PARP1-IN-12
PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells.
For research use only. We do not sell to patients.
- Formula: C43H56FN5O5
- Molecular Weight:741.93
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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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PARP-1 2.99 nM (IC50) |
PARP1-IN-12 (compound 20e) (0.1, 0.3, 1 µM; 48 h) exhibits activities of antiproliferation and selectively killing BRCA-deficient cells, can also induce DNA double strand breaks (DSBs) in BRCA-deficient cells in a concentration-dependent manner[1].
PARP1-IN-12 (10 µM, 48 h) enhances the protein levels of phosphorylated Chk1[1].
PARP1-IN-12 (1, 3, 10 µM; 48 h) activats cell cycle checkpoints, then induces G2/M arrest in BRCA-deficient cells and (1, 5, 10 µM; 96 h) also induces MDA-MB-436 cells apoptosis in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:UWB1.289 (BRCA1-deficient), UWB1.289+BRCA1 (BRCA1 restored), MDA-MB-436 (BRCA1-deficient), Capan-1 (BRCA2-deficient) cells
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Concentration:0.1, 0.3, 1 µM
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Incubation Time:48 h
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Result:Showed antiproliferative activity with IC50s of 0.27, 1.43, 0.87, 0.19 µM for UWB1.289, UWB1.289+BRCA1, Capan-1 and MDA-MB-436 cells, respectively.
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Cell Line:MDA-MB-436, Capan-1 cells
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Concentration:10 µM
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Incubation Time:48 h
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Result:Enhanced the protein levels of phosphorylated Chk1 but the levels of corresponding total proteins were not altered.
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Cell Line:Capan-1 cells
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Concentration:1, 3, 10 µM
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Incubation Time:48 h
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Result:Induced G2/M arrest in BRCA-deficient cells in a concentration-dependent manner.
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Cell Line:MDA-MB-436 cells
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Concentration:1, 5, 10 µM
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Incubation Time:96 h
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Result:Caused apoptosis in a concentration-dependent manner in MDA-MB-436 cells.
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Cell Line:MDA-MB-436, Capan-1 cells
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Concentration:0.1, 0.3, 1 µM
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Incubation Time:48 h
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Result:Induced increased levels of γH2AX in a concentration-dependent manner in both MDA-MB-436 and Capan-1 cells.
Chemical Information
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Molecular Weight 741.93
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Formula C43H56FN5O5
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SMILES
FC1=CC=C(CC(C2C=CC=CC23)=NNC3=O)C=C1C(N4CCN(CC4)C(CCCCCCCNCC5C(OC6C5C=C7[C@@](C)(C6)CCC[C@@H]7C)=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)
PARP1-IN-12 Related Classifications
HY-150765 Related Classifications
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