| Field | Specification |
|---|---|
| Alternative names | GW108X |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H11Cl2NO4 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GW406108X, also known as GW108X, is a specific inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in ATPase assays. It is also a potent autophagy inhibitor that shows ATP-competitive inhibition of ULK1, with a pIC50 of 6.37 (427 nM); it suppresses ULK1 kinase activity and blocks autophagic flux without affecting the upstream signaling kinases mTORC1 and AMPK[1][2]. It is supplied as a light yellow to yellow solid (C20H11Cl2NO4, MW 400.21) at 98.0% purity.
Physical & Chemical Properties
| CAS Number | 1644443-92-4 |
|---|---|
| Molecular Formula | C20H11Cl2NO4 |
| Molecular Weight | 400.21 g/mol |
| Purity | 98.0% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C1NC2=C(C=C(C(C3=CC=CO3)=O)C=C2)/C1=C/C4=CC(Cl)=C(O)C(Cl)=C4 |
| Signaling Pathway | Cytoskeleton; Cell Cycle/DNA Damage; Autophagy |
| Solubility | In Vitro: DMSO: 50 mg/mL (124.93 mM; Requires sonication; 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, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
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 | 50 mg/mL (124.93 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); 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 | 2.08 mg/mL (5.20 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.08 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (20.8 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
GW406108X acts on ULK1 and autophagy without affecting mTOR or AMPK activity, as monitored by ULK1 pS758 (mTOR site) and pS556 (AMPK site) levels. VPS34 and AMPK are inhibited by GW406108X with pIC50 values of 6.34 (457 nM) and 6.38 (417 nM), respectively. With 5 μΜ GW406108X present, the starvation-induced rise in ATG13 phosphorylation is significantly reduced[1]. Kif15-N420 ATPase activity is inhibited by 76% with GW406108X[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Deficiency of Kif15 gene inhibits tumor growth due to host CD8+T lymphocytes increase. Biochem Biophys Res Commun 2023 May 7:655:110-117. PMID: 36934586
