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KPT-6566

Name: KPT-6566
Brand: TargetMol
SKU: T5994
Price: 97 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5994Cas No. 881487-77-0

KPT-6566 is a novel selective covalent pin1 inhibitor, KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain,and has anti-cancer activity.

KPT-6566

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Purity: 97.24%

Catalog No. T5994Cas No. 881487-77-0

KPT-6566 is a novel selective covalent pin1 inhibitor, KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain,and has anti-cancer activity.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$97	-	In Stock
2 mg	$148	-	In Stock
5 mg	$297	-	In Stock
10 mg	$455	-	In Stock
25 mg	$753	-	In Stock
50 mg	$1,060	-	In Stock
100 mg	$1,430	-	In Stock
1 mL x 10 mM (in DMSO)	$289	-	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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Batch Information

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Purity:97.24%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	KPT-6566 is a novel selective covalent pin1 inhibitor, KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain,and has anti-cancer activity.
Targets&IC50	PIN1 PPIase:640 nM
In vitro	KPT-6566 covalently binds to the catalytic site of PIN1,inhibited the PPIase activity of PIN1 and turned out to have an IC50 of 0.64 μM.?This interaction results in the release of a quinone-mimicking drug that generates reactive oxygen species and DNA damage, inducing cell death specifically in cancer cells.
Cell Research	For IC50 determination, human recombinant PIN1 was preincubated with different concentrations of KPT-6566 and PPIase activity was measured after 180 min. K values of PPIase activity were plotted against inhibitor concentration in a semi-logarithmic plot.

Chemical Properties

Molecular Weight	443.54
Formula	C₂₂H₂₁NO₅S₂
Cas No.	881487-77-0
Smiles	CC(C)(C)c1ccc(cc1)S(=O)(=O)\N=C1/C=C(SCC(O)=O)C(=O)c2ccccc12
Relative Density.	1.32 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature,keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 120 mg/mL (270.55 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Saline: 1 mg/mL (2.25 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	2.2546 mL	11.2729 mL	22.5459 mL	112.7294 mL
5 mM	0.4509 mL	2.2546 mL	4.5092 mL	22.5459 mL
10 mM	0.2255 mL	1.1273 mL	2.2546 mL	11.2729 mL
20 mM	0.1127 mL	0.5636 mL	1.1273 mL	5.6365 mL
50 mM	0.0451 mL	0.2255 mL	0.4509 mL	2.2546 mL
100 mM	0.0225 mL	0.1127 mL	0.2255 mL	1.1273 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