Kenpaullone

• CAT Number: I001633
• CAS Number: 142273-20-9
• Molecular Formula: C₁₆H₁₁BrN₂O
• Molecular Weight: 327.18
• Purity: ≥95%
• Target: Cyclin-Dependent Kinases
• Solubility: DMSO: ≥ 35 mg/mL
• Storage: 2-8°C
• IC50: 0.23 μM (GSK-3β), 0.4 μM (CDK1/cyclin B), 0.68 μM (CDK2/cyclin A), 0.85μM (CDK5/p25), and 0.47 μM ( lymphocyte kinase)
• IUPAC Name: 9-bromo-7,12-dihydro-5H-indolo[3,2-d][1]benzazepin-6-one
• InChI: InChI=1S/C16H11BrN2O/c17-9-5-6-14-11(7-9)12-8-15(20)18-13-4-2-1-3-10(13)16(12)19-14/h1-7,19H,8H2,(H,18,20)
• InChIKey: QQUXFYAWXPMDOE-UHFFFAOYSA-N
• SMILES: C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)Br

Kenpaullone（Cat No.: I001633）， also known as 9-Bromopaullone and NSC-664704, is a potent ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It is particularly notable for its inhibitory activity against CDKs and glycogen synthase kinase 3 beta (GSK3β), with an IC50 of 0.23 μM against GSK3β. This compound has valuable applications in cell cycle regulation research and drug development. If you require further information or assistance regarding Kenpaullone, please feel free to contact us.

Reference

1:Eur J Med Chem. 2005 Aug;40(8):757-63. Epub 2005 Apr 12. New thiophene analogues of kenpaullone: synthesis and biological evaluation in breast cancer cells.Brault L,Migianu E,Néguesque A,Battaglia E,Bagrel D,Kirsch G, PMID: 16122578 DOI: 10.1016/j.ejmech.2005.02.010 Abstract: Thieno analogues of kenpaullone have been synthesized using an established method. We investigated the effect of five structural analogues of kenpaullone on vincristine sensitive and resistant MCF7 (human mammary adenocarcinoma) cells. One analogue, 8-Bromo-6,11-dihydro-thieno-[3/’,2/’:2,3]azepino[4,5-b]indol-5(4H)-one (3a), showed an antiproliferative activity in the drug sensitive cell line that led to cell accumulation in G2/M phase. In addition, repression of cdk1, a G2/M transition key regulator, as well as induction of p21 were observed at the mRNA level. Programmed cell death (apoptosis) was induced in early time treatments and was accompanied by p53 mRNA induction. The antiproliferative and proapoptotic properties of 3a make this CDK inhibitor an interesting candidate for further investigations.