PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC50 of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.
Para uso exclusivo en investigación. No vendemos a pacientes.
PD 169316 Estructura química
No. CAS : 152121-53-4
This product is a controlled substance and not for sale in your territory.
Based on 17 publication(s) in Google Scholar
PD 169316 purchased from MedChemExpress. Usage Cited in:
Oncol Lett. 2018 Jan;15(1):235-242.
[Abstract]
Cells are treated with 15 and 20 μM Lapatinib for 24 h, the expression of p AKT, AKT, p p38 MAPK, p38 MAPK, p JNK, and JNK are measured by western blotting. Quantification analysis of western blotting, β actin is served as a control. D: 1 DMSO; 2 PD169316; 3 15 μM Lapatinib; 4 PD169316+15 μM Lapatinib).
Western blot analysis evaluated p-p38, p38, LC3 and quantification of LC3-II in untreated (control), treated with the p38 inhibitor PD169316, cisplatin, and both these agents in MDA-MB-231 cells.
PD 169316 purchased from MedChemExpress. Usage Cited in:
Int J Med Sci. 2016 Jul 18;13(8):611-9.
[Abstract]
PD169316 (10 μM) inhibits the effects of all-trans retinoic acid(ATRA) on nuclear localization signal retinoic acid receptor alpha (NLS-RARα)-overexpressed NB4 cells incluing an increase of the expressions of p-p38α, C/EBPβ and CD11b.
The protein levels of Bax and Bcl-2 detected by Western blot. PD169316 decreases EGCG-mediated increases in Bax protein expression.
Powered by Bioz
See more details on Bioz
Ver todos los productos específicos de isoformas p38 MAPK:
Ver todas las isoformas
p38 MAPK p38α p38β MAPK13 p38δ p38γ
Descripciòn
PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC50 of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.
IC50 & Target
IC50: 89 nM (p38 MAPK)[5]
In Vitro
PD169316 (10 μM) inhibits TGFβ and Activin A, but not BMP4 signaling in CaOV3 cells. PD169316 (0.2-20 μM) inhibits TGFβ-induced Smad2 nuclear translocation, Smad7 mRNA induction, and reporter gene activity in CaOV3 cells[1]. PD169316 (10 μM) shows a significantly increased rate of proliferation in Nestin knockdown cells, and can rescue the effect of Nestin knockdown on cell viability in the absence of EGF[2]. PD169316 significantly inhibits p38 MAP kinase activity with no significant change in ERK activity in PC12 cells. PD169316 (10 μM) blocks apoptosis induced by trophic factor withdrawal in differentiated PC12 cells[3].PD169316 (10 μM, 30 min) selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. Increased phospho p-38 levels in the presence of PD169316 are most likely due to blockade of negative feedback loop of dephosphorylation of p38 MAPK by MAPK phosphatases[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PD 169316 Related Antibodies
Western Blot Analysis[1]
Cell Line:
Ishikawa PRB or PRA cells.
Concentration:
10 μM.
Incubation Time:
30 min.
Result:
Did not inhibit MEKK1-induced p38 phosphorylation.
In Vivo
PD169316 (1 mg/kg, intramuscular injection every day for 14 consecutive days) shows antiviral activity in a suckling mouse model[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
EV71-challenged suckling mouse model (7-day-old Kunming mice)[5].
Dosage:
1 mg/kg.
Administration:
Intramuscular injection every day for 14 consecutive days.
Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
2 years
-20°C
1 year
Solvente y solubilidad
In Vitro:
DMSO : 12.5 mg/mL (34.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.7752 mL
13.8758 mL
27.7516 mL
5 mM
0.5550 mL
2.7752 mL
5.5503 mL
10 mM
0.2775 mL
1.3876 mL
2.7752 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.25 mg/mL (3.47 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (12.5 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.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.25 mg/mL (3.47 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (12.5 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.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (12.5 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. 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.
Protocol 1
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (13.88 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
[1]. Fu Y, et al. The p38 MAPK inhibitor, PD169316, inhibits transforming growth factor beta-induced Smad signaling in human ovarian cancer cells. Biochem Biophys Res Commun. 2003 Oct 17;310(2):391-7.
[Content Brief]
[2]. Hu W, et al. Suppression of Nestin reveals a critical role for p38-EGFR pathway in neural progenitor cell proliferation. Oncotarget. 2016 Dec 27;7(52):87052-87063.
[Content Brief]
[3]. Kummer JL, et al. Apoptosis induced by withdrawal of trophic factors is mediated by p38 mitogen-activated protein kinase. J Biol Chem. 1997 Aug 15;272(33):20490-4.
[Content Brief]
[4]. Khan JA, et al. p38 and p42/44 MAPKs differentially regulate progesterone receptor A and B isoform stabilization. Mol Endocrinol. 2011 Oct;25(10):1710-24.
[Content Brief]
[5]. Zhang Z, et al. PD169316, a specific p38 inhibitor, shows antiviral activity against Enterovirus71. Virology. 2017 Aug;508:150-158.
[Content Brief]
[1]. Fu Y, et al. The p38 MAPK inhibitor, PD169316, inhibits transforming growth factor beta-induced Smad signaling in human ovarian cancer cells. Biochem Biophys Res Commun. 2003 Oct 17;310(2):391-7.
[2]. Hu W, et al. Suppression of Nestin reveals a critical role for p38-EGFR pathway in neural progenitor cell proliferation. Oncotarget. 2016 Dec 27;7(52):87052-87063.
[3]. Kummer JL, et al. Apoptosis induced by withdrawal of trophic factors is mediated by p38 mitogen-activated protein kinase. J Biol Chem. 1997 Aug 15;272(33):20490-4.
[4]. Khan JA, et al. p38 and p42/44 MAPKs differentially regulate progesterone receptor A and B isoform stabilization. Mol Endocrinol. 2011 Oct;25(10):1710-24.
[5]. Zhang Z, et al. PD169316, a specific p38 inhibitor, shows antiviral activity against Enterovirus71. Virology. 2017 Aug;508:150-158.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
2.7752 mL
13.8758 mL
27.7516 mL
69.3789 mL
5 mM
0.5550 mL
2.7752 mL
5.5503 mL
13.8758 mL
10 mM
0.2775 mL
1.3876 mL
2.7752 mL
6.9379 mL
15 mM
0.1850 mL
0.9251 mL
1.8501 mL
4.6253 mL
20 mM
0.1388 mL
0.6938 mL
1.3876 mL
3.4689 mL
25 mM
0.1110 mL
0.5550 mL
1.1101 mL
2.7752 mL
30 mM
0.0925 mL
0.4625 mL
0.9251 mL
2.3126 mL
PD 169316 Related Classifications
MAPK/ERK PathwayAutophagyAnti-infection
p38 MAPKAutophagyEnterovirus
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.