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Home > Biochemical Engineering > Inhibitors (Find 42 items)

Inhibitors

Gabapentin hydrochloride

(60142-95-2)
Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.IC50 Value: 140 nM (α2δ subunit of calcium channel) [1]Target: Calcium Channelin vitro: Gabapentin, baclofen and CGP 44532 all reduced the electrically stimulated release of [3H]glutamic acid (IC50=20 microM, 0.8 microM and 2 microM, respectively). Gabapentin was without effect on the release of [3H]GABA, whilst

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Gestodene

(60282-87-3)
Estrogens and progestins are female hormones. They are produced by the body and are necessary for the normal sexual development of the female and for the regulation of the menstrual cycle during the childbearing years. Gestodene is a progestogen hormonal

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GW441756

(504433-23-2)
GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.IC50 Value: 2 nM [1]Target: TrkAin vitro: GW441756 specifically blocked TrkA-induced cell death in a dose-dependent manner, but there was no effect in uninduced cells. TrkA ability to induce γH2AX production was significantly downregulated by both K-252a and GW441756 in the absence of DNA damage inducer. In addition, it was also suppressed by K-252a during

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Galunisertib

(700874-72-2)
LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1 kinase (IC50 = 56 nM). It has been used to study the role of TGF-β signaling in chemotherapy-induced expansion of cancer stem-like cells in triple negative breast cancer cell lines and xenografts. LY2157299 has also been shown to inhibit the migration and tumor growth of hepatocellular carcinoma cell lines by disrupting Smad-2 phosphorylation.[Cayman Chemical]

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Gedatolisib

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

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GDC 0068

(1001264-89-6)
(2S)-2-(4-Chlorophenyl)-1-[4-[(5R,7R)-6,7-dihydro-7-hydroxy-5-methyl-5H-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-1-propanone is a highly selective AKT inhibitor targeting Akt1, Akt2 and Akt3. Studies have shown its use in combination with vemurafenib (V118500), have demonstrated therapeutic value in the treatment of hyperproliferative disorders such as cancer.

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GW9508

(885101-89-3)
GW9508 is a GPR40 full agonist, used to regulate glucose in rats. Can be applied to the treatment of diabetes type 2. GPR120 selective and potent agonist also used in the treatment of diabetes type 2 due to GPR120—ability to mediate GLP-1 secretion, insulin sensitization and anti-obesity effects.

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GSK1070916

(942918-07-2)
GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.

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GSK2636771

(1372540-25-4)
GSK2636771 is a potent, selective and oral inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

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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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