Chemical Structure : Pin1 inhibitor API-1
CAS No.: 680622-70-2
Catalog No.: PC-35874Not For Human Use, Lab Use Only.
Pin1 inhibitor API-1 (API-1) is a potent, specific inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) and inhibits Pin1 cis-trans isomerizing activity with IC50 of 72.3 nM.
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Pin1 inhibitor API-1 (API-1) is a potent, specific inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) and inhibits Pin1 cis-trans isomerizing activity with IC50 of 72.3 nM.
API-1 displays remarkable selectivity over other peptidyl-prolyl cis-trans isomerases, including Pin4, FKBP12, and cyclophilin A.
API-1 suppresses in vitro cell proliferation and migration of HCC cells with low IC50 values, which is depended on both Pin1 expression and XPO5 phosphorylation.
API-1 recognizes and isomerizes the phosphorylated serine-proline motif of phosphorylated XPO5 and passivates phosphorylated XPO5, maintains the active pXPO5 conformation, rescues the pre-miRNA loading of pXPO5 and increases mature miRNA biogenesis; suppresses tumour growth in mice.
M.Wt | 366.304 | |
Formula | C15H13F3N6O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-(4-(((2-amino-9H-purin-6-yl)oxy)methyl)benzyl)-2,2,2-trifluoroacetamide |
1. Pu W, et al. Hepatology. 2018 Aug;68(2):547-560.
2. Pauly GT, et al. J Med Chem. 2008 Nov 27;51(22):7144-53.
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