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Home > Biochemical Engineering > Inhibitors (Find 1094 items)

Inhibitors

Talazoparib

(1207456-01-6)
This novel, orally bioavailable poly(ADP-ribose) polymerase, or PARP, inhibitor (FW = 380.35 g/mol; CAS 1207456-01-6), also known as (8S,9R)- 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro- 2H-pyrido[4,3,2-de]phthalazin-3(7H)-one, targets PARP-mediated DNA repair (IC50 = 0.58 nM) of single-strand DNA breaks by the base-excision repair pathway. By enhancing the accumulation of DNA strand breaks, BMN 673 promotes genomic instability, eventually leading to apoptosis

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N-3-Pyridinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methyl]-1-piperidinecarboxamide

(1196109-52-0)
Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines (NAEs), including the endocannabinoid arachidonoyl ethanolamide (AEA). PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM). It covalently binds FAAH on Ser241 at the catalytic site, resulting in prolonged elevation of AEA in the brain and plasma in rats after treatment. PF-3845 significantly and persistently reduces inflammatory pain in rats through a cannabinoid receptor-dependent mechanism.[Cayman Che

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Evacetrapib

(1186486-62-3)
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.

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LY 2874455

(1254473-64-7)
LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.

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AZD5363

(1143532-39-1)
Capivasertib (AZD5363) is a potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.

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AT9283

(896466-04-9)
AT-9283 is a broad spectrum kinase inhibitor that potently inhibits Aurora A, Aurora B, JAK2, JAK3, and c-ABL (IC50s = 3, 3, 1.2, 1.1, and 4 nM, respectively). It also potently (IC50 = <1 μM) inhibits many other kinases, including serine/threonine kinases as well as receptor and non-receptor tyrosine kinases. As Aurora kinases have roles in mitosis, inhibitors of these kinases, including AT-9283, have potential in cancer therapy. Consistent with this, AT-9283 is effective in preventing prolifera

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Birinapant

(1260251-31-7)
This rotationally symmetric SMAC mimetic antagonist and anticancer agent (FW = 806.94 g/mol; CAS 1260251-31-7) targets cellular Inhibitor of Apoptosis Protein (or cIAP1; Kd of <1 nM), arguably the most potent mammalian caspase inhibitor, showing single-agent efficacy due to its panIAP antagonism and causing rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation. When administered in combination with TNF-α, Birinapant is effective against a melanoma cell line with

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Gedatolisib

(1197160-78-3)
This compound shows inhibitory activity against PI3K-α, PI3K-γ and mTOR.

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Orantinib

(252916-29-3)
TSU-68 is a inhibitor that targets vascular endothelial growth factor receptor 2, platelet-derived growth factor receptor β, and fibroblast growth factor receptor 1. The inhibitory effects of TSU-68 towards these growth factors lead to substantial antitumor activity and showed potential in its development in therapeutic uses.

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N-(3-fluoro-4-(2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yloxy)phenylcarbamothioyl)-2-phenylacetamide

(875337-44-3)
MGCD-265 is a novel dual c-Met/ VEGFR2 receptor tyrosine kinase inhibitor possessing favorable pharmacokinetic profiles and showed high efficacy in vivo in several human tumor xenograft models in mice.

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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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