Territorial Availability: Available through Bertin Technologies only in France
- Synonyms
- 5-[6-[(4-methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide
- Correlated keywords
- 1000873-97-1 biochemical inhibitor protein kinase intracellular signaling cell cycle cancer inhibit GSK 461364 461364A GSK461364-A Plk-1 reversible polo-like Plk1
- Product Overview:
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} GSK461364 is a potent, reversible inhibitor of Plk1 (Ki = 2.2 nM).{29227} It is less effective against Plk2 and Plk3 (Kis = 860 and 1,000 nM, respectively) and at least 1,000-fold selective for Plk1 over a panel of 48 other kinases.{29227} GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis.{29227} It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier.{29226,29225} GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.{29228,29227}
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.