ZXH-4-130 是一种高效、选择性的CRBN降解剂。ZXH-4-130 是一种 CRBN-VHL 化合物 (hetero-PROTAC)。
| 生物活性 | ZXH-4-130 is a highly potent and selective degrader ofCRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC)[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | 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: | MM1.S cells | | Concentration: | 100 nM | | Incubation Time: | 2 h pre-treatments; followed by 96-hour treatment with 1 μM of Pomalidomide | | Result: | Prevented Pomalidomide cytotoxicity to a significant extent, ZXH-4-130 has statistically significant amounts of prevention. |
Western Blot Analysis[1] | Cell Line: | MM1.S cells | | Concentration: | 50 nM | | Incubation Time: | 2 h pretreatment with ZXH-4-130, followed by 4 h treatment with CC-885 | | Result: | Rescued GSPT1 degradation. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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