IWP-2

Name: IWP-2
Brand: MedChemExpress
SKU: HY-13912
Rating: 5.0 (30 reviews)

Cat. No.: HY-13912 Purity: 99.93%: Data Sheet
COA

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Handling Instructions
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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.

For research use only. We do not sell to patients.

CAS No. : 686770-61-6

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of IWP-2:

IWP-2 (GMP) In-stock

30 Publications Citing Use of MCE IWP-2

RT-PCR

Flow Cytometry

2D/3D Cell Culture and Differentiation

: 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).

: 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.

: 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).

: 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.

: 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).

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CK1 CK2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

CK1γ2

40 nM (IC₅₀)

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.

Molecular Weight

466.60

Formula

C₂₂H₁₈N₄O₂S₃

CAS No.

686770-61-6

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (249 KB) HNMR (273 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration	MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

IWP-2 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IWP-2686770-61-6IWP2IWP 2WntPorcupineCasein KinaseInhibitorinhibitorinhibit

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IWP-2

Customer Review

Other Forms of IWP-2:

IWP-2 Related Antibodies

30 Publications Citing Use of MCE IWP-2

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Wnt Isoform Specific Products:

View All Casein Kinase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

IWP-2 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

IWP-2 Related Classifications

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