您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > MALT1 inhibitor MI-2
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
MALT1 inhibitor MI-2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MALT1 inhibitor MI-2图片
CAS NO:1047953-91-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
MI 2 (MALT1 inhibitor)
MALT1 inhibitor
MI 2
产品介绍
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。

产品描述

MI-2 (MALT1 inhibitor) is an irreversible MALT1 inhibitor.

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)

Cas No.

1047953-91-2

分子式

C19H17Cl3N4O3

分子量

455.72

别名

MI 2 (MALT1 inhibitor);MALT1 inhibitor;MI 2

储存和溶解度

DMSO:45.6 mg/mL (100 mM)
Ethanol:9.1 mg/mL (20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years