PIN1 inhibitor API-1 是特殊的Pin1抑制剂，可直接特异性地与 Pin1 肽基脯氨酰异构酶结构域结合，并抑制 Pin1 顺反异构活性。它保留 pXPO5 的活性构象，恢复 pXPO5 将前 miRNA 从细胞核转运到细胞质的能力，从而上调抗癌 miRNA 的生物发生，抑制体内外肝癌的发生。

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.

PIN1 inhibitor API-1 significantly suppresses SK-Hep-1, SNU-423, and Hep3B cell proliferation (IC50=0.683-4.16 μM)[1].

PIN1 inhibitor API-1 inhibits tumor growth by up-regulating mature miRNA biogenesis in mice [1].

680622-70-2

C15H13F3N6O2

366.3

PIN1 inhibitor API-1

DMSO:250 mg/mL (682.50 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years