PIN1 inhibitor API-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PIN1 抑制剂 API-1 是一种特异性 Pin1 抑制剂 (IC50: 72.3 nM)。 PIN1 抑制剂 API-1 保留了 pXPO5 的活性构象，并恢复了 pXPO5 将 pre-miRNA 从细胞核转运至细胞质的能力，从而上调抗癌 miRNA 的生物合成，抑制体外和体内肝细胞癌的发展。

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 obviously inhibits SK-Hep-1, SNU-423, and Hep3B cell proliferation with low IC50 values (IC50=0.683-4.16 μM).

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

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Others

Other Targets

Pin1

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680622-70-2

366.3

C15H13F3N6O2

>98% (HPLC)

DMSO:250 mg/mL (682.50 mM; Need ultrasonic)

C1=CC(=CC=C1CNC(=O)C(F)(F)F)COC2=NC(=NC3=C2NC=N3)N

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(-20℃)

With Ice Pack

≥ 2 years