MI 2 MALT1 inhibitor is a small molecule and irreversible inhibitor of MALT1 with IC50 of 5.84 μM (suppression of proliferation in ABCDLBCL).
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描述 | MI-2, a MALT1 inhibitor (IC50=5.84 μM), directly targets MALT1, irreversibly inhibiting its protease activity. This inhibition is associated with decreased NF-κB reporter activity, blocked c-REL nuclear translocation, and reduced expression of NF-κB-dependent genes. MI-2 is non-toxic to animals[1]. |
体内研究 | The MALT1 inhibitor MI-2 (administered intraperitoneally at a dose of 25 mg/kg daily for 14 days) significantly inhibits the growth of both TMD8 and HBL-1 ABC-DLBCL xenografts. |
体外研究 | The MALT1 inhibitor MI-2 (1-1000 nM; 48 hours) specifically reduces the activity of MALT1-dependent DLBCL cell lines. The GI50 values of HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells are 0.2, 0.5, 0.4, and 0.4 μM, respectively [1]. The MALT1 inhibitor MI-2 (62-1000 nM; 24 hours) induces a reduction in MALT1-mediated cleavage in a dose-dependent manner[1]. |
Dose | Mice: 0.05 mg/kg[2] (i.p.), 30 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.19mL 0.44mL 0.22mL |
10.97mL 2.19mL 1.10mL |
21.94mL 4.39mL 2.19mL |
CAS号 | 1047953-91-2 |
分子式 | C19H17Cl3N4O3 |
分子量 | 455.722 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 45 mg/mL(98.74 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
2% DMSO+30% PEG 300+2% Tween 80+water 3 mg/mL |