| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C25H34N8O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSK2334470 is a highly specific and potent inhibitor of PDK1, with an IC50 of 10 nM. It is supplied as a light yellow to yellow solid (C25H34N8O, MW 462.59) at 99.79% purity.
Physical & Chemical Properties
| CAS Number | 1227911-45-6 |
|---|---|
| Molecular Formula | C25H34N8O |
| Molecular Weight | 462.59 g/mol |
| Purity | 99.79% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C([C@@H]1CN(C2=NC(NC)=NC(C3=CC4=C(C=C3)C(N)=NN4)=C2)[C@H](C)CC1)NC5CCCCC5 |
| Signaling Pathway | PI3K/Akt/mTOR |
| Solubility | In Vitro: DMSO: ≥ 50 mg/mL (108.09 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, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 10 nM(PDK1)[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 | ≥ 50 mg/mL (108.09 mM) | 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.
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 (5.40 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. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (5.40 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 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (5.40 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
The small molecule GSK2334470 inhibits PDK1 with an IC50 of ~10 nM, yet at 500-fold higher concentrations it leaves 93 other protein kinases, including 13 AGC-kinases most closely related to PDK1, unsuppressed. GSK2334470 abolishes serum- or IGF-1 (insulin-like growth factor 1)-induced phosphorylation of T-loop residues and the activation of SGK isoforms and S6K1. GSK2334470 and AZD8055 effectively inhibit PDK1 and mTOR phosphorylation, respectively, and also produce a higher G0–G1 ratio in LAN-1-MK than in LAN-1. PDK1 and mTOR inhibitors affect GSK3β phosphorylation in some of the resistant sublines[2].
In Vivo
GSK2334470, a PDK1 inhibitor (PDKi), is tested for efficacy in newborn BrafV600E::Pten / mice given 4-HT systemically. Administering PDK1 inhibitor twice weekly markedly inhibits pigmented lesions and the accompanying melanomagenesis, and significantly inhibits lung metastases, quantified by H&E staining (~80%), and lymph node metastases, assessed by S100 immunostaining, resembling the phenotype seen with genetic ablation of Pdk1[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[2]
Dissolve GSK2334470 in DMSO and dilute with appropriate medium before use. To examine the effect of GSK2334470 on the mTOR-S6K pathway, treat non-resistant cells and resistant sublines with 5 μM GSK2334470 for 1.5 and 12 h in medium containing 10 % FBS, with or without MK-2206 (5 μM)[2].
Animal Administration[3]
Dissolve the compound in DMSO and then dilute with PBS or saline. Generate BrafV600E::Pten−/− mice as previously described. Use cohorts of six animals per group in each experimental group. Administer GSK2334470 by IP injection (100 mg/kg) 3 times per week, starting on the same day as topical 4-hydroxytamoxifen administration and continuing until mouse collection, based on earlier studies[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. Nat Commun 2026 Feb 12;17(1):1214. PMID: 41680175
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. Sci Transl Med 2018 Jul 18;10(450):eaaq1093.
Discovery, delineation, and therapeutic targeting of a hyper-translation pathway driving cytokine release syndrome. Cell Rep Med 2025 Dec 30:102531. PMID: 41475340
A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity. Br J Cancer 2020 Aug;123(4):542-555. PMID: 32439931
Gynostemma Pentaphyllum ameliorates CCl4-induced liver injury via PDK1/Bcl-2 pathway with comprehensive analysis of network pharmacology and transcriptomics. Chin Med 2024 May 15;19(1):70. PMID: 38750545
Deletion of PDK1 in oligodendrocyte lineage cells causes white matter abnormality and myelination defect in the central nervous system. Neurobiol Dis 2021 Jan:148:105212. PMID: 33276084
GSK2334470 attenuates high salt-exacerbated rheumatoid arthritis progression by restoring Th17/Treg homeostasis. iScience 2024 Apr 26;27(6):109798. PMID: 38947509
Cellular stress induces non-canonical activation of the receptor tyrosine kinase EphA2 through the p38-MK2-RSK signaling pathway. J Biol Chem 2023 May;299(5):104699. PMID: 37059179
Axin1 regulates tooth root development by inhibiting AKT1-mTORC1 activation and Shh translation in Hertwig's epithelial root sheath. Development 2024 Nov 1;151(21):dev202899. PMID: 39344774
Non-canonical Activation of RSK1 Induces EphA2-Mediated Cell Migration under Cellular Stress Conditions. Biol Pharm Bull 2025;48(7):1089-1095. PMID: 40721370
