Cat. No.: HY-12879

IWP-4

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

IWP-4 is a Wnt inhibitor with an IC₅₀ of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC₅₀ of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC₅₀ = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure.

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

Purity: 99.81%
CAS No.: 686772-17-8
Formula: C₂₃H₂₀N₄O₃S₃
Molecular Weight:496.62

Storage:

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

IWP-4 Chemical Structure

CAS No.: 686772-17-8

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 25 nM (Wnt)^[1]

All Wnt Isoforms :

All Casein Kinase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CAPAN-1	EC₅₀	0.23 μM Compound: IWP-4	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	0.28 μM Compound: IWP-4	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	0.34 μM Compound: IWP-4	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	0.23 μM Compound: IWP-4	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	0.23 μM Compound: IWP-4	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	0.23 μM Compound: IWP-4	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-4 (48 h) inhibits the proliferation of all tested cancer cell lines, with submicromolar EC₅₀ values ranging from 0.23 μM to 0.93 μM^[1].
IWP-4 (1 μM; 24 h) antagonizes the protective effect of Ginkgolide B (HY-N0784) on primary rat cortical astrocytes against glutamate-induced injury by reversing Ginkgolide B-mediated regulation of apoptosis-related genes and proteins, as well as glutamate transporter genes and proteins^[2].

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

Chemical Information

CAS No. 686772-17-8
Appearance Solid
Molecular Weight 496.62
Formula C₂₃H₂₀N₄O₃S₃
Color White to light yellow
SMILES

O=C(NC1=NC2=CC=C(C)C=C2S1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5OC)=O
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

Publications (2)

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Chin Med

Astragalus membranaceus (Huangqi) and Rhizoma curcumae (Ezhu) decoction suppresses colorectal cancer via downregulation of Wnt5/β-Catenin signal. [Abstract]

2022 Jan 6;17(1):11. PMID: 34991661
Biol Pharm Bull

5-Demethylnobiletin Ameliorates Isoproterenol-Induced Cardiac Fibrosis and Apoptosis by Repressing the Sirt1/FOXO3a/NF-κB and Wnt/β-Catenin Pathways. [Abstract]

2024;47(10):1774-1785. PMID: 39477471

Solvent & Solubility

In Vitro:

DMSO : 1.72 mg/mL (3.46 mM; ultrasonic and warming and heat to 60°C; 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

2.0136 mL

10.0681 mL

20.1361 mL

5 mM

---

10 mM

---

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.

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Protocol

Cell Assay^[1]

hESC cultures are obtained in mTeSR-1 medium and expanded with daily medium exchange until colonies reach the desired level of conﬂuence (~70% to 80%). At this time (marked day 0), mTeSR-1 is replaced with a basal medium comprised of RPMI 1640 medium supplemented with 2% B27 supplement and 1% penicillin/streptomycin. 20 ng/mL BMP-4 and/or 6 ng/mL activin A are added to the basal medium for primitive streak induction, and exchanged daily until day 3. Then, basal media with or without 5 mM IWP-4 is added to the cells and exchanged every 2 days [dimethyl sulfoxide (DMSO) at the same concentration is used as a vehicle control] until day 15, after which basal medium is supplied every 2 days^[1].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 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)

References

[1]. 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;61(9):4087-4102. [Content Brief]

[2]. Wang J, et al. A RNA-seq approach for exploring the protective effect of ginkgolide B on glutamate-induced astrocytes injury. J Ethnopharmacol. 2021;270:113807. [Content Brief]

[3]. Hudson J, et al. Primitive cardiac cells from human embryonic stem cells. Stem Cells Dev. 2012 Jun 10;21(9):1513-23. [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, 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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0136 mL	10.0681 mL	20.1361 mL	50.3403 mL

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IWP-4

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Anti-Cardiovascular Disease Compound Library

Cytoskeleton Compound Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Antihypertensive Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Publications Citing Use of MedChemExpress (MCE) IWP-4

All Wnt Isoforms

All Casein Kinase Isoforms