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IWR-1-endo

Name: IWR-1-endo
Brand: Selleck Chemicals
SKU: S7086
Rating: 5 (120 reviews)

Synonyms: endo-IWR 1, IWR-1

Catalog No.S7086 Purity: 99.94%

IWR-1-endo (endo-IWR 1, IWR-1) is a Wnt pathway inhibitor with IC50 of 180 nM in L-cells expressing Wnt3A, induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes.

IWR-1-endo Chemical Structure

CAS: 1127442-82-3

Selleck's IWR-1-endo has been cited by 120 publications

Purity & Quality Control

Batch: Purity: 99.94%

99.94

Products often used together with IWR-1-endo

Laduviglusib (CHIR-99021)

IWR-1-endo and CHIR99021 support continuous cell proliferation to certain degrees in human prostate epithelial cells (PrECs).

Zhang C, et al. Cell Rep. 2018 Oct 16;25(3):598-610.e5.

WH-4-023

IWR-1-endo and WH-4-023 along with other small molecules and cytokines are used for the preparation of 3i/LAF medium to culture Pig pluripotent stem cell lines E10 pregastrulation epiblasts (pgEpiSCs).

Zhi M, et al. Cell Res. 2022 Apr;32(4):383-400.

SB431542

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

Popova G, et al. Elife. 2023 Jul 20;12:RP87696.

XAV-939

IWR-1-endo and XAV-939 use abrogates 17β-estradiol inhibition of HIV replication by inhibiting β-catenin signaling in HIV-infected peripheral blood mononuclear cells (PBMCs).

Szotek EL, et al. Virology. 2013 Sep 1;443(2):375-83.

ICG-001

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

Gao L, et al. PLoS One. 2017 Aug 24;12(8):e0181346.

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	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
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

Wnt ^[1]
(L-cells expressing Wnt3A)

180 nM

In vitro
In vitro	Although both IWR-1 and XAV939 act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects both in vitro and in vivo, IWR-1 exerts its effect via interaction with Axin, while XAV939 binds TNKS directly. ^[1]
Cell Research	Cell lines	Pig EpiSCs
	Concentrations	2.5 μM
	Incubation Time	2 days
	Method	For neural induction, the 3i/LAF culture medium was replaced with neural induction medium I (2.5 μM IWR-1-endo, 5 μM SB431542, and 10 ng/mL FGF2 in BM) on day 2 after pgEpiSC passage.
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Western blot	Survivin p-Akt / Akt E-cadherin / N-cadherin / Snail / Vimentin		26450645

In Vivo
In vivo	IWR-1 is a β‐catenin inhibitor.^[3]

References

Chemical lnformation & Solubility

Molecular Weight	409.44	Formula	C₂₅H₁₉N₃O₃
CAS No.	1127442-82-3	SDF	--
Smiles	C1C2C=CC1C3C2C(=O)N(C3=O)C4=CC=C(C=C4)C(=O)NC5=CC=CC6=C5N=CC=C6
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 82 mg/mL ( (200.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.1mg/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.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 Corn oil	1.5mg/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	1.5mg/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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

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

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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