Emprumapimod (ARRY-797) inhibits LPS-induced IL-6 production from RPMI-8226 cell with an IC50 value of 100 pM[1].
Emprumapimod (ARRY-797) (30 mg/kg; p.o.) inhibits the expression of IL-6 (91%) and TNF-α (95%) in SCID-beige mice, inhibits the phosphorylation of p38 in RPMI-8226 xenografts, inhibits the growth of RPMI-8226 tumour (72%) in multiple myeloma (MM) xenograft models[1].
Emprumapimod (30 mg/kg; p.o.; twice daily for 4 weeks) prevents left ventricular (LV) dilatation and deterioration of fractional shortening (FS) in LmnaH222P/H222P mice[2].
References:
[1]. Dale Wright, et al. ARRY-797, a Potent and Selective Inhibitor of p38 Map Kinase, Inhibits LPS-Induced IL-6 and In Vivo Growth of RPMI-8226 Human Multiple Myeloma Cells.
[2]. Antoine Muchir, et al. Abnormal p38α mitogen-activated protein kinase signaling in dilated cardiomyopathy caused by lamin A/C gene mutation. Hum Mol Genet. 2012 Oct 1;21(19):4325-33.