PARP1-IN-10 是一种无毒、有效的PARP1抑制剂，IC50为 50.62 nM。PARP1-IN-10 导致细胞周期在 G2/M 期停滞和Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)，并能够增强替莫唑胺 (TMZ) 的细胞毒性。

PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC 50 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].

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 IC 50 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 ( IC 50 = 3.64 μM) in A549 cell line compared to TMZ alone ( IC 50 =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.

2494001-21-5

C20H23N3O5

385.41

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years