A selective inhibitor of Plk1 (IC50 = 0.83 nM); induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice; also an inhibitor of BRD4 (IC50 = 25 nM)

BI-2536 – 50 mg

Brand:
Cayman
CAS:
755038-02-9
Storage:
-20
UN-No:
Non-Hazardous - /

Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).{29246,24210} It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.{29246} It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.{29225} BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.{29245}  

 

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Description

A selective inhibitor of Plk1 (IC50 = 0.83 nM); induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice; also an inhibitor of BRD4 (IC50 = 25 nM)

Formal name: 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide

Synonyms: 

Molecular weight: 521.7

CAS: 755038-02-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Plks||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PLK Signaling||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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