IWR-1 (Synonyms: endo-IWR 1; IWR-1-endo)

Name: IWR-1
Brand: MedChemExpress
SKU: HY-12238
Rating: 5.0 (38 reviews)

Cat. No.: HY-12238 Purity: 99.49%: FAQs
Data Sheet SDS COA Handling Instructions

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IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.

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

IWR-1 Chemical Structure

CAS No. : 1127442-82-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 118	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 455	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 690	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 38 publication(s) in Google Scholar

36 Publications Citing Use of MCE IWR-1

: IWR-1 purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2018 Aug;40(2):877-886. [Abstract]; IWR-1 induces cell differentiation. (A) NB4 and (B) HL-60 cells are treated with 0 (DMSO), 5 and 10 μM IWR-1 for three days, and the expression of β-catenin and differentiation marker CD11b is assessed by western blotting.

: IWR-1 purchased from MedChemExpress. Usage Cited in: Cell Biol Int. 2017 May;41(5):534-543. [Abstract]; SCAPs are cultured with modified neural differentiation medium for the indicated time periods. The neuron-like cells in control group, SFRP2 over-expressed group and 10 uM IWR1-endo treated group are positive for βIII-tubulin (red) expression by using immunofluorescence staining.

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Description

IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.

IC₅₀ & Target

IC50: 180 nM (Wnt)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	> 100 μM Compound: IWR1	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 24950489]
HEK293	IC₅₀	136 μM Compound: 1, IWR1	Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay	[PMID: 23316926]
HEK-293T	IC₅₀	26 nM Compound: 1, IWR-1	Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay	[PMID: 22191557]
HepG2	GI₅₀	95.4 μM Compound: IWR1	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 24950489]
HT-29	GI₅₀	> 100 μM Compound: IWR1	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 24950489]
HT-29	IC₅₀	24.4 μM Compound: IWR1	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 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	[PMID: 24950489]
HT-29	IC₅₀	9.52 μM Compound: IWR-1	Cytotoxicity against human HT-29 cells assessed as cell viability at 1.563 to 50 uM measured after 72 hrs by plate reader method Cytotoxicity against human HT-29 cells assessed as cell viability at 1.563 to 50 uM measured after 72 hrs by plate reader method	[PMID: 34062253]
LoVo	GI₅₀	63.1 μM Compound: IWR1	Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay	[PMID: 24950489]
SW480	IC₅₀	0.25 μM Compound: 1, IWR1	Inhibition of tankyrase in human SW480 cells assessed as degradation of beta catenin after 40 to 48 hrs Inhibition of tankyrase in human SW480 cells assessed as degradation of beta catenin after 40 to 48 hrs	[PMID: 23701517]
SW480	EC₅₀	2.5 μM Compound: 1, IWR1	Inhibition of tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method Inhibition of tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method	[PMID: 23701517]

In Vitro

Both IWR-1 and XAV939 act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects in vitro. IWR-1 exerts its effect via interaction with Axin, while XAV939 binds TNKS directly^[1]. IWR-1 (10 μM) induces stabilization of β-catenin disruption complex. IWR-1 (10 μM) is added to the medium together with MIF, the size of cell colonies is extremely decreased, and that indicates the promoting effect of MIF on NSPC proliferation is inhibited by IWR-1 in any MIF concentration group. 2, 5 and 10 μM of IWR-1 significantly inhibits the proliferation of NSPC dose-dependently. IWR-1 inhibites the promoting effect of MIF on NSPC differentiation to neuron lineage^[2]. IWR-1 treatment in the presence of maximal stimulatory dose of FSH (0.5 ng/mL) results in a dose dependent inhibition of the stimulatory effect of FSH with > 75% inhibition observed at the maximal inhibitory dose of IWR-1 (1 μM). IWR-1 treatment partially reverses the FSH-induced inhibition of granulosa cell CARTPT mRNA expression^[3].

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

Molecular Weight

409.44

Formula

C₂₅H₁₉N₃O₃

CAS No.

1127442-82-3

Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(NC1=C2N=CC=CC2=CC=C1)C3=CC=C(N(C([C@]4([H])[C@](C5)([H])C=C[C@]5([H])[C@]64[H])=O)C6=O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (122.12 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	2.4424 mL	12.2118 mL	24.4236 mL
5 mM	0.4885 mL	2.4424 mL	4.8847 mL
10 mM	0.2442 mL	1.2212 mL	2.4424 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.5 mg/mL (6.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.49%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (252 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Lu J, et al. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7. [Content Brief]

[2]. Zhang X, et al. Macrophage migration inhibitory factor promotes proliferation and neuronal differentiation of neural stem/precursor cells through Wnt/β-catenin signal pathway. Int J Biol Sci. 2013 Nov 28;9(10):1108-20. [Content Brief]

[3]. Gupta PS, et al. Regulation and Regulatory Role of WNT Signaling in Potentiating FSH Action during Bovine Dominant Follicle Selection. PLoS One. 2014 Jun 17;9(6):e100201. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4424 mL	12.2118 mL	24.4236 mL	61.0590 mL
	5 mM	0.4885 mL	2.4424 mL	4.8847 mL	12.2118 mL
	10 mM	0.2442 mL	1.2212 mL	2.4424 mL	6.1059 mL
	15 mM	0.1628 mL	0.8141 mL	1.6282 mL	4.0706 mL
	20 mM	0.1221 mL	0.6106 mL	1.2212 mL	3.0530 mL
	25 mM	0.0977 mL	0.4885 mL	0.9769 mL	2.4424 mL
	30 mM	0.0814 mL	0.4071 mL	0.8141 mL	2.0353 mL
	40 mM	0.0611 mL	0.3053 mL	0.6106 mL	1.5265 mL
	50 mM	0.0488 mL	0.2442 mL	0.4885 mL	1.2212 mL
	60 mM	0.0407 mL	0.2035 mL	0.4071 mL	1.0177 mL
	80 mM	0.0305 mL	0.1526 mL	0.3053 mL	0.7632 mL
	100 mM	0.0244 mL	0.1221 mL	0.2442 mL	0.6106 mL

IWR-1 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:

IWR-11127442-82-3endo-IWR 1 IWR-1-endoIWR1IWR 1OrganoidWntInhibitorinhibitorinhibit

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IWR-1 (Synonyms: endo-IWR 1; IWR-1-endo)

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IWR-1 Related Antibodies

36 Publications Citing Use of MCE IWR-1

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