Chemical Structure : M1i-124
货号: PC-24363Not For Human Use, Lab Use Only.
M1i-124 is a first-in-class, small-molecule inhibitor of BCL10-MALT1 interaction with IC50 of 16 uM, abrogates MALT1 scaffolding and protease activities, promotes degradation of BCL10 and MALT1 proteins.
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M1i-124 is a first-in-class, small-molecule inhibitor of BCL10-MALT1 interaction with IC50 of 16 uM, abrogates MALT1 scaffolding and protease activities, promotes degradation of BCL10 and MALT1 proteins.
M1i-124 shows binding affinity of M1i-124 to immobilized full-length MALT1 with SPR KD of 296 uM.
M1i-124 (1 uM) inhibits MALT1-dependent cytokine expression and secretion in stimulated Jurkat T cells and primary splenocytes.
M1i-124 (1 uM) inhibits MALT1 protease and scaffolding functions, and MALT1-dependent cytokine secretion, in ABC-DLBCL cells, induces specific protein loss for BCL10 and MALT1.
M1i-124 selectively inhibits ABC-DLBCL cell proliferation and survival of MALT1-dependent ABC-DLBCL cells, but not MALT1-independent GCB-DLBCL cells.
M1i-124 (50 mg/kg i.p. per day) inhibits ABC-DLBCL lymphoma tumor growth in a xenograft mouse model.
分子量 | 594.65 | |
分子式 | C29H26N2O8S2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Kang H, et al. J Clin Invest. 2025 Apr 15;135(8):e164573.
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