Bioactivity | 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[1]. |
Invitro | 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[1].ZXH-4-130 TFA (pretreatment with 50 nM) rescues GSPT1 degradation induced by CC-885 in MM1.S cells[1].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-032's activity against CDK9 is only partially prevented[1]. |
Name | ZXH-4-130 TFA |
CAS | 2711006-67-4 |
Formula | C48H59F3N6O11S |
Molar Mass | 985.08 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -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) |
Reference | [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. |