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首页-小分子抑制剂&激动剂-Apoptosis-Bcl-2-BI-3802
BI-3802

Chemical Structure : BI-3802

CAS No.: 2166387-65-9

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BI-3802 (BI3802, BI 3802)

货号: PC-60949Not For Human Use, Lab Use Only.

BI-3802 (BI3802) is a highly potent and efficacious BCL6 degrader that potently inhibits the interaction of the BTB/POZ domain of BCL6 with several co-repressors in vitro with IC50 of <3 nM.

规格 价格 库存 数量
5 mg ￥3280 In stock
10 mg ￥5280 In stock
25 mg ￥8980 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

BI-3802 (BI 3802) is a small molecule B cell lymphoma 6 (BCL6) degrader, binds the Broad complex/Tramtrack/Bric-a-brac (BTB) domain and induces BCL6 degradation.
BI-3802 induced degradation of the full-length BCL6 reporter, while the inhibitor, BI-3812, did not alter stability of the reporter, which can be attenuated by chemical inhibition of the 26S proteasome with MG132 or inhibition of the ubiquitin activating enzyme UBA1 by MLN7243 (TAK-243).
BI-3802 induces cellular BCL6 foci and BCL6 polymerization.
Mutation of Y58 to alanine in BCL6 prevents BI-3802 binding in vitro.
The non-cullin E3 ubiquitin ligase SIAH1 is involved in degradation of polymerized BCL6, BI-3802 increased the interaction between BCL6 and SIAH1 (EC50=64 nM) both in vitro and in cells.

物理化学性质&存储条件

分子量 484.985
分子式 C24H29ClN6O3
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

2-((6-((5-chloro-2-((3S,5R)-3,5-dimethylpiperidin-1-yl)pyrimidin-4-yl)amino)-1-methyl-2-oxo-1,2-dihydroquinolin-3-yl)oxy)-N-methylacetamide

参考文献

1. Kerres N, et al. Cell Rep. 2017 Sep 19;20(12):2860-2875.
2. Mikołaj Słabicki, et al. Nature. 2020 Dec;588(7836):164-168.

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