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Home > Biochemical Engineering > Inhibitors (Find 1083 items)

Inhibitors

Dolutegravir

(1051375-16-6)
Dolutegravir is a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir is currently in Phase III clinical trials for the treatment of HIV infection. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.

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ABT 199

(1257044-40-8)
Venetoclax has high affinity for BCL-2, binding to the protein with an affinity more than three orders of magnitude greater than to BCL-XL or BCL-W in vitro. By binding to BCL-2, the drug displaces BCL-2-bound proapoptotic proteins (such as BIM), resulting in the permeabilization of mitochondrial outer membranes, activation of caspases, and restoration of cancer cell apoptosis, with this process requiring the apoptosis regulators BAX or BAK.

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Ponatinib

(943319-70-8)
Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively

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2-Propenamide, N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-, methanesulfonate (1:1)

(1421373-66-1)

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Palbociclib

(571190-30-2)
Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib is a drug for the treatment of ER-positive and HER2-negative breast cancer.

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Prucalopride

(179474-81-8)
This novel enterokinetic drug (FW = 367.87 g/mol; CAS 179474-81-8), also known by the tradename Resolor and its systematic name, 4-amino-5- chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7- carboxamide, is a selective, high affinity serotonin 5-HT4 receptor agonist with that stimulates colonic mass movements, which provide the main propulsive force for defecation. It exhibits high affinity to both 5-HT4 receptor isoforms, with respective pKi values of 8.60 and 8.10 for th

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Safinamide

(133865-89-1)
Safinamide may exert its in vivo effects through different mechanisms of action. It did not display activity against >80 different types of dopamine, glutamate, adenosine, serotonin, muscarinic, nicotinic, and GABA receptors. Conversely, potent modulation of DA metabolism, blockade of Na+/Ca2+ channels, and inhibition of glutamate release have been demonstrated. It has pointed out that the electrophysiological and neurochemical effects of safinamide are apparent at effective anticonvulsant conc

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Afatinib dimaleate

(850140-73-7)
Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

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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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