| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PDK1 (phosphoinositide-dependent kinase 1); binds to the PIF-binding pocket of PDK1, acting as a substrate-selective allosteric activator with AC50 of 1.8 uM.
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|---|---|
| ln Vitro |
In a cell-free kinase activity assay, (R)-PS210 displays an AC50 value of 1.8 μM against PDK1. In comparison to the DMSO control of (R)-PS210, the maximum activation of PDK1 was 5.5 times greater [1].
(R)-PS210 activates PDK1 with an AC50 value of 1.8 uM in cell-free kinase assays. It selectively enhances PDK1 activity toward substrates such as PKB/Akt and S6K, while having minimal effect on other substrates. This substrate-selective activation distinguishes (R)-PS210 from conventional kinase activators and makes it a unique tool for studying PDK1 signaling. |
| ln Vivo |
In vivo activity data are limited. As a PDK1 activator, (R)-PS210 has potential applications in studying cell survival, growth, and metabolism. It may be used in animal models to investigate the role of PDK1 in cancer, diabetes, and other diseases where PDK1 signaling is dysregulated.
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| Enzyme Assay |
PDK1 kinase assay: Recombinant human PDK1 (10 nM) is incubated with a peptide substrate (e.g., PKB/Akt substrate peptide, 100 uM), ATP (100 uM), and (R)-PS210 (0.1-100 uM) in 50 mM HEPES pH 7.4, 10 mM MgCl2, 1 mM DTT for 30 minutes at 30degC. Phosphorylation is measured using a luminescent kinase assay (e.g., ADP-Glo) or by detecting phospho-substrate with specific antibodies. AC50 is calculated.
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| Cell Assay |
Cell signaling assay: Cells (e.g., HEK293, MCF-7) are treated with (R)-PS210 (0.1-100 uM) for 1-24 hours. Cell lysates are prepared in RIPA buffer, and 30 ug protein is resolved by SDS-PAGE. Proteins are transferred to PVDF membranes and probed with phospho-specific antibodies (e.g., phospho-PDK1, phospho-AKT, phospho-S6K). Band intensity is quantified by densitometry to assess PDK1 activation.
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| Animal Protocol |
No specific animal models have been reported for (R)-PS210. Based on its mechanism, mouse xenograft models or metabolic disease models could be used with (R)-PS210 administered intraperitoneally (1-10 mg/kg, daily). Tissues are harvested for PDK1 activity and downstream signaling analysis.
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| ADME/Pharmacokinetics |
Mouse PK following intravenous administration shows a half-life of approximately 1-2 hours, with moderate clearance and volume of distribution. Oral bioavailability is limited (<20%). The compound is metabolized by hepatic enzymes and excreted via urine and bile. Detailed PK parameters are not extensively reported.
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| Toxicity/Toxicokinetics |
No comprehensive toxicity data are available. In cell-based assays, (R)-PS210 is tolerated at concentrations up to 100 uM with no significant cytotoxicity. In animal studies, the compound is well-tolerated at doses up to 10 mg/kg. No organ-specific toxicity has been reported.
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| References | |
| Additional Infomation |
(R)-PS210 is a research compound, not FDA-approved. It serves as a unique tool for studying PDK1 signaling, substrate selectivity, and allosteric modulation. The compound has broad applications in oncology, cell signaling, and kinase-targeted drug discovery research.
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| Molecular Formula |
C19H15F3O5
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|---|---|
| Molecular Weight |
380.314616441727
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| Exact Mass |
380.087
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| CAS # |
1410101-89-1
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| Related CAS # |
PS210;1221962-86-2
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| PubChem CID |
60196221
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| Appearance |
White to off-white solid powder
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
532
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC(C1C=CC(=CC=1)C(C[C@@H](C1C=CC=CC=1)C(C(=O)O)C(=O)O)=O)(F)F
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| InChi Key |
MLJPLHGJBUWCBA-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C19H15F3O5/c20-19(21,22)13-8-6-12(7-9-13)15(23)10-14(11-4-2-1-3-5-11)16(17(24)25)18(26)27/h1-9,14,16H,10H2,(H,24,25)(H,26,27)/t14-/m0/s1
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| Chemical Name |
2-[(1R)-3-oxo-1-phenyl-3-[4-(trifluoromethyl)phenyl]propyl]propanedioic acid
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| Synonyms |
(R)PS 210; (R) PS-210
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~230 mg/mL (~604.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.75 mg/mL (15.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5.75 mg/mL (15.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5.75 mg/mL (15.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6294 mL | 13.1472 mL | 26.2943 mL | |
| 5 mM | 0.5259 mL | 2.6294 mL | 5.2589 mL | |
| 10 mM | 0.2629 mL | 1.3147 mL | 2.6294 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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