For research use only.
CAS No. 142273-20-9
Kenpaullone is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It also inhibit glycogen synthase kinase 3β (GSK3β) with IC50 of 0.23 µM.
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Effect of Kenpaullone on GSK-3β and CDKs. (A and B) Naïve CD4+ T cells were stimulated with anti-CD3/CD28 (TCR), TGF-β (5 ng/ml) and IL-6 (20 ng/ml) in the presence of the indicated Kenpaullone (Kenp) concentrations for 30 min (A) or 24 h (A and B).
Biochem Biophys Res Commun, 2013, 435(3):378-84. . Kenpaullone purchased from Selleck.
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|Description||Kenpaullone is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It also inhibit glycogen synthase kinase 3β (GSK3β) with IC50 of 0.23 µM.|
In HEK-293 cells, phosphorylation of the endogenous GSK3α on Tyr279 is greatly decreased after prolonged incubation with Kenpaullone. Also, the Phosphorylation of the endogenous GSK3β also decreases, although less markedly. Kenpaullone also induces the dephosphorylation of both GSK3 isoforms in SH-SY5Y cells and PC12 cells. Kenpaullone (20µM) strongly suppresses the autophosphorylation of GSK3β at Tyr216 in vitro whether GSK3 is expressed in Sf21 cells or in E. coli.
|In vitro||DMSO||65 mg/mL (198.66 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+50% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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