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PIN1 inhibitor API-1 is a specific Pin1 inhibitor (IC50: 72.3 nM) that retains the active conformation of pXPO5, restoring its ability to transport pre-miRNAs from the nucleus to the cytoplasm, thereby up-regulating anticancer miRNA biogenesis to suppress hepatocellular carcinoma development both in vitro and in vivo. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase domain, effectively inhibiting Pin1 cis-trans isomerizing activity.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $55 | In Stock | |
| 5 mg | $129 | In Stock | |
| 10 mg | $247 | In Stock | |
| 25 mg | $363 | In Stock | |
| 50 mg | $538 | In Stock | |
| 100 mg | $679 | In Stock | |
| 200 mg | $945 | In Stock | |
| 500 mg | $1,380 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $143 | In Stock |
| Description | PIN1 inhibitor API-1 is a specific Pin1 inhibitor (IC50: 72.3 nM) that retains the active conformation of pXPO5, restoring its ability to transport pre-miRNAs from the nucleus to the cytoplasm, thereby up-regulating anticancer miRNA biogenesis to suppress hepatocellular carcinoma development both in vitro and in vivo. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase domain, effectively inhibiting Pin1 cis-trans isomerizing activity. |
| Targets&IC50 | Pin1:72.3 nM |
| In vitro | PIN1 inhibitor API-1 significantly suppresses SK-Hep-1, SNU-423, and Hep3B cell proliferation (IC50=0.683-4.16 μM)[1]. |
| In vivo | PIN1 inhibitor API-1 inhibits tumor growth by up-regulating mature miRNA biogenesis in mice [1]. |
| Molecular Weight | 366.3 |
| Formula | C15H13F3N6O2 |
| Cas No. | 680622-70-2 |
| Smiles | Nc1nc(OCc2ccc(CNC(=O)C(F)(F)F)cc2)c2[nH]cnc2n1 |
| Relative Density. | 1.525 g/cm3 (Predicted) |
| Color | White |
| Appearance | solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 250 mg/mL (682.50 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (13.65 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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