosen as the amino acid moiety because of its presence as the carboxy terminal amino acid residue in teprotide and other ACE inhibitors found in snake venoms. (wikipedia.org)
- So it was proposed that succinyl amino acid derivative should be an ACE inhibitor and succinyl-L-proline was found to be such an inhibitor. (wikipedia.org)
- Cysteinyl leukotrienes (Cys-LTs) are potent inflammatory lipid mediators derived from the 5-lypoxygenase (5-LO) pathway of arachidonic acid (AA) metabolism [ 1 ], initially identified to have important effects on pathogenetic aspects of allergic rhinitis and bronchial asthma and approved in the late 1990s for the relief of perennial and seasonal allergic rhinitis symptoms, and the treatment of mild persistent bronchial asthma [ 2 - 5 ]. (hindawi.com)
Highly1
- ML323 is a selective and highly potent USP1-UAF1 inhibitor links deubiquitination to DNA damage responses. (adooq.com)
Dual1
- SR-4835 is a potent dual inhibitor of CDK12/CDK13 kinase. (cancer-research-network.com)
Active1
- Methotrexate is a potent, competitive inhibitor of dihydrofolate reductase (DHFR), and reduces metabolically active intracellular folates decreasing the de novo synthesis of purines and pyrimidines (precursors of DNA and RNA) required for cellular proliferation. (axonmedchem.com)
Small1
- Our study demonstrates that 16 weeks of treatment with the Janus kinase 1 (JAK1) inhibitor filgotinib reduced proteinuria in a small number of patients with LMN. (bmj.com)