IMG-7289 (tosylate)

IMG-7289 is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1). It induces cell cycle arrest at the S phase in SET-2 acute megakaryoblastic leukemia cells and apoptosis in Ba/F3 murine hematopoietic cells expressing Jak2 containing a valine-to-phenylalanine substitution at position 617 (Jak2V617F) when used at a concentration of 1 µM. IMG-7289 (45 mg/kg per day) decreases blood levels of leukocytes, neutrophils, monocytes, and platelets, increases bone marrow cell levels of trimethylated lysine 4 histone 3 (H3K4me3) and H3K9me2, decreases spleen fibrosis and weight, and increases survival in a Jak2V617F mouse model of myelofibrosis. InChI: InChI=1S/C28H34FN7O2.2C7H8O3S/c1-34-15-17-35(18-16-34)28(38)25(3-2-12-30-26-19-24(26)20-4-8-22(29)9-5-20)32-27(37)21-6-10-23(11-7-21)36-14-13-31-33-36,2*1-6-2-4-7(5-3-6)11(8,9)10/h4-11,13-14,24-26,30H,2-3,12,15-19H2,1H3,(H,32,37),2*2-5H,1H3,(H,8,9,10)/t24-,25-,26+,,/m0../s1 InChIKey: WLRWBXFBIJMKHG-DVNXTAPYSA-N SMILES: O=S(O)(C1=CC=C(C=C1)C)=O.O=C(N2CCN(CC2)C)[C@@H](NC(C3=CC=C(N4C=CN=N4)C=C3)=O)CCCN[C@H]5[C@H](C6=CC=C(C=C6)F)C5.O=S(O)(C7=CC=C(C=C7)C)=O