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产品名称：Selleck Chemicals/IMD 0354/S2864

产品编号：S2864

市场价：¥9400.00

场地：美国(厂家直采)

产品分类：蛋白类>聚合物>

联系QQ：1570468124

电话号码：4000-520-616

邮箱： info@ebiomall.com

美元价：$470.00

品牌： Selleck Chemicals

公司：Selleckchem

公司分类：

商品介绍

Description

IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

Targets

IKKβ ^[1]

In vitro

IMD-0354 (< 5="" μm)="" inhibits="" the="" expression="" of="" nf-κb="" as="" well="" as="" the="" translocation="" of="" nf-κb="" to="" the="" nucleus="" in="" hmc-1="" cells.="" imd-0354="" suppresses="" cell="" proliferation="" in="" a="" time-="" and="" dose-dependent="" manner="" in="" hmc-1="" cells.="" imd-0354="" (0.5="" μm)="" almost="" inhibits="" the="" proliferation="" of="">^G559 cells and IC-2^V814 cells. IMD-0354 (0.5 μM) results in arrest of the cell cycle at the G0/G1 phase in HMC-1 cells. IMD-0354 (1 μM) increases the number of cells with hypodiploid DNA content in HMC-1 cells. IMD-0354 (<1 μm)="" decreases="" the="" ratio="" of="" cells="" in="" s="" and="" g2/m="" phases="" in="" hmc-1="" cells.="" imd-0354="" (1="" μm)="" downregulates="" cyclin="" d3="" expression="" as="" well="" as="" prb="" phosphorylation="" level="" in="" a="" time-dependent="" manner="" in="" hmc-1="" cells.="" imd-0354="">< 10="" μm)="" has="" no="" influence="" on="" the="" signals="" of="" stat3="" and="" stat6,="" whereas="" the="" phosphorylation="" of="" stat1="" and="" stat5="" is="" very="" slightly="" suppressed="" at="" high="" concentrations="" in="" hmc-1="" cells.="" imd-0354="" suppresses="" the="" translocation="" of="" nf-κb="" to="" the="" nucleus="" in="" cbhcmcs="" after="" 24="" hours="" in="" a="" dose-dependent="" manner.="">^[1] IMD-0354 inhibits 98.5% of NF-κB activity at a concentration of 10 μg/ml in HepG2 cells. ^[2] IMD-0354 (1 μM) ameliorates the TNFα-induced decrease in the adiponectin concentration in the media, when the TNFα (6 nM) and insulin (100 nM) are administered simultaneously in 3T3-L1 adipocytes serum-starved for 12 h. IMD-0354 (1 μM) restores the phosphorylation of Akt down-regulated by the TNFα treatment, when the TNFα (6 nM) and insulin (100 nM) are administered simultaneously in 3T3-L1 adipocytes serum-starved for 12 h. ^[3] IMD-0354 (1 μM) inhibits phosphorylation of IκBα and nuclear translocation of nuclear factor-kappa B (NF-κB) induced by tumor necrosis factor-α (TNF-α) in cultured cardiomyocytes. IMD-0354 (1 μM) significantly reduces TNF-α-induced production of interleukin-1β and monocyte chemoattractant protein-1 from cultured cardiomyocytes. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
HFF cells	NHnhWnZHfW6ldHnvckBie3OjeR?=		NFTWW2g4OiCq		MljvRY51cWGyaXPvcZBtXijbjDhZ5Rqfmm2eTDh[4FqdnO2IGTvfI9xdGG\|bXGg[49vGmrIGLIJJRi[2i7en;peIV{KGW6cILld5NqdmdieXXscI94KG[udX;y[ZNkW62IIDyc5RmcW5iaX7m[YN1WRiaX6gTGZHKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDmcJVwemW\|Y3XuZ4Uh[XO\|YYmsJGlEPTB;MD6wNVYh\|ryP	M2DkZVIzQTdyOUO3

