I-BET151

I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively[1][2].

Product Specifications

CAS Number

[1300031-49-5]

Product Name Alternative

GSK1210151A

UNSPSC

12352005

Hazard Statement

H301

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/I-BET151.html

Concentration

10mM

Purity

99.81

Solubility

DMSO : ≥ 100 mg/mL

Smiles

C[C@@H](N1C(C(C=C(OC)C(C2=C(C)ON=C2C)=C3)=C3N=C4)=C4NC1=O)C5=CC=CC=N5

Molecular Formula

C23H21N5O3

Molecular Weight

415.44

Precautions

H301

References & Citations

[1]Seal J, et al. Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A) . Bioorg Med Chem Lett. 2012 Apr 15;22 (8) :2968-72.|[2]Chaidos A, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123 (5) :697-705.