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KP-457

Name: KP-457
Brand: TargetMol
SKU: T77778
Price: 93 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T77778Cas No. 1365803-52-6

Alias KP457, KP 457

KP-457 is a specific inhibitor of a disintegrin-metalloproteinase 17 (ADAM17) and a TNFα converting enzyme TACE inhibitor that blocks the production of soluble TNF (sTNF).

KP-457

🥰Excellent

Purity: 98.33%

Catalog No. T77778Alias KP457, KP 457Cas No. 1365803-52-6

KP-457 is a specific inhibitor of a disintegrin-metalloproteinase 17 (ADAM17) and a TNFα converting enzyme TACE inhibitor that blocks the production of soluble TNF (sTNF).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$93	In Stock	In Stock
5 mg	$228	In Stock	In Stock
10 mg	$372	In Stock	In Stock
25 mg	$689	In Stock	In Stock
50 mg	$1,090	-	In Stock
100 mg	$1,480	-	In Stock
1 mL x 10 mM (in DMSO)	$243	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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Batch Information

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Purity:98.33%

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	KP-457 is a specific inhibitor of a disintegrin-metalloproteinase 17 (ADAM17) and a TNFα converting enzyme TACE inhibitor that blocks the production of soluble TNF (sTNF).
Targets&IC50	MMP17:7.1 μM, MMP2:0.717 μM, MMP3:9.760 μM, MMP8:2.2 μM, MMP14:2.14 μM, ADAM17:0.111 μM, ADAM10:0.748 μM, MMP9:5.41 μM, MMP13:0.93 μM
In vitro	b>METHODS: The ability of KP-457 (15 μM) to inhibit GPIbα shedding during in vitro generation of iPSC platelets was studied when administered during the MK differentiation and thrombopoietic stages of HPC cultured at 37°C. RESULTS: KP-457 had no significant effect on MK numbers; retention of GPIbα by KP-457 was consistently observed in platelets derived from human embryonic stem cells and imMKCLs. [1] KP-457 is a selective metalloproteinase 17 (ADAM17) inhibitor, with selectivity for ADAM17 over other MMPs and ADAM10, with IC50 values of 0.011 μM (ADAM17), 0.748 μM (ADAM10), 0.717 μM (MMP2), 9.760 μM (MMP3), 2.2 μM (MMP8), 5.41 μM (MMP9), 0.93 μM (MMP13), 2.140 μM (MMP14), and 7.1 μM (MMP17), respectively. [1]
Synonyms	KP457, KP 457

Chemical Properties

Molecular Weight	480.56
Formula	C₂₁H₂₄N₂O₇S₂
Cas No.	1365803-52-6
Smiles	C(CS(=O)(=O)C1=CC=C(OCC#CC)C=C1)(N(C=O)O)C2=CC=C(CNS(C)(=O)=O)C=C2

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (208.09 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.32 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	2.0809 mL	10.4045 mL	20.8091 mL	104.0453 mL
5 mM	0.4162 mL	2.0809 mL	4.1618 mL	20.8091 mL
10 mM	0.2081 mL	1.0405 mL	2.0809 mL	10.4045 mL
20 mM	0.1040 mL	0.5202 mL	1.0405 mL	5.2023 mL
50 mM	0.0416 mL	0.2081 mL	0.4162 mL	2.0809 mL
100 mM	0.0208 mL	0.1040 mL	0.2081 mL	1.0405 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

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