CC-647
Based on 1 Customer Validation
CC-647 is a molecular glue-type cereblon modulator and ZBTB16 degrader. CC-647 primarily utilizes the C2H2 ZnF3 degron of ZBTB16 to promote CRL4CRBN-mediated ubiquitination and proteasomal degradation. CC-647 also induces the degradation of the oncogenic RARα-ZBTB16 fusion protein, while exerting a weaker degrading effect on the reciprocal fusion ZBTB16-RARα. CC-647 can be used in studies related to targeted protein degradation and ZBTB16/RARA-rearranged acute promyelocytic leukemia.
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- Pureté : 99.58%
- CAS No.: 1061605-35-3
- Formule: C23H22N2O5
- Masse moléculaire:406.43
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
ZBTB16 |
In Vitro
CC-647 (0.001-10 μM; 6 h) potently induces proteasomal degradation of ePL-tagged ZBTB16 in HT-1080 cells, with a DC50 of 103 nM, and this activity is dependent on CRBN and the proteasome[1].
CC-647 (1 nM-10 μM; 6 h) induces CRBN- and proteasome-dependent degradation of endogenous ZBTB16 in HEL 92.1.7 cells, reducing protein levels to 12% of that in the vehicle control group at a concentration of 10 μM[1].
CC-647 (10 μM; 6 h) selectively induces the degradation of endogenous ZBTB16 (log2 fold change = -1.25) in KG-1a cells, causes mild degradation of IKZF1, but has no effect on GSPT1 or CSNK1A1[1].
CC-647 promotes robust ubiquitination of ZBTB16 ZnF3 in the CRL4CRBN in vitro ubiquitination system, while the ZnF3 G467A mutation significantly impairs this effect; in HT-1080 ZBTB16-ePL cells, G410A ZBTB16 exhibits a degradation response to CC-647 similar to that of WT, whereas G467A ZBTB16 shows significant resistance to degradation, indicating that CC-647 mainly utilizes the ZnF3 structural degron to induce ZBTB16 degradation[1].
C-647 (6 h; HT-1080 RARα-ZBTB16-ePL cells) reduces the level of RARα-ZBTB16 fusion protein in a dose-dependent manner, with a Ymin of 55; this effect can be reversed by 1 μM MLN4924 (HY-70062) or 10 μM Bortezomib (HY-10227), while the ZnF3 G467A mutation prevents CC-647-induced degradation of RARα-ZBTB16[1].
CC-647 promotes ubiquitination of recombinant RARα-ZBTB16 in the CRL4CRBN in vitro ubiquitination system, while the ZnF3 G467A mutation blocks this effect, supporting that the ZnF3 degron of RARα-ZBTB16 mediates its CRBN-dependent ubiquitination and proteasomal degradation[1].
CC-647 exhibits no obvious degradation effect on the ZBTB16-RARα fusion protein containing ZBTB16 ZnF1 but lacking ZnF3, nor does it significantly promote ubiquitination of recombinant ZBTB16-RARα, indicating that CC-647 shows degron-dependent differences toward distinct ZBTB16/RARα reciprocal fusions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEL 92.1.7 human erythroleukemia cells
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Concentration:1 nM-10 μM (single treatment);
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Incubation Time:6 h
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Result:Dose-dependently reduced endogenous ZBTB16; 10 μM reduced relative ZBTB16 to approximately 12%.
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Cell Line:HEL 92.1.7 human erythroleukemia cells
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Concentration:10 μM CC-647+ 1 μM MLN4924; 10 μM CC-647 + 10 μM MG132
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Incubation Time:6 h
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Result:MLN4924 or MG132 blocked endogenous ZBTB16 degradation.
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Cell Line:CRBN knockout (KO) HEL 92.1.7 cells
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Concentration:(co-treatment); 10 μM (CRBN KO cells)
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Incubation Time:6 h
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Result:CRBN knockout suppressed CC-647-mediated endogenous ZBTB16 degradation.
Chemical Information
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CAS No. 1061605-35-3
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Appearance Solid
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Masse moléculaire 406.43
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Formule C23H22N2O5
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Color White to off-white
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SMILES
O=C1C2=C(C(N1C3C(NC(CC3)=O)=O)=O)C(OC4=CC=CC(C(C)(C)C)=C4)=CC=C2
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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 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 35 mg/mL (86.12 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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 (286 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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. 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 | 2.4604 mL | 12.3022 mL | 24.6045 mL | 61.5112 mL |
| 5 mM | 0.4921 mL | 2.4604 mL | 4.9209 mL | 12.3022 mL | |
| 10 mM | 0.2460 mL | 1.2302 mL | 2.4604 mL | 6.1511 mL | |
| 15 mM | 0.1640 mL | 0.8201 mL | 1.6403 mL | 4.1007 mL | |
| 20 mM | 0.1230 mL | 0.6151 mL | 1.2302 mL | 3.0756 mL | |
| 25 mM | 0.0984 mL | 0.4921 mL | 0.9842 mL | 2.4604 mL | |
| 30 mM | 0.0820 mL | 0.4101 mL | 0.8201 mL | 2.0504 mL | |
| 40 mM | 0.0615 mL | 0.3076 mL | 0.6151 mL | 1.5378 mL | |
| 50 mM | 0.0492 mL | 0.2460 mL | 0.4921 mL | 1.2302 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4101 mL | 1.0252 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3076 mL | 0.7689 mL |
CC-647 Related Classifications
HY-173614 Related Classifications
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