cdki 83.

Metaxalone-D6 is intended for use as an internal standard for the quantification of metaxalone by GC-or LC-MS. Metaxalone (T1610) is a skeletal muscle relaxant. It inhibits the proliferation of,and induces apoptosis in,RAW 264.7 cells in vitro when used at concentrations ranging from 1 to 100 µM. Metaxalone (T1610)also reduces LPS-induced increases in COX-1,COX-2,and NF-kB levels and inhibits LPS-induced production of TNF-α,IL-6,and prostaglandin E2 in RAW 264.7 cells. Formulations containing metaxalone have been used in the treatment of lower back pain.

CDKI-83 is a potent CDK9 inhibitor. The compound shows effective anti-proliferative activity in human tumour cell lines with GI50 <1 μM, and is capable of inducing apoptosis in A2780 human ovarian cancer cells as determined by the activated caspase-3, Annexin V/PI double staining and accumulated cells at the sub-G1 phase of cellcycle. The research results suggest that combined inhibition of CDK9 and CDK1 may result in the effective induction of apoptosis and CDKI-83 has the potential to be developed as an anti-cancer agent.