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Kenpaullone

Chemical Structure : Kenpaullone

CAS No.: 142273-20-9

Kenpaullone (9-Bromopaullone;NSC-664704)

Catalog No.: PC-42965Not For Human Use, Lab Use Only.

Kenpaullone (9-Bromopaullone,NSC-664704) is a potent inhibitor of CDK1/cyclin B with IC50 of 0.4 uM, also inhibited CDK2/cyclin A (IC50=0.68 uM), CDK2/cyclin E (IC50-7.5 uM) and CDK5/p25 (IC50=0.85 uM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Kenpaullone (9-Bromopaullone,NSC-664704) is a potent inhibitor of CDK1/cyclin B with IC50 of 0.4 uM, also inhibited CDK2/cyclin A (IC50=0.68 uM), CDK2/cyclin E (IC50-7.5 uM) and CDK5/p25 (IC50=0.85 uM).
Kenpaullone shows less effect on other kinases, only c-Src, CK2, ERK1/2 (IC50=15-20 uM) with IC50s less than 30 uM.
Kenpaullone displays delayed cell cycle progression in treated cells; also is a potent inhibitor of GSK-3β (IC50=23 nM), activates Nanog expression in mouse fibroblasts transduced with a subset of reprogramming factors lacking Klf4, can replace Klf4 in the reprogramming of primary and secondary fibroblasts and NPCs.

Physicochemical Properties

M.Wt 327.1754
Formula C16H11BrN2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 35 mg/mL

Chemical Name/SMILES

Indolo[3,2-d][1]benzazepin-6(5H)-one, 9-bromo-7,12-dihydro-

References

1. Zaharevitz DW, et al. Cancer Res. 1999 Jun 1;59(11):2566-9.

2. Schultz C, et al. J Med Chem. 1999 Jul 29;42(15):2909-19.

3. Bain J, et al. Biochem J. 2003 Apr 1;371(Pt 1):199-204.

4. Lyssiotis CA, et al. Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.

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