| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C23H20N4O3S3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. It also specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with IC50 values of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε, and it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). It is applicable to research on cancer, Alzheimer's disease (AD), and heart failure[1][2][3]. It is supplied as a white to light yellow solid (C23H20N4O3S3, MW 496.62) at 99.81% purity.
Physical & Chemical Properties
| CAS Number | 686772-17-8 |
|---|---|
| Molecular Formula | C23H20N4O3S3 |
| Molecular Weight | 496.62 g/mol |
| Purity | 99.81% |
| Appearance | Solid |
| Color | White to light yellow |
| SMILES | O=C(NC1=NC2=CC=C(C)C=C2S1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5OC)=O |
| Signaling Pathway | Stem Cell/Wnt; Cell Cycle/DNA Damage |
| Solubility | In Vitro: DMSO: 1.72 mg/mL (3.46 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 25 nM (Wnt)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 1.72 mg/mL (3.46 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
Across all tested cancer cell lines, IWP-4 (48 h) inhibits proliferation, with submicromolar EC50 values spanning 0.23 μM to 0.93 μM[1]. In primary rat cortical astrocytes, IWP-4 (1 μM; 24 h) antagonizes the protection that Ginkgolide B gives against glutamate-induced injury, by reversing the Ginkgolide B-mediated regulation of genes and proteins involved in apoptosis and in glutamate transport[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Culture hESCs in mTeSR-1 medium and expand with daily medium exchange until colonies reach the desired confluence (~70% to 80%). At this point (day 0), replace mTeSR-1 with a basal medium made of RPMI 1640 containing 2% B27 supplement and 1% penicillin/streptomycin. For primitive streak induction, add 20 ng/mL BMP-4 and/or 6 ng/mL activin A to the basal medium and exchange daily until day 3. Then add basal medium with or without 5 mM IWP-4 to the cells and exchange every 2 days [use dimethyl sulfoxide (DMSO) at the same concentration as a vehicle control] until day 15; after that, supply basal medium every 2 days[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Astragalus membranaceus (Huangqi) and Rhizoma curcumae (Ezhu) decoction suppresses colorectal cancer via downregulation of Wnt5/β-Catenin signal. Chin Med 2022 Jan 6;17(1):11. PMID: 34991661
5-Demethylnobiletin Ameliorates Isoproterenol-Induced Cardiac Fibrosis and Apoptosis by Repressing the Sirt1/FOXO3a/NF-κB and Wnt/β-Catenin Pathways. Biol Pharm Bull 2024;47(10):1774-1785. PMID: 39477471