BCL6 inhibitor YK01

Chemical Structure : BCL6 inhibitor YK01

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货号: PC-25337Not For Human Use, Lab Use Only.

BCL6 inhibitor YK01 is a potent, specific small molecule inhibitor of BCL6-BTB with binding IC50 of 11.7 nM, directly binds to BCL6BTB with SPR KD of 148 nM, inhibits BCL6 transcriptional activity.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

BCL6 inhibitor YK01 is a potent, specific small molecule inhibitor of BCL6-BTB with binding IC50 of 11.7 nM, directly binds to BCL6BTB with SPR KD of 148 nM, inhibits BCL6 transcriptional activity.
YK01 inhibited BCL6-BTB domain repression but did not affect the BTB domains associated with the Kaiso and PLZF proteins.
YK01 inhibits the proliferation of glioma cells with high BCL6 expression in vitro (U87-MG, IC50=0.66 uM).
YK01 reactivates BCL6 downstream genes and induces apoptosis in GBM cells. YK01 induces the degradation of BCL6 and inhibits the activation of AKT and ERK and promotes the enhancement of the DNA damage response by blocking the ability of BCL6 to inhibit cell proliferation.
YK01 (12.5 mg/kg/d) inhibits tumor growth in U87-MG xenograft mouse models.
YK01 combined with temozolomide (TMZ) can synergically inhibit glioblastoma multiforme growth.

物理化学性质&存储条件

分子量	498.34
分子式	C21H20BrN7O3
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-bromo-N-(1-(7-((2-oxo-2H-chromen-6-yl)amino)-[1,2,4]triazolo[1,5-a]pyrimidin-5-yl)piperidin-3-yl)acetamide

参考文献

1. Wu M, et al. Genes Dis. 2025 Apr 15;12(6):101644.