ICG-001

製品コードS2662

ICG-001化学構造

分子量(MW):548.63

ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

サイズ 価格(税別)  
JPY 29800
JPY 21900
JPY 80000
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バルク問合せ

文献中Selleckの製品使用例(38)

製品安全説明書

Wnt/beta-catenin阻害剤の選択性比較

生物活性

製品説明 ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.
ターゲット
CBP [1]
(Cell-free assay)
3 μM
体外試験

ICG-001 has no effect on the related reporter construct, FOPFLASH, which contains mutated TCF sites. After treatment with 25μM of ICG-001 for 8 hours, SW480 cell reduces the steady-state levels of Survivin and Cyclin D1 RNA and protein, both of which can be up-regulated by β-catenin. ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells, reduces in vitro growth of colon carcinoma cells. [1] ICG-001, can phenotypically rescue normal nerve growth factor (NGF) -induced neuronal differentiation and neurite outgrowth in the presenilin-1 mutant cells, emphasizing the importance of the TCF/β-catenin signaling pathway on neurite outgrowth and neuronal differentiation. [2] A recent study demonstrates that 5μM ICG-001 inhibits leptin-induced EMT, invasion and tumorsphere formation in MCF7 cells. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y NX3p[WNSSXCxcITvd4l{KEG|c3H5 Mnj4OVDDqM7:bR?= NFnMSHozPMLiaB?= MYHEUXNQ M1;3fIJtd2Otc9MgeIhmKHC{b4TlZ5RqfmViZX\m[YN1KG:oIH3lcIF1d26rbjDh[4FqdnO2IGDyVEApOTB44pETNVI3MS2rbnT1Z4VlKGGyb4D0c5Rq[yC|aXfuZYx{ NIqyWJIzPTJ3MUCyPC=>
AsPC-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzxR3QzOS1{MDFOwG0> NWfvcIhCOi92L{[g[C=> MVrpcohq[mm2czD0bIUh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NX\QPZlWOjVyOEK5OlA>
MiaPaCa-2 M33iTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\sNU0zOCEQvF2= M1\KTFIwPC94IHS= MoHJbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ Mn[0NlUxQDJ7NkC=
PANC-1 M3HHV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvXVVcyNTJyIN88US=> NXzt[3dROi92L{[g[C=> M3jIeIlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NF\ZSGozPTB6Mkm2NC=>
L3.6pl M3nETGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDJO|k1OS1{MDFOwG0> NUDlTphuOi92L{[g[C=> NVH4[2hscW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MoPUNlUxQDJ7NkC=
SH-SY5Y MX;BdI9xfG:|aYOgRZN{[Xl? M2XYZ|ExKM7:TR?= NEHPe|czPCCq MlS3bY5pcWKrdIOgeIhmKG6ndYLvdJJwfGWldHn2[UBm\m[nY4TzJI9nKGi7cH;4bYEh[WejaX7zeEBRelBiKEGwOk0yOjZrLX3l[IlifGWmIH7leZJwdmGuIHPlcIwh\GWjdHi= MlLwNlM6ODB3Nk[=
HKC-8  NGi3SVlHfW6ldHnvckBCe3OjeR?= MmXRNVDDqML3TR?= MlfXNlQhcA>? NHHxc|hi[m:uaYPo[ZPDqM7{LXPheIVvcW8kgKPt[YRq[XSnZDDSRXMhcW6mdXP0bY9v MXyyOVAyOjF4Nh?=
HK-2  MY\GeY5kfGmxbjDBd5NigQ>? M4m2[lExKML3TR?= M4rxWlMhcA>? NW\GSHdyemWmdXPl[EB1cGViZYjwdoV{e2mxbjDv[kBVT0ZvzsKxMEDPuS2VTVGsJIFv\CCFVFfGJIFnfGW{IITy[YF1dWWwdDD3bZRpKEiKRR?= NFPrfFkzOzZ7MEm5Oy=>
HepT1 MXzBdI9xfG:|aYOgRZN{[Xl? M13HXVAuOTBywrFOwG0> MVKyOEBp NWrMbG5IUUN3ME2zOOKh|ryP M2DPWlI{OjZ4N{G4
HuH6 M{jG[mFxd3C2b4Ppd{BCe3OjeR?= NUnVfmZzOC1zMEFCpO69VQ>? MljwNlQhcA>? NInqU2RKSzVyPUO5xsDPxE1? MnPiNlMzPjZ5MUi=
MCF7 MnzOSpVv[3Srb36gRZN{[Xl? M{D0PVUh|ryvwrC= NUf2[pBocW6qaXLpeJMhdGWydHnuMY1m\GmjdHXkJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIGPuZYltNCCVbIXnMEBidmRiWnXiNi=> NXflTWRGOjJ{N{CzOVk>
RLE-6TN  Mlz5SpVv[3Srb36gRZN{[Xl? M{K1UlIvPS93L{euOUDPxE1? M3LjN|Q5KGh? MVnpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRizsGtV21CKGmwZIXjeIlwdiCjbnSgSW1V NHvzVIQzOjJ2MUS3PC=>
HKC-8 MmHYSpVv[3Srb36gRZN{[Xl? MX21M|ExNzJyIN88US=> M1r4UVQ5KGh? M2D1OoJtd2OtczFOtk1k[XSnbnnuMYRzcX[nbjDn[Y5mKGW6cILld5Nqd25? NW\KcndEOjF6MU[5N|c>
SW480 NUTMS4FoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmyMVExOCEQvF2= NHvwe2lKSzVyPUWuPOKyOC54ODFOwG0> M17mO|E2Pzh{MUO4

