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PKCβ inhibitor 1

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Catalog No. T8376Cas No. 257879-35-9
Alias KUN79359

PKCβ inhibitor 1 (KUN79359)(KUN79359) is a potent, selective and ATP-competitive inhibitor of PKC isozymes(IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively).

PKCβ inhibitor 1

PKCβ inhibitor 1

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Purity: 99.33%
Catalog No. T8376Alias KUN79359Cas No. 257879-35-9
PKCβ inhibitor 1 (KUN79359)(KUN79359) is a potent, selective and ATP-competitive inhibitor of PKC isozymes(IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
500 μg$33In StockIn Stock
1 mg$46In StockIn Stock
5 mg$108In StockIn Stock
10 mg$196In StockIn Stock
25 mg$435In StockIn Stock
50 mg$768In StockIn Stock
100 mg$1,050In StockIn Stock
1 mL x 10 mM (in DMSO)$118In StockIn 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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Purity:99.33%
Appearance:Solid
Color:Yellow
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Product Introduction

PKCβ inhibitor 1 AI Summary
PKCβ inhibitor 1 exhibits potent inhibitory activity against multiple protein kinase C (PKC) isoforms, particularly PKC beta 2 with an IC50 value of 5.0 nM, indicating high potency against this isoform. It also inhibits PKC beta 1, PKC alpha, and PKC epsilon, though to a lesser extent. Additionally, PKCβ inhibitor 1 shows selectivity in inhibiting JAK3 over JAK2, with an IC50 value of 17.0 nM for JAK3 and a selectivity ratio of 226.0. It also inhibits TYK2, JAK2, and JAK1 with respective IC50 values of 2310.0 nM, 3850.0 nM, and 770.0 nM. Furthermore, the compound demonstrates varying degrees of thermal melting changes on several protein targets involved in cellular signaling pathways, such as AMPKA2, CAMKs, CDKs, GSK3B, JAK1~B, PLKs, RSKs, SLK, and RIOK2, suggesting potential bioactivity in modulating the stability and function of these proteins..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
PKCβ inhibitor 1 (KUN79359)(KUN79359) is a potent, selective and ATP-competitive inhibitor of PKC isozymes(IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively).
Targets&IC50
PKCα:331 nM, PKCβ1 (human):21 nM , PKCβ2 (human):5 nM
SynonymsKUN79359
Chemical Properties
Molecular Weight411.46
FormulaC24H21N5O2
Cas No.257879-35-9
SmilesO=C1NC(=O)C(=C1Nc1ccccc1)c1cn(CCCn2ccnc2)c2ccccc12
Relative Density.no data available
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: 4.12 mg/mL (10.01 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.43 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
1mg5mg10mg50mg
1 mM2.4304 mL12.1518 mL24.3037 mL121.5185 mL
5 mM0.4861 mL2.4304 mL4.8607 mL24.3037 mL
10 mM0.2430 mL1.2152 mL2.4304 mL12.1518 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

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