CC0651
Based on 1 Customer Validation
CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.
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- Pureté : 98.83%
- CAS No.: 1319207-44-7
- Formule: C20H21Cl2NO6
- Masse moléculaire:442.29
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
IC50: 1.72 μM (p27Kip1 ubiquitination)[1]
In Vitro
CC0651 strongly impairs the rate of ubiquitin chain initiation on substrate by SCFCdc4, as measured by the monoubiquitination of Sic1 by K0 ubiquitin. CC0651 actually potentiates the formation of both ubiquitin dimers and monoubiquitinated hCdc34, concordant with the observed accumulation of the hCdc34 conjugate in cells treated with the ester derivative of CC0651. CC0651 completely inhibits the assembly of polyubiquitin chains and decreased formation of free triubiquitin and, to a lesser extent, hCdc34 monoubiquitin, but has no effect on production of diubiquitin[1]. CC0651 is an inhibitor of the E2 ubiquitin conjugating enzyme Cdc34A, acts by trapping a weak interaction between ubiquitin and the E2 donor ubiquitin binding site. A quantitative SCF ubiquitination assay with a β-Catenin substrate peptide yields a value of IC50 of 18±1 μM for CC0651 inhibition, similar to the effective concentrations observed in the NMR and TR-FRET assays[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1319207-44-7
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Appearance Solid
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Masse moléculaire 442.29
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Formule C20H21Cl2NO6
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Color White to off-white
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SMILES
ClC1=CC(Cl)=CC(C2=CC=C(C=C2)C[C@@H]([C@@H]([C@H](C(O)=O)O)O)NC(COC)=O)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
In Vitro:
DMSO : ≥ 56 mg/mL (126.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ceccarelli DF, et al. An allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. Cell. 2011 Jun 24;145(7):1075-87. [Content Brief]
[2]. Huang H, et al. E2 enzyme inhibition by stabilization of a low-affinity interface with ubiquitin. Nat Chem Biol. 2014 Feb;10(2):156-63. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2610 mL | 11.3048 mL | 22.6096 mL | 56.5240 mL |
| 5 mM | 0.4522 mL | 2.2610 mL | 4.5219 mL | 11.3048 mL | |
| 10 mM | 0.2261 mL | 1.1305 mL | 2.2610 mL | 5.6524 mL | |
| 15 mM | 0.1507 mL | 0.7537 mL | 1.5073 mL | 3.7683 mL | |
| 20 mM | 0.1130 mL | 0.5652 mL | 1.1305 mL | 2.8262 mL | |
| 25 mM | 0.0904 mL | 0.4522 mL | 0.9044 mL | 2.2610 mL | |
| 30 mM | 0.0754 mL | 0.3768 mL | 0.7537 mL | 1.8841 mL | |
| 40 mM | 0.0565 mL | 0.2826 mL | 0.5652 mL | 1.4131 mL | |
| 50 mM | 0.0452 mL | 0.2261 mL | 0.4522 mL | 1.1305 mL | |
| 60 mM | 0.0377 mL | 0.1884 mL | 0.3768 mL | 0.9421 mL | |
| 80 mM | 0.0283 mL | 0.1413 mL | 0.2826 mL | 0.7065 mL | |
| 100 mM | 0.0226 mL | 0.1130 mL | 0.2261 mL | 0.5652 mL |
CC0651 Related Classifications
HY-15301 Related Classifications
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