PS-210 |
カタログ番号GC48003
One-Click Copy Product Info
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PS-210 は、Kd が 3 μM の強力で選択的な PDK1 アクチベーターであり、PDK1 の PIF 結合ポケットを標的とします。 PS-210 は、S6K、PKB/Akt、GSK3 などの PDK1 下流シグナル伝達コンポーネントを含む他のプロテインキナーゼに対して不活性です。細胞内では、PS-210 (PS423) のプロドラッグが PDK1 の基質選択的阻害剤として作用し、S6K のリン酸化と活性化を阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1221962-86-2
Sample solution is provided at 25 µL, 10mM.
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PS-210 is an activator of phosphoinositide-dependent protein kinase 1 (PDK1) that increases its thermal stability.1,2 It is selective for PDK-1 over a panel of 120 kinases at 10 µM.1 PS-210 (2 µM) increases the activity of wild-type PDK1 but not PDK1 with a mutation in the PIF-binding pocket.
1.Busschots, K., Lopez-Garcia, L.A., Lammi, C., et al.Substrate-selective inhibition of protein kinase PDK1 by small compounds that bind to the PIF-pocket allosteric docking siteChem. Biol.19(9)1152-1163(2012) 2.Wilhem, A., Lopez-Garcia, L.A., Busschots, K., et al.2-(3-Oxo-1,3-diphenylpropyl)malonic acids as potent allosteric ligands of the PIF pocket of phosphoinositide-dependent kinase-1: Development and prodrug conceptJ. Med. Chem.55(22)9817-9830(2012)
| Cas No. | 1221962-86-2 | SDF | |
| Canonical SMILES | FC(F)(F)C1=CC=C(C(CC(C2=CC=CC=C2)C(C(O)=O)C(O)=O)=O)C=C1 | ||
| Formula | C19H15F3O5 | M.Wt | 380.3 |
| 溶解度 | DMSO: soluble | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6295 mL | 13.1475 mL | 26.295 mL |
| 5 mM | 525.9 μL | 2.6295 mL | 5.259 mL |
| 10 mM | 263 μL | 1.3148 mL | 2.6295 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)