For research use only. Not for therapeutic Use.
ML604440 is a specific and cell-permeable Proteasome β1i (LMP2) subunit inhibitor. ML604440 can be used in experimental colitis, EAE and autoimmune disease research. ML604440 shows synergistic effects and advantageous when combined with LMP7 inhibitor[1][2][3].
ML604440 (300 nM; overnight) treatment shows no influence on the surface expression of H-2Kb in wt or LMP7-deficient mice splenocytes[2].
ML604440 (300 nM; 24 h) treatment shows no significant inhibition of IL-6 secretion by mouse splenocytes or human PBMCs[2].
ML604440 (300 nM; 3 d) shows no influence on the percentage of IL-17A-producing CD4+ T cells[2].
ML604440 (intraperitoneal injection; 10 mg/kg; once daily; 7 d) treatment inhibits LMP2 in vivo, shows no significant changes in platelet counts[3].
| Catalog Number | I018174 |
| CAS Number | 1140517-08-3 |
| Synonyms | [(1R)-3-methyl-1-[[2-methyl-2-[[2-(trifluoromethyl)benzoyl]amino]propanoyl]amino]butyl]boronic acid |
| Molecular Formula | C17H24BF3N2O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H24BF3N2O4/c1-10(2)9-13(18(26)27)22-15(25)16(3,4)23-14(24)11-7-5-6-8-12(11)17(19,20)21/h5-8,10,13,26-27H,9H2,1-4H3,(H,22,25)(H,23,24)/t13-/m0/s1 |
| InChIKey | IRZZVDHGNHGNAI-ZDUSSCGKSA-N |
| SMILES | B(C(CC(C)C)NC(=O)C(C)(C)NC(=O)C1=CC=CC=C1C(F)(F)F)(O)O |
| Reference | [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. [3]. Sheng-Hong Du, et al. Co-Inhibition of the Immunoproteasome Subunits LMP2 and LMP7 Ameliorates Immune Thrombocytopenia. Front Immunol. 2021 Jan 20;11:603278. |
