ZXH-4-130 TFA

ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC)[1].

Signaling Pathways >> PROTAC >> PROTAC

Research Areas >> Neurological Disease

VHL

ZXH-4-130 (100 nM; 2 h pre-treatments; 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]. MM1.S cells are pre-treated for 2 h with 50 nM of ZXH-4-130 TFA, before exposing them to CC-885, a compound that induces G1 to S phase transition protein 1 (GSPT1) degradation via CRBN E3 ligase recruitment. Pretreatment with 50 nM of ZXH-4-130 TFA rescues GSPT1 degradation[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].

[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.