GSK-503 | 9538

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.

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.

9538 | GSK-503 DataSheet

Alternate Name/Synonyms: 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

Appearance: Off-white solid

Formulation: N/A

CAS Number: 1346572-63-1

Structure Available?: Yes

Peptide sequence: N/A

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

Country of Origin: USA

Tag Line: A potent EZH2 inhibitor

MDL Number: N/A

PubChem CID: N/A

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