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KenPaullone [142273-20-9]

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Référence NB-64-11730-2mg

Conditionnement : 2mg

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KenPaullone

(Synonyms: NSC-664704, 9-Bromopaullone) Copy Product Info

Synonyms: NSC-664704, 9-Bromopaullone

Catalog No. T2247 Copy Product Info

Purity: 98.99%

KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway.

Cas No. 142273-20-9

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.99%

Color:Yellow

Product Introduction

Bioactivity

Description	KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway.
Targets & IC50	CDK5-p35:0.85μM, ERK2:9 μM, CDK2-CyclinE:7.5μM, ERK1:20 μM, C-Raf:38 μM, CDK2-CyclinA:0.68μM, CDK1-CyclinB:0.4μM, GSK-3β:0.23μM
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 (20 μM) strongly suppresses the autophosphorylation of GSK3β at Tyr216 in vitro whether GSK3 is expressed in Sf21 cells or in E. coli[2][3].
Synonyms	NSC-664704, 9-Bromopaullone
Kinase Assay	IC50 determination: Active GST-LRRK2 (1326-2527), GST-LRRK2 [G2019S] (1326-2527), GST-LRRK2 [A2016T] (1326-2527) and GST-LRRK2 [A2016T+G2019S] (1326-2527) enzyme is purified with glutathione sepharose from HEK293 cell lysate 36 h following transient transfection of the appropriate cDNA constructs. Peptide kinase assays, performed in duplicate, are set up in a total volume of 40 μL containing 0.5 μg LRRK2 kinase (which at approximately 10% purity gives a final concentration of 8 nM) in 50 mM Tris/HCl, pH 7.5, 0.1 mM EGTA, 10 mM MgCl2, 20 μM Nictide, 0.1 μM [γ-32P]ATP (~500 cpm/pmol) and the indicated concentrations of inhibitor dissolved in DMSO. After incubation for 15 min at 30 °C, reactions are terminated by spotting 35 μL of the reaction mix onto P81 phosphocellulose paper and immersion in 50 mM phosphoric acid. Samples are washed extensively and the incorporation of [γ-32P]ATP into Nictide is quantified by Cerenkov counting. IC50 values are calculated with GraphPad Prism using non-linear regression analysis.

Chemical Properties

Molecular Weight	327.18
Formula	C₁₆H₁₁BrN₂O
Cas No.	142273-20-9
Smiles	Brc1ccc2[nH]c-3c(CC(=O)Nc4ccccc-34)c2c1
Relative Density.	1.596 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 1.6 mg/mL (4.89 mM), Heating is recommended.

DMSO: 41.67 mg/mL (127.36 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn oil: < 4.17 mg/mL (12.75 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

10% DMSO+90% (20% SBE-β-CD in Saline): < 4.17 mg/mL (12.75 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: < 4.17 mg/mL (12.75 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

10% DMSO+90% Saline: < 4.17 mg/mL (12.75 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

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

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0564 mL	15.2821 mL	30.5642 mL	152.8211 mL

DMSO

	1mg	5mg	10mg	50mg
5 mM	0.6113 mL	3.0564 mL	6.1128 mL	30.5642 mL
10 mM	0.3056 mL	1.5282 mL	3.0564 mL	15.2821 mL
20 mM	0.1528 mL	0.7641 mL	1.5282 mL	7.6411 mL
50 mM	0.0611 mL	0.3056 mL	0.6113 mL	3.0564 mL
100 mM	0.0306 mL	0.1528 mL	0.3056 mL	1.5282 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 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 DMSO 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 DMSO stock solution to 400 µL PEG300 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 ddH₂O 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.

Dose Conversion

Keywords

NSC664704NSC 664704KenPaulloneInhibitorinhibitGSK-3βGSK-3GSK3Glycogen synthase kinase-3Glycogen synthase kinase 3Cyclin dependent kinaseCDK5/p35CDK2/CyclinECDK2/CyclinACDK1/CyclinBCDK

Related Tags: KenPaullone chemical structure | KenPaullone in vitro | KenPaullone formula | KenPaullone molecular weight