Kenpaullone A Cdk and GKS-3 inhibitor

Kenpaullone (CAS 142273-20-9)

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Sinónimo: 9-Bromo-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5H)-one;NSC 664704
Solicitud: A Cdk and GKS-3 inhibitor
Número de CAS: 142273-20-9
Pureza: ≥98%
Peso Molecular: 327.17
Fórmula Molecular: C16H11BrN2O
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Kenpaullone is an ATP-competitive inhibitor of several CDKs (cyclin-dependent kinases) as well as GSK-3β (glycogen synthase kinase 3β). It has been shown to inhibit GSK-3 with an IC50 value of 0.23 μM and CDK1/cyclin B, CDK2/cyclin A, CDK5/p25, and lymphocyte kinase with IC50 values of 0.4, 0.68, 0.85, and 0.47 μM, respectively. Due to the compound's activity, Kenpaullone is useful in the study of cell cycle regulators. Kenpaullone is an inhibitor of cyclin E, ERK 2 and p35.


References

1. Zaharevitz, D W., et al., 1999. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer research. 59(11): 2566-9. PMID: 10363974
2. Leclerc, S., et al., 2001. Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors? The Journal of biological chemistry. 276(1): 251-60. PMID: 11013232
3. Bain, Jenny., et al., 2003. The specificities of protein kinase inhibitors: an update. The Biochemical journal. 371(Pt 1): 199-204. PMID: 12534346

Apariencia :
Brown to yellow powder
Estado de Materia :
Solid
Solubilidad :
Soluble in DMSO (>25 mg/ml), ethyl acetate, DMSO:PBS(pH7.2)(1:1), and DMF. Insoluble in ethanol, and water.
ALMACENAMIENTO :
Store at -20° C
Punto de Fusión :
>300° C
Punto de ebullición :
~613.0° C at 760 mmHg (Predicted)
Densidad :
~1.6 g/cm3 (Predicted)
Indice de Refracción :
n20D 1.73
IC50 :
CDK1/cyclin B: IC50 = 400 nM; CDK2/cyclin A: IC50 = 680 nM; CDK5: IC50 = 850 nM; GSK-3β: IC50 = 23 nM; CDK2/cyclin E: IC50 = 7.5 µM; CDK5/cyclin/p35: IC50 = 850 nM; c-src: IC50 = 150 nM; casein kinase 2: IC50 = 200 nM; ERK1: IC50 = 20 µM; ERK2: IC50 = 9 µM; lymphocyte kinase: IC50 = 470 nM
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
3820
Número MDL :
MFCD02683595
SMILES :
C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)Br

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Kenpaullone  Menciones del Producto

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Citaciones 1 a 1 de un total de 1

PMID: # 16162845  Plante, I. et al. 2005. Toxicol. Sci. 88: 346-357.

Citaciones 1 a 1 de un total de 1
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