2. PROTAC
  3. PROTACs
  4. 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).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (ZXH-4-130 TFA) usually boasts enhanced water solubility and stability.

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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ZXH-4-130 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE ZXH-4-130

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

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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 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.

ZXH-4-130 Related Antibodies

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.
SMILES

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ZXH-4-130 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZXH-4-1302711006-66-3PROTACsInhibitorinhibitorinhibit

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