Name: IWR-1-endo
Brand: Selleck Chemicals
SKU: S7086
Rating: 5 (168 reviews)

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Batch: Zuiverheid: 99.94%

99.94

Producten Vaak Samen Gebruikt Met IWR-1-endo

CHIR-99021 (Laduviglusib)

This compound and CHIR99021 support continuous cell proliferation to certain degrees in human prostate epithelial cells (PrECs).

WH-4-023

Along with WH-4-023, other small molecules and cytokines, it is used for the preparation of 3i/LAF medium to culture Pig pluripotent stem cell lines E10 pregastrulation epiblasts (pgEpiSCs).

SB431542

It and SB431542 are WNT and SMAD inhibitors that are used to supplement neural induction media for the 1st 9 days.

ICG-001

Compared to IWR-1-endo, ICG-001 significantly reduces the accumulation of the nucleic β-catenin in U87 cells.

Gerelateerde doelwitten	JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase
Overige Wnt/beta-catenin Inhibitoren	PRI-724 (Foscenvivint) IWP-2 Tegatrabetan (BC-2059) Isoquercitrin SKL2001 BML-284 Hydrochloride (Wnt agonist 1, AMBMP) PNU-74654 Salinomycin (Procoxacin) FH535 LF3

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
BL21 (DE3)	Function assay		90 mins	Activity of N-terminus hexaHis-tagged human TNSK2 expressed in Escherichia coli BL21 (DE3) cells using biotinylated NAD+ as substrate after 90 mins by Western blot analysis, EC50 = 0.2 μM.	22233320
SW480	Function assay		24 hrs	Inhibition of tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method, EC50 = 2.5 μM.	23701517
HEK293T	Function assay			Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay, IC50 = 0.026 μM.	22191557
SW480	Function assay		40 to 48 hrs	Inhibition of tankyrase in human SW480 cells assessed as degradation of beta catenin after 40 to 48 hrs, IC50 = 0.25 μM.	23701517
L-Wnt-STF	Function assay		24 hrs	Inhibition of TNKS-2 in mouse L-Wnt-STF cells assessed as disruption of Wnt signaling after 24 hrs by luciferase reporter gene assay, IC50 = 0.056 μM.	24527792
L-Wnt-STF	Function assay		24 hrs	Inhibition of TNKS-1 in mouse L-Wnt-STF cells assessed as disruption of Wnt signaling after 24 hrs by luciferase reporter gene assay, IC50 = 0.131 μM.	24527792
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 = 24.4 μM.	24950489
DLD1	Function assay	10 uM		Induction of Axin2 in human DLD1 cells overexpressing IWR-IS assessed as decrease in Wnt pathway activity at 10 uM by STF reporter assay method	19125156
HEK293	Function assay			Displacement of IWR-PB from Axin2 in HEK293 cells by Western blot method	19125156
DLD1	Function assay			Inhibition of Axin2 protein degradation in human DLD1 cells by Western blot analysis	19125156
DLD1	Function assay			Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Thr41 phosphorylated beta-casein levels by Western blot analysis	19125156
DLD1	Function assay			Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Ser37 phosphorylated beta-casein levels by Western blot analysis	19125156
DLD1	Function assay			Decrease in beta-casein accumulation in human DLD1 cells expressing in APC mutant	19125156
DLD1	Function assay		2 hrs	Induction of Axin2 stabilization in human DLD1 cells assessed as decreased transcription of Axin2 after 2 hrs by RT-PCR method	19125156
DLD1	Function assay			Induction of Axin2 accumulation in human DLD1 cells assessed as decrease in free beta-casein levels by Western blot analysis	19125156
DLD1	Function assay			Induction of Axin2 stabilization in human DLD1 cells assessed as inhibition of Wnt/beta-casein pathway	19125156
DLD1	Function assay			Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Ser33 phosphorylated beta-casein levels by Western blot analysis	19125156
DLD1	Function assay			Induction of Axin2 accumulation in human DLD1 cells by Western blot analysis	19125156
DLD1	Function assay	1 to 20 uM	24 hrs	Inhibition of tankyrase in human DLD1 cells assessed as inhibition of TCF-dependent transcriptional activity at 1 to 20 uM after 24 hrs by dual luciferase reporter gene assay	24527792
DLD1	Cytotoxicity assay	1 to 20 uM	10 days	Cytotoxicity against human DLD1 cells assessed as growth inhibition at 1 to 20 uM measured on day 10 by crystal violet staining	24527792
HT29	Function assay	25 uM	24 hrs	Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity at 25 uM after 24 hrs by dual luciferase reporter gene assay relative to control	24950489
HT29	Function assay	25 uM	24 hrs	Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity at 25 uM after 24 hrs by dual luciferase reporter gene assay relative to control in presence of GSK-3beta inhibitor LiCl	24950489
HT29	Function assay	25 uM	24 hrs	Inhibition of Wnt/beta-catenin signaling in human HT29 cells assessed as increase in axin2 mRNA expression at 25 uM after 24 hrs by quantitative real-time PCR assay	24950489
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	409.44	Formule	C₂₅H₁₉N₃O₃	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	1127442-82-3	--		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	endo-IWR 1, IWR-1			Smiles	C1C2C=CC1C3C2C(=O)N(C3=O)C4=CC=C(C=C4)C(=O)NC5=CC=CC6=C5N=CC=C6

Oplosbaarheid

In vitro
Batch:

DMSO : 82 mg/mL (200.27 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 82 mg/mL (200.27 mM) Geultrasoneerd;
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

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.
Clear solution	5%DMSO 1 Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.500mg/ml (3.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	4.100mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 82 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.
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.
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.500mg/ml (3.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	Wnt (L-cells expressing Wnt3A) 180 nM
In vitro	Hoewel zowel IWR-1 als XAV939 fungeren als omkeerbare Wnt pathway-remmers en vergelijkbare farmacologische effecten vertonen, zowel in vitro als in vivo, oefent IWR-1 zijn effect uit via interactie met Axin, terwijl XAV939 rechtstreeks aan TNKS bindt.
In vivo	IWR-1 is een -catenine-remmer.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/19410457/ [2] https://pubmed.ncbi.nlm.nih.gov/34848870/ [3] https://pubmed.ncbi.nlm.nih.gov/35522902/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	E-cadherin / N-cadherin / Snail / Vimentin p-Akt / Akt Survivin		26450645

Technische ondersteuning

Gebruiksaanwijzing

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

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IWR-1-endo WNT Pathway-remmer

Chemische structuur

Moleculair gewicht: 409.44