PS48
Based on 5 publication(s) in Google Scholar
PS48 is an activator of PDK1 with an AC50 of 8 μM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.71%
- No. CAS: 1180676-32-7
- Fòrmula: C17H15ClO2
- Peso molecular:286.75
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) PS48
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Customer Validation & Images
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WB
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RT-PCR
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
Actividad biológica
AC50: 8 μM (PDK1)[1]
PDK1 activator, PS48, has the ability to reverse the cell proliferation inhibition role of Triptolide (HY-32735) in vitro. The inhibition role of Triptolide in cell number is significantly reversed by PS48. Triptolide significantly increases the cell proportion in G0-G1 phase and decreases the cell proportion in G2-M and S phase. However, the effect of Triptolide on cell cycle distribution is all reversed by PS48. In addition, suppression of PDK1/Akt/mTOR pathway by Triptolide in high glucose (HG)-treated human renal mesangial cells (HRMCs) is also reversed by PS48, as well as the expression of Ki-67 and proliferating cell nuclear antigen (PCNA)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1180676-32-7
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Appearance Solid
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Peso molecular 286.75
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Fòrmula C17H15ClO2
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Color White to off-white
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SMILES
O=C(O)/C=C(C1=CC=CC=C1)/CCC2=CC=C(Cl)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Redox Biol
Silencing COX-2 blocks PDK1/TRAF4-induced AKT activation to inhibit fibrogenesis during skeletal muscle atrophy. [Abstract]2021 Jan;38:101774. PMID: 33152664 -
Int J Biol Sci
Triptolide Suppresses Glomerular Mesangial Cell Proliferation in Diabetic Nephropathy Is Associated with Inhibition of PDK1/Akt/mTOR Pathway. [Abstract]2017 Sep 21;13(10):1266-1275. PMID: 29104493
PS48 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2017 Sep 21;13(10):1266-1275. [Abstract]
Suppression of PDK1/Akt/mTOR pathway by TP in HG-treated HRMCs was also reversed by PS48.
PS48 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2017 Sep 21;13(10):1266-1275. [Abstract]
PS48 (5 μM; 24, 48, 72 h) significantly reversed the inhibitory role of TP (10 ug/L) in cell number in Human renal mesangial cells (HRMCs).
PS48 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2017 Sep 21;13(10):1266-1275. [Abstract]
PS48 (5 μM; 72 h) significantly reversed the effect of TP (10 ug/L) on cell cycle distribution in Human renal mesangial cells (HRMCs). TP significantly increased the cell proportion in G0-G1 phase and decreased the cell proportion in G2-M and S phase.
PS48 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2017 Sep 21;13(10):1266-1275. [Abstract]
PS48 (5 μM; 72 h) significantly reversed the effect of TP (10 ug/L) induced the protein Ki-67 and PCNA expression in Human renal mesangial cells (HRMCs).
PS48 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2017 Sep 21;13(10):1266-1275. [Abstract]
PS48 (5 μM; 72 h) significantly reversed the effect of TP (10 μg/L) induced the protein Ki-67 and PCNA expression in Human renal mesangial cells (HRMCs).
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Stem Cell Res Ther
Characterisation of extraembryonic endoderm-like cells from mouse embryonic fibroblasts induced using chemicals alone. [Abstract]2020 Apr 16;11(1):157. PMID: 32299508 -
Virol Sin
2021 Dec;36(6):1532-1542. PMID: 34519916
PS48 purchased from MedChemExpress. Usage Cited in: Virol Sin. 2021 Dec;36(6):1532-1542. [Abstract]
PS48 (5, 10 mM; 24 h) increased the protein expression of NP in A549 cells were infected with H1N1 at an MOI of 1.
PS48 purchased from MedChemExpress. Usage Cited in: Virol Sin. 2021 Dec;36(6):1532-1542. [Abstract]
PS48 (5, 10 mM; 24 h) increased viral RNA in A549 cells were infected with H1N1 at an MOI of 1.
