ZXH-4-130
Based on 2 publication(s) in Google Scholar
ZXH-4-130 is a potent and selective Cereblon (CRBN) degrader. ZXH-4-130 recruits the VHL E3 ligase to specifically target CRBN as a substrate for selective degradation as a hetero-PROTAC molecule. ZXH-4-130 can be applied in studies on the biological functions of CRBN and related research of frontotemporal dementia.
(Pink: Cereblon ligand (HY-14658); Blue: VHL ligand (HY-125845); Black: linker (HY-W142804)).
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- Pureté: 99.70%
- CAS No.: 2711006-66-3
- Formule: C46H58N6O9S
- Masse moléculaire:871.05
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Stockage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ZXH-4-130
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Activité biologique
Description
IC50 & Target
[1]|
Cereblon |
VHL |
In Vitro
ZXH-4-130 (10-500 nM; 1-24 h) potently and selectively degrades CRBN in MM1.S cells[1].
ZXH-4-130 (50-100 nM; 6-24 h) exhibits high selectivity for CRBN in Kelly, SK-N-DZ, HEK293T, and MOLT-4 cell lines, and does not affect the expression of other components (DDB1, CUL4A, ROC1) of the CRBN E3 ligase complex[1].
ZXH-4-130 (50 nM; 2 h) mediates CRBN knockdown in MM1.S cells and blocks CC-885 (HY-101488)-induced, CRBN-dependent GSPT1 degradation[1].
ZXH-4-130 (0.1 μM; 2 h) partially blocks THAL-SNS-032 (HY-123937)-induced degradation of CDK9 in MOLT-4 cells[1].
ZXH-4-130 (100 nM; 2 h pretreatment) significantly reverses the decrease in cell viability induced by Pomalidomide (HY-10984) (1 μM; 96 h) in MM1.S cells[1].
ZXH-4-130 (1 μM; 6 h pre-incubation + 24 h co-treatment) blocks the rescue effect of QC-01-175 (HY-134850) on the LDL-induced increase in the p-tau/total tau ratio in P301L tau induced pluripotent stem cell (iPSC)-derived neurons, indicating that ZXH-4-130 inhibits the Cereblon-dependent activity of QC-01-175[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM1.S
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Concentration:10, 50, 100, 500 nM
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Incubation Time:1, 2, 4, 8, 16, 24 h
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Result:Potently and dose-dependently degraded CRBN to an extent comparable to CRBN-6-5-5-VHL and superior to St-15a.
Induced sustained CRBN degradation, exhibiting maximal degradative activity between 2 and 8 hours.
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Cell Line:MM1.S
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Concentration:100 nM pre-treatment for 2 h, followed by 1 μM Pomalidomide
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Incubation Time:96 h
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Result:Significantly blocked pomalidomide-induced cytotoxicity, restoring cell viability.
Chemical Information
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CAS No. 2711006-66-3
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Appearance Solid
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Masse moléculaire 871.05
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
Solvant et solubilité
In Vitro:
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)
Pureté et documentation
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Fiche technique (284 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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Instruction de manipulation (2659 KB)
Références
[1]. Powell CE, et al. Selective degradation-inducing probes for studying cereblon (CRBN) biology. RSC medicinal chemistry. 2021 Aug 18;12(8):1381-1390. [Content Brief]
[2]. Lam M, et al. Cholesterol Dysregulation Drives Seed-Dependent Tau Aggregation in Patient Stem Cell-Derived Models of Tauopathy. bioRxiv [Preprint]. 2023 Dec 12:2023.12.11.571147. [Content Brief]
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 |
ZXH-4-130 Related Classifications
HY-132857 Related Classifications
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