ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor[1].ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naÏve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE[2].
[1]. de Bruin G, et al. Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. J Med Chem. 2014 Jul 24;57(14):6197-209 [2]. Basler M, et al. Co-inhibition of immunoproteasome subunits LMP2 and LMP7 is required to block autoimmunity. EMBO Rep. 2018 Dec;19(12). pii: e46512.
















