PIN1 inhibitor API-1 |
رقم الكتالوجGC38036 |
مثبط PIN1 API-1 هو مثبط محدد لـ Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-التفاعلي 1) (API-1) مع IC 50 من 72.3 نانومتريرتبط مثبط PIN1 API-1 بشكل مباشر وعلى وجه التحديد بمجال Pin1 peptidyl-prolyl isomerase (PPIase) ويمنع نشاط المشابهات Pin1 cis-trans بشكل فعاليحتفظ مثبط PIN1 API-1 بالتشكيل النشط لـ pXPO5 ويعيد قدرة pXPO5 على نقل ما قبل miRNAs من النواة إلى السيتوبلازم ، وبالتالي تنظيم التكوّن الحيوي ميرنا المضاد للسرطان لقمع تطور سرطان الخلايا الكبدية في المختبر وفي الجسم الحي
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Cas No.: 680622-70-2
Sample solution is provided at 25 µL, 10mM.
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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