1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. PARP1-IN-5

PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (PARP1-IN-5 dihydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

PARP1-IN-5 Chemical Structure

PARP1-IN-5 Chemical Structure

CAS No. : 2735645-53-9

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Description

PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer[1].

IC50 & Target[1]

PARP-1

14.7 nM (IC50)

PARP-2

0.9 μM (IC50)

In Vitro

PARP1-IN-5 (0.1~10 μM; A549 cells) can significantly increase the cytotoxicity of CBP on A549 cells in a dose-dependent manner. PARP1-IN-5 (0.1~10 μM; SK-OV-3 cells) decreases the expressions of MCM2-7. PARP1-IN-5 (0.1~320 μM; A549 cells) has little cytotoxic effects on A549 cells. PARP1-IN-5 (SK-OV-3 cells) can significantly decrease the PAR level[1].
PARP1-IN-5 exerts antitumor effects through PARP-1. PARP1-IN-5 could increase the γ-H2AX expression[1].

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

In Vivo

PARP1-IN-5 (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine[1].
PARP1-IN-5 (25 and 50 mg/kg; p.o.; 12 days) significantly enhances the inhibitory effect of carboplatin on A549 cells at 50 mg/kg[1].
PARP1-IN-5 (50 mg/kg; p.o.) positively correlates with the expression of PARP-1[1].
PARP1-IN-5 can upregulate the expression of γ-H2AX and decrease the expression of PAR[1].

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

Animal Model: Mice[1]
Dosage: 1000 mg/kg
Administration: P.o.
Result: There was no significant difference in the body weight and blood routine.
Animal Model: Mice[1]
Dosage: 25 and 50 mg/kg
Administration: P.o.; 12 days
Result: Significantly enhanced the inhibitory effect of CBP on A549 cells at 50 mg/kg.
Animal Model: Male Sprague−Dawley (SD) rats[1]
Dosage: 50 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.; 12 days
Result: Positively correlated with the expression of PARP-1.
Molecular Weight

464.53

Formula

C25H24N2O5S

CAS No.
SMILES

O=C1C=C(OC2=C1C(O)=CC(O)=C2CN3CCN(CC3)CC4=CC=CS4)C5=CC=C(C=C5)O

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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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.

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PARP1-IN-5
Cat. No.:
HY-132297
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