GSK503 ( GSK-503 )

Catalog No. M11402 CAS No. 1346572-63-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GSK503
Note

Research use only, not for human use.
Brief Description

GSK503 is a potent, specific EZH2 methyltransferase inhibitor that inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency (Ki app=3-27 nM).
Description

GSK503 is a potent, specific EZH2 methyltransferase inhibitor that inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency (Ki app=3-27 nM); GSK503 is highly selective for the SET domain of EZH2, >200 fold selective over EZH1 and > 4000 fold selective over other HMTases; inhibits GCB lymphoma cell lines with IC50 of 0.5-20 uM; impairs proliferation and invasiveness, accompanied by re-expression of tumour suppressor in melanoma cells; stabilizes the disease through inhibition of growth and virtually abolishes metastases formation without affecting normal melanocyte biology in melanoma mouse model.
Synonyms

GSK-503
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

EZH2
Research Area

Cancer
Indication

——

CAS Number

1346572-63-1
Formula Weight

526.67
Molecular Formula

C31H38N6O2
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 44 mg/mL
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
Chemical Name

1H-Indole-4-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-

1. Zingg D, et al. Nat Commun. 2015 Jan 22;6:6051.
2. Béguelin W, et al. Cancer Cell. 2013 May 13;23(5):677-92.

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