| Description | PIN1 inhibitor API-1 is a specific Pin1 inhibitor (IC50: 72.3 nM). PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from the nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase domain and effectively inhibits Pin1 cis-trans isomerizing activity. |
| In vitro | PIN1抑制剂API-1显著抑制了SK-Hep-1、SNU-423和Hep3B细胞增殖，其半抑制浓度(IC50)范围为0.683-4.16 μM[1]。 |
| In vivo | PIN1 inhibitor API-1 通过在小鼠中上调成熟miRNA的生物合成来抑制肿瘤生长[1]。 |
| Target activity | Pin1:72.3 nM |
| molecular weight | 366.3 |
| Molecular formula | C15H13F3N6O2 |
| CAS | 680622-70-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 250 mg/mL (682.50 mM), Sonication is recommended. |
| References | 1. Pu W, et al. Targeting Pin1 by inhibitor API-1 regulates microRNA biogenesis and suppresses hepatocellularcarcinoma development. Hepatology. 2018 Aug;68(2):547-560. |