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 27888.00
JPY 19920.00
JPY 78020.00

カスタマーフィードバック(7)

  • 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.

    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.

    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 Mn7ERZBweHSxc3nzJGF{e2G7 MlTUOVDDqM7:bR?= MXWyOOKhcA>? MVjEUXNQ MkHmZoxw[2u|wrD0bIUheHKxdHXjeIl3\SCnZn\lZ5Qhd2ZibXXsZZRwdmmwIHHnZYlve3RiUILQJEgyODckgKOxNlYqNWmwZIXj[YQh[XCxcITveIlkKHOrZ37hcJM> MmXUNlUzPTFyMki=
AsPC-1 M3n3cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TJSFEuOjBizszN NF3wOnczNzRxNjDk NFjm[mNqdmirYnn0d{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NET4NY0zPTB6Mkm2NC=>
MiaPaCa-2 MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37uVlEuOjBizszN NV\mVYdzOi92L{[g[C=> NGLRU2hqdmirYnn0d{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NYWzRmhEOjVyOEK5OlA>
PANC-1 NIGzS2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHKwTo4yNTJyIN88US=> MWSyM|QwPiCm M4D1OYlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NX;JfZlyOjVyOEK5OlA>
L3.6pl NIjIVlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml24NU0zOCEQvF2= MmHWNk81NzZiZB?= M1vqRYlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MkHHNlUxQDJ7NkC=
SH-SY5Y MnnYRZBweHSxc3nzJGF{e2G7 MX2xNEDPxE1? MlLtNlQhcA>? NFr6fHlqdmirYnn0d{B1cGVibnX1do9xem:2ZXP0bZZmKGWoZnXjeJMhd2ZiaInwc5hq[SCjZ3HpcpN1KFC{UDCoNVA3NTF{NjmtcYVlcWG2ZXSgcoV2em:wYXygZ4VtdCCmZXH0bC=> NG\ud3czOzlyMEW2Oi=>
HKC-8  M3LoOGZ2dmO2aX;uJGF{e2G7 NVXOephDOTEEoNM1US=> M4WyU|I1KGh? NILsNJRi[m:uaYPo[ZPDqM7{LXPheIVvcW8kgKPt[YRq[XSnZDDSRXMhcW6mdXP0bY9v MlPxNlUxOTJzNk[=
HK-2  NX;2N2QzTnWwY4Tpc44hSXO|YYm= MofVNVAhyrWP NUnuelc3OyCq NYjFdoF1emWmdXPl[EB1cGViZYjwdoV{e2mxbjDv[kBVT0ZvzsKxMEDPuS2VTVGsJIFv\CCFVFfGJIFnfGW{IITy[YF1dWWwdDD3bZRpKEiKRR?= MnrpNlM3QTB7OUe=
HepT1 NFrPfmtCeG:ydH;zbZMhSXO|YYm= MlrJNE0yODEEoN88US=> NHHWO4IzPCCq MmjZTWM2OD1|NNMg{txO NI[2NZIzOzJ4NkexPC=>
HuH6 NIO0U5NCeG:ydH;zbZMhSXO|YYm= MXKwMVExOMLizszN NGe2cXEzPCCq NF;rNJFKSzVyPUO5xsDPxE1? NVzyW|Z1OjN{Nk[3NVg>
MCF7 MULGeY5kfGmxbjDBd5NigQ>? NWS5S3FWPSEQvH5CpC=> NE\acGtqdmirYnn0d{Bt\XC2aX6tcYVlcWG2ZXSgbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZiU37hbYwtKFOudXesJIFv\CCcZXKy NWfHb|NwOjJ{N{CzOVk>
RLE-6TN  NY\zcYU2TnWwY4Tpc44hSXO|YYm= NYXlPFZpOi53L{WvO{42KM7:TR?= M{jndFQ5KGh? M4r6WYlvcGmkaYTzJHRITi4QskGtbY5lfWOnZDFOtU1UVUFiaX7keYN1cW:wIHHu[EBGVVR? NWf6[od2OjJ{NEG0O|g>
HKC-8 NW\qU|h4TnWwY4Tpc44hSXO|YYm= M4HCWlUwOTBxMkCg{txO NWj3VpJ{PDhiaB?= NWWySVVm[myxY3vzJO6zNWOjdHXubY4u\HKrdnXuJIdmdmViZYjwdoV{e2mxbh?= MknONlE5OTZ7M{e=
SW480 M4rjUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm[1Nk0yODBizszN Ml\2TWM2OD13LklCtVAvPjhizszN MX[xOVc5OjF|OB?=

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

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