CPP-13
CPP-13 is a selective PARP1 PROTAC degrader with a DC50 of 0.48 nM. CPP-13 induces CRBN-dependent ubiquitination and proteasomal degradation of PARP1. CPP-13 induces DNA damage. CPP-13 inhibits the growth of BRCA-deficient breast cancer and pancreatic cancer. CPP-13 can be used in studies related to BRCA-deficient breast cancer and BRCA-deficient pancreatic cancer.
(Pink: PARP1 Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- Formula: C44H52N10O7
- Molecular Weight:832.95
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PARP1 0.48 nM (DC50) |
Cereblon |
CPP-13 (0.01-1000 nM; 24 h) potently degrades PARP1 in breast cancer MDA-MB-231 cells, with a DC50 of 0.48 nM and a Dmax of up to 90% after 24 h of treatment[1].
CPP-13 (100 nM; 1-24 h) exhibits rapid and potent PARP1 degradation kinetics in breast cancer cells MDA-MB-231 and MDA-MB-436, whereas a slower degradation rate is observed in pancreatic cancer cells Capan-1 treated with 100 nM for up to 24 h[1].
CPP-13 (0.01-1000 nM; 12-24 h) is a selective PARP1 degrader that induces concentration-dependent PARP1 degradation in MDA-MB-231, MDA-MB-436 and Capan-1 cancer cells, without affecting PARP2 levels at concentrations up to 1000 nM[1].
CPP-13 (100 nM-1 μM; 24 h) induces dose-dependent γH2AX foci formation in MDA-MB-436 and Capan-1 cancer cells, where γH2AX serves as a marker of DNA double-strand breaks; the effect is more pronounced in MDA-MB-436 cells following treatment with 1 μM for 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 human breast cancer cells
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Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
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Incubation Time:24 h
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Result:Induced concentration-dependent reduction of PARP1 levels.
Exhibited a half-maximal degradation concentration (DC50) of 0.48 nM.
Achieved a maximum degradation efficacy (Dₘₐₓ) of 90% relative to vehicle control.
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Cell Line:MDA-MB-231, MDA-MB-436, and Capan-1 human cancer cells
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Concentration:100 nM
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Incubation Time:1, 3, 6, 12, 24 h
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Result:Began PARP1 degradation at 1 h, reached >50% reduction by 3 h, and achieved maximal depletion at 12 h, with slight recovery at 24 h in MDA-MB-231 cells.
Achieved 50% PARP1 degradation within 1 h and maximal depletion at 12 h, with more pronounced depletion than MDA-MB-231 cells and slight recovery at 24 h in MDA-MB-436 cells.
Showed significant PARP1 degradation not evident until 6 h and only 50% depletion achieved by 12 h in Capan-1 cells.
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Cell Line:MDA-MB-436 and Capan-1 human cancer cells
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Concentration:100 nM, 1 μM
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Incubation Time:24 h
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Result:Caused no significant γH2AX induction with 100 nM in either cell line.
Significantly upregulated γH2AX levels at 1 μM in both cell lines, with approximately three-fold higher induction in MDA-MB-436 cells than in Capan-1 cells.
Chemical Information
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Molecular Weight 832.95
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Formula C44H52N10O7
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SMILES
CCC1=CC2=C(NC1=O)C=C(C=N2)CN3CCN(CC3)C4=CN=C(C=C4)C(NCCCCCCCC(NCCNC5=CC=CC6=C5C(N(C6=O)C7CCC(NC7=O)=O)=O)=O)=O
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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)
CPP-13 Related Classifications
HY-187176 Related Classifications
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