Name: ICG-001
Brand: Selleck Chemicals
SKU: S2662
Rating: 5 (202 reviews)

Hoppa till

Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.75%

99.75

Produkter som ofta används tillsammans med 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.

Relaterade mål	JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase
Övrigt Wnt/beta-catenin Inhibitorer	IWR-1-endo PRI-724 (Foscenvivint) IWP-2 Tegatrabetan (BC-2059) Isoquercitrin SKL2001 BML-284 Hydrochloride (Wnt agonist 1, AMBMP) PNU-74654 LF3 Salinomycin (Procoxacin)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer	Analystyp	Koncentration	Inkubationstid	Formulering	Aktivitetsbeskrivning	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
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	548.63	Formel	C₃₃H₃₂N₄O₄	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	780757-88-2 (relative stereochemistry); 847591-62-2 (absolute stereochemistry)	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel

Löslighet (Solubility)

In vitro
Batch:

DMSO : 30 mg/mL (54.68 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	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-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (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.
Kinasanalys	DUAL-Luciferase Reporter Assay
Kinasanalys	The Dual-Luciferase Reporter (DLR) Assay System ger ett effektivt sätt att utföra dual reporter-analyser. I DLR^TM Assay mäts aktiviteterna hos firefly (Photinus pyralis) och Renilla (Renilla reniformis, även känd som sea pansy) luciferaser sekventiellt från ett enda prov. Firefly-luciferasreportern mäts först genom att tillsätta Luciferase Assay Reagent II (LAR II) för att generera en ”glow-type” luminescent signal. Efter kvantifiering av firefly-luminescensen släcks denna reaktion, och Renilla-luciferasreaktionen initieras genom att samtidigt tillsätta Stop & Glo® Reagent till samma rör. Stop & Glo® Reagent producerar också en ”glow-type” signal från Renilla-luciferasen, som bryts ner långsamt under mätningen. I DLR^TM Assay System ger båda reportrarna linjära analyser med subattomol (<10-18) känsligheter och ingen endogen aktivitet av någon av reportrarna i de experimentella värdcellerna. Dessutom ger det integrerade formatet av DLR^TM Assay snabb kvantifiering av båda reportrarna antingen i transfekterade celler eller i cellfria transkriptions-/translationsreaktioner.
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.
Referenser	[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/

Applikationer (Applications)

Metoder	Biomarkörer	Bilder	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

Vanliga frågor (Frequently Asked Questions)

Fråga 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?

Svar:
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.

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):

ICG-001 Wnt/β-catenin Inhibitor

Molekylvikt: 548.63

Kvalitetskontroll (Quality Control)

Produkter som ofta används tillsammans med ICG-001

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Vanliga frågor (Frequently Asked Questions)

ICG-001 Wnt/β-catenin Inhibitor

Molekylvikt: 548.63

Kvalitetskontroll (Quality Control)

Produkter som ofta används tillsammans med ICG-001

Cellodling, behandling & arbetskoncentration (Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Vanliga frågor (Frequently Asked Questions)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)