PIN1 inhibitor API-1
Names
[ CAS No. ]:
680622-70-2
[ Name ]:
PIN1 inhibitor API-1
[Synonym ]:
N-[[4-[(2-amino-7H-purin-6-yl)oxymethyl]phenyl]methyl]-2,2,2-trifluoroacetamide
Biological Activity
[Description]:
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].
[Related Catalog]:
[Target]
IC50: 72.3 nM (Pin1)[1]
[In Vitro]
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].
[In Vivo]
PIN1 inhibitor API-1 suppresses tumor growth in mice by up-regulating mature miRNA biogenesis[1].
[References]
Chemical & Physical Properties
[ Melting Point ]:
208-211C
[ Molecular Formula ]:
C15H15F3N6O2
[ Molecular Weight ]:
366.29800
[ Exact Mass ]:
366.10500
[ PSA ]:
123.03000
[ LogP ]:
2.46300