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

PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model.

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

PARP-1-IN-1 Chemical Structure

PARP-1-IN-1 Chemical Structure

CAS No. : 2763840-83-9

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Description

PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model[1].

In Vitro

PARP-1-IN-1 (compound Y49) (48 hours) has effective inhibition on different cancer cells (IC50s of 9.64, 123.5 106.3 μM for MX-1, MCF7 and A548 cells, respectively)[1].
PARP-1-IN-1 (2.5-10 μM, 48 hours) successfully inhibits the activity of PARP-1 and reduces the production of PAR in A549 cells, which is dose-dependent to some extent[1].

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

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 2.5 μM, 5 μM and 10 μM
Incubation Time: 48h
Result: Inhibited the activity of PARP-1 successfully and reduced the production of PAR in cancer cells. PARP-1-IN-1 was dose-dependent to some extent.
In Vivo

PARP-1-IN-1 (compound Y49) (50 mg/kg/day; p.o.; daily for 18 days) inhibits the growth of MDA-MB-436 tumor in BALB/c nude mice[1].

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

Animal Model: Female athymic BALB/c nude mice (inoculated MDA-MB-436 cells)[1]
Dosage: 50 mg/kg
Administration: p.o., daily for 18 days
Result: Inhibited the growth of MDA-MB-436 tumor significantly, and no significant change in the body weight of PARP-1-IN-1 treated mice.
Molecular Weight

392.47

Formula

C23H25FN4O

CAS No.
SMILES

NC1CCN(CC1)CC2=CC(C3=C4CCNC(C5=C4C(N3)=CC(F)=C5)=O)=CC=C2

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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PARP-1-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.

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Product Name:
PARP-1-IN-1
Cat. No.:
HY-144642
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