Kenpaullone

Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.

Product Specifications

CAS Number

[142273-20-9]

Product Name Alternative

9-Bromopaullone; NSC-664704

UNSPSC

12352005

Hazard Statement

H315, H319

Target

CDK; GSK-3

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Kenpaullone.html

Purity

98.20

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1NC2=CC=CC=C2C(NC3=C4C=C(Br)C=C3)=C4C1

Molecular Formula

C16H11BrN2O

Molecular Weight

327.18

Precautions

H315, H319

References & Citations

[1]Zaharevitz DW, et al. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 1999 Jun 1;59 (11) :2566-9.|[2]Lyssiotis CA, et al. Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. Proc Natl Acad Sci U S A. 2009 Jun 2;106 (22) :8912-7.|[3]F Yu, et al. Kruppel-like factor 4 (KLF4) is required for maintenance of breast cancer stem cells and for cell migration and invasion. Oncogene. 2011 May 5;30 (18) :2161-72.