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Cat. No. Name Size Price Add Cart
KI1460Kenpaullone1 mg$158

Chemical Characteristic

Product NameKenpaullone
Synonyms9-bromopaullone, NSC-664704
CAS No.142273-20-9
Molecular Weight 327.18
FormulaC16H11BrN2O
Chemical Name9-bromo-7,12-dihydrobenzo[2,3]azepino[4,5-b]indol-6(5H)-one
SmilesN1C(=O)Cc2c(c3c1cccc3)[nH]c1c2cc(cc1)Br
Chemical Structure

Biological activities

Kenpaullone is a potent ATP-competitive GSK3-β and CDK inhibitor. The IC50 of kenpaullone is 23 nM against GSK3-β.[1] The IC50 of kenpaullone is 0.4 µM against CDK1.[2] Kenpaullone inhibits CDK2/cyclin A, CDK2/cyclin E and CDK4/cyclin D1 with an IC50 of 0.68, 7.5 and 100 µM, respectively.[3] Kenpaullone dose-dependently inhibits TGF-β-induced RORγt induction. Kenpaullone suppresses Th17 differentiation. Kenpaullone strongly promotes iTreg development under Th17 conditions. Kenpaullone also promotes Foxp3 protein levels. Kenpaullone significantly ameliorates the severity of EAE and reduced infiltration of Th17 cells into the central nerve system (CNS). Kenpaullone at 1 µM slightly decreases GSK-3β phosphorylation and enhances β-catenin accumulation. Kenpaullone inhibits CDKs more strongly than GSK-3β under Th17 conditions. [1] Kenpaullone decreases mutant SOD1 levels. Kenpaullone promotes survival of motor neurons derived from human ALS iPSCs.[4] Kenpaullone induces a slight increase in proliferation of MCF7 cells.[5] Kenpaullone requires transduction of c-Myc for reprogramming.[6] Kenpaullone inhibits NF-κB in U251, T98, and U87 cells.[7] Kenpaullone suppresses experimental autoimmune encephalomyelitis (EAE), a typical Th17-mediated autoimmune disease model in mice.[1]

Protocols

In vitro: Kenpaullone are dissolved in 100% DMSO.[7]

References

[1] Yoshida H, et al. CDK inhibitors suppress Th17 and promote iTreg differentiation, and ameliorate experimental autoimmune encephalomyelitis in mice. Biochem Biophys Res Commun. 2013.
[2] Al-Sha'er MA, et al. Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay. Eur J Med Chem. 2010, 45(9): 4316-4330.
[3] Crews CM, et al. Small-molecule inhibitors of the cell cycle. Curr Opin Chem Biol. 2000, 4(1): 47-53.
[4] Yang YM, et al. A Small molecule screen in stem-cell-derived motor neurons identifies a kinase inhibitor as a candidate therapeutic for ALS. Cell Stem Cell. 2013.
[5] Kim HM, et al. CG0009, a novel glycogen synthase kinase 3 inhibitor, induces cell death through cyclin D1 depletion in breast cancer cells. PLoS One. 2013, 8(4): e60383.
[6] Lyssiotis CA, et al. Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. Proc Natl Acad Sci. 2009, 106(22): 8912-8917.

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