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KHK-IN-1

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Catalog No. T15660Cas No. 1303469-70-6
Alias KHK-IN-8, Ketohexokinase inhibitor 8

KHK-IN-1 (KHK-IN-8) is a selective and cell membrane permeable inhibitor of ketohexokinase (KHK, IC50=12 nM; F=34%). KHK-IN-1 inhibits F1P production in HepG2 cell lysates with IC50 of 400 nM. KHK-IN-1 has potential for the study of obesity and diabetes.

KHK-IN-1

KHK-IN-1

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Purity: 99.00%
Catalog No. T15660Alias KHK-IN-8, Ketohexokinase inhibitor 8Cas No. 1303469-70-6
KHK-IN-1 (KHK-IN-8) is a selective and cell membrane permeable inhibitor of ketohexokinase (KHK, IC50=12 nM; F=34%). KHK-IN-1 inhibits F1P production in HepG2 cell lysates with IC50 of 400 nM. KHK-IN-1 has potential for the study of obesity and diabetes.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$92In StockIn Stock
5 mg$223In StockIn Stock
10 mg$333In StockIn Stock
25 mg$538In StockIn Stock
50 mg$732In StockIn Stock
100 mg$990In StockIn Stock
200 mg$1,330In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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:99.00%
Appearance:Solid
Color:White
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Product Introduction

KHK-IN-1 AI Summary
KHK-IN-1 is a bioactive compound that inhibits human ketohexokinase isoform C (KHKC) with an IC50 of 12.0 nM. In human HepG2 cells, it demonstrates inhibition of KHKC with an IC50 of 400.0 nM. The compound shows selective inhibition across various kinases compared to human ketohexokinase and maintains good metabolic stability in both human and rat liver microsomes. In Sprague-Dawley rats, KHK-IN-1 exhibits moderate oral bioavailability, with a half-life ranging from 2.0 to 4.0 hours, a relatively high volume of distribution at steady state, and efficient clearance. Additionally, KHK-IN-1 demonstrates antiviral activity by inhibiting SARS-CoV-2 induced cytotoxicity in both Caco-2 and VERO-6 cells at 10 µM concentration, with inhibition percentages of -0.26% and -0.31%, respectively, after 48 hours. It also shows inhibition of SARS-CoV-2 3CL-Pro protease activity at 20 µM, with an inhibition percentage of -3.388%. Furthermore, the compound inhibits human HDAC6 enzyme activity, evidenced by -12.91% inhibition in an enzymatic assay using a commercial peptide substrate and -3.89% inhibition with a custom peptide substrate..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
KHK-IN-1 (KHK-IN-8) is a selective and cell membrane permeable inhibitor of ketohexokinase (KHK, IC50=12 nM; F=34%). KHK-IN-1 inhibits F1P production in HepG2 cell lysates with IC50 of 400 nM. KHK-IN-1 has potential for the study of obesity and diabetes.
Targets&IC50
KHK:12 nM
SynonymsKHK-IN-8, Ketohexokinase inhibitor 8
Chemical Properties
Molecular Weight422.55
FormulaC21H26N8S
Cas No.1303469-70-6
SmilesN(C=1C2=C(C(NCC3CC3)=NC=N2)N=C(N1)N4CCNCC4)C5=C(SC)C=CC=C5
Relative Density.1.37 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: Insoluble

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
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% Tween 80
% Saline/PBS/ddH2O

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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

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