PIN1 inhibitor API-1是一种选择性 PIN1 抑制剂,通过阻断 PIN1 的顺反异构化作用,恢复相关蛋白质的功能。它在肝癌和其他肿瘤研究中具有潜在的治疗价值。
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描述 | PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 binds directly and specifically to the PIN1 inhibitor API-1 directly and specifically binds to the PPIase domain and effectively inhibits the cis-trans isomerisation activity of Pin1. PIN1 inhibitor API-1 preserves the active conformation of pXPO5 and restores its ability to transport pre-miRNA from the nucleus to the cytoplasm, thereby up-regulating the biogenesis of anticancer miRNAs, and inhibiting hepatocellular carcinoma both in vitro and in vivo[1].PIN1 inhibitor API-1 significantly inhibited the proliferation of SK-Hep-1, SNU-423 and Hep3B cells with low IC50 values (IC50=0.683-4.16 μM)[1]. |
Animal study | The PIN1 inhibitor API-1 inhibits tumour growth in mice by upregulating the biogenesis of mature miRNAs[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.73mL 0.55mL 0.27mL |
13.65mL 2.73mL 1.37mL |
27.30mL 5.46mL 2.73mL |
CAS号 | 680622-70-2 |
分子式 | C15H13F3N6O2 |
分子量 | 366.298 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 250 mg/mL(682.5 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |