ICG-001

目录号:S2662

ICG-001 Chemical Structure

Molecular Weight(MW): 548.63

ICG-001拮抗Wnt/β-catenin/TCF介导的转录,并特异性结合到启动子结合蛋白(CBP),IC50为3 μM,但不能结合到相关的转录共激活因子p300上。

规格 价格 库存 购买数量  
RMB 1377.83 现货
RMB 976.49 现货
RMB 3835.04 现货
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客户使用该产品的7个实验数据:

  • Immunocytochemical analysis of SOX1 (a–d), SOX2 (e–h) and SOX3 (i–l) expression in NT2/D1 cells treated with either DMSO (a, b, e, f, i, j) or ICG-001 (c, d, g, h, k, l). Cell nuclei were stained with DAPI (b, d, f, h, j, l). Scale bar 50 μm.

    Histochem Cell Biol, 2015, 10.1007/s00418-015-1352-0. ICG-001 purchased from Selleck.

    ICG-001 variably influences Wnt transcriptional activity across pancreatic cancer lines. Nuclear extracts from AsPC-1 cells treated with vehicle or 30 umol/L ICG-001 for 6 hours were immunoprecipitated with anti-CBP or control IgG antibodies followed by Western blot analyses for β-catenin and CBP.

    Mol Cancer Ther 2014 13(10), 2303-14. ICG-001 purchased from Selleck.

  • The fully differentiated 3T3L1 cells were collected. mRNA and protein levels of FAS and CD36 were measured. Dose effect of IWR-1-endo, PRI-724, and ICG-001 on FAS and CD36 protein levels measured by immunoblots and the figures show quantification of the immunoblots.

    Biochim Biophys Acta, 2018, 1863(8):834-843. ICG-001 purchased from Selleck.

    Marker protein of fibroblast-to-myofibroblast transition vimentin, a-SMA and collagen I overexpression in HELF cells caused by TGF-b1 for 24 hrs.

    J Cell Mol Med, 2017, 21(8):1545-1554. ICG-001 purchased from Selleck.

  • J Biol Chem 2013 56(4), 423-33. ICG-001 purchased from Selleck.

    Coimmunoprecipitation analysis of HCT-116 and SW620 cells treated with ICG-001. (A) Coimmunoprecipitation of HCT-116 CRC cells, using 75 uM ICG-001. Anti-CBP or anti-p300 antibody was used for the immunoprecipitation and beta-catenin was detected with an anti-beta-catenin antibody after SDS-PAGE. (B) Coimmunoprecipitation assay, similar to that described in (A), showing activity of 100 uM ICG-001 against CBP-beta-catenin association in SW620 CRC cells.

    J Cancer 2013 4(6), 481-90. ICG-001 purchased from Selleck.

  • Mol Immunol 2013 56(4), 423-33. ICG-001 purchased from Selleck.

产品安全说明书

Wnt/beta-catenin抑制剂选择性比较

生物活性

产品描述 ICG-001拮抗Wnt/β-catenin/TCF介导的转录,并特异性结合到启动子结合蛋白(CBP),IC50为3 μM,但不能结合到相关的转录共激活因子p300上。
靶点
CBP [1]
(Cell-free assay)
3 μM
体外研究