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
CCNB1 / Cyclin D1 ; 

PubMed: 28893318     


ICG-001 reduced expression of CCNB1 and CyclinD1 in MGC-803. Data are the mean ± SEM of three independent experiments.

ABC / Beta-catenin / E-cadherin / N-cadherin / MMP-9 / c-MYC / Actin / Histone H3; 

PubMed: 28893318     


Western blotting analysis of Wnt related proteins from total proteins and extracted nuclear and cytoplasmic proteins.

beta-catenin / F-actin; 

PubMed: 28893318     


Confocal analysis of the expression and distribution of β-catenin in MGC-803 with or without ICG-001.

pβ-catenin; 

PubMed: 29986466     


Cells were exposed to ICG-001 for 24 h at the indicated concentrations and with DMSO as control, and cell lysates were probed with phosphor- and total antibodies of β-catenin signaling pathway. β-actin was used as a loading control. The representative ima䲧疝Ỵ疞㧀疜膉痘 

SOX-2 / CD44 / Survivin / EGFR / FOXM1 / EZH2 / Vimentin; 

PubMed: 25897700     


In EBV-positive C666-1 cells, (b) Western blotting analysis of SOX2, CD44, Survivin, EGFR, FOXM1, and EZH2 expression on day-7. (c) Western blotting analysis of epithelial-mesenchymal transition (EMT) markers, E-cadherin and vimentin on day-7. 

28893318 29986466 25897700
体内試験 Administration of a water-soluble analog of ICG-001 for 9 weeks reduces the formation of colon and small intestinal polyps by 42% as effectively as the nonsteroidal antiinflammatory agent Sulindac, which has consistently demonstrated efficacy in this model. No overt toxicity is detected throughout the course of treatment. In the SW620 nude mouse xenograft model of tumor regression, 150 mg/kg, i.v. of analog demonstrates a dramatic reduction in tumor volume over the 19-day course of treatment, with no mortality or weight loss. [1] ICG-001 (5 mg/kg per day) significantly inhibits beta-catenin signaling and attenuates bleomycin-induced lung fibrosis in mice, while concurrently preserving the epithelium. [4]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

DUAL-Luciferase Reporter Assay:

The Dual-Luciferase Reporter (DLR) Assay System provides an efficient means of performing dual reporter assays. In the DLRTM Assay, the activities of firefly (Photinus pyralis) and Renilla (Renilla reniformis, also known as sea pansy) luciferases are measured sequentially from a single sample. The firefly luciferase reporter is measured first by adding Luciferase Assay Reagent II (LAR II) to generate a “glow-type” luminescent signal. After quantifying the firefly luminescence, this reaction is quenched, and the Renilla luciferase reaction is initiated by simultaneously adding Stop & Glo® Reagent to the same tube. The Stop & Glo® Reagent also produces a “glow-type” signal from the Renilla luciferase, which decays slowly over the course of the measurement. In the DLRTM Assay System, both reporters yield linear assays with subattomole (<10-18) sensitivities and no endogenous activity of either reporter in the experimental host cells. Furthermore, the integrated format of the DLRTM Assay provides rapid quantitation of both reporters either in transfected cells or in cell-free transcription/translation reactions.
細胞試験: [1]
+ 展開
  • 細胞株: Human colon carcinoma cell lines SW480, SW620, and HCT116, normal colonic epithelial cell line CCD-841Co
  • 濃度: ~25 μM
  • 反応時間: 24 hours
  • 実験の流れ: 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
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: Seven-week-old male C57BL/6J-Apc Min/+
  • 製剤: Water-soluble analog of ICG-001 is used.
  • 投薬量: 300 mg/kg
  • 投与方法: Water-soluble analog of ICG-001 is treated orally for 9 weeks everyday.
    (参考用のみ)

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 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+50% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 548.63
化学式

C33H32N4O4

CAS No. 780757-88-2
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問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.

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID