PV-1019 (NSC 744039) 是一种有效的选择性Chk2抑制剂，IC50值为 24 nM。PV-1019 抑制 Topotecan (HY-13768) 诱导的 Chk2 自磷酸化。PV-1019 抑制 IR 诱导的细胞凋亡。
| 生物活性 | PV-1019 (NSC 744039) is a potent, selectiveChk2inhibitor with anIC50value of 24 nM. PV-1019 inhibits theTopotecan(HY-13768)-inducedChk2autophosphorylation. PV-1019 inhibits IR-inducedapoptosis[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | PV-1019 (NSC 744039; 0.1-100 μM; 48 h) 在人类肿瘤细胞中具有抗增殖作用[1]。
PV-1019 抑制 Chk2 自磷酸化和组蛋白 H1 磷酸化，IC50值为 138 nM[1]。
PV-1019 (1-50 μM; 1 h; OVCAR-5 细胞) 抑制Topotecan-诱导的 Chk2 自磷酸化，IC50值为 2.8 μM[1]。
PV-1019 (1 μM; 16 h) 消除小鼠胸腺细胞中 IR 诱导的细胞凋亡[1]。
Cell Viability Assay[1] | Cell Line: | human tumor cells | | Concentration: | 0.1-100 μM | | Incubation Time: | 48 hours | | Result: | Inhibited cell growth in a dose-dependent manner. |
Western Blot Analysis[1] | Cell Line: | OVCAR-5 cells | | Concentration: | 1, 5, 10, and 25 μM | | Incubation Time: | 1 hours | | Result: | Decreased the level of Chk2 autophosphorylation (Ser516) in a dose-dependent manner. |
Cell Cycle Analysis[1] | Cell Line: | mouse thymocytes | | Concentration: | 1 μM | | Incubation Time: | 16 hours | | Result: | Decreased in the sub-G1 fraction (56%). |
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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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