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首页-小分子抑制剂&激动剂-Apoptosis-Bcl-2-WK692
WK692

Chemical Structure : WK692

CAS No.: 2694055-38-2

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WK692 (WK-692)

货号: PC-23130Not For Human Use, Lab Use Only.

WK692 is a specific small molecule BCL6 inhibitor, directly binds to BCL6 BTB domain (SPR, KD=324 nM), disrupts BCL6BTB/SMRT interaction (IC50=16 nM) and activates the expression of BCL6 downstream genes in cancer cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

WK692 is a specific small molecule BCL6 inhibitor, directly binds to BCL6 BTB domain (SPR, KD=324 nM), disrupts BCL6BTB/SMRT interaction (IC50=16 nM) and activates the expression of BCL6 downstream genes in cancer cells.
WK692 is specific for BCL6 rather than other BTB-zinc finger proteins, attenuates BCL6-mediated transcriptional repression but had minimal impact on other BTB proteins.
WK692 disrupts BCL6BTB/SMRT complex formation and activates BCL6 downstream genes expression. 
WK692 inhibits cells proliferation at IC50 1-5 µM for GCB-DLBCL cell lines including SUDHL4, SUDHL6, OCI-LY7, Farage and DOHH2.
WK692 abrogates germinal center formation in vivo, effectively inhibits lymphoma growth with no toxic side effects in vivo
WK692 inhibits the DLBCL growth without toxic effects in vivo and synergizes with the EZH2 and PRMT5 inhibitors.

物理化学性质&存储条件

分子量 692.37
分子式 C26H28Br2N8O5
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

(R)-(1-(7-((3-(2-(2-bromoacetamido)ethoxy)-1-methyl-2-oxo-1,2-dihydroquinolin-6-yl)amino)-[1,2,4]triazolo[1,5-a]pyrimidin-5-yl)pyrrolidin-2-yl)methyl 2-bromoacetate

参考文献

1. Xing Y, et al. Mol Cancer Ther. 2024 Oct 10. doi: 10.1158/1535-7163.MCT-23-0830.

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