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GSK-503 (1346572-63-1)

GSK503 inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency. In a panel of seven DLBCL cell lines, GSK503 causes growth inhibition and the effects are enhanced by ABT737 or Obatoclax.

Not Intended for Therapeutic Use. For research use only.

CAS: 1346572-63-1 Category

GSK-503 (1346572-63-1) Description:

GSK-503 is a potent EZH2 inhibitor with potential anticancer activity. Increased activity of the epigenetic modifier EZH2 has been associated with different cancers. In a melanoma mouse model, conditional Ezh2 ablation as much as treatment with the preclinical EZH2 inhibitor GSK503 stabilizes the disease through inhibition of growth and virtually abolishes metastases formation without affecting normal melanocyte biology. Comparably, in human melanoma cells, EZH2 inactivation impairs proliferation and invasiveness, accompanied by re-expression of tumour suppressors connected to increased patient survival. These EZH2 target genes suppress either melanoma growth or metastasis in vivo, revealing the dual function of EZH2 in promoting tumour progression. Thus, EZH2-mediated epigenetic repression is highly relevant especially during advanced melanoma progression, which makes EZH2 a promising target for novel melanoma therapies. ( Nat Commun. 2015 Jan 22;6:6051. doi: 10.1038/ncomms7051. )

GSK-503 (1346572-63-1) Specifications:

Product Name GSK-503
Chemical Name GSK503; 1346572-63-1; GSK-503; N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide; SCHEMBL2595868; CHEMBL3909511
Purity ≥98% (HPLC)
CAS Number 1346572-63-1
Molecular Formula C31H38N6O2
Molecular Weight 526.685 g/mol
Monoisotopic Mass 526.306 g/mol
InChi Code InChI=1S/C31H38N6O2/c1-19(2)37-18-21(4)29-25(30(38)33-17-26-20(3)13-22(5)34-31(26)39)14-24(15-27(29)37)23-7-8-28(32-16-23)36-11-9-35(6)10-12-36/h7-8,13-16,18-19H,9-12,17H2,1-6H3,(H,33,38)(H,34,39)


Form Powder
Color Yellow
Solubility  Soluble in DMSO, not in water
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling  Dry, dark
Application causes growth inhibition


RIDADR NONH for all modes of transport


1: Zingg D, Debbache J, Schaefer SM, Tuncer E, Frommel SC, Cheng P, Arenas-Ramirez N, Haeusel J, Zhang Y, Bonalli M, McCabe MT, Creasy CL, Levesque MP, Boyman O, Santoro R, Shakhova O, Dummer R, Sommer L. The epigenetic modifier  EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors. Nat Commun. 2015 Jan 22;6:6051. doi: 10.1038/ncomms7051. PubMed PMID: 25609585.