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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
EZH2
Available Sizes
Curated Selection
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