PARP1-IN-12 是一种有效的PARP1抑制剂，其IC50值为 2.99 nM。PARP1-IN-12 具有较好的抗癌细胞增殖活性，可诱导细胞凋亡并使细胞周期停滞在 G2/M 期。PARP1-IN-12 能在BRCA缺陷的细胞中诱导 DNA 双链断裂 (DSBs)。
| 生物活性 | PARP1-IN-12 is a potentPARP1inhibitor with anIC50of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cellapoptosisand cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) inBRCA-deficient cells[1]. |
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体外研究
(In Vitro) | PARP1-IN-12 (compound 20e) (0.1, 0.3, 1 μM; 48 h) exhibits activities of antiproliferation and selectively killing BRCA-deficient cells, can also induce DNA double strand breaks (DSBs) in BRCA-deficient cells in a concentration-dependent manner[1].
PARP1-IN-12 (10 μM, 48 h) enhances the protein levels of phosphorylated Chk1[1].
PARP1-IN-12 (1, 3, 10 μM; 48 h) activats cell cycle checkpoints, then induces G2/M arrest in BRCA-deficient cells and (1, 5, 10 μM; 96 h) also induces MDA-MB-436 cells apoptosis in a concentration-dependent manner[1].
Cell Proliferation Assay[1] | Cell Line: | UWB1.289 (BRCA1-deficient), UWB1.289+BRCA1 (BRCA1 restored), MDA-MB-436 (BRCA1-deficient), Capan-1 (BRCA2-deficient) cells | | Concentration: | 0.1, 0.3, 1 μM | | Incubation Time: | 48 h | | Result: | Showed antiproliferative activity with IC50s of 0.27, 1.43, 0.87, 0.19 μM for UWB1.289, UWB1.289+BRCA1, Capan-1 and MDA-MB-436 cells, respectively. |
Immunofluorescence[1] | Cell Line: | MDA-MB-436, Capan-1 cells | | Concentration: | 10 μM | | Incubation Time: | 48 h | | Result: | Enhanced the protein levels of phosphorylated Chk1 but the levels of corresponding total proteins were not altered. |
Cell Cycle Analysis[1] | Cell Line: | Capan-1 cells | | Concentration: | 1, 3, 10 μM | | Incubation Time: | 48 h | | Result: | Induced G2/M arrest in BRCA-deficient cells in a concentration-dependent manner. |
Apoptosis Analysis[1] | Cell Line: | MDA-MB-436 cells | | Concentration: | 1, 5, 10 μM | | Incubation Time: | 96 h | | Result: | Caused apoptosis in a concentration-dependent manner in MDA-MB-436 cells. |
Western Blot Analysis[1] | Cell Line: | MDA-MB-436, Capan-1 cells | | Concentration: | 0.1, 0.3, 1 μM | | Incubation Time: | 48 h | | Result: | Induced increased levels of γH2AX in a concentration-dependent manner in both MDA-MB-436 and Capan-1 cells. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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