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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]

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Purity:97.24%

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COA HPLC HNMR

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)
Color	Yellow
Appearance	solid

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.

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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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