Art. -Nr.: HY-13912

IWP-2

35 Cited Publications

Kundenbewertung

Based on 35 publication(s) in Google Scholar

IWP-2 is an inhibitor of Wnt processing and secretion with an IC₅₀ of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC₅₀ of 40 nM for the gatekeeper mutant ^M82FCK1δ.

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Reinheit: 99.93%
CAS. Nr.: 686770-61-6
Formel: C₂₂H₁₈N₄O₂S₃
Molecular Weight:466.60

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

IWP-2 Chemical Structure

CAS. Nr.: 686770-61-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (35)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

CK1γ2

40 nM (IC₅₀)

Alle Wnt Isoform-spezifische Produkte anzeigen :

Alle Casein Kinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CAPAN-1	EC₅₀	2.05 μM Compound: IWP-2	Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay	[PMID: 29630366]
HEK293	EC₅₀	2.76 μM Compound: IWP-2	Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay	[PMID: 29630366]
HT-29	EC₅₀	4.67 μM Compound: IWP-2	Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay	[PMID: 29630366]
MIA PaCa-2	EC₅₀	1.9 μM Compound: IWP-2	Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay	[PMID: 29630366]
PANC-1	EC₅₀	2.33 μM Compound: IWP-2	Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay	[PMID: 29630366]
SW-620	EC₅₀	1.9 μM Compound: IWP-2	Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay	[PMID: 29630366]

In Vitro

IWP-2 inhibits the proliferation of the investigated cell lines within the single digit μM range. IWP-2 inhibits cell proliferation in A818-6, MiaPaCa2, Panc-1, Panc-89, HT29, HEK293, SW620 and Capan cell with EC₅₀s of 8.96 μM, 1.90 μM, 2.33 μM, 3.86 μM, 4.67 μM, 2.76 μM, 1.90 μM and 2.05 μM, respectively^[2].
Panc-1 cells are either untreated or treated with 2.33 μM IWP-2 for 48 h. In IWP-2 treated cells, the CK1δ kinase peak activity is reduced to approximately 66% residual activity compared to the activity in untreated cells, respectively. IWP-2 reduces the activity of CK1δ in Panc1 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

To evaluate the efficacy of IWP-2 in vivo, 200 μL each of IWP-2-liposome or free liposome i separately injected into C57BL/6 mice intraperitoneally about 2 h before injection of a similar volume of either blue-dye-filled latex beads or E. coli DH5α. IWP-2 causes significant reduction in the uptake of blue beads as well as E. coli as assessed by CFUs in peritoneal lavage cells within 2 h. In addition, the levels of TNF-α and IL-6 in the lavage fluid of the corresponding mice are reduced by 2-4-fold compared with control values. Interestingly, IWP-2 even induces a considerable increase in secretion of the anti-inflammatory cytokine IL-10^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 686770-61-6
Appearance Solid
Molecular Weight 466.60
Formel C₂₂H₁₈N₄O₂S₃
Color White to off-white
SMILES

O=C(NC1=NC2=CC=C(C)C=C2S1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (35)

All RT-PCRWBFlow Cytometry2D/3D Cell Culture and Differentiation

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Journal Impact Factor

Adv Mater

Microbially Catalyzed Biomaterials for Bone Regeneration. [Abstract]

2021 Dec;33(49):e2104829. PMID: 34632631

IWP-2 purchased from MedChemExpress. Usage Cited in: Adv Mater. 2021 Dec;33(49):e2104829. [Abstract]

ITGA2, ALP and OPN expression in rBMSCs cultured on CBM-CS scaffolds with microbially catalyzed micro/nanostructures for 3 days after blocking Wnt processing by IWP-2 (6 μM; 3 days).
Nat Metab

Obesity impairs gut repair via AFABP-mediated iron overload in intestinal stem cells. [Abstract]

2026 Jan;8(1):74-95. PMID: 41507665
Adv Healthc Mater

Flexible Sensing Technology for Myocardial Tissue Contractile Force With Integrated Magnetically Actuated Mechanical Stimulation. [Abstract]

2026 Jun 11:e04956. PMID: 42277624
Dev Cell

Mechanical Tension Promotes Formation of Gastrulation-like Nodes and Patterns Mesoderm Specification in Human Embryonic Stem Cells. [Abstract]

2020 Dec 21;55(6):679-694.e11. PMID: 33207224

IWP-2 purchased from MedChemExpress. Usage Cited in: Dev Cell. 2020 Dec 21;55(6):679-694.e11. [Abstract]

