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Home > Biochemical Engineering > Inhibitors (Find 1094 items)

Inhibitors

LRRK2-kinase inhibitor

(1285515-21-0)
GSK2578215A is a potent and highly selective LRRK2 inhibitor; exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.IC50 value: ~10 nM(wt-LRRK2; LRRK2 G2019S) [1]Target: LRRK2 inhibitorGSK2578215A exhibits exceptionally high selectivity for LRRK2 across the kinome, substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.3–1.0 μM in cells and in mouse spleen and kidney, but not in brain, followi

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UNC2881

(1493764-08-1)
UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. IC50 value: 22 nM [1]Target: Mer kinase inhibitorTreatment with UNC2281 is also sufficient to block EGF-mediated stimulation of a chimeric receptor containing the intracellular domain of Mer fused to the extracellular domain of EGFR. In addition, UNC2881 potently inhibits collagen-induced platelet aggregation, suggesting that this class of inhibitors may ha

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BMX-IN-1

(1431525-23-3)
BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

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BMS707035

(729607-74-3)
BMS-707035 is an HIV-1 integrase (IN) inhibitor with an IC50 value of 15 nM. IC50 Value: 15 nMTarget: HIV IntegraseBMS-707035 was scheduled to be evaluated in a Phase II study to assess the antiretroviral activity, safety, pharmacodynamics, and pharmacokinetics in 50 HIV-infected subjects using a 10-day randomized, double-blind, placebo-controlled, ascending multiple-dose study design.

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N-(2-METHYL-6-BENZOOXAZOLYL)-N''-1,5-NAPHTHYRIDIN-4-YL UREA

(792173-99-0)
SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.IC50 value: 7.2 (pKb) [1]Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses (pK(B)=7.27+/-0.04 and 7.23+/-0.03 respectively, n=8), but had no effect on the UTP (3 microM)-induced calcium response in CHO-OX(1) cells. SB-334867-A (10 microM) also inhibited OX(2) mediated calcium responses (32.7+/-1.9% versus orex

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MK-3207 HCl

(957116-20-0)
MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC50 of 0.12 nM and Ki of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.

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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.

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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