GSK1324726A

GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM) .

Product Specifications

CAS Number

[1300031-52-0]

Product Name Alternative

I-BET726

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GSK1324726A.html

Purity

99.92

Solubility

DMSO : ≥ 46 mg/mL

Smiles

ClC1=CC=C(N[C@H]2C3=C(C=CC(C4=CC=C(C(O)=O)C=C4)=C3)N(C(C)=O)[C@@H](C)C2)C=C1

Molecular Formula

C25H23ClN2O3

Molecular Weight

434.91

Precautions

H302, H315, H319, H335

References & Citations

[1]Wyce A, et al. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One. 2013 Aug 23;8 (8) :e72967.|[2]Gosmini R, et al. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57 (19) :8111-31.