Relative mesoderm gene expression levels after 36 h BMP4 plus vehicle (DMSO) or Wnt inhibitor (IWP-2; 2 μM).
Neoplasia

β-Catenin mediated TAM phenotype promotes pancreatic cancer metastasis via the OSM/STAT3/LOXL2 axis. [Abstract]

2024 Dec 30:60:101096. PMID: 39740539

IWP-2 purchased from MedChemExpress. Usage Cited in: Neoplasia. 2024 Dec 30:60:101096. [Abstract]

Western blot analysis of TAM markers following treatment with TCM derived from IWP-2-pretreated (2.5 μM; 6 h) PANC-1 cells (n=3).
Clin Sci

Chronic GPER activation prompted the proliferation of ileal stem cell in ovariectomized mice depending on Paneth cell-derived Wnt3. [Abstract]

2023 Jan 13;137(1):109-127. PMID: 36503938
Stem Cell Res Ther

SMYD1 modulates the proliferation of multipotent cardiac progenitor cells derived from human pluripotent stem cells during myocardial differentiation through GSK3β/β-catenin&ERK signaling. [Abstract]

2024 Oct 8;15(1):350. PMID: 39380045

IWP-2 purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2024 Oct 8;15(1):350. [Abstract]

Flow cytometry for comparisons of TNNT2+ after CHIR-99021 (5 μM; 24 h) and IWP2 (5 μM; 24 h) were added to cells, respectively.
Mol Metab

Systems genetics reveals ITIH5 as a key mediator of adipocyte-Endothelial crosstalk. [Abstract]

2026 Jun:108:102373. PMID: 42025695
J Agric Food Chem

T-2 Toxin Induces Macrophage Extracellular Trap Formation via CLOCK-WNT10B-PAD2/ROS Signaling. [Abstract]

2026 Jun 10;74(22):17392-17404. PMID: 42207496
Curr Res Microb Sci

The lncRNA GAS5-encoded micropeptide facilitates influenza virus replication through modulation of the Wnt/β-catenin signaling pathway. [Abstract]

2026 Jan 27:10:100559. PMID: 41657547
Biochem Pharmacol

Pharmacological enhancement of repolarization reserve in human induced pluripotent stem cells derived cardiomyocytes. [Abstract]

2019 Nov;169:113608. PMID: 31465775
Stem Cells Transl Med

High-throughput screening in postimplantation haploid epiblast stem cells reveals Hs3st3b1 as a modulator for reprogramming. [Abstract]

2021 May;10(5):743-755. PMID: 33511777

IWP-2 purchased from MedChemExpress. Usage Cited in: Stem Cells Transl Med. 2021 May;10(5):743-755. [Abstract]

A schematic overview of the establishment of haEpiSCs from mouse post-implantation epiblast. Newly sorted haploid p53-KO haESCs were injected into the blastocysts. The reconstructed embryos were transferred to the oviducts of pseudopregnant CD-1 mice at 0.5 day.p.c, and subsequently developed to E6.5 stage for the establishment of haEpiSCs. Factors and inhibitors including activin A, bFGF and IWP-2 (2 μM) were added into the medium.
Cell Rep Methods

Effective cryopreservation of human brain tissue and neural organoids. [Abstract]

2024 May 8:100777. PMID: 38744289
iScience

Otic organoids: A model to study spiral ganglion neuron characteristics in Tmprss3-deficiency. [Abstract]

2025 Dec 5;29(1):114355. PMID: 41509903
J Inflamm Res

Early-Life Stress Induced by Neonatal Maternal Separation Leads to Intestinal 5-HT Accumulation and Causes Intestinal Dysfunction. [Abstract]

2024 Nov 19:17:8945-8964. PMID: 39588137
J Cell Physiol

Wnt signaling associated small molecules improve the viability of pPSCs in a PI3K/Akt pathway dependent way. [Abstract]

2020 Jul;235(7-8):5811-5822. PMID: 32003013
J Gerontol A Biol Sci Med Sci

Mitochondrial Dysfunction in Myoblasts: A TSPO-Dependent Mechanism of Sarcopenia. [Abstract]

2026 Jun 2:glag145. PMID: 42226012
Bioengineering (Basel)

Integrated Manufacturing of Suspended and Aligned Nanofibrous Scaffold for Structural Maturation and Synchronous Contraction of HiPSC-Derived Cardiomyocytes. [Abstract]

2023 Jun 9;10(6):702. PMID: 37370633
Microb Pathog

Natural small molecule compounds targeting Wnt signaling pathway inhibit HPV infection. [Abstract]

