PIN1 inhibitor API-1 |
| カタログ番号GC38036 |
PIN1 阻害剤 API-1 は、特定の Pin1 (ペプチジル-プロリル シス-トランス イソメラーゼ NIMA 相互作用 1) 阻害剤 (API-1) であり、IC50 は 72.3 nM です。 PIN1 阻害剤 API-1 は、Pin1 ペプチジル-プロリルイソメラーゼ (PPIase) ドメインに直接的かつ特異的に結合し、Pin1 cis-trans 異性化活性を強力に阻害します。 PIN1 阻害剤 API-1 は、pXPO5 の活性立体構造を保持し、pXPO5 が pre-miRNA を核から細胞質に輸送する能力を回復させ、抗がん miRNA の生合成をアップレギュレートして、in vitro および in vivo での肝細胞がんの発生を抑制します。
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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