2. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease Apoptosis
  3. PARP NAMPT DNA/RNA Synthesis Apoptosis
  4. 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).

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PARP1/NAMPT-IN-1

PARP1/NAMPT-IN-1 Chemical Structure

CAS No. : 3084810-86-3

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PARP1/NAMPT-IN-1 Related Antibodies

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

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)[1].

IC50 & Target[1]

PARP1

1.2 nM (IC50)

NAMPT

6.7 nM (IC50)

In Vitro

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.

PARP1/NAMPT-IN-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.3 μM, 1 μM
Incubation Time: 48 h
Result: Dose-dependently arrested MDA-MB-231 cells at G2/M phase with a low concentration (0.3 μM).

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.3 μM, 1 μM
Incubation Time: 48 h
Result: Induced a dose-dependent increase in apoptosis.
Upregulated pro-apoptotic Bax and cleaved PARP while downregulating antiapoptotic Bcl-2.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.3 μM, 1 μM
Incubation Time: 48 h
Result: Induced significantly higher nuclear γH2AX levels.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.3 μM, 1 μM
Incubation Time: 48 h
Result: Significantly suppressed expression of all tested HRR components (BRCA1, CtIP, Mre11, RAD51, p-RPA32).

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells
Concentration: 0.3 μM, 1 μM
Incubation Time: 48 h
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).

Western Blot Analysis[1]

Cell Line: 4T1 cells and MDA-MB-231 cells
Concentration: 0.3 μM, 1 μM
Incubation Time: 48 h
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.
In Vivo

PARP1/NAMPT-IN-1 (compound 10 n) (5-10 mg/kg; i.p.; once a day; for 14 days) has antitumor efficacy with a good safety profile in MDA-MB-231 xenograft models[1].
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.

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].
Dosage: 5 mg/kg, or 10 mg/kg
Administration: Intraperitoneal (IP) injection; once daily; for 14 days
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.
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].
Dosage: 5 mg/kg
Administration: Intraperitoneal (IP) injection; once daily; for 5 days
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.
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].
Dosage: 5 mg/kg
Administration: Intraperitoneal (IP) injection; once daily; for 14 days
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.
Molecular Weight

602.66

Formula

C35H31FN6O3
CAS No.
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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References
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PARP1/NAMPT-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PARP1/NAMPT-IN-13084810-86-3PARPNAMPTDNA/RNA SynthesisApoptosispoly ADP ribose polymerase Nicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorPARP1 and NAMPT inhibitordisrupt the homologous recombination repair (HRR) pathwayDNA double-strand (dsDNA) breakscell cycle arrest and apoptosistriple-negative breast cancer (TNBC)MDA-MB-231 cells4T1 cellsInhibitorinhibitorinhibit

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