GSK-503

Alternative_name

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
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.
CAS Number

1346572-63-1
Structure Available

Yes
Salt Form

No
Molecular Formula

C₃₁H₃₈N₆O₂
Molecular Weight

526.67
Cell Permeable

Yes
Purity

≥98% by HPLC
Solubilities

DMSO (>5 mg/ml)
Handling

Protect from air and light
Tag Line

A potent EZH2 inhibitor
Storage Condition

-20°C
Shipping Condition

gel pack
Shelf Life

36 months
SMILES

O=C(C1=CC(C2=CC=C(N3CCN(C)CC3)N=C2)=CC4=C1C(C)=CN4C(C)C)NCC5=C(C)C=C(C)NC5=O
InChi

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)
InChi Key

HRDQQHUKUIKFHT-UHFFFAOYSA-N
Data Sheet Link
MSDS Available

Yes