PARP1/ERK IN-1
PARP1/ERK IN-1 is a dual PARP1/ERK inhibitor, with a PARP1 IC50 of 0.9 nM and an ERK2 IC50 of 1.8 nM. PARP1/ERK IN-1 inhibits proliferation and migration of various cancer cell lines, and induces apoptosis and DNA damage. PARP1/ERK IN-1 suppresses tumor growth in mouse models of colorectal cancer, and reduces the expression of Ki‑67, BRCA1 and Rad51. PARP1/ERK IN-1 can be used in the research of colorectal cancer, triple-negative breast cancer and pancreatic cancer.
For research use only. We do not sell to patients.
- Formula: C23H19FN8O2
- Molecular Weight:458.45
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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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ERK2 1.8 nM (IC50) |
PARP1 0.9 nM (IC50) |
PARP1/ERK IN-1 (I-16) (7 days) inhibits the proliferation of various cancer cell lines, with IC50 values of 0.41 μM for HCT116, 2.58 μM for HT29, 5.51 μM for CFPAC-1, and 2.13 μM for W1990, and exhibits extremely low toxicity toward normal MCF-10A and AML-12 cells[1].
PARP1/ERK IN-1 (0.25-1 μM; 7 days) decreases the protein levels of PARP1 and p-ERK1/2 in a concentration-dependent manner and impairs the DNA repair pathway in HCT116 cells[1].
PARP1/ERK IN-1 (100 μM; 6-8 h) directly binds to PARP1 and ERK proteins in HCT116 cell lysates and increases their thermal stability[1].
PARP1/ERK IN-1 (0.25-1 μM; 0-14 days) inhibits long-term colony formation of HCT116 cells in a dose-dependent manner and suppresses the directional migration of HCT116 cells[1].
PARP1/ERK IN-1 (0.25-1 μM; 7 days) induces apoptosis in HCT116 cells in a dose-dependent manner, arrests cells at the G2/M phase of the cell cycle, and induces significant DNA damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116
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Concentration:0.25, 0.5, 1 μM
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Incubation Time:7 days
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Result:Concentration-dependently reduced PARP1, p-ERK1/2, p-p90RSK1, BRCA1, and Rad51 protein levels, while increasing γH2AX protein levels.
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Cell Line:HCT116
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Concentration:0.25, 0.5, 1 μM
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Incubation Time:14 days
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Result:Markedly inhibited colony formation in a dose-dependent manner, with greater potency than Olaparib, BVD-523, or their combination.
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Cell Line:HCT116
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Concentration:0.25, 0.5, 1 μM
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Incubation Time:Up to 48 h；12, 24, or 48 h
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Result:Concentration-dependently inhibited wound closure, with effects at 1 μM surpassing those of the Olaparib and BVD-523 combination.
Potently suppressed cell migration in a time- and dose-dependent manner, with stronger efficacy than Olaparib or BVD-523 alone at tested concentrations in a Transwell model.
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Cell Line:HCT116
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Concentration:0.25, 0.5, 1 μM
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Incubation Time:7 days
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Result:Induced dose-dependent increase in apoptosis, with an apoptosis rate of 39.67% at 1 μM, significantly higher than the Olaparib-BVD-523 combination.
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Cell Line:HCT116
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Concentration:0.25, 0.5, 1 μM
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Incubation Time:7 days
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Result:Arrested cells in the G2/M phase in a dose-dependent manner, with 1 μM treatment resulting in 30.25% of cells in G2/M phase.
| Species | Dose | Route | AUC0-t | AUC0-inf | Cmax | Tmax | T1/2 | Vdss | CL |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 527.3 ng·h/mL | 532.1 ng·h/mL | 3126.7 ng/mL | 0.033 h | 0.86 h | 2.39 L/kg | 1.91 L/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 6-week-old, 18-22 g, HCT116 cell xenograft)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 21 days
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Result:Achieved tumor growth inhibition (TGI) rate of 57.7% at 20 mg/kg, superior to Olaparib (50 mg/kg, TGI=37.0%) and BVD-523 (5 mg/kg, TGI=45.8%), and comparable to Olaparib + BVD-523 combination (TGI=54.2%).
Showed no significant body weight loss across all treatment groups.
Reduced Ki-67 expression in 20 mg/kg group tumor tissues, indicating inhibited tumor cell proliferation.
Reduced BRCA1 and Rad51 expression in 20 mg/kg group tumor tissues.
Markedly reduced PARP1 and p-ERK1/2 fluorescence signal intensity in 20 mg/kg group tumor tissues.
Chemical Information
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Molecular Weight 458.45
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Formula C23H19FN8O2
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SMILES
O=C(NC1=CC2=C(C=N1)C(C3=CC=C(C=C3)F)=NN2)N[C@@H](C4=NC5=C(N4)C=CC=C5C(N)=O)C
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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/ERK IN-1 Related Classifications
HY-181842 Related Classifications
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