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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-I-BET762
I-BET762

Chemical Structure : I-BET762

CAS No.: 1260907-17-2

I-BET762 (GSK525762A;GSK-525762A;I-BET-762;Molibresib)

货号: PC-43340Not For Human Use, Lab Use Only.

I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins BRD2, BRD3 and BRD4 with IC50 of 32.5-42.5 nM, does not interact with other bromodomain-containing proteins (BAZ2B, ATAD2, CREBBP and PCAF).

规格 价格 库存 数量
25 mg ¥1980 In stock
50 mg ¥2980 In stock
100 mg ¥4880 In stock
200 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

I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins BRD2, BRD3 and BRD4 with IC50 of 32.5-42.5 nM, does not interact with other bromodomain-containing proteins (BAZ2B, ATAD2, CREBBP and PCAF).
I-BET762 inhibits binding of BET proteins to acetylated histones, disrupts chromatin complexes responsible for the expression of key inflammatory genes in activated macrophages, suppresses TNF-inducible key proinflammatory cytokine (il1b, il1a) and chemokine genes (ccl5, cxcl10, cxcl2/3) in BMDMs.
I-BET762 inhibits the ability of Th1-differentiated 2D2 T cells to induce neuroinflammation in vivo in mouse model of EAE.
I-BET762 inhibits myeloma cell proliferation both in vitro and myeloma xenograft models.

物理化学性质&存储条件

分子量 423.8954
分子式 C22H22ClN5O2
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

4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)-

参考文献

1. Nicodeme E, et al. Nature. 2010 Dec 23;468(7327):1119-23.

2. Bandukwala HS, et al. Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14532-7.

3. Mirguet O, et al. J Med Chem. 2013 Oct 10;56(19):7501-15.

4. Chaidos A, et al. Blood. 2014 Jan 30;123(5):697-705.

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