For research use only. Not for therapeutic Use.
Kenpaullone（Cat No.:I001633）is a potent and selective inhibitor of cyclin-dependent kinases (CDKs), particularly CDK2 and CDK5, which play critical roles in cell cycle regulation and neuronal function. Initially developed as an anticancer agent, kenpaullone has demonstrated potential in modulating cell proliferation and apoptosis in various cancer types. Additionally, its ability to inhibit CDK5 suggests applications in neurodegenerative diseases, as dysregulation of this kinase is associated with disorders like Alzheimer’s disease. Ongoing research aims to explore kenpaullone’s efficacy in different therapeutic contexts, making it a compound of significant interest in biomedical research.
| Catalog Number | I001633 |
| CAS Number | 142273-20-9 |
| Synonyms | 9-bromo-7,12-dihydrobenzo[2,3]azepino[4,5-b]indol-6(5H)-one |
| Molecular Formula | C₁₆H₁₁BrN₂O |
| 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 |
| 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 </br><span>Abstract:</span> 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. |
