Name | ZXH-4-130 TFA |
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Description | ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC)[1]. |
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Related Catalog | |
Target |
VHL |
In Vitro | 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]. |
References |
Molecular Formula | C48H59F3N6O11S |
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Molecular Weight | 985.08 |