MALT1 inhibitor MI-2 |
| カタログ番号GC36534 |
MALT1 阻害剤 MI-2 は MALT1 阻害剤です (IC50=5.84 μM)。 MALT1 阻害剤 MI-2 は MALT1 に直接結合し、不可逆的にプロテアーゼ機能を抑制し、NF-κB レポーター活性抑制、c-REL 核局在化阻害、および NF-κB 標的遺伝子のダウンレギュレーションを伴います。 MALT1 阻害剤 MI-2 は、動物に対して無毒であることを示しています。
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Cas No.: 1047953-91-2
Sample solution is provided at 25 µL, 10mM.
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MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to mice[1]. IC50: 5.84 μM (MALT1)[1]
MALT1 inhibitor MI-2 (1-1000 nM; 48 hours) selectively suppresses MALT1-dependent DLBCL cell lines, and the GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells is 0.2, 0.5, 0.4, and 0.4 µM, respectively[1].MALT1 inhibitor MI-2 (62-1000 nM; 24 hours) causes a dose-dependent decrease in MALT1-mediated cleavage[1]. Cell Proliferation Assay[1] Cell Line: HBL-1, TMD8, OCI-Ly3, OCI-Ly10 cells
MALT1 inhibitor MI-2 (25 mg/kg; i.p.; daily for 14 days) profoundly suppresses the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts[1]. Animal Model: Eight-week-old male SCID NOD (bearing HBL-1 and TMD8 cells)[1]
[1]. Fontan L, et al. MALT1 small molecule inhibitors specifically suppress ABC-DLBCL in vitro and in vivo. Cancer Cell. 2012 Dec 11;22(6):812-24.
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