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Home > Biochemical Engineering > Inhibitors (Find 1098 items)

Inhibitors

N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide

(811803-05-1)
Apatinib (YN968D1) is a small-molecule selective multitargeted tyrosine kinase inhibitor with an IC50 of 2.43 nM for the inhibition of VEGFR2.

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VX 765

(273404-37-8)
VX-765 shows anti-convulsant activity by inhibiting interlukin-1β biosynthesis.

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1-Cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-1H-indazole-4-carboxamide

(1396772-26-1)
EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2). It acts competitively with the EZH2 substrate S-adenosylmethionine. EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1. It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant

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1-Cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]piperazine

(1227158-85-1)
This Hif1a inhibitor (FW = 525.53 g/mol; CAS 1227158-85-1; Solubility: <1 mg/mL DMSO or H2O) targets the transcription factor hypoxia-inducible factor-1 (HIF-1), which plays an essential role in tumor development, tumor progression, and resistance to chemo- and radiotherapy. BAY 87-2243 inhibits HIF-1α and HIF-2α accumulation under hypoxic conditions in the H460 Non-Small Cell Lung Cancer (NSCLC) cell line but is without effect on HIF-1α protein levels that are induced by such hypoxia mim

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JAK3 Inhibitor

(211555-04-3)
WHI-P154 can act as antileukemic agent with apoptosis inducing activity.

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[(3aR*,4S*,7R*,7aS)-1,3,3a,4,7,7a-Hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinylbenzamide

(1127442-82-3)
IWR-3 act as inhibitors of Wnt response. It appear that IWR compounds induce stabilization of Axin proteins via a direct interaction, which is a part of the b-catenin destruction complex (consists of Apc, Axin, Ck1 and Gsk3b).Such compounds may be used in the treatment of Wnt protein signaling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.

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TCS 359

(301305-73-7)
Fms-like tyrosine kinase (FLT3) is a cell-surface receptor with important roles in stem cell development, hematopoiesis, and cancer.FLT3 Inhibitor is a cell-permeable, ATP-competitive inhibitor of FLT3 (IC50 = 27 nM) that blocks the proliferation of myelomonocytic leukemia MV4-11 cells (IC50 = 0.41 μM). It is selective for FLT3 over a panel of 22 other kinases. FLT3 Inhibitor synergistically increases the cytotoxicity of an AF4-mimetic peptide against MV4-11 cells.

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UNC 0631

(1320288-19-4)
UNC0631 is a potent and selective inhibitor of G9a activity in vitro (IC50 = 4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 25 nM). It potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 cell line.[Cayman Chemical]

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WYE-687

(1062161-90-3)
WYE-687 is an ATP-competitive and selective inhibitor of mammalian target of rapamycin (mTOR). Studies have shown the combination of Ras-Raf-MEK1/2 inhibitors with WYE-687 may overcome resistance to mTorKIs thus may be an effective additive therapy for treatment of patient with renal cell carcinoma or colorectal cancer.

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WYE-354

(1062169-56-5)
A pyrazolopyrimidines derivative that is a potent and ATP-competitive mTOR inhibitor with much reduced activity against PI 3-Kα or PI 3-Kγ. WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC50 <200 nM; [ATP] = 100 μM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-der

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Small molecule inhibitors are a type of molecules that can interact with proteins and reduce the biological activity of target proteins, including enzyme inhibitors, transcription factor inhibitors, and ion channel blockers. It acts on popular signaling pathways, popular targets and popular research fields: MAPK, PI3K, JAK / STAT and other signaling pathways, HDAC, Aurora kinase, CDK and cell cycle regulators, integrase / protease, etc. Research fields such as epigenetics, CNS, GPCR, anti-virus, antibacterial / anti-inflammatory. It is an effective tool for cell biology research.

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Frequently Asked Questions

What are Inhibitors in biochemical and pharmaceutical contexts?

Inhibitors are molecules that bind to enzymes or other biological targets to decrease or block their activity. In pharmaceutical research, enzyme inhibitors are widely used to modulate disease-related pathways, making them essential in drug discovery for conditions such as cancer, viral infections, and metabolic disorders. Common types include competitive, non-competitive, and irreversible inhibitors, each with distinct mechanisms of action.

How do enzyme inhibitors contribute to drug development?

Enzyme inhibitors play a critical role in drug development by selectively targeting disease-causing enzymes, thereby halting pathological processes. For example, protease inhibitors are used in HIV treatment, while kinase inhibitors are key in oncology therapies. Their specificity, potency, and pharmacokinetic properties make them valuable candidates in therapeutic pipelines, often serving as lead compounds during preclinical and clinical stages.

What are common applications of Inhibitors in life science research?

Inhibitors are extensively used in life science research for:1. Elucidating signaling pathways by selectively blocking key enzymes.2. Validating drug targets through functional studies.3. Serving as positive controls in high-throughput screening assays.4. Studying disease mechanisms in cellular and animal models.5. Developing diagnostic tools and companion biomarkers.Their versatility makes them indispensable in both academic and industrial R&D settings.

How can I verify the authenticity and quality of purchased Inhibitors?

To verify the authenticity and quality of Inhibitors, request a Certificate of Analysis (CoA) from the supplier, which should include HPLC or NMR data confirming identity and purity. Cross-reference the compound’s CAS number and structure with authoritative databases like PubChem or ChEMBL. Additionally, check if the supplier adheres to international quality standards (e.g., ISO 9001) and provides lot-specific testing data. Reputable vendors often offer sample testing or third-party validation reports upon request.

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