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Chemical Structure : GSK503
CAS No.: 1346572-63-1
Catalog No.: PC-43259Not For Human Use, Lab Use Only.
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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $218 | In stock | |
| 50 mg | $368 | In stock | |
| 100 mg | Get quote |
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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.
GSK503 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.
GSK503 stabilizes the disease through inhibition of growth and virtually abolishes metastases formation without affecting normal melanocyte biology in melanoma mouse model.
| M.Wt | 526.6724 | |
| Formula | C31H38N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 44 mg/mL |
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| Chemical Name/SMILES |
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]- |
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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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