Kenpaullone
Kenpaullone is an inhibitor of GSK-3β, HGK, and CDKs that exhibits anti-inflammatory, immunomodulatory, and neuroprotective activities. Kenpaullone increases levels of SREBP-1 as well as GIRK-4 and acetylcholine-activated inwardly rectifying K+ (IKACh) channels in diabetic mice. Kenpaullone also inhibits TGF-β-induced induction of RORγt and increases expression of Foxp3 in T cells, inhibiting pathology of experimental autoimmune encephalitis (EAE) in vivo. In pluripotent stem cells derived from autotrophic lateral sclerosis (ALS) patients, kenpaullone improves motor neuron survival. Additionally, this compound inhibits MPP+-induced cell death in cellular models of Parkinson’s disease by preventing changes in the mitochondrial membrane potential and inhibiting activation of caspases.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18936492
| Cas No. |
142273-20-9 |
|---|---|
| Purity |
≥95% |
| Formula |
C16H11BrN2O |
| Formula Wt. |
327.18 |
| Chemical Name |
9-Bromo-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5H)-one |
| IUPAC Name |
9-bromo-7,12-dihydro-5H-indolo[3,2-d][1]benzazepin-6-one |
| Melting Point |
>330°C |
| Solubility |
Soluble in DMSO. Insoluble in water and ethanol. |
| Appearance |
Light brown powder |
Zhang Y, Welzig CM, Picard KL, et al. Glycogen synthase kinase-3β inhibition ameliorates cardiac parasympathetic dysfunction in type 1 diabetic akita mice. Diabetes. 2014 Jun;63(6):2097-113. PMID: 24458356.
Yoshida H, Kotani H, Kondo T, et al. CDK inhibitors suppress Th17 and promote iTreg differentiation, and ameliorate experimental autoimmune encephalomyelitis in mice. Biochem Biophys Res Commun. 2013 Jun 7;435(3):378-84. PMID: 23665028.
Yang YM, Gupta SK, Kim KJ, 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 Jun 6;12(6):713-26. PMID: 23602540.
Petit-Paitel A, Brau F, Cazareth J, et al. Involvment of cytosolic and mitochondrial GSK-3beta in mitochondrial dysfunction and neuronal cell death of MPTP/MPP-treated neurons. PLoS One. 2009;4(5):e5491. PMID: 19430525.
