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Pin1 inhibitor API-1

Chemical Structure : Pin1 inhibitor API-1

CAS No.: 680622-70-2

Pin1 inhibitor API-1 (API-1)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 366.304
Formula C15H13F3N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-(((2-amino-9H-purin-6-yl)oxy)methyl)benzyl)-2,2,2-trifluoroacetamide

References

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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