I-BET151 (GSK1210151A), BET Inhibitor

Overview
Catalog #	bs-66053c-2mg-solid
Product Name	I-BET151 (GSK1210151A), BET Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 415.44 Formula: C23 H21 N5 O3 CAS Number: 1300031-49-5 InChi Key: VUVUVNZRUGEAHB-CYBMUJFWSA-N InChi: InChI=1S/C23H21N5O3/c1-12-21(14(3)31-27-12)16-9-18-15(10-20(16)30-4)22-19(11-25-18)26-23(29)28(22)13(2)17-7-5-6-8-24-17/h5-11,13H,1-4H3,(H,26,29)/t13-/m1/s1 Smiles: COC1C=C2C3=C(C=NC2=CC=1C1C(C)=NOC=1C)NC(=O)N3[C@H](C)C1C=CC=CN=1 Purity: 98.0 Solubility: DMSO up to 100mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	I-BET151 (GSK1210151A) is a novel and selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4 with IC50 of ~0.5 μM, 0.25 μM, and 0.79 μM respectively. It has profound effects on human and murine MLL-fusion leukaemic cell lines, through the induction of early cell cycle arrest and apoptosis. The mode of action of I-BET151 is, at least in part, due to the inhibition of transcription at key genes (BCL2, C-MYC and CDK6) through the displacement of BRD3/4, PAFc and SEC components from chromatin. In vivo studies indicate that I-BET151 can provide survival benefit in two distinct mouse models of murine MLL–AF9 and human MLL–AF4 leukaemia. I-BET151 is also an ApoA1 upregulator that was also found to mediate potent anti-inflammatory effects. It showed a broad anti-inflammatory profile in a LPS-challenged Balb/C mouse model.