Description
AR-A014418 is an inhibitor of GSK-3β that exhibits anticancer, analgesic, cognition enhancing, neuroprotective, and anti-inflammatory activities. AR-A014418 decreases cell viability and downregulates expression of splicing factors, Bcl-2, Bcl-xl, survivin, and MCL-1 in glioma cells. In models of neuropathic pain, AR-A014418 inhibits thermal hyperalgesia and mechanical allodynia, potentially through suppressing expression of glutamate transporter GLT-1. This compound also inhibits the development of learning and memory deficits in animal models of diabetes. In spinal cord injury models, AR-A014418 prevents mitochondrial apoptosis and decreases levels of pro-inflammatory cytokines.
References
Yadav AK, Vashishta V, Joshi N, et al. AR-A 014418 Used against GSK3beta Downregulates Expression of hnRNPA1 and SF2/ASF Splicing Factors. J Oncol. 2014;2014:695325. PMID: 24550987.
Weng HR, Gao M, Maixner DW. Glycogen synthase kinase 3 beta regulates glial glutamate transporter protein expression in the spinal dorsal horn in rats with neuropathic pain. Exp Neurol. 2014 Feb;252:18-27. PMID: 24275526.
King MR, Anderson NJ, Guernsey LS, et al. Glycogen synthase kinase-3 inhibition prevents learning deficits in diabetic mice. J Neurosci Res. 2013 Apr;91(4):506-14. PMID: 23362012.
Tunçdemir M, Yıldırım A, Karaoğlan A, et al. AR-A014418 as a glycogen synthase kinase-3 inhibitor: anti-apoptotic and therapeutic potential in experimental spinal cord injury. Neurocirugia (Astur). 2013 Jan-Feb;24(1):22-32. PMID: 23116585.
