For research use only. Not for therapeutic Use.
Senexin B(CAT: I009437) is a potent inhibitor targeting Cdk8 and Cdk19, key cyclin-dependent kinases involved in cell cycle regulation and transcriptional control. With remarkable selectivity, it inhibits Cdk8 and Cdk19 by 97.8% and 98.6%, respectively, among more than 450 kinases at 2 μM concentration. By suppressing their activity (IC50 values ranging from 24 to 50 nM), Senexin B shows promising pharmacologic action as an anti-cancer agent, inhibiting cell growth in estrogen-containing media in breast cancer cells (MCF-7, BT474, and T47D-ER/Luc) in a concentration-dependent manner (1.25-5 μM).
| Catalog Number | I009437 |
| CAS Number | 1449228-40-3 |
| Synonyms | Senexin B;4-((2-(6-(4-methylpiperazine-1-carbonyl)naphthalen-2-yl)ethyl)amino)quinazoline-6-carbonitrile |
| Molecular Formula | C27H26N6O |
| Purity | ≥95% |
| Target | CDK8/19 inhibitor |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| InChI | InChI=1S/C27H26N6O/c1-32-10-12-33(13-11-32)27(34)23-6-5-21-14-19(2-4-22(21)16-23)8-9-29-26-24-15-20(17-28)3-7-25(24)30-18-31-26/h2-7,14-16,18H,8-13H2,1H3,(H,29,30,31) |
| InChIKey | VNADJTWHOAMTLY-UHFFFAOYSA-N |
| SMILES | O=C(C1=CC2=CC=C(CCNC3=C4C(C=CC(C#N)=C4)=NC=N3)C=C2C=C1)N5CCN(C)CC5 |
| Reference | </br>Abstract PR08: Targeting tumor microenvironment with selective small-molecule inhibitors of CDK8/19. Donald C. Porter1, Mengqian Chen2, Jiaxin Liang2, Vimala Kaza1, Alexander Chumanevich1, Serena Altilia1, Elena Farmaki3, Marj Pena2, Gary P. Schools2, Ioulia Chatzistamou3, Lawrence T. Friedhoff1, Mark P. Wentland4, Eugenia V. Broude2, Hippokratis Kiaris3, and Igor B. Roninson2. Abstracts: AACR Special Conference on Cellular Heterogeneity in the Tumor Microenvironment; February 26 — March 1, 2014; San Diego, CA |
