GW 856553X

GW 856553X is a dual inhibitor of p38α and p38β MAPK (K_is = 0.0079 and 0.025 µM, respectively, in cell-free assays).¹ It is selective for p38α and p38β MAPK over p38γ and p38δ MAPK when used at a concentration of 10 µM. GW 856553X inhibits LPS-induced TNF-α production in isolated rat and human peripheral blood mononuclear cells (PBMCs; IC₅₀s = 0.6 and 0.13 µM, respectively). It decreases disease severity in a mouse model of collagen-induced arthritis when administered at doses ranging from 0.8 to 20 mg/kg.² GW 856553X (1.2 and 12 mg/kg) improves survival, normalizes blood pressure, and reduces increases in plasma levels of HDL, LDL, and triglycerides in spontaneously hypertensive stroke-prone rats fed a high-salt high-fat diet.¹

WARNING This product is not for human or veterinary use.

1. Willette, R.N., Eybye, M.E., Olzinski, A.R., et al. Differential effects of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model of cardiovascular disease. J. Pharmacol. Exp. Ther. 330(3), 964-970 (2009).

2. Triantaphyllopoulos, K., Madden, L., Rioja, I., et al. In vitro target validation and in vivo efficacy of p38 MAP kinase inhibition in established chronic collagen-induced arthritis model: A pre-clinical study. Clin. Exp. Rheumatol. 28(2), 176-185 (2010).

Maronde, E. Trehalose activates CRE-dependent transcriptional signaling in HT22 mouse hippocampal neuronal cells: A central role for PKA without cAMP elevation. Front. Mol. Neurosci. 11:386, (2018).