|2-氯-N-(4-(5-(3,4-二氯苯基)-3-(2-甲氧基乙氧基)-1H-1,2,4-三唑-1-基)苯基)乙酰胺|CsnPharm

CAS No.: 1047953-91-2

2-Chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide Catalog No. CSN16629

Synonyms: MI 2;MALT1 inhibitor

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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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 MALT1

IC50:5.84μM
描述Pathogenesis of activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) is largely associated with MALT1, a unique Paracaspase protein with cleavage activity which can induce aberrant oncogenic signaling. MI-2 is the lead MALT1 inhibitor with IC50 of 5.84μM that can kill ABC-DLBCLs directly without toxicity to animals. Treatment with MI-2 at different concentrations to HBL-1, TMD8 and OCI-Ly1 cell lines consistently induced significant and selective dose-dependent suppression. After further treatment with increasing concentrations of MI-2, a dose-dependent decrease in MALT1-mediated cleavage and an increase in the uncleaved CYLD were observed in HBL-1 cells. A robust interaction between MALT1 and MI-2 was indicated by utilizing of HSQC-NMR spectroscopy. LC-MS study showed that MI-2 binds covalently to MALT1 at the C464 site. Pre-incubation with different concentrations of MI-2 led a time-course and dose-dependent MALT1 inactivation. MI-2 at 2μM diminished the abundance of cleaved forms and increased the abundance of full-length proteins in HBL-1 and TMD8 cell lines. Meanwhile, it led a reduction of nuclear c-REL in HBL-1 and TMD8 cells at concentration of 200nM and 500nM, respectively. Also, MI-2 reduced 50% of NF-kB reporter activity at 24 hour in HBL-1 cells transfected with the NF-kB reporter. MI-2 demonstrated GI50 values ranging in 0.2-0.5μM for 8 different cell lines, including OCI-Ly3 and OCI-Ly10. Besides, no toxicity of MI-2 to animals were showed by a test of five C57BL/6 mice exposed to MI-2 at doses ranging in 0.05-25 mg/kg.
动物研究
剂量
Mice: 0.05 mg/kg^[2] (i.p.), 30 mg/kg^[3] (i.p.)

给药途径
i.p.

动物研究
剂量	Mice: 0.05 mg/kg^[2] (i.p.), 30 mg/kg^[3] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1943 mL
- 10.9716 mL
- 21.9433 mL
- 5 mM
- 0.4389 mL
- 2.1943 mL
- 4.3887 mL
- 10 mM
- 0.2194 mL
- 1.0972 mL
- 2.1943 mL

技术信息

CAS号

1047953-91-2

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H17Cl3N4O3

运输

蓝冰

分子量

455.72

别名

MI 2;MALT1 inhibitor

溶解度

DMSO	91.0 mg/mL (199.7 mM)
Water	Insoluble
Ethanol	90.0 mg/mL (197.5 mM)

动物实验配方

2% DMSO+30% PEG 300+2% Tween 80+water

3 mg/mL

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2-Chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide Catalog No. CSN16629

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