| Identification | Back Directory | [Name]
ML 604440 | [CAS]
1140517-08-3 | [Synonyms]
ML 604440
(R)-(3-Methyl-1-(2-methyl-2-(2-(trifluoromethyl)benzamido)propanamido)butyl)boronic acid
Boronic acid, B-[(1R)-3-methyl-1-[[2-methyl-1-oxo-2-[[2-(trifluoromethyl)benzoyl]amino]propyl]amino]butyl]-
CD4+T cell,human PBMCs,Inhibitor,ML 604440,Proteasome,ML604440,LMP7-deficient mice splenocytes,EAE,cell-permeable,ML-604440,inhibit,autoimmune disease,experimental colitis | [Molecular Formula]
C17H24BF3N2O4 | [MDL Number]
MFCD32201041 | [MOL File]
1140517-08-3.mol | [Molecular Weight]
388.19 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
ML604440 (intraperitoneal injection; 10 mg/kg; once daily; 7 d) treatment inhibits LMP2 in vivo, shows no significant changes in platelet counts[3]. | Animal Model: | Male C57BL/6J mice (6-8-wks old) injected with anti-platelet monoclonal antibody[3] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; 10 mg/kg; once daily; 7 days | | Result: | Inhibited LMP2 in vivo.
Showed no significant improvement in platelet counts in mice immunized by monoclonal rat anti-mouse CD41 platelet antibody. |
| [References]
[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 DOI:10.1021/jm500716s
[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. DOI:10.15252/embr.201846512
[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. DOI:10.3389/fimmu.2020.603278 |
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