1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. PARP Apoptosis
  3. PARP1-IN-10

PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC50 value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) .

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PARP1-IN-10 Chemical Structure

PARP1-IN-10 Chemical Structure

CAS No. : 2494001-21-5

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Description

PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC50 value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) [1].

IC50 & Target

PARP1

50.62 nM (IC50, [1])

In Vitro

PARP1-IN-10 (compound 12c) (10 μM, 48 h) shows no cytotoxic effects against NCI-60 human tumor cell lines[1].
PARP1-IN-10 inhibits MDA-MB-436 cell line with an IC50 value of 3.73 μM[1].
PARP1-IN-10 (1 and 3.73 μM, 48 h) causes cell cyle arrest at G2/M with dose-dependent manner[1].
PARP1-IN-10 (0.5 μM, 48 h) shows antiprolifetative effect of temozolomide (TMZ) about 7 times (IC50 = 3.64 μM) in A549 cell line compared to TMZ alone (IC50=24.2 μM)[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: NCI-60 human tumor cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: Showed no toxicity.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 0, 1, 3.73 μM
Incubation Time: 48 hours
Result: Caused cell cycle arrest at G2/M and showed apoptotic effect in dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: A549 human lung cancer cells
Concentration: 0, 0.5, 7.94 μM
Incubation Time: 48 hours
Result: Potentiated the antiproliferative effect of temozolomide (TMZ) 7 times compared with TMZ alone.
Molecular Weight

385.41

Formula

C20H23N3O5

CAS No.
SMILES

O=C1/C(C(N(C)C(N1C)=O)=O)=C\C2=CC=C(C=C2)OCC(N3CCCCC3)=O

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

Purity & Documentation
References
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PARP1-IN-10 Related Classifications

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    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-10
Cat. No.:
HY-149003
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