2024 Sep 21:106960. PMID: 39313132
Exp Cell Res

Up-regulation of Dsg2 confered stem cells with malignancy through wnt/β-catenin signaling pathway. [Abstract]

2022 Nov 11;422(1):113416. PMID: 36375513
Autoimmunity

Endonuclease G promotes preeclampsia by regulating the Wnt signaling pathway. [Abstract]

2023 Dec;56(1):2182741. PMID: 36852641
J Appl Polym Sci

2024 Sep 25.
eNeuro

MicroRNA-155 Inhibition Activates Wnt/β-Catenin Signaling to Restore Th17/Treg Cell Balance and Protect against Acute Ischemic Stroke. [Abstract]

2025 Jan 9:ENEURO.0347-24.2024. PMID: 39788733
PLoS One

Identification and characterization of two novel KCNH2 mutations contributing to long QT syndrome. [Abstract]

2024 Jan 5;19(1):e0287206. PMID: 38181028
Toxicon

Deoxynivalenol-induced anorexia is mediated by brain-gut peptides through CaSR-TRPM5 signaling axis. [Abstract]

2026 Jan:269:108660. PMID: 41241198
Exp Ther Med

Inhibition of Rho-associated protein kinase improves the survival of human induced pluripotent stem cell-derived cardiomyocytes after dissociation. [Abstract]

2020 Mar;19(3):1701-1710. PMID: 32104223
Biocell

2025 Feb 28.
Cell Press Blue

2026 Apr 22.
Animal Research and One Health

2026 Mar 19.
bioRxiv

2026 Mar 15.
bioRxiv

2026 Jan 12.
bioRxiv

2024 Mar 13.
SSRN

2024 Mar 26.
ACS Comb Sci

Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]

2019 Dec 9;21(12):805-816. PMID: 31689077
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMF : 12.5 mg/mL (26.79 mM; ultrasonic and warming and heat to 60°C)

DMSO : 2 mg/mL (4.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1432 mL

10.7158 mL

21.4316 mL

5 mM

0.4286 mL

2.1432 mL

4.2863 mL

10 mM

0.2143 mL

1.0716 mL

2.1432 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.2 mg/mL (0.43 mM); Clear solution

This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 0.1 mg/mL (0.21 mM); Clear solution

Protocol 3

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.1 mg/mL (0.21 mM); Clear solution

Protocol 4

Add each solvent one by one: 5% DMSO 95% Corn Oil

Solubility: ≥ 0.1 mg/mL (0.21 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (21.43 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

The human RCC cell lines 786O and Caki-2 (5×10³) are seeded into 96-well plates. Cell viability is estimated by MST assay after Caki-2 acells are incubated with ncreasing concentrations of LEF together with 20 μM IWP-2 for 48 h.After treatment, 10 μL MTS is added into each well for 2 h incubation. The absorbance is measured using a model ELX800 Micro Plate Reader at 490 nm. For colony formation assay, Caki-2 cells are trypsinized to single cell suspensions and seeded into fresh 6-well plates at 1000 cells/well. Then cells are incubated with LEF at depicted concentrations for 7 days. Colonies are fixed with absolute methanol for 15 min and then stained with 0.1% crystal violet for 20 min. After washing with PBS three times, the colonies with a diameter over 2 mm are visualized by a digital camera^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7. [Content Brief]

[2]. García-Reyes B, et al. Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε. J Med Chem. 2018 May 10;61(9):4087-4102. [Content Brief]

[3]. Maiti G, et al. The Wingless homolog Wnt5a stimulates phagocytosis but not bacterial killing. Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16600-5. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / DMF	1 mM	2.1432 mL	10.7158 mL	21.4316 mL	53.5791 mL
DMF	5 mM	0.4286 mL	2.1432 mL	4.2863 mL	10.7158 mL
	10 mM	0.2143 mL	1.0716 mL	2.1432 mL	5.3579 mL
	15 mM	0.1429 mL	0.7144 mL	1.4288 mL	3.5719 mL
	20 mM	0.1072 mL	0.5358 mL	1.0716 mL	2.6790 mL
	25 mM	0.0857 mL	0.4286 mL	0.8573 mL	2.1432 mL

Keywords

IWP-2

35 Cited Publications

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IWP-2

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) IWP-2

Alle Wnt Isoform-spezifische Produkte anzeigen

Alle Casein Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (35)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

IWP-2

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) IWP-2

Alle Wnt Isoform-spezifische Produkte anzeigen

Alle Casein Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (35)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

IWP-2 Related Classifications

HY-13912 Related Classifications