CCT367766
CCT367766 is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein.
(Pink: Pirin ligand (HY-184542); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2229856-58-8
- Formula: C49H48ClN7O11
- Molecular Weight:946.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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CRBN-DDB1 490 nM (IC50) |
CCT367766 (50-1500 nM; 24 hours) demonstates the depletion of pirin protein as a the time-dependent hook-effect in SK-OV-3 human ovarian cancer cells[1]. CCT367766 (0.5-50 nM; 2 hours) demonstrates the concentration-dependent depletion of pirin protein after 2 h exposure in SK-OV-3 cells[1]. CCT367766 (0.5-50 nM; 2 hours) dose-dependently rescuses pirin expression from pretreatment of chlorobisamide in SK-OV-3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-OV-3 human ovarian cancer cells
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Concentration:50, 150, 250, 500 and 1500 nM
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Incubation Time:2 hours, 4 hours, 24 hours
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Result:Decreased pirin protein expression.
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Cell Line:SK-OV-3 human ovarian cancer cells
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Concentration:0.5, 1, 2.5, 5, 7.5, 10, 25, and 50 nM
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Incubation Time:2 hours
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Result:Completely degraded pirin just at 50 nM treatment.
Chemical Information
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CAS No. 2229856-58-8
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Molecular Weight 946.40
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Formula C49H48ClN7O11
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SMILES
O=C(C1=CC=C2N=C(CN3CCN(CCOCCOCCOC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)CC3)C=CC2=C1)NC7=CC(NC(C8=CC=C(OCCO9)C9=C8)=O)=CC=C7Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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