| Bioactivity | ZXH-4-130 is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC)[1]. |
| Invitro | ZXH-4-130 (100 nM; 2 h pre-treatments; followed by 96-hour treatment with 1 μM of Pomalidomide) prevents Pomalidomide (1 μM) cytotoxicity to a significant extent, ZXH-4-130 has statistically significant amounts of prevention[1].MM1.S cells are pre-treated for 2 h with 50 nM of ZXH-4-130, 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 rescues GSPT1 degradation[1].ZXH-4-130 (100 nM 2 h pre-treatment; followed by 6 h treatment with THAL-SNS-032) induces nearly complete CRBN degradation, but THAL-SNS-032's activity against CDK9 is only partially prevented[1]. Cell Viability Assay[1] Cell Line: |
| Name | ZXH-4-130 |
| CAS | 2711006-66-3 |
| Formula | C46H58N6O9S |
| Molar Mass | 871.05 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. |