PIN1 inhibitor API-1 |
| Katalog-Nr.GC38036 |
Der PIN1-Inhibitor API-1 ist ein spezifischer Pin1-Inhibitor (Peptidyl-Prolyl-cis-trans-Isomerase NIMA-interacting 1) (API-1) mit einem IC50-Wert von 72,3 nM. Der PIN1-Inhibitor API-1 bindet direkt und spezifisch an die Pin1-Peptidyl-Prolyl-Isomerase (PPIase)-DomÄne und hemmt wirksam die cis-trans-IsomerisierungsaktivitÄt von Pin1. Der PIN1-Inhibitor API-1 behÄlt die aktive Konformation von pXPO5 bei und stellt die FÄhigkeit von pXPO5 wieder her, prÄ-miRNAs vom Zellkern zum Zytoplasma zu transportieren, wodurch die Antikrebs-miRNA-Biogenese hochreguliert wird, um die Entwicklung von hepatozellulÄrem Karzinom sowohl in vitro als auch in vivo zu unterdrÜcken.
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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