Name: ICG-001
Brand: Selleck Chemicals
SKU: S2662
Availability: InStock
Rating: 5 (201 reviews)

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Quality Control

Batch: Purity: 99.75%

99.75

Products Often Used Together with ICG-001

(+)-JQ1

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

Wnt-C59 (C59)

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

Related Targets	JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase
Other Wnt/beta-catenin Inhibitors	IWR-1-endo IWP-2 Isoquercitrin Tegatrabetan (BC-2059) SKL2001 BML-284 (Wnt agonist 1) PRI-724 (Foscenvivint) Salinomycin (from Streptomyces albus) FH535 PNU-74654

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
SH-SY5Y	Apoptosis Assay	50 μm	24 h	DMSO	blocks the protective effect of melatonin against PrP (106–126)-induced apoptotic signals	25251028
AsPC-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
PANC-1	Growth Inhibition Assay	1-20 μM	2/4/6 d		inhibits the cell growth in a dose-dependent manner	25082960
L3.6pl	Growth Inhibition Assay	1-20 μM	2/4/6 d		inhibits the cell growth in a dose-dependent manner	25082960
SH-SY5Y	Apoptosis Assay	10 μM	24 h		inhibits the neuroprotective effects of hypoxia against PrP (106-126)-mediated neuronal cell death	23900566
HKC-8	Function Assay	10 µM	24 h		abolishes β-catenin–mediated RAS induction	25012166
HK-2	Function Assay	10 µM	3 h		reduced the expression of TGF-β1, α-SMA, and CTGF after treatment with HHE	23690997
HepT1	Apoptosis Assay	0-100 μM	24 h		IC50=34 μM	23266718
HuH6	Apoptosis Assay	0-100 μM	24 h		IC50=39 μM	23266718
MCF7	Function Assay	5 μm			inhibits leptin-mediated increased expression of Snail, Slug, and Zeb2	22270359
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
SW480	Growth Inhibition Assay	2-100 μM			IC50=5.8±0.68 μM	15782138
SW480	Function assay				Inhibition of CBP binding to beta-casein in human SW480 cells by immunoblot analysis, IC50 = 1.3 μM.	23232060
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
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
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 30 mg/mL (54.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.11mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.650mg/ml (1.18mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	548.63	Formula	C₃₃H₃₂N₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	780757-88-2 (relative stereochemistry); 847591-62-2 (absolute stereochemistry)	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	CBP (Cell-free assay) 3 μM
In vitro	ICG-001 has no effect on the related reporter construct, FOPFLASH, which contains mutated TCF sites. After treatment with 25μM of this compound 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. This compound selectively induces apoptosis in transformed cells but not in normal colon cells, reduces in vitro growth of colon carcinoma cells. It 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. A recent study demonstrates that 5μM of this chemical inhibits leptin-induced EMT, invasion and tumorsphere formation in MCF7 cells.
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.
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 this compound demonstrates a dramatic reduction in tumor volume over the 19-day course of treatment, with no mortality or weight loss. This chemical (5 mg/kg per day) significantly inhibits beta-catenin signaling and attenuates bleomycin-induced lung fibrosis in mice, while concurrently preserving the epithelium.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15314234/ [2] https://pubmed.ncbi.nlm.nih.gov/16093313/ [3] https://pubmed.ncbi.nlm.nih.gov/22270359/ [4] https://pubmed.ncbi.nlm.nih.gov/20660310/ [5] https://pubmed.ncbi.nlm.nih.gov/34214613/

Applications

Methods	Biomarkers	Images	PMID
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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 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 it?

Answer:
It 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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ICG-001 Wnt/β-catenin Inhibitor

Chemical Structure

Molecular Weight: 548.63