ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). ZXH-4-130 TFA induces ~80% CRBN degradation at 10 nM in MM1.S cells.
性状
Solid
IC50 & Target[1][2]
VHL
体外研究(In Vitro)
ZXH-4-130 (100 nM; 2 h pre-treatment; followed by 96-hour treatment with 1 μM of Pomalidomide) TFA prevents Pomalidomide (1 μM) cytotoxicity to a significant extent, ZXH-4-130 TFA has statistically significant amounts of prevention.ZXH-4-130 TFA (pretreatment with 50 nM) rescues GSPT1 degradation induced by CC-885 in MM1.S cells.ZXH-4-130 (100 nM; 2 h pre-treatment; followed by 6 h treatment with THAL-SNS-032)TFA induces nearly complete CRBN degradation, but THAL-SNS-032s activity against CDK9 is only partially prevented. 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
-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Chelsea E Powell, et al. Selective degradation-inducing probes for studying cereblon (CRBN) biology. RSC Med Chem. 2021 Jul 6;12(8):1381-1390.
溶解度数据
In Vitro: DMSO : 170 mg/mL (172.57 mM; Need ultrasonic)配制储备液