ICG-001

製品コード：S2662 純度：99.75%

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. ICG-001 induces apoptosis.

CAS No. 780757-88-2 (relative stereochemistry); 847591-62-2 (absolute stereochemistry)

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 70500	国内在庫なし(納期7~10日)
100mg	JPY 145500	国内在庫あり
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（189）

製品安全説明書

現在のバッチを見る：純度： 99.75%

99.75

ICG-001と併用されることが多い化合物

(+)-JQ1

Foscenvivint and JQ1 combination treatment induces strong cytotoxic effects in H3.3K27M-mutated diffuse intrinsic pontine gliomas (DIPG) cell lines.

Wiese M, et al. Cell Death & Disease 11.8 (2020): 673.

Wnt-C59 (C59)

Foscenvivint and Wnt-C59 inhibit in vitro growth of human cholangiocarcinoma cells and reduce tumor area and number in xenograft and thioacetamide models.

Noll AT, et al. World J Hepatol. 2016 Sep 18;8(26):1093-6.

ICG-001関連製品

関連ターゲット	BET p300/CBP BRPF bromodomain	もっと見る
関連製品	Birabresib (OTX015) I-BET151 (GSK1210151A) Molibresib (I-BET-762) SGC-CBP30 EED226 Apabetalone (RVX-208) KG-501 CPI-203 compound 3i (666-15) PFI-3 AZD5153 6-hydroxy-2-naphthoic acid PFI-1 (PF-6405761) Mivebresib (ABBV-075) ABBV-744 UNC1215 I-BRD9 Bromosporine PLX51107 GSK1324726A (I-BET726) Pelabresib (CPI-0610) PF-CBP1 HCl INCB054329 MS436 GSK2801 UNC669 MZ-1 NEO2734 OF-1 CPI-637 GSK6853 I-CBP112 BI-7273 PFI-4 INCB057643 GSK 5959 dBET57 BI-9564 Histone Acetyltransferase Inhibitor II	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Stem Cell Signaling Compound Library GPCR Compound Library Stem Cell Differentiation Compound Library	もっと見る

シグナル伝達経路

Epigenetic Reader Domainシグナル伝達経路

Epigenetic Reader Domain阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HK-2	Function Assay	10 µM	3 h	reduced the expression of TGF-β1, α-SMA, and CTGF after treatment with HHE	23690997
HKC-8	Function Assay	10 µM	24 h	abolishes β-catenin–mediated RAS induction	25012166
SH-SY5Y	Apoptosis Assay	10 μM	24 h	inhibits the neuroprotective effects of hypoxia against PrP (106-126)-mediated neuronal cell death	23900566
L3.6pl	Growth Inhibition Assay	1-20 μM	2/4/6 d	inhibits the cell growth in a dose-dependent manner	25082960
PANC-1	Growth Inhibition Assay	1-20 μM	2/4/6 d	inhibits the cell growth in a dose-dependent manner	25082960
MiaPaCa-2	Growth Inhibition Assay	1-20 μM	2/4/6 d	inhibits the cell growth in a dose-dependent manner	25082960
AsPC-1	Growth Inhibition Assay	1-20 μM	2/4/6 d	inhibits the cell growth in a dose-dependent manner	25082960
SH-SY5Y	Apoptosis Assay	50 μm	24 h	blocks the protective effect of melatonin against PrP (106–126)-induced apoptotic signals	25251028
HepT1	Apoptosis Assay	0-100 μM	24 h	IC50=34 μM	23266718
HuH6	Apoptosis Assay	0-100 μM	24 h	IC50=39 μM	23266718
RLE-6TN	Function Assay	2.5/5/7.5 μM	48 h	inhibits TGF-β1-induced α-SMA induction and EMT	22241478
HKC-8	Function Assay	5/10/20 μM	48 h	blocks β-catenin-driven gene expression	21816937
LoVo	Cytotoxicity assay	10 uM	72 hrs	Cytotoxicity against Wnt/beta-catenin signalling dependent human LoVo cells assessed as cell viability at 10 uM after 72 hrs by ATPlite assay	ChEMBL
NCI-H1703	Function assay	10 uM	24 hrs	Inhibition of TNIK in human NCI-H1703 cells transfected with lentiviral vector 7TFP assessed as reduction of GSK3 inhibitor X activated TNIK-mediated Wnt/TCF/beta-catenin-dependent transcription at 10 uM after 24 hrs by luciferase reporter assay	ChEMBL
HCT116	Cytotoxicity assay	10 uM	72 hrs	Cytotoxicity against Wnt/beta-catenin signalling dependent human HCT116 cells assessed as cell viability at 10 uM after 72 hrs by ATPlite assay	ChEMBL
MCF7	Function Assay	5 μm		inhibits leptin-mediated increased expression of Snail, Slug, and Zeb2	22270359
SW480	Growth Inhibition Assay	2-100 μM		IC50=5.8±0.68 μM	15782138
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, GI50 = 6.1 μM.	24950489
HepG2	Antiproliferative assay		72 hrs	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, GI50 = 12.7 μM.	24950489
LoVo	Antiproliferative assay		72 hrs	Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay, GI50 = 15.6 μM.	24950489
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, GI50 = 17.2 μM.	24950489
HT29	Function assay		24 hrs	Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity after 24 hrs by dual luciferase reporter gene assay relative to control, IC50 = 18.7 μM.	24950489
SW480	Function assay			Inhibition of CBP binding to beta-casein in human SW480 cells by immunoblot analysis, IC50 = 1.3 μM.	23232060
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
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生物活性

製品説明

Targets

CBP ^[1]
(Cell-free assay)

3 μM

In Vitro
In vitro	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]
Kinase Assay	DUAL-Luciferase Reporter Assay
Kinase Assay	The Dual-Luciferase Reporter (DLR) Assay System provides an efficient means of performing dual reporter assays. In the DLR^TM 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 DLR^TM 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 DLR^TM Assay provides rapid quantitation of both reporters either in transfected cells or in cell-free transcription/translation reactions.
細胞実験	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
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	SOX-2 / CD44 / Survivin / EGFR / FOXM1 / EZH2 / Vimentin pβ-catenin beta-catenin / F-actin ABC / Beta-catenin / E-cadherin / N-cadherin / MMP-9 / c-MYC / Actin / Histone H3 CCNB1 / Cyclin D1		25897700

In Vivo
In Vivo	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, 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]
動物実験	動物モデル	C57BL/6 and nude mice tumor models
	投与量	20 mg/ kg
	投与経路	i.p.

参考
[1] Emami KH, et al, Proc Natl Acad Sci USA, 2004, 101(34), 12682-12687. [2] Teo JL, et al, Proc Natl Acad Sci USA, 2005, 102(34), 12171-12176. [3] Yan D, et al, J Biol Chem, 2012, 287(11), 8598-8612. [4] Henderson WR Jr, et al, Proc Natl Acad Sci USA, 2010, 107(32), 14309-14314. [5] Huang Y, et al. Radiother Oncol. 2021 Sep;162:34-44. + 展開

参考

+ 展開

化学情報

分子量	548.63	化学式	C₃₃H₃₂N₄O₄
CAS No.	780757-88-2 (relative stereochemistry); 847591-62-2 (absolute stereochemistry)	SDF	Download ICG-001 SDFをダウンロードする
Smiles	C1CN(C2CN(C(=O)C(N2C1=O)CC3=CC=C(C=C3)O)CC4=CC=CC5=CC=CC=C54)C(=O)NCC6=CC=CC=C6
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 30 mg/mL ( (54.68 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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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.

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):