Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MI 2 (MALT1 inhibitor) 是一种MALT1抑制剂 (IC50=5.84 μM),对动物无毒性。它能够直接与 MALT1 结合,不可逆地抑制蛋白酶功能,并伴有 NF-κB 报告子活性抑制、c-REL 核定位抑制和 NF-κB 靶基因下调。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 343 | 现货 | ||
2 mg | ¥ 496 | 现货 | ||
5 mg | ¥ 818 | 现货 | ||
10 mg | ¥ 1,180 | 现货 | ||
25 mg | ¥ 2,290 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 5,680 | 现货 | ||
500 mg | ¥ 11,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 918 | 现货 |
产品描述 | MI-2 (MALT1 inhibitor) is an irreversible MALT1 inhibitor. |
靶点活性 | MALT1:5.84 μM |
体外活性 | 每天腹腔注射25 mg/kg MI-2高效抑制TMD8 和 HBL-1 ABC-DLBCL异种移植物的生长,而对OCI-Ly1肿瘤的生长无作用. |
体内活性 | MI-2具有良好的细胞渗透性,抑制ABC-DLBCL细胞系中MALT1功能。MI-2对MALT1依赖性细胞系产生选择性生长抑制作用,在HBL-1,TMD8,OCI-Ly3和OCI-Ly10细胞中GI50分别为0.2,0.5,0.4和0.4 μM,而ABC-DLBCL MALT1不依赖的细胞系U2932 和 HLY-1以及两种GCB-DLBCL细胞系对MI-2都具有抗性。 |
激酶实验 | High-Throughput Screening for MALT1 Proteolytic Activity Inhibitors: Ac-LRSR-AMC is used as substrate and reactions are measured with excitation/emission wavelengths of 360/465 nm. Two time points are measured for each reaction to eliminate false positives due to compound autofluorescence. The final percent inhibition is calculated with the formula {[fluorescencetest compound (T2-T1)-fluorescenceneg ctrl (T2-T1)]/[fluorescencepos ctrl (T2-T1)-fluorescenceneg ctrl (T2-T1)]} × 100, where Z-VRPR-FMK (300 nM) is used as positive control and buffer only as negative control. The positive hits are validated in concentration-response experiments within a dose range of 0.122–62.5 μM to determine IC50 of the compounds. Activity is validated using recombinant full-length wild-type MALT1. |
细胞实验 | Cell proliferation is determined by ATP quantification using a luminescent method and trypan blue dye exclusion. Standard curves for each cell line are calculated by plotting the cell number (determined using trypan blue) against their luminescence values, and cell number is calculated accordingly. Cell viability in drug-treated cells is normalized to their respective controls (fractional viability), and results are given as 1-fractional viability. CompuSyn software is used to determine GI25 and GI50 values.(Only for Reference) |
别名 | MALT1 inhibitor, MI 2, MI 2 (MALT1 inhibitor) |
分子量 | 455.72 |
分子式 | C19H17Cl3N4O3 |
CAS No. | 1047953-91-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45.6 mg/mL (100 mM)
Ethanol: 9.1 mg/mL (20 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.1943 mL | 10.9716 mL | 21.9433 mL | 54.8582 mL |
5 mM | 0.4389 mL | 2.1943 mL | 4.3887 mL | 10.9716 mL | |
10 mM | 0.2194 mL | 1.0972 mL | 2.1943 mL | 5.4858 mL | |
20 mM | 0.1097 mL | 0.5486 mL | 1.0972 mL | 2.7429 mL | |
DMSO | 50 mM | 0.0439 mL | 0.2194 mL | 0.4389 mL | 1.0972 mL |
100 mM | 0.0219 mL | 0.1097 mL | 0.2194 mL | 0.5486 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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