PIN1 inhibitor API-1 |
| Catalog No.GC38036 |
PIN1 억제제 API-1은 IC50이 72.3nM인 특정 Pin1(펩티딜-프롤릴 시스-트랜스 이성질화효소 NIMA-상호작용 1) 억제제(API-1)입니다. PIN1 억제제 API-1은 Pin1 펩티딜-프롤릴 이성화효소(PPIase) 도메인에 직접 및 특이적으로 결합하여 Pin1 시스-트랜스 이성화 활성을 강력하게 억제합니다. PIN1 억제제 API-1은 pXPO5의 활성 형태를 유지하고 pXPO5가 pre-miRNA를 핵에서 세포질로 수송하는 능력을 복원하여 항암 miRNA 생합성을 상향 조절하여 시험관 내 및 생체 내 간세포 암종 발병을 모두 억제합니다.
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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