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KenPaullone

Catalog No. T2247 CAS 142273-20-9

Synonyms: 9-Bromopaullone, NSC-664704

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.

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KenPaullone, CAS 142273-20-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
2 mg	In stock	$ 45.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 96.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 336.00
100 mg	In stock	$ 498.00
500 mg	In stock	$ 1,130.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

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Purity: 98.99%

Purity: 98%

Purity: 97.92%

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Storage & Solubility Information

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, CDK2-CyclinE:7.5μM, 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].
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.

Synonyms	9-Bromopaullone, NSC-664704
Molecular Weight	327.18
Formula	C16H11BrN2O
CAS No.	142273-20-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 1.6 mg/mL (5 mM)), Heating is recommended.

DMSO: 32.7 mg/mL (100 mM)

References and Literature

1. Zaharevitz et al. Cancer Res. 1999, 59(11):2566-2569. 2. Adam COLE, et al. Biochem. J. 2004, 377(1):249-255. 3. Leclerc S, et al. J Biol Chem. 2001, 276(1):251-260. 4. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity[J]. Biochemical and biophysical research communications. 2019 Jun 11;513(4):967-973.

Citations

1. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity. Biochemical and Biophysical Research Communications. 2019 Jun 11;513(4):967-973

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library Anti-Cancer Active Compound Library Target-Focused Phenotypic Screening Library Wnt/Hedgehog/Notch Compound Library Anti-Lung Cancer Compound Library Bioactive Lipid Compound Library Autophagy Compound Library Glycolysis Compound Library

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Cyanoacetohydrazide AR-A014418 9-Hydroxycanthin-6-one GSK-3β inhibitor 11 Dehydroglyasperin D AT7519 Hydrochloride MeBIO A 1070722

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Keywords

KenPaullone 142273-20-9 Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling Stem Cells GSK-3 CDK Glycogen synthase kinase 3 NSC 664704 9-Bromopaullone inhibit NSC-664704 Inhibitor NSC664704 Cyclin dependent kinase Glycogen synthase kinase-3 inhibitor

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