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CAS: 978-62-1
分子式: C15H8ClF6NO2
分子量: 383.67
英文名称: 
imd-0354
n-(3,5-bis-trifluoromethylphenyl)-5-chloro-2-hydroxybenzamide
用途: IMD 0354是一种IKKβ抑制剂,作用于NF-κβ通路,抑制IκBα磷酸化。在HMC-1细胞中IMD-0354 (< 5 μM)抑制NF-κB的表达以及它的移动入核。IMD-0354抑制HMC-1细胞增殖,具有时间和剂量依赖特性。 IMD-0354 (0.5 μM)几乎可以抑制IC-2G559和IC-2V814的细胞增殖。IMD-0354 (0.5 μM)导致HMC-1细胞周期停滞在G0/G1期。IMD-0354 (1 μM)增加带有亚二倍DNA的HMC-1细胞数。在HMC-1细胞中IMD-0354 (<1 μM)降低了S期与G2/M期细胞数的比值,IMD-0354 (1 μM) 降低Cyclin D3表达和pRb磷酸化并且具有时间依赖特性。在HMC-1细胞中IMD-0354 (< 10 μM)对STAT3 和 STAT6的信号没有影响,而在高浓度时会轻微抑制STAT1 和 STAT5的磷酸化。 CBhCMCs中IMD-0354处理24小时后抑制NF-κB转移入核并且具有剂量依赖特性[1]。在HepG2细胞中10 μg/mL的IMD-0354可以抑制NF-κB 98.5%的活性[2]。血清饥饿处理12小时后3T3-L1脂肪细胞中同时使用TNFα (6 nM) 和胰岛素(100 nM)时,IMD-0354 (1 μM)可以促进TNFα诱导的脂联素浓度的下降,还可以使TNFα处理后下降的Akt磷酸化水平恢复[3]。在培养的心肌细胞中IMD-0354 (1 μM)抑制IκBα磷酸化以及TNF-α诱导的NF-κB核转位,明显抑制TNF-α诱导的白细胞介素-1β和单核细胞趋化蛋白-1的产生[4]。
推荐供应商
货号品牌产品名称规格包装、参考价格详情
I872357MACKLINIMD 035499%39元/1mg;   129元/5mg;   299元/25mg;   788元/100mg;   展开
储存:-20℃
状态:白色到灰白色固体
I792283MACKLINIMD 035410mM in DMSO538元/1ml;   展开
储存:-20°C
978460J&KIMD-035499%, 一种合成的选择性NF-kB 抑制剂2456元/5MG;   9971元/25MG;   展开

基本信息

分子式C15H8ClF6NO2
分子量383.67
MDL编码MFCD00218820
存储条件Freezer -20℃
401482Sigma-AldrichIKK-2 Inhibitor V-CAS 978-62-1-CalbiochemThe IKK-2 Inhibitor V, also referenced under CAS 978-62-1, controls the biological activity of IKK-2. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.3806.77元/5 MG;   展开

产品说明

一般描述

A cell-permeable salicylamide compound that acts as an IKK-2 inhibitor by selectively blocking IκBα phosphorylation (IC50 ~ 250 nM) and thereby prevents the induction of NF-κB p65 nuclear translocation. Shown to offer cardioprotection by reducing IL-1β and MCP-1 production (IC50<1 µM) in cardiomyocytes, and ameliorate insulin resistance in KKAy mice by regulating adiponectin release.
A cell-permeable IKK-2 inhibitor that selectively blocks IκBα phosphorylation (IC50 ~250 nM) and prevents the induction of NF-κB p65 nuclear translocation. Reported to suppress neoplastic proliferation of mast cells with constitutively activated c-kit receptor. Shown to offer cardioprotection by reducing IL-1β and MCP-1 production (IC50<1 µM) in cardiomyocytes, and ameliorate insulin resistance in diabetic KKAy mice by regulating adiponectin release.

包装

5 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Primary Target
IKK-2
Product does not compete with ATP.
Reversible: no
Target IC50: ~ 250 nM blocking IκBα phosphorylation

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Kamon, J., et al. 2004. Biochem. Biophys. Res. Commun.323, 242.
Onai, Y., et al. 2004. Cardiovasc. Res.63, 51.
Tanaka, A., et al. 2004. Blood105, 2324.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C15H8ClF6NO2
分子量383.67
MDL编号MFCD00218820

产品性质

质量水平100
测定≥95% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 white
溶解性ethanol: 1 mg/mL
DMSO: 5 mg/mL
运输ambient
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
I3159Sigma-AldrichIMD-0354≥98% (HPLC), solid2717.89元/5 MG;   5007.85元/10 MG;   展开

产品说明

应用

IMD-0354 has been used to study the effect of NF-κB (nuclear factor) inhibition on differentially expressed in chondrocytes 2. It has also been used to study the role of NF-κB signaling in tumor necrosis factor-induced certain transcription factors expression using human primary fibroblasts.

包装

5, 10 mg in glass bottle
Light sensitive. Packaged under nitrogen.

生化/生理作用

IMD-0354 acts as an inhibitor by inhibiting the phosphorylation of the NF-κB (nuclear factor) and its translocation into the nucleus. It blocks IκBα phosphorylation (IC50 ~ 250 nM). Cardioprotectant, that reduces IL-1β and MCP-1 production (IC50 < 1 μM) in cardiomyocytes. IMD-0354 affects angiogenesis, which has been observed in human umbilical vein endothelial cells. It prevents tube formation and migration of the cells. In vivo studies also prove that IMD-0354 inhibits retinal vessel growth. IMD-0354 also acts as an inhibitor of Aquaporin 4 (AQP4) inhibitor (IC50 0.2μM) with no inhibitory potency to IKK-β. [4]

基本信息

经验(实验)分子式C15H8ClF6NO2
分子量383.67
MDL编号MFCD00218820
PubChem化学物质编号24724513
NACRESNA.77

产品性质

质量水平100
测定≥98% (HPLC)
形式solid
溶解性DMSO: >20 mg/mL
运输wet ice
储存温度−20℃
SMILES stringOc1ccc(Cl)cc1C(=O)Nc2cc(cc(c2)C(F)(F)F)C(F)(F)F
InChI1S/C15H8ClF6NO2/c16-9-1-2-12(24)11(6-9)13(25)23-10-4-7(14(17,18)19)3-8(5-10)15(20,21)22/h1-6,24H,(H,23,25)
InChI keyCHILCFMQWMQVAL-UHFFFAOYSA-N

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
个人防护装备dust mask type N95 (US), Eyeshields, Gloves
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