| Bioactivity | 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]. | ||||||||||||
| Target | proteasome β1i (LMP2) subunit inhibitor | ||||||||||||
| Invitro | 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]. | ||||||||||||
| 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: | ||||||||||||
| Name | ML604440 | ||||||||||||
| CAS | 1140517-08-3 | ||||||||||||
| Formula | C17H24BF3N2O4 | ||||||||||||
| Molar Mass | 388.19 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
ML604440
CAS: 1140517-08-3 F: C17H24BF3N2O4 W: 388.19
ML604440 is a specific and cell-permeable Proteasome β1i (LMP2) subunit inhibitor. ML604440 can be used in experimental
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