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PIN1 inhibitor API-1

Name: PIN1 inhibitor API-1
Brand: TargetMol
SKU: T16538
Price: 55 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16538Cas No. 680622-70-2

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.

PIN1 inhibitor API-1

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Purity: 98.48%

Catalog No. T16538Cas No. 680622-70-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$55	In Stock	In Stock
5 mg	$129	In Stock	In Stock
10 mg	$247	In Stock	In Stock
25 mg	$363	In Stock	In Stock
50 mg	$538	In Stock	In Stock
100 mg	$679	In Stock	In Stock
200 mg	$945	-	In Stock
500 mg	$1,380	-	In Stock
1 mL x 10 mM (in DMSO)	$143	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.48%

Appearance:solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

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].

Chemical Properties

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)

Storage & Solubility Information

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 (682.5 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

	1mg	5mg	10mg	50mg
1 mM	2.7300 mL	13.6500 mL	27.3000 mL	136.5001 mL
5 mM	0.5460 mL	2.7300 mL	5.4600 mL	27.3000 mL
10 mM	0.2730 mL	1.3650 mL	2.7300 mL	13.6500 mL
20 mM	0.1365 mL	0.6825 mL	1.3650 mL	6.8250 mL
50 mM	0.0546 mL	0.2730 mL	0.5460 mL	2.7300 mL
100 mM	0.0273 mL	0.1365 mL	0.2730 mL	1.3650 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc