MK-8745

• CAT Number: I005315
• CAS Number: 885325-71-3
• Molecular Formula: C₂₀H₁₉ClFN₅OS
• Molecular Weight: 431.91
• Purity: ≥95%
• Target: Aurora Kinase
• Solubility: DMSO: 86 mg/mL; Ethanol: 1 mg/mL
• Storage: Store at -20 C
• InChI: InChI=1S/C20H19ClFN5OS/c21-16-5-2-4-15(18(16)22)19(28)27-10-8-26(9-11-27)13-14-3-1-6-17(24-14)25-20-23-7-12-29-20/h1-7,12H,8-11,13H2,(H,23,24,25)
• InChIKey: YCRFPWKUUNKNDN-UHFFFAOYSA-N
• SMILES: C1CN(CCN1CC2=NC(=CC=C2)NC3=NC=CS3)C(=O)C4=C(C(=CC=C4)Cl)F

MK-8745 (Cat.No:I005315) is a selective and orally active inhibitor of acetyl-CoA carboxylase (ACC). It is being studied for its potential in the treatment of metabolic diseases such as obesity and type 2 diabetes. MK-8745 works by inhibiting ACC, an enzyme involved in fatty acid synthesis, leading to decreased lipid production and improved metabolic control.

Reference

1:Leuk Lymphoma. 2012 Mar;53(3):462-71. doi: 10.3109/10428194.2011.619018. Epub 2011 Oct 24. A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines.Chowdhury A,Chowdhury S,Tsai MY, PMID: 21879811 DOI: 10.3109/10428194.2011.619018 Abstract: Selective small-molecule kinase inhibitors have encouraging clinical efficacy in several malignancies. These agents are still limited to a subset of patients, indicating the need to develop therapeutic biomarkers that influence clinical benefit. In this study, we demonstrate that treatment with MK-8745, a novel Aurora-A specific inhibitor, leads to cell cycle arrest at the G2/M phase with accumulation of tetraploid nuclei followed by cell death in non-Hodgkin lymphoma (NHL) cell lines. The sensitivity of the cell lines to MK-8745 is correlated with the expression level of Aurora-A activator. The siRNA knockdown of Aurora-A activator TPX2 (targeting protein for Xenopus kinase-like protein 2) increased MK-8745 sensitivity in less-MK-8745-sensitive NHL cell lines, whereas overexpression of TPX2 in high-MK-8745-sensitive NHL cell lines increased drug resistance. Our results indicate that TPX2 may serve as a biomarker for identifying subpopulations of patients sensitive to Aurora-A inhibitor treatment.