| Name | O6-[4-(Trifluoroacetamidomethyl)benzyl]guanine |
|---|---|
| Synonyms |
Inhibitor,MicroRNA,PIN1 inhibitor API 1,PIN1 inhibitor API-1,PIN1 inhibitor API1,inhibit,PIN-1 inhibitor API-1,miRNA
N-(4-(((2-Amino-1H-purin-6-yl)oxy)methyl)benzyl)-2,2,2-trifluoroacetamide N-[[4-[(2-amino-7H-purin-6-yl)oxymethyl]phenyl]methyl]-2,2,2-trifluoroacetamide Acetamide, N-[[4-[[(2-amino-1H-purin-6-yl)oxy]methyl]phenyl]methyl]-2,2,2-trifluoro PIN1 inhibitor API-1 ,S6893 N-[4-(2-Amino-9H-purin-6-yloxymethyl)-benzyl]-2,2,2-trifluoroacetamide O6-[4-(TRIFLUOROACETAMIDOMETHYL)BENZYL]GUANINE PIN1 inhibitor API-1, 10 mM in DMSO |
| 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 |
| Melting Point | 208-211C |
|---|---|
| Molecular Formula | C15H15F3N6O2 |
| Molecular Weight | 366.29800 |
| Exact Mass | 366.10500 |
| PSA | 123.03000 |
| LogP | 2.46300 |
| Precursor 0 | |
|---|---|
| DownStream 1 | |