ICG-001 作用于TOPFLASH 时,IC50为3 μM,而对含突变TCF位点的相关报告基因结构, FOPFLASH没有作用效果。使用25μM ICG-001处理SW480 细胞8小时后,降低Survivin和 Cyclin D1 RNA和蛋白的稳定水平,这两者都可通过β-catenin上调。ICG-001 作用于转化细胞而不是正常结肠细胞,选择性诱导凋亡,降低结肠癌细胞生长。[1] ICG-001作用于presenilin-1突变细胞,可表型营救正常神经生长因子(NGF)诱导的神经元分化和神经轴突生长,强调TCF/β-catenin 信号通路在神经轴突生长和神经元分化中的重要性。[2] 最新研究显示 5μM ICG-001作用于MCF7细胞,抑制leptin诱导的EMT, 入侵和肿瘤干细胞球形成。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y M{e3Z2Fxd3C2b4Ppd{BCe3OjeR?= NF6yeIQ2OMLizszt M1TVd|I1yqCq NVf4OW9MTE2VTx?= NVznUmxP[myxY3vzxsB1cGVicILveIVkfGm4ZTDl[oZm[3Rib3[gcYVt[XSxbnnuJIFo[Wmwc4SgVJJRKChzMEdihLMyOjZrLXnu[JVk\WRiYYDvdJRwfGmlIIPp[45idHN? MUOyOVI2OTB{OB?=
AsPC-1 M3\Ccmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HLO|EuOjBizszN M13NdFIwPC94IHS= NEf1fY1qdmirYnn0d{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M{PmXVI2ODh{OU[w
MiaPaCa-2 NWD5epNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rmdVEuOjBizszN MX6yM|QwPiCm M2W3PYlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MnrYNlUxQDJ7NkC=
PANC-1 MkDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3OxfVEuOjBizszN NVKwOZFWOi92L{[g[C=> MX\pcohq[mm2czD0bIUh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlqwNlUxQDJ7NkC=
L3.6pl MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3J[XpXOS1{MDFOwG0> MV[yM|QwPiCm NXjmU2hycW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NYnoOoE3OjVyOEK5OlA>
SH-SY5Y MUDBdI9xfG:|aYOgRZN{[Xl? NITnVmwyOCEQvF2= MXyyOEBp M2m4folvcGmkaYTzJJRp\SCwZYXyc5Bzd3SnY4TpeoUh\W[oZXP0d{Bw\iCqeYDvfIliKGGpYXnud5QhWHKSIDixNFYuOTJ4KT3t[YRq[XSnZDDu[ZVzd26jbDDj[YxtKGSnYYTo NIfqTIkzOzlyMEW2Oi=>
HKC-8  NUXm[FVsTnWwY4Tpc44hSXO|YYm= MXGxNOKhyrWP M3\Ob|I1KGh? MUThZo9tcXOqZYRCpO6zNWOjdHXubY7jiJOvZXTpZZRm\CCUQWOgbY5lfWO2aX;u NYHsVG5qOjVyMUKxOlY>
HK-2  NX\NXm54TnWwY4Tpc44hSXO|YYm= MYexNEDDvU1? NEjROZQ{KGh? M3vMTJJm\HWlZXSgeIhmKGW6cILld5Nqd25ib3[gWGdHNc7{MTyg{tEuW02DLDDhcoQhS1SJRjDh[pRmeiC2cnXheI1mdnRid3n0bEBJUEV? MoOxNlM3QTB7OUe=
HepT1 MlnZRZBweHSxc3nzJGF{e2G7 NVXMPIZ6OC1zMEFCpO69VQ>? MmDMNlQhcA>? MlPITWM2OD1|NNMg{txO M13QelI{OjZ4N{G4
HuH6 MoTaRZBweHSxc3nzJGF{e2G7 NFWz[GsxNTFyMNMg{txO NVnRbHpxOjRiaB?= NEDiUlFKSzVyPUO5xsDPxE1? MlfUNlMzPjZ5MUi=
MCF7 M3;mbWZ2dmO2aX;uJGF{e2G7 MljROUDPxG4EoB?= NIG1SpVqdmirYnn0d{Bt\XC2aX6tcYVlcWG2ZXSgbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZiU37hbYwtKFOudXesJIFv\CCcZXKy M3;GfFIzOjdyM{W5
RLE-6TN  M2LlOWZ2dmO2aX;uJGF{e2G7 M37JW|IvPS93L{euOUDPxE1? NXvvNmh5PDhiaB?= NGiybVdqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSg{tEuW02DIHnu[JVkfGmxbjDhcoQhTU2W MljwNlIzPDF2N{i=
HKC-8 MlqzSpVv[3Srb36gRZN{[Xl? NH3aXFg2NzFyL{KwJO69VQ>? MUS0PEBp MXzicI9kc3NizsKtZ4F1\W6rbj3kdol3\W5iZ3Xu[UBmgHC{ZYPzbY9v MlznNlE5OTZ7M{e=
SW480 NIXtXnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[yMVExOCEQvF2= NUHCPGd1UUN3ME21MljDuTBwNkig{txO M{DwTVE2Pzh{MUO4

