Ralimetinib dimysylate (LY2228820 dimysylate)

Description: Ralimetinib dimysylate (also known as LY-2228820; LY2228820) is a novel, potent and selective ATP-competitive inhibitor of p38 MAPK with potential anti-inflammatory activity. It inhibits p38 MAPK with an IC50 of 7 nM in a cell-free assay, and does not alter p38 MAPK activation. In cell-based assays, LY2228820 potently and selectively inhibited phosphorylation of MK2 (Thr334) in anisomycin-stimulated HeLa cells (at 9.8 nmol/L by Western blot analysis) and anisomycin-induced mouse RAW264.7 macrophages (IC(50) = 35.3 nmol/L) with no changes in phosphorylation of p38alpha MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc <= 10 umol/L.

References: Bioorg Med Chem Lett. 2008 Jan 1; 18(1):179-83; Br J Haematol. 2008 May; 141(5):598-606.

Related CAS: 862505-00-8 (free base); 862507-23-1 (mesylate)

LY-2228820; LY 2228820; Ralimetinib; LY2228820; LY2228820 dimesylate; Ralimetinib dimesylate

Chemical Name: 5-(2-(tert-butyl)-5-(4-fluorophenyl)-1H-imidazol-4-yl)-3-neopentyl-3H-imidazo[4, 5-b]pyridin-2-amine

InChi Key: XPPBBJCBDOEXDN-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H29FN6/c1-23(2, 3)13-31-20-17(28-22(31)26)12-11-16(27-20)19-18(14-7-9-15(25)10-8-14)29-21(30-19)24(4, 5)6/h7-12H, 13H2, 1-6H3, (H2, 26, 28)(H, 29, 30)

SMILES Code: NC1=NC2=CC=C(C3=C(C4=CC=C(F)C=C4)NC(C(C)(C)C)=N3)N=C2N1CC(C)(C)C