ZXH-4-130 

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

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

871.05

C₄₆H₅₈N₆O₉S

2711006-66-3

Solid

White to off-white

O=C([C@H]1N(C([C@@H](NC(CCCCCCCCCCOC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]