PIN1 inhibitor API-1
Modify Date: 2024-01-09 20:55:05
PIN1 inhibitor API-1 structure
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Common Name | PIN1 inhibitor API-1 | ||
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| CAS Number | 680622-70-2 | Molecular Weight | 366.29800 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C15H15F3N6O2 | Melting Point | 208-211C | |
| MSDS | N/A | Flash Point | N/A | |
Use of PIN1 inhibitor API-1PIN1 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]. |
| Name | O6-[4-(Trifluoroacetamidomethyl)benzyl]guanine |
|---|---|
| Synonym | More Synonyms |
| 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]. |
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| 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 | |
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| DownStream 1 | |
CAS#:674799-96-3| N-[[4-[(2-amino-7H-purin-6-yl)oxymethyl]phenyl]methyl]-2,2,2-trifluoroacetamide |