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	Cyclin D1 / Cyclin D2 / Cyclin D3 / Cyclin E / Bcl-2 ; PubMed: 24510578Cancer Med The expression of cyclins D1, D2, and D3 was suppressed in MSTO-211H cells and that of cyclin D3 was decreased in NCI-H28 and NCI-H2052 cells by treatment with IMD-0354 (1μmol/L) for 24h. In NCI-H2052 cells, Bcl-2 expression was suppressed by IMD-0354 treatment (representative of three different experiments). p-IκBα / IκBα ; PubMed: 24531845Sci Rep Involvement of constitutive NF-κB activation in tumorigenic proliferation was examined using 2 different cell lines, namely, ER-positive MCF-7 and ER-negative HMC1-8 cells. After serum starvation, the cells were incubated in complete culture media with the indicated concentrations of IMD-0354 for 16 h; whole cell lysates were obtained to detect the IκB phosphorylation responsible for NF-κB activation by Western blot analysis. The constitutive phosphorylation of IκB and the downregulation of the phosphorylated form by IMD-0354 were detected in both cells. Concerning the expression of IκBα, 2 immunoreactive bands were identified in lysates from the HMC1-8 cells. The upper band was estimated as intact IκBα and the lower one was its partial proteolytic product.	24510578 24531845
Immunofluorescence	NF-κB p65 ; PubMed: 29332242Angiogenesis Effect of IMD0354 treatment on NF-κB nuclear translocation and phospho-IκBα expression on 24h serum-starved HUVEC. Inhibitory effect of IMD0354 (10ng/ml) on NF-κB (red) nuclear translocation (pink). VEGFA; PubMed: 29332242Angiogenesis Immunofluorescent detection of VEGF-A (green) in HUVEC treated with IMD0354 (10, 5, 2.5ng/ml). Cell nuclei visualized with DAPI staining (blue).	29332242
Growth inhibition assay	Cell viability; PubMed: 24014113PLoS One Viability of MDA-MB-231 cells was assessed by MTT assay after treatment with IMD-0354 for 24 h (A), 48 h (B) and 72 h (C).Viability of 4T1 cells was assessed by MTT assay after treatment with IMD-0354 for 24 h (E), 48 h (F) and 72 h (G). Data are shown as mean ± SEM.	24014113

In vivo

IMD-0354 at 5 mg/kg also significantly decreases NF-κB, but the magnitude of the decrease is lower than with 20 mg/kg IMD-0354 in lungs of OVA-sensitized mice. IMD-0354 (20 mg/kg) ameliorates airway hyperresponsiveness and reduces the numbers of bronchial eosinophils and mucus-producing cells in OVA-sensitized mice. IMD-0354 (20 mg/kg) also reduces the total numbers of cells and eosinophils in bronchoalveolar lavage fluid in OVA-sensitized mice. IMD-0354 (20 mg/kg) inhibits the production of Th2 cytokines such as interleukin (IL)-5 and IL-13 and eotaxin in the airways and/or lungs of OVA-sensitized mice, but it does not affect the restoration of Th1 cytokines such as IL-12 and interferon-gamma under the same experimental conditions. IMD-0354 (20 mg/kg) results in a partial decrease in serum IgE concentration in OVA-sensitized mice. ^[2] IMD-0354 significantly decreases the plasma glucose levels in KKAy mice treated with and fed an HF diet in an dose-dependent manner without influence of body weight. ^[3] IMD-0354 (10 mg/kg) results in a significant dose-dependent reduction of the infarction area/area at risk ratio and the preservation of fractional shortening ratio. ^[4]

品牌介绍

Selleck Chemicals提供了超过120,000种用于细胞信号通路研究的抑制剂。我们积极跟踪最新科学，因此我们的客户可以依靠我们成为最新抑制剂的领先供应商。

Selleck的生物活性化合物库由8,000多个具有经过验证的生物学和药理活性的小分子组成。这些分子的安全性和有效性已通过临床前和临床研究证明，其中许多是FDA批准的化合物。

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