BI-3802 is a highly potent BCL6 degrader and inhibits the Bric-à-brac (BTB) domain of BCL6 with an IC 50 of ≤3 nM. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1. BI-3802 has antitumor activity.
性状
Solid
IC50 & Target[1][2]
IC50: ≤ 3 nM (BCL6 BTB)
体外研究(In Vitro)
BI-3802 shows an IC50 of 43 nM for the cellular BCL6.BI-3802 increases the interaction between BCL6 and SIAH1 (EC50 = 64 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Kerres N, et al. Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6. Cell Rep. 2017 Sep 19;20(12):2860-2875.[2]. Miko?aj S?abicki, et al. Small-molecule-induced polymerization triggers degradation of BCL6. Nature. 2020 Nov 18.
溶解度数据
In Vitro: DMSO : 6.67 mg/mL (13.75 mM; ultrasonic and warming and heat to 60°C)配制储备液