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
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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