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 27888.00
JPY 19920.00
JPY 78020.00


  • 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.

  • J Biol Chem 2013 56(4), 423-33. 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.

  • 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.




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.
CBP [1]
(Cell-free assay)
3 μM

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]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y NH3TfY1CeG:ydH;zbZMhSXO|YYm= M136eFUxyqEQvH2= M1uxSlI1yqCq M{P2TWROW09? NXm0SIlC[myxY3vzxsB1cGVicILveIVkfGm4ZTDl[oZm[3Rib3[gcYVt[XSxbnnuJIFo[Wmwc4SgVJJRKChzMEdihLMyOjZrLXnu[JVk\WRiYYDvdJRwfGmlIIPp[45idHN? M4jpVVI2OjVzMEK4
AsPC-1 M1j0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rhXVEuOjBizszN MnH5Nk81NzZiZB?= Mnu4bY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MkLlNlUxQDJ7NkC=
MiaPaCa-2 M1fKeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPiNU0zOCEQvF2= MlrqNk81NzZiZB?= MVfpcohq[mm2czD0bIUh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4\5fVI2ODh{OU[w
PANC-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjXNU0zOCEQvF2= M4PJbVIwPC94IHS= M1PF[YlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NULP[2d[OjVyOEK5OlA>
L3.6pl NFy2bFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTNVWIyNTJyIN88US=> NIXTN2QzNzRxNjDk NHPaSVdqdmirYnn0d{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M2G4[VI2ODh{OU[w
SH-SY5Y NVvlUmJySXCxcITvd4l{KEG|c3H5 MUSxNEDPxE1? MnTxNlQhcA>? MnTGbY5pcWKrdIOgeIhmKG6ndYLvdJJwfGWldHn2[UBm\m[nY4TzJI9nKGi7cH;4bYEh[WejaX7zeEBRelBiKEGwOk0yOjZrLX3l[IlifGWmIH7leZJwdmGuIHPlcIwh\GWjdHi= Ml7qNlM6ODB3Nk[=
HKC-8  M2nqR2Z2dmO2aX;uJGF{e2G7 M2PrcFExyqEEtV2= M2\XSFI1KGh? MnzaZYJwdGm|aHXzxsDPui2lYYTlcolv6oDVbXXkbYF1\WRiUlHTJIlv\HWldHnvci=> MVuyOVAyOjF4Nh?=
HK-2  MnnPSpVv[3Srb36gRZN{[Xl? NY\2fnJVOTBiwsXN MWWzJIg> NF7zcY5z\WS3Y3XkJJRp\SCneIDy[ZN{cW:wIH;mJHRITi4QskGsJO6yNVOPQTygZY5lKEOWR1[gZYZ1\XJidILlZZRu\W62IIfpeIghUEiH M1XDU|I{PjlyOUm3
HepT1 Mn3lRZBweHSxc3nzJGF{e2G7 NIjiWnIxNTFyMNMg{txO M{O2fVI1KGh? M3LPfWlEPTB;M{VCpO69VQ>? NV;WTJJWOjN{Nk[3NVg>
HuH6 NGm0eFNCeG:ydH;zbZMhSXO|YYm= NGewS4kxNTFyMNMg{txO NGe0cogzPCCq M2jVPWlEPTB;M{pCpO69VQ>? NFvUeW4zOzJ4NkexPC=>
MCF7 NGXObJFHfW6ldHnvckBCe3OjeR?= NIfndoY2KM7:bdMg MofxbY5pcWKrdIOgcIVxfGmwLX3l[IlifGWmIHnuZ5Jm[XOnZDDlfJBz\XO|aX;uJI9nKFOwYXnsMEBUdHWpLDDhcoQhYmWkMh?= NXHUdXViOjJ{N{CzOVk>
RLE-6TN  M2rROWZ2dmO2aX;uJGF{e2G7 MofLNk42NzVxNz61JO69VQ>? MXm0PEBp NFTPeZZqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSg{tEuW02DIHnu[JVkfGmxbjDhcoQhTU2W M{XiWVIzOjRzNEe4
HKC-8 M3jwSmZ2dmO2aX;uJGF{e2G7 MnfZOU8yOC9{MDFOwG0> M{K3V|Q5KGh? MWLicI9kc3NizsKtZ4F1\W6rbj3kdol3\W5iZ3Xu[UBmgHC{ZYPzbY9v M{LkdlIyQDF4OUO3
SW480 NFnqfVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUKyMVExOCEQvF2= MX;JR|UxRTVwONMxNE43QCEQvF2= MV[xOVc5OjF|OB?=


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]


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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]
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  • 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
+ 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.

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:
2% DMSO+50% PEG 300+5% Tween 80+ddH2O

* 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。


分子量 548.63


CAS No. 780757-88-2
in solvent
別名 N/A





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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


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

  • C1



  • 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):




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


マス 濃度 ボリューム 分子量



Handling Instructions


  • * 必須


  • 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