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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-GSK620
GSK620

Chemical Structure : GSK620

CAS No.: 2088410-46-0

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GSK620 (GSK-620)

货号: PC-72179Not For Human Use, Lab Use Only.

GSK620 (GSK-620) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.1 (BRD4 BD2), 220-fold selectivity over BD1.

规格 价格 库存 数量
5 mg ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK620 (GSK-620) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.1 (BRD4 BD2), 220-fold selectivity over BD1.
GSK620 significantly and dose-dependently inhibited both the arthritic score and IgG1 production in response to the immunisation in collagen-induced arthritis model in rats.
GSK620 showed similar level of efficacy to the pan-BET inhibitor I-BET151 and also dramatically reduced joint swelling, synovitis, cartilage damage, pannus formation and bone resorption.

物理化学性质&存储条件

分子量 325.37
分子式 C18H19N3O3
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

10 mM in DMSO
Chemical Name/SMILES

1-Benzyl-N5-cyclopropyl-N3-methyl-2-oxo-1,2-dihydropyridine-3,5-dicarboxamide

参考文献

1. Gilan O, et al. Science. 2020 Apr 24;368(6489):387-394.

2. Seal JT, et al. J Med Chem. 2020 Sep 10;63(17):9093-9126.

3. Aylott HE, et al. J Med Chem. 2021 Mar 25;64(6):3249-3281.

4. Rianjongdee F, et al. J Med Chem. 2021 Aug 12;64(15):10806-10833.

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