| Field | Specification |
|---|---|
| Target | |
| Alternative names | AR 0133418; GSK 3β inhibitor VIII; AR 014418 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C12H12N4O4S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
AR-A014418, also known as AR 0133418, GSK 3β inhibitor VIII and AR 014418, is a potent, selective, ATP-competitive inhibitor of GSK-3β, with an IC50 of 104 nM and a Ki of 38 nM[1]. It is supplied as a light yellow to yellow solid (C12H12N4O4S, MW 308.31) at 99.21% purity.
Physical & Chemical Properties
| CAS Number | 487021-52-3 |
|---|---|
| Molecular Formula | C12H12N4O4S |
| Molecular Weight | 308.31 g/mol |
| Purity | 99.21% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C(NCC1=CC=C(OC)C=C1)NC2=NC=C([N+]([O-])=O)S2 |
| Target | GSK-3β |
| Signaling Pathway | PI3K/Akt/mTOR; Stem Cell/Wnt |
| Solubility | In Vitro: DMSO: ≥ 100 mg/mL (324.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 1 year; -20°C, 6 months. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
GSK-3β 104 nM (IC50) |
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 | ≥ 100 mg/mL (324.35 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 1 year) or -20°C (up to 6 months); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (8.11 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Data provided by the manufacturer.
In Vitro
In 3T3 fibroblasts expressing human four-repeat tau protein, AR-A014418 blocks tau phosphorylation at the GSK3-specific site (Ser-396; IC50 2.7 μM), and shields cultured N2A cells from death caused by PI3K/PKB pathway blockage. AR-A014418 also inhibits neurodegeneration mediated by beta-amyloid peptide in hippocampal slices[1]. In NGP and SH-5Y-SY cells, AR-A014418 lowers neuroendocrine markers and suppresses neuroblastoma cell growth[2].
In Vivo
In an ALS mouse model carrying the G93A mutant human SOD1, AR-A014418 (0-4 mg/kg, i.p.) delays symptom onset, enhances motor activity, blocks disease progression, and postpones the disease endpoint[3]. AR-A014418 suppresses acetic acid- and formalin-induced nociception in mice, by acting on NMDA and metabotropic receptor signaling, along with TNF-α and IL-1β transmission in the spinal cord[4].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Measure cell viability through uptake of calcein/propidium iodide. Calcein AM enters living cells and is cleaved there by esterases, yielding yellowish-green fluorescence, whereas PI enters only dead cells, which become orange-red fluorescent. Culture N2A cells for 2 days in vitro, then treat with 50 μM LY-294002 together with AR-A014418 or vehicle (DMSO) for 24 h. Next, incubate N2A cells for 30 min with 2 μM PI and 1 μM calcein-AM. Rinse the cultures three times in Hanks' buffered saline solution that contains 2 mM CaCl2, and visualize cells by fluorescence microscopy on a Zeiss Axiovert 135 microscope. Analyze three fields (selected at random) per well (appr 300 cells/field) in at least three different experiments. Express cell death as the percentage of PI-positive cells out of the total cell number. In every experiment, obtain specific cell death by subtracting the number of dead cells in vehicle-treated cultures.
Animal Administration[3]
First, to examine the effects of GSK-3 inhibition on clinical symptoms, life span, and motor behavior function in ALS, divide 56 Tg mice into four groups. In each group, mix 0.5 mL of normal saline with AR-A014418 per gram of mouse (control group, 0 μg; group A, 1 μg; group B, 2 μg; group C, 4 μg), and inject intraperitoneally into 14 animals per group, 5 days a week, beginning 60 days after birth. Sacrifice the mice at the endpoint described below.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Prolonged inhibition of class I PI3K promotes liver cancer stem cell expansion by augmenting SGK3/GSK-3β/β-catenin signalling. J Exp Clin Cancer Res 2018 Jun 25;37(1):122.
Endogenous Coriobacteriaceae enriched by a high-fat diet promotes colorectal tumorigenesis through the CPT1A-ERK axis. NPJ Biofilms Microbiomes 2024 Jan 20;10(1):5. PMID: 38245554
The kava chalcone flavokawain B exerts inhibitory activity and synergizes with BCL-2 inhibition in malignant B-cell lymphoma. Phytomedicine 2023 Nov:120:155074. PMID: 37716033
NL101 synergizes with the BCL-2 inhibitor venetoclax through PI3K-dependent suppression of c-Myc in acute myeloid leukaemia. J Transl Med 2024 Sep 27;22(1):867. PMID: 39334157
GSK3β-driven SOX2 overexpression is a targetable vulnerability in esophageal squamous cell carcinoma. Oncogene 2023 Jul;42(30):2297-2314. PMID: 37349645
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. Cell Syst 2018 Apr 25;6(4):424-443.e7.
Engineered Alzheimer Organoids Validate the Link Between Intracellular and Soluble p-Tau Biomarkers and Highlight the Contribution of Astrocytic Tau. Neurosci Bull 2026 Apr 11. PMID: 41964788
Food Biosci. 2026 Apr 17;80:108946.
Licochalcone A induces mitochondria-dependent apoptosis and interacts with venetoclax in acute myeloid leukemia. Eur J Pharmacol 2024 Apr 5:968:176418. PMID: 38350590
Platycodin D induces apoptotic cell death through PI3K/AKT and MAPK/ERK pathways and synergizes with venetoclax in acute myeloid leukemia. Eur J Pharmacol 2023 Oct 5:956:175957. PMID: 37541375
