Name | PARP1-IN-10 |
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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]. |
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Related Catalog | |
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]. 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. |
References |
Molecular Formula | C20H23N3O5 |
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Molecular Weight | 385.41 |