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Kenpaullone CDK inhibitor

Name: Kenpaullone
Brand: Selleck Chemicals
SKU: S7917
Rating: 5 (6 reviews)

Cat.No.S7917

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

Chemical Structure

Molecular Weight: 327.18

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Quality Control

Batch: Purity: 99.01%

99.01

Related Targets	HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase Casein Kinase
Other CDK Inhibitors	AS2863619 Ro-3306 SEL120 (SEL120-34A) hydrochloride INX-315 Tagtociclib (PF-07104091) PF-07220060 (CDK4/6-IN-6) AZD4573 ON123300 Enitociclib (BAY 1251152) Samuraciclib (ICEC0942) hydrochloride

Chemical Information, Storage & Stability

Molecular Weight	327.18	Formula	C₁₆H₁₁BrN₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	142273-20-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	9-Bromopaullone, NSC-664704			Smiles	C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)Br

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (198.66 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 50%PEG300 2 5%Tween80 3 43%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (7.64mM)	Taking the 1 mL working solution as an example, add 20 μL of 125 mg/ml clarified DMSO stock solution to 500 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 430 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (2.45mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (2.45mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	GSK-3β (Cell-free assay) 0.23μM CDK1/CyclinB (Cell-free assay) 0.4μM CDK2/CyclinA (Cell-free assay) 0.68μM CDK5/p35 (Cell-free assay) 0.85μM CDK2/CyclinE (Cell-free assay) 7.5μM ERK2 (Cell-free assay) 9μM c-Src (Cell-free assay) 15μM Casein Kinase 2 (Cell-free assay) 20μM ERK1 (Cell-free assay) 20μM
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. This compound also induces the dephosphorylation of both GSK3 isoforms in SH-SY5Y cells and PC12 cells. It (20µM) strongly suppresses the autophosphorylation of GSK3β at Tyr216 in vitro whether GSK3 is expressed in Sf21 cells or in E. coli.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10363974/ [2] https://pubmed.ncbi.nlm.nih.gov/14570592/ [3] https://pubmed.ncbi.nlm.nih.gov/11013232/

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Handling Instructions

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