... Click to View More Cell Line Experimental Data

体内研究 ICG-001 水溶性类似物处理9周,降低42%结肠和小肠息肉的形成,和非甾体类抗炎试剂Sulindac效果类似,Sulindac是一贯治疗这种疾病模型的药物。在整个的处理期间观察不到明显的毒性。类似物按150 mg/kg 剂量静脉注射处理SW620裸鼠肿瘤衰退移植瘤模型,处理19天,显著降低肿瘤体积,没有死亡,体重也没有降低。[1] ICG-001 每天按5 mg/kg剂量处理小鼠,显著抑制beta-catenin信号,且降低 Bleomycin诱导的肺纤维化,同时保护上皮细胞。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

双重-荧光素酶报告基因实验:

双重-荧光素酶报告基因实验系统提供形成双重报告基因实验的有效方法。在DLR™ 实验中, 顺序测量萤火虫型和花虫型荧光素酶活性。加入荧光素酶实验试剂 II (LAR II),获得“辉光型”发光信号,测量萤火虫型荧光素酶报告基因。定量测量萤火虫荧光素酶后, 淬灭反应,同时在相同试管中加入Stop & Glo® 试剂开始花虫型荧光素酶反应。通过花型荧光素酶,Stop & Glo® 试剂也产生“光辉型”信号,在测量过程中缓慢降解。在 DLR™ 实验系统中, 两种报告基因都使用亚原子(<10-18) 敏感性进行线性分析,在实验宿主细胞中都没有内在活性。而且, DLR™ 实验的集成格式可以使在转化细胞或无细胞转录/翻译反应中快速测量报告基因。
细胞实验:[1]
+ 展开
  • Cell lines: Human colon carcinoma cell lines SW480, SW620, and HCT116, normal colonic epithelial cell line CCD-841Co
  • Concentrations: ~25 μM
  • Incubation Time: 24 hours
  • Method: 1. Prior to starting the assay, prepare the Apo-ONE Caspase-3/7 Reagent, and mix thoroughly. 2. For best results, empirical determination of the optimal cell number, apoptosis induction treatment and incubation period for the cell culture system may be necessary. 3. Use identical cell numbers and volumes for the assay and the negative control samples. 4. Do not mix Apo-ONE Caspase-3/7 Reagent and samples by manual pipetting. Mixing in this manner is unnecessary and may create bubbles that interfere with fluorescence readings or cross-contaminate the samples. Gentle mixing may be performed using a plate shaker. 5. Total incubation time for the assay depends upon the amount of caspase- 3/7 present in the sample. 6. The Apo-ONE Caspase-3/7 Reagent is formulated to mediate cellular lysis and support optimal caspase-3/7 activity. In rare instances, the reagent does not affect complete lysis of cultured cells. In such cases, lysis is enhanced by a freeze-thaw cycle. For best results, freeze at -70 °C, then thaw at room temperature. After equilibration, mix to homogeneity and incubate until measurable fluorescence is achieved
    (Only for Reference)
动物实验: [1]
+ 展开
  • Animal Models: 7周大的雄性C57BL/6J-Apc Min/+小鼠
  • Formulation: 使用ICG-001水溶性类似物
  • Dosages: 300 mg/kg
  • Administration: ICG-001水溶性类似物每天口服处理,持续9周
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (182.27 mM)
Ethanol 10 mg/mL (18.22 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+50% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 548.63
化学式

C33H32N4O4

CAS号 780757-88-2
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    If the compound is stored in DMSO at -80, how long would it be stable? For cell culture, how long should I change for the fresh medium with ICG-001?

  • 回答:

    The product in DMSO solution can be stored at 4 degree for 1 week and -20 degree for 1 month. The best storage condition is solid powder, even at -80 the solution is not stable enough for long term storage. For cell culture, you need change medium every 48h.

Wnt/beta-catenin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID