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ZXH-4-130 

Cat. No.: HY-132857
Handling Instructions

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

For research use only. We do not sell to patients.

ZXH-4-130 Chemical Structure

ZXH-4-130 Chemical Structure

CAS No. : 2711006-66-3

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Description

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

IC50 & Target[1]

VHL

 

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 rescued 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].

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

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.
Molecular Weight

871.05

Formula

C₄₆H₅₈N₆O₉S

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Product Name:
ZXH-4-130
Cat. No.:
HY-132857
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