Chemical Name: 4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
Dual Plk/BRD4 inhibitor - Destabilizes Myc
Molecular Weight:
521.67
Purity:
97% by HPLC, NMR (conforms)
Form:
Off-white solid
CAS Number:
[755038-02-9]
Formula:
C28H39N7O3
Application Notes:
BI 2536 was originally reported as a potent (IC50s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) and selective2 Polo-like kinase inhibitor (IC50s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) that caused mitotic arrest and apoptosis induction in various human cancer cell lines.1 It was later found to be a potent inhibitor (IC50 = 100nM) of BET family member BRD4 and able to potently suppress c-Myc expression in MM.1S multiple myeloma cells.3 BI 2536 destabilizes N-Myc by inhibiting the deactivation of the ubiquitin E3 ligase Fbw7 by Plk1.4
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