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PKC-IN-1

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Catalog No. T12494Cas No. 1046787-18-1

PKC-IN-1 is an ATP-competitive and reversible conventional PKC enzymes inhibitor (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM, respectively).

PKC-IN-1

PKC-IN-1

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Purity: 98.79%
Catalog No. T12494Cas No. 1046787-18-1
PKC-IN-1 is an ATP-competitive and reversible conventional PKC enzymes inhibitor (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM, respectively).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$1988-10 weeks8-10 weeks
5 mg$3478-10 weeks8-10 weeks
25 mg$1,1408-10 weeks8-10 weeks
50 mg$1,4908-10 weeks8-10 weeks
100 mg$1,9908-10 weeks8-10 weeks
1 mL x 10 mM (in DMSO)$3838-10 weeks8-10 weeks
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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:98.79%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
PKC-IN-1 is an ATP-competitive and reversible conventional PKC enzymes inhibitor (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM, respectively).
Targets&IC50
PKCβII (human):7.6 nM, PKCβ (human):5.3 nM (ki), PKCβI (human):8.1 nM, PKCε (human):808 nM, PKCγ (human):57.5 nM, PKCμ (human):314 nM, PKCα (human):10.4 nM (ki), PKCα (human):2.3 nM, PKCθ (human):25.6 nM
In vitro
PKC-IN-1 is a potent, ATP-competitive, and reversible of conventional PKC enzymes (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM, respectively) [1].
In vivo
In Lewis rats, PKC-IN-1 dose-dependently and significantly reduces maximum EAE severity and end severity in the autoimmune encephalitis (EAE) model [1].
Chemical Properties
Molecular Weight500.61
FormulaC25H37FN8O2
Cas No.1046787-18-1
SmilesC[C@@H]1CN([C@@H](C)CN1CC1CCOCC1)C(=O)N1Cc2c(Nc3nc(C)ncc3F)n[nH]c2C1(C)C
Relative Density.1.253 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore 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: 25 mg/mL (49.94 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9976 mL9.9878 mL19.9756 mL99.8781 mL
5 mM0.3995 mL1.9976 mL3.9951 mL19.9756 mL
10 mM0.1998 mL0.9988 mL1.9976 mL9.9878 mL
20 mM0.0999 mL0.4994 mL0.9988 mL4.9939 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:
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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

Keywords

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