Kenpaullone

Catalog No.S7917 Synonyms: 9-Bromopaullone, NSC-664704

For research use only.

Kenpaullone (9-Bromopaullone, NSC-664704) is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It also inhibit glycogen synthase kinase 3β (GSK3β) with IC50 of 0.23 µM.

Kenpaullone Chemical Structure

CAS No. 142273-20-9

Selleck's Kenpaullone has been cited by 4 Publications

1 Customer Review

Purity & Quality Control

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Biological Activity

Description Kenpaullone (9-Bromopaullone, NSC-664704) is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It also inhibit glycogen synthase kinase 3β (GSK3β) with IC50 of 0.23 µM.
Targets
GSK-3β [1]
(Cell-free assay)
CDK1/CyclinB [1]
(Cell-free assay)
CDK2/CyclinA [1]
(Cell-free assay)
CDK5/p35 [1]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
Click to View More Targets
0.23μM 0.4μM 0.68μM 0.85μM 7.5μM
In vitro

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[2][3].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 65 mg/mL
(198.66 mM)
Water Insoluble
Ethanol Insoluble

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.

2.5mg/mL

Chemical Information

Molecular Weight 327.18
Formula

C16H11BrN2O

CAS No. 142273-20-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)Br

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

Molarity Calculator

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Tech Support

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.

Handling Instructions

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