PS48 purchased from MedChemExpress. Usage Cited in: Virol Sin. 2021 Dec;36(6):1532-1542. [Abstract]
PS48 (10 mM; 24 h) aggravated H1N1 induced cell injury in A549 cells were infected with H1N1 at an MOI of 1.
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Reprod Domest Anim
PS48 promotes in vitro maturation and developmental competence of porcine oocytes through activating PI3K/Akt signalling pathway. [Abstract]2020 Dec;55(12):1678-1687. PMID: 32946622
Solvente y solubilidad
DMSO : 100 mg/mL (348.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
PDK1 activity tests are performed using T308tide as a substrate for PDK1. In brief, PDK1 activity assay is performed at room temperature (22°C) in a 20 μL mix containing 50 mM Tris pH 7.5, 0.05 mg/mL BSA, 0.1% β-mercaptoethanol, 10 mM MgCl2, 100 μM [γ32P]ATP (5-50 cpm/pmol) , 0.003% Brij, 150-500 ng PDK1, and T308tide (from 0.1 to 1 mM). When appropriate, the PDK1 activity assay is performed in a 96 well format and 4 μL aliquots spotted on p81 phosphocellulose papers using ep motion 5070, washed in 0.01% phosphoric acid, dried, and then exposed and analysed using PhosphoImager technology. Activity measurements are performed in duplicates or triplicates with less than 10% difference between replicates. Experiments are repeated at least twice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Human renal mesangial cells (HRMCs) are cultured with 1640 media, containing 10% fetal bovin serum at 37 °C in 5% CO2. Cells are cultured with D-glucose at normal (5.5 mM) or high (25 mM) concentrations in serum-free medium. D-Mannitol (25 mM) is used for a control of osmolality. TP is reconstituted in 0.01% DMSO and freshly diluted with culture medium to 10 ug/L before using. To determine the specific role of PDK1 in TP-potentiated anti-proliferation, 5 μM PS48 (MedChem Express, USA) is applied following the treatment of TP. MTT assay is used to detect cell proliferation. HRMCs are seeded at a density of 1x105/mL into 96-well plates. After 12, 24, 48 and 72 h incubation with different compounds, 20 uL MTT (5 mg/mL) is added to each well. Cells are then cultured for an additional 2 h and subsequently lysed using DMSO (150 uL/well). When the formazan crystals completely dissolve, the optical density (OD) is measured at 570 nm. The arithmetic mean OD of six wells for each group is calculated[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hindie V, et al. Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1. Nat Chem Biol. 2009 Oct;5(10):758-64. [Content Brief]
[2]. Han F, et al. Triptolide Suppresses Glomerular Mesangial Cell Proliferation in Diabetic Nephropathy Is Associated with Inhibition of PDK1/Akt/mTOR Pathway. Int J Biol Sci. 2017 Sep 21;13(10):1266-1275. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4874 mL | 17.4368 mL | 34.8736 mL | 87.1840 mL |
| 5 mM | 0.6975 mL | 3.4874 mL | 6.9747 mL | 17.4368 mL | |
| 10 mM | 0.3487 mL | 1.7437 mL | 3.4874 mL | 8.7184 mL | |
| 15 mM | 0.2325 mL | 1.1625 mL | 2.3249 mL | 5.8123 mL | |
| 20 mM | 0.1744 mL | 0.8718 mL | 1.7437 mL | 4.3592 mL | |
| 25 mM | 0.1395 mL | 0.6975 mL | 1.3949 mL | 3.4874 mL | |
| 30 mM | 0.1162 mL | 0.5812 mL | 1.1625 mL | 2.9061 mL | |
| 40 mM | 0.0872 mL | 0.4359 mL | 0.8718 mL | 2.1796 mL | |
| 50 mM | 0.0697 mL | 0.3487 mL | 0.6975 mL | 1.7437 mL | |
| 60 mM | 0.0581 mL | 0.2906 mL | 0.5812 mL | 1.4531 mL | |
| 80 mM | 0.0436 mL | 0.2180 mL | 0.4359 mL | 1.0898 mL | |
| 100 mM | 0.0349 mL | 0.1744 mL | 0.3487 mL | 0.8718 mL |
PS48 Related Classifications
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