| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C19H15F3O5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
PS210 is a potent, selective activator of PDK1, with a Kd of 3 μM, targeting the PIF-binding pocket of PDK1. It is inactive against other protein kinases, including PDK1 downstream components such as S6K, PKB/Akt, and GSK3. In cells, its prodrug PS423 acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K[1][2]. It is supplied as a white to off-white solid (C19H15F3O5, MW 380.31) at 98.03% purity.
Physical & Chemical Properties
| CAS Number | 1221962-86-2 |
|---|---|
| Molecular Formula | C19H15F3O5 |
| Molecular Weight | 380.31 g/mol |
| Purity | 98.03% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(C(C(O)=O)C(CC(C1=CC=C(C=C1)C(F)(F)F)=O)C2=CC=CC=C2)O |
| Signaling Pathway | PI3K/Akt/mTOR |
| Solubility | In Vitro: DMSO: 100 mg/mL (262.94 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. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
Kd: 3 μM (PDK1)[2]
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 (262.94 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 | ≥ 2.5 mg/mL (6.57 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 (6.57 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 (6.57 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
PS210 stabilizes PDK1 across the temperature gradient, and under these conditions it stabilizes the residue Arg131, which lies opposite helix a-B at the far end of helix a-C. The residues that form the phosphate-binding site therefore appear to act as a fixed point, permitting relative movement of the helices during PDK1 activation[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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