PARP1/NAMPT-IN-1
PARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC50 values of 1.2 nM and 6.7 nM, respectively. PARP1/NAMPT-IN-1 can disrupt the homologous recombination repair (HRR) pathway, leading to the accumulation of DNA double-strand breaks (DSBs), inducing cell cycle arrest and apoptosis, and also has antimigratory effects. PARP1/NAMPT-IN-1 exhibits excellent antitumor effects in a breast cancer xenograft model. PARP1/NAMPT-IN-1 can be used for the study of triple-negative breast cancer (TNBC).
For research use only. We do not sell to patients.
- CAS No.: 3084810-86-3
- Formula: C35H31FN6O3
- Molecular Weight:602.66
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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
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Biological Activity
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PARP1 1.2 nM (IC50) |
NAMPT 6.7 nM (IC50) |
PARP1/NAMPT-IN-1 (compound 10 n) (24 h-7 days) shows selective antiproliferative activity against MDA-MB-231 cells (IC50 = 1.28 nM) and MDA-MB-468 cells (IC50 = 0.46 nM). PARP1/NAMPT-IN-1 shows the negligible cytotoxic effects (IC50 > 20 μM) against MCF-10A cells[1].
PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) induces cell cycle arrest and apoptosis in MDA-MB-231 cells[1].
PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) disrupts HRR pathway to induce synthetic lethality and rrigger DSBs in MDA-MB-231 cells[1].
PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) exhibits marked antimigratory effects in MDA-MB-231 cells[1].
PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) significantly increases cGAS level and phosphorylation of STING, TBK1, and IRF3 in 4T1 cells in vitro, suggesting its intratumoral activation of STING signaling pathway[1].
PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) enhances TBK1 and IRF3 phosphorylation in MDA-MB-231 cells[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 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Dose-dependently arrested MDA-MB-231 cells at G2/M phase with a low concentration (0.3 μM).
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Cell Line:MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Induced a dose-dependent increase in apoptosis.
Upregulated pro-apoptotic Bax and cleaved PARP while downregulating antiapoptotic Bcl-2.
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Cell Line:MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Induced significantly higher nuclear γH2AX levels.
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Cell Line:MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Significantly suppressed expression of all tested HRR components (BRCA1, CtIP, Mre11, RAD51, p-RPA32).
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Cell Line:MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Inhibited MDA-MB-231 cell migration.
Potently downregulated the promigratory markers MMP2 and N-cadherin (typically elevated in epithelial-mesenchymal transition (EMT)) while upregulating E-cadherin (an epithelial marker associated with reduced motility that is frequently lost in EMT).
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Cell Line:4T1 cells and MDA-MB-231 cells
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Concentration:0.3 μM, 1 μM
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Incubation Time:48 h
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Result:Significantly increased cGAS level and phosphorylation of STING, TBK1, and IRF3 in 4T1 cells.
Enhanced TBK1 and IRF3 phosphorylation in MDA-MB-231 cells.
PARP1/NAMPT-IN-1 (5 mg/kg; i.p.; once a day; for 5 days) effectively inhibits in 4T1 mouse xenograft models[1].
PARP1/NAMPT-IN-1 (5 mg/kg; i.p.; once a day; for 14 days) activates the STING pathway to drive antitumor immunity in 4T1murine BRCA wild-Type TNBC model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice (6-8 weeks old), received subcutaneous injections of MDA-MB-231 cells (5 × 106 cells per mouse in 0.1 mL PBS) in the right flank[1].
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Dosage:5 mg/kg, or 10 mg/kg
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Administration:Intraperitoneal (IP) injection; once daily; for 14 days
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Result:At 5 mg/kg achieved a notable tumor growth inhibition (TGI = 59.98%).
No significant weight loss or mortality at 5 mg/kg.
At 10 mg/kg, significantly enhanced TGI to 83.37%, while maintaining a favorable safety profile, as evidenced by no mortality and significant weight loss.
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Animal Model:Female immunocompetent BALB/c mice (6-8 weeks old) were intravenously injected with 4T1 cells (5 × 105 cells per mouse in 0.1 mL PBS)[1].
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Dosage:5 mg/kg
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Administration:Intraperitoneal (IP) injection; once daily; for 5 days
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Result:Markedly reduced the formation of lung metastatic nodules compared to the control group.
H&E staining revealing significantly fewer metastatic lesions in lung tissues.
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Animal Model:Female immunocompetent BALB/c mice (6-8 weeks old) were intravenously injected with 4T1 cells (5 × 105 cells per mouse in 0.1 mL PBS)[1].
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Dosage:5 mg/kg
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Administration:Intraperitoneal (IP) injection; once daily; for 14 days
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Result:Demonstrated excellent antitumor efficacy (TGI = 70.18%) without significant weight loss or mortality.
Significantly reduced proliferation (Ki67 IHC) and caused extensive tissue destruction (H&E).
Markedly increased tumor-infiltrating CD3+ and CD8+ T cells.
Suppressed the recruitment of MDSCs, evidenced by reduced coexpression of CD11b and Ly6G in multiplex immunofluorescence staining.
Significantly elevated cGAS levels and phosphorylation of STING, TBK1, and IRF3.
Chemical Information
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CAS No. 3084810-86-3
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Molecular Weight 602.66
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Formula C35H31FN6O3
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SMILES
O=C1C2=CC=CC=C2C(CC3=CC(C(N4CCC(CC4)C5=CC=C(C=C5)NC(N6CC7=C(C6)C=NC=C7)=O)=O)=C(C=C3)F)=NN1
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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/NAMPT-IN-1 Related Classifications
HY-181254 Related Classifications
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