GSK126

GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM[1].

Product Specifications

CAS Number

[1346574-57-9]

Product Name Alternative

GSK2816126A

UNSPSC

12352005

Hazard Statement

H302, H410

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GSK126.html

Purity

99.98

Solubility

DMSO : 12.5 mg/mL (ultrasonic)

Smiles

O=C(C1=CC(C2=CC=C(N3CCNCC3)N=C2)=CC4=C1C(C)=CN4[C@@H](C)CC)NCC5=C(C)C=C(C)NC5=O

Molecular Formula

C31H38N6O2

Molecular Weight

526.67

Precautions

H302, H410

References & Citations

[1]McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012 Dec 6;492 (7427) :108-12.|[2]Sato T, et al. PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer. Sci Rep. 2013 May 29;3:1911.