MALT1 inhibitor MI-2

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。

产品编号 T2350Cas号 1047953-91-2

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MALT1 inhibitor MI-2

产品编号 T2350别名 MALT1 inhibitor, MI 2, MI 2 (MALT1 inhibitor)Cas号 1047953-91-2

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规格	价格	库存
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 x 10 mM (in DMSO)	¥ 918	现货

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产品介绍

生物活性

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)

化学信息

分子量	455.72
分子式	C₁₉H₁₇Cl₃N₄O₃
CAS No.	1047953-91-2

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 55 mg/mL (120.69 mM)

Ethanol: 9.1 mg/mL (20 mM)

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1943 mL	10.9716 mL	21.9433 mL	109.7165 mL
5 mM	0.4389 mL	2.1943 mL	4.3887 mL	21.9433 mL
10 mM	0.2194 mL	1.0972 mL	2.1943 mL	10.9716 mL
20 mM	0.1097 mL	0.5486 mL	1.0972 mL	5.4858 mL