2. Cell Cycle/DNA Damage Epigenetics Stem Cell/Wnt MAPK/ERK Pathway Apoptosis
  3. PARP ERK Apoptosis
  4. 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.

PARP1/ERK IN-1

PARP1/ERK IN-1 Chemical Structure

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PARP1/ERK IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

ERK2

1.8 nM (IC50)

PARP1

0.9 nM (IC50)

In Vitro

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.

PARP1/ERK IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT116
Concentration: 0.25, 0.5, 1 μM
Incubation Time: 7 days
Result: Concentration-dependently reduced PARP1, p-ERK1/2, p-p90RSK1, BRCA1, and Rad51 protein levels, while increasing γH2AX protein levels.

Cell Proliferation Assay[1]

Cell Line: HCT116
Concentration: 0.25, 0.5, 1 μM
Incubation Time: 14 days
Result: Markedly inhibited colony formation in a dose-dependent manner, with greater potency than Olaparib, BVD-523, or their combination.

Cell Migration Assay [1]

Cell Line: HCT116
Concentration: 0.25, 0.5, 1 μM
Incubation Time: Up to 48 h；12, 24, or 48 h
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.

Apoptosis Analysis[1]

Cell Line: HCT116
Concentration: 0.25, 0.5, 1 μM
Incubation Time: 7 days
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.

Cell Cycle Analysis[1]

Cell Line: HCT116
Concentration: 0.25, 0.5, 1 μM
Incubation Time: 7 days
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.
Parmacokinetics
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
In Vivo

PARP1/ERK IN-1 (5-20 mg/kg; i.p.; once daily; 21 days) inhibits colorectal cancer tumor growth in a dose-dependent manner in the HCT116 xenograft mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (male, 6-week-old, 18-22 g, HCT116 cell xenograft)[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: i.p.; daily; 21 days
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.
Molecular Weight

458.45

Formula

C23H19FN8O2
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PARP1/ERK 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/ERK IN-1PARPERKApoptosispoly ADP ribose polymerase Extracellular signal regulated kinasesHCT116 cellsxenograft modelsMCF-10A cellsBRCA-wild-type modelscolorectal cancerpancreatic cancerPARP1BRCA mutant modelsERK2triple-negative breast cancerInhibitorinhibitorinhibit

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