Kenpaullone A Cdk and GKS-3 inhibitor

Kenpaullone (CAS 142273-20-9)

Kenpaullone | CAS 142273-20-9 is rated 5.0 out of 5 by 1.
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Synonym: 9-Bromo-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5H)-one; NSC 664704
Application: A Cdk and GKS-3 inhibitor
CAS Number: 142273-20-9
Purity: ≥98%
Molecular Weight: 327.17
Molecular Formula: C16H11BrN2O
* Refer to Certificate of Analysis for lot specific data (including water content).
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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

Appearance :
Brown to yellow powder
Physical State :
Solid
Solubility :
Soluble in DMSO (>25 mg/ml), ethyl acetate, DMSO:PBS(pH7.2)(1:1), and DMF. Insoluble in ethanol, and water.
Storage :
Store at -20° C
Melting Point :
>300° C
Boiling Point :
~613.0° C at 760 mmHg (Predicted)
Density :
~1.6 g/cm3 (Predicted)
Refractive Index :
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
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
3820
MDL Number :
MFCD02683595
SMILES :
C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)Br

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Certificate of Analysis

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Kenpaullone  Product Citations

See how others have used Kenpaullone. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

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

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Plante Plante, et. al. (PubMed ID 16162845) found that by treating MH1C1 cells with kenpaullone, a GSK inhibitor, at 5 M or 10 M concentrations, there was a marked increase in the inactive form of GSK3 (compared to controls). This suggests that kenpaullone inhibits GSK3 in the cell line tested. -SCBT Publication Review
Date published: 2015-06-21
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