BI-2536 --- PLK1 and BRD4 Dual Inhibitor

Overview
Catalog #	bs-60171c-5-mg-solid
Product Name	BI-2536 --- PLK1 and BRD4 Dual Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 521.65 Formula: C28 H39 N7 O3 CAS Number: 755038-02-9 InChi Key: XQVVPGYIWAGRNI-JOCHJYFZSA-N InChi: InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1 Smiles: CC[C@@H]1C(=O)N(C)C2C=NC(NC3C=CC(=CC=3OC)C(=O)NC3CCN(C)CC3)=NC=2N1C1CCCC1 Purity: 98.0 Solubility: DMSO up to 40 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	BI-2536 is a potent inhibitor of PLK1 (Polo-like kinase 1, IC50 ~0.83 nM) and BRD4 (IC50 ~37 nM). It also inhibits PLK2 and PLK3 with IC50 of 3.5 nM and 9.0 nM, respectively. BI-2536 treatment ranging from 10 nM to 100 nM leads to the blocking of the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibition of cohesin release from chromosome arms, induction of monopolar spindles, and other Plk1 dependent processes. BI-2536 inhibits the growth of a panel of 32 human cancer cell lines with EC50 of 2-25 nM. It also displaces BRD4 from chromatin and suppresses c-Myc expression. The combination of inhibitory activities on independent kinase and bromodomain oncogenic pathways exemplifies a new strategy for rational single-agent polypharmacological targeting.