ZXH-4-130
Based on 2 publication(s) in Google Scholar
ZXH-4-130 is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC).
(Pink: Cereblon ligand (HY-14658); Blue: VHL ligand (HY-125845); Black: linker (HY-W142804)).
For research use only. We do not sell to patients.
- Purity: 99.70%
- CAS No.: 2711006-66-3
- Formula: C46H58N6O9S
- Molecular Weight:871.05
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications Citing Use of MedChemExpress (MCE) ZXH-4-130
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Biological Activity
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VHL |
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.
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Cell Line:MM1.S cells
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Concentration:100 nM
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Incubation Time:2 h pre-treatments; followed by 96-hour treatment with 1 μM of Pomalidomide
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Result:Prevented Pomalidomide cytotoxicity to a significant extent, ZXH-4-130 has statistically significant amounts of prevention.
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Cell Line:MM1.S cells
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Concentration:50 nM
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Incubation Time:2 h pretreatment with ZXH-4-130, followed by 4 h treatment with CC-885
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Result:Rescued GSPT1 degradation.
Chemical Information
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CAS No. 2711006-66-3
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Appearance Solid
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Molecular Weight 871.05
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Formula C46H58N6O9S
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Med Chem
Discovery and Characterization of a First-In-Class HCK/BTK PROTAC DFCI-002-06 for the Treatment of MYD88 Mutated B Cell Malignancies. [Abstract]2026 Jan 22;69(2):1119-1134. PMID: 41482966 -
bioRxiv
Cholesterol Dysregulation Drives Seed-Dependent Tau Aggregation in Patient Stem Cell-Derived Models of Tauopathy. [Abstract]2023 Dec 12:2023.12.11.571147. PMID: 38168389
Solvent & Solubility
DMSO : 25 mg/mL (28.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1480 mL | 5.7402 mL | 11.4804 mL | 28.7010 mL |
| 5 mM | 0.2296 mL | 1.1480 mL | 2.2961 mL | 5.7402 mL | |
| 10 mM | 0.1148 mL | 0.5740 mL | 1.1480 mL | 2.8701 mL | |
| 15 mM | 0.0765 mL | 0.3827 mL | 0.7654 mL | 1.9134 mL | |
| 20 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4350 mL | |
| 25 mM | 0.0459 mL | 0.2296 mL | 0.4592 mL | 1.1480 mL |