GSK-126

Aliases: Glycogen Synthase Kinase-3, N-[1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide
Catalog No: 14154 Format: 25 mg $535 Add to Cart
Catalog No: 14155 Format: 5 mg $130 Add to Cart
Application: Histone Acetylation (HAT & HDAC)

Chemical Properties


MW = 526.7
C31H38N6O2
CAS 1346574-57-9
>98% (HPLC); NMR (Conforms)

Description

A potent, selective, S-adenosyl-methionine-competitive inhibitor of EZH2 methyltransferase, Ki=0.5-3 nM, >150-fold selective for EZH2 over EZH1 and >1000-fold selective over 20 methyltransferases (ref 1). Decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK-126 inhibits proliferation of diffuse large B-cell lymphoma (DLBCL) cell lines as well as DLBCL xenografts in mice (ref 1). Rescues exhausted CD8+ T cells in HCV infection (ref 2). Facilitates the transition of embryonic stem cells to feeder-free extended pluripotent stem cells in combination with a cocktail of other agents (ref 3).

Contents

Cream-colored powder. May be dissolved in DMSO (16 mg/ml).

Storage Conditions

Store desiccated as supplied at room temperature for up to 1 year. Store solutions at -20°C for up to 2 months.

References

1. MT McCabe et al. Nature 2012 492:108
2. V Barili et al. Nat. Commun. 2020 11:604
3. R Zheng et al. Stem Cell Rep. 2021 16:1686

 
Chemical Structure of GSK-126.

Chemical Structure of GSK-126