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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-GSK503
GSK503

Chemical Structure : GSK503

CAS No.: 1346572-63-1

GSK503 (GSK-503)

货号: 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).

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10 mg ¥1280 In stock
25 mg ¥2180 In stock
50 mg ¥3680 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 526.6724
分子式 C31H38N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 44 mg/mL

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]-

参考文献

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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