| Bioactivity | PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 inhibits the Topotecan (HY-13768)-induced Chk2 autophosphorylation. PV-1019 inhibits IR-induced apoptosis[1]. |
| Invitro | 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: |
| Name | PV-1019 |
| CAS | 1093793-05-5 |
| Formula | C18H17N7O3 |
| Molar Mass | 379.37 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Jobson AG, et, al. Cellular inhibition of checkpoint kinase 2 (Chk2) and potentiation of camptothecins and radiation by the novel Chk2 inhibitor PV1019 [7-nitro-1H-indole-2-carboxylic acid {4-[1-(guanidinohydrazone)-ethyl]-phenyl}-amide]. J Pharmacol Exp Ther. 2009 Dec;331(3):816-26. |