Emprumapimod

Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain.

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 Lmna^H222P/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.