IWR-1-endo

Synonyms: endo-IWR 1, IWR-1

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

IWR-1-endo Chemical Structure

CAS: 1127442-82-3

Selleck's IWR-1-endo has been cited by 116 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.

IWR-1-endo Related Products

Choose Selective Wnt/beta-catenin Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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 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.
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
Western blot E-cadherin / N-cadherin / Snail / Vimentin p-Akt / Akt Survivin 26450645
In Vivo
In vivo

IWR-1 is a β‐catenin inhibitor.[3]

Chemical Information & 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)

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble


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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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