PIN1 inhibitor API-1 |
| Catalog No.GC38036 |
El inhibidor de PIN1 API-1 es un inhibidor especÍfico de Pin1 (peptidil-prolil cis-trans isomerasa NIMA-interacting 1) (API-1) con una IC50 de 72,3 nM. El inhibidor de PIN1 API-1 se une directa y especÍficamente al dominio Pin1 peptidil-prolil isomerasa (PPIasa) e inhibe potentemente la actividad isomerizante cis-trans de Pin1. El inhibidor de PIN1 API-1 retiene la conformaciÓn activa de pXPO5 y restaura la capacidad de pXPO5 para transportar pre-miARN desde el nÚcleo al citoplasma, regulando asÍ la biogénesis de miARN contra el cÁncer para suprimir el desarrollo de carcinoma hepatocelular tanto in vitro como in vivo.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 680622-70-2
Sample solution is provided at 25 µL, 10mM.
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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 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development[1].
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)[1].
PIN1 inhibitor API-1 suppresses tumor growth in mice by up-regulating mature miRNA biogenesis[1].
[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.
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