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Home > Biochemical Engineering > Inhibitors (Find 73 items)

Inhibitors

PHA-848125

(802539-81-7)
Milciclib (PHA-848125) is a potent, dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.

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PIK-75 Hydrochloride

(372196-77-5)
PIK-75 is a DNA-PK and PI3K inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM).

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PF 00477736

(952021-60-2)
Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. PF-477736 is an ATP-competitive inhibitor of Chk1 with a Ki value of 0.49 nM that demonstrates 100-fold selectivity over Chk2. When used in combination with various chemotherapeutics, PF-477736 abrogates DNA damage-induced cell cycle arrest, potentiating the antiproliferative effects of these compounds in tumor cell lines and xenografts.[Cayman Chemical]

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Purmorphamine

(483367-10-8)
An activator of the hedgehog (Hh) signaling pathway.

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PF03716556

(928774-43-0)
A novel, potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease.

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Palomid 529

(914913-88-5)
Palomid 529 is a potent inhibitor of mTORC1 and mTORC2 complexes.

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PF 543

(1415562-82-1)
PF-543 is a novel cell-permeant inhibitor of SPHK1 with a Ki of 4.3 nM and more than 100-fold selectivity for SPHK1 over SPHK2.

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PFI-2

(1627676-59-8)
This SETD7 inhibitor (FW = 499.52 g/mol; CAS 1627676-59-8; IUPAC: 8- fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3- (trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide, targets the SET domain containing lysine methyltransferase, or SETD7 (Ki = 0.33 nM; IC50 = 2 nM), showing 1000-times selectivity versus other methyltransferases and other non-epigenetic targets. (R)-PFI-2 exhibits an unusual cofactor-dependent and substrate-competitive inhibitory mechanism by o

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PCI 34051

(950762-95-5)
PCI-34051 is a potent, histone deacetylase 8 (HDAC8)-specific inhibitor. PCI-34051 induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias. PCI-34051 did not affect other hematopoietic or solid tumor lines. PCI-34051 treatment has been shown to significantly reduce cholesterol accumulation in Niemann-Pick type C1 gene mutated human fibroblast.

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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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