| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
| Targets |
p38 MAPK (IC50 = 89 nM); TGF-β; Activin A; Enterovirus71
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| ln Vitro |
PD169316 (10 μM) inhibits TGFβ and Activin A signaling but not BMP4 signaling in CaOV3 cells. In CaOV3 cells, PD169316 (0.2–20 μM) inhibits TGFβ-induced Smad2 nuclear translocation, Smad7 mRNA induction, and reporter gene activity[1]. In Nestin knockdown cells, PD169316 (10 μM) exhibits a noticeably higher rate of proliferation, and it can reverse the effect of Nestin knockdown on cell viability in the absence of EGF[2]. In PC12 cells, PD169316 significantly reduces p38 MAP kinase activity while having no effect on ERK activity. In differentiated PC12 cells, PD169316 (10 μM) inhibits the apoptosis that is brought on by the removal of trophic factors[3]. Without preventing upstream kinases from phosphorylating p38, PD169316 (10 μM, 30 min) selectively inhibits the kinase activity of the phosphorylated p38. Increased phospho p-38 levels in the presence of PD169316 are most likely caused by MAPK phosphatases blocking the negative feedback loop of p38 MAPK dephosphorylation[4].
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| ln Vivo |
PD169316 PD169316 (1 mg/kg, intramuscular injection every day for 14 days straight) exhibits antiviral activity in a suckling mouse model[5].
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| Enzyme Assay |
The cells are incubated in the absence or presence of insulin (50 ng/mL) for 15 min at 37°C sixteen hours after the removal of serum from Rat-1 fibroblasts or NGF from differentiated PC12 cells. The cells are then solubilized in 400 μL of ice-cold immunoprecipitation buffer, which contains 10 mM Tris, pH 7.4, 1% Triton X-100, 0.5% Nonidet P-40, 150 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.2 mM sodium orthovanadate, and 0.2 mM phenylmethylsulfonyl fluoride. The cell lysates are centrifuged to remove insoluble material, and 200 g of the supernatant protein (400 μL, total volume) is incubated with 1 μg of anti-p38 antibodies for 1 h at 4°C before being incubated with 30 μL of Protein G Plus/Protein A-agarose for an additional hour. The immunocomplexes are pelleted, washed three times in immunoprecipitation buffer, and then once in kinase ish buffer (50 mM β-glycerolphosphate, 1 mM EGTA, 20 mM MgCl2, and 100 μM sodium orthovanadate). The protein kinase assay is initiated by the addition of 20 μL of 2× reaction buffer (50 mMβ-glycerolphosphate, 1 mM EGTA, 20 mM MgCl2, 100 μM sodium orthovanadate, 0.1 mg/mL ATF-2 (N-terminal half), 50 μg/mL IP20, a peptide inhibitor of c-AMP dependent protein kinase, 200 μM ATP, and 0.9 mCi/mL [32P]ATP) to 20 μL of immune complex. The reaction is allowed to run for 10 minutes at 30 degrees Celsius before being stopped by adding 2× LaemmLi sample buffer. This reaction is then examined using 12% acrylamide gels and SDS-polyacrylamide gel electrophoresis. The gels are dried and then put through phosphoimaging after electrophoresis.
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| Cell Assay |
KBU cells are subjected to 12 ppm G. pps either alone or in combination with 1 hour of pre-exposure to the P38 inhibitor PD169316, and their proliferation (MTT), apoptosis (Ann V), and changes in the degree of protein modifications in the SAPK/JNK and P38 signaling pathways are assessed.
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| Animal Protocol |
EV71-challenged suckling mouse model (7-day-old Kunming mice)[5].
1 mg/kg. Intramuscular injection every day for 14 consecutive days. |
| References |
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| Molecular Formula |
C20H13FN4O2
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|---|---|---|
| Molecular Weight |
360.34
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| Exact Mass |
360.1023
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| Elemental Analysis |
C, 66.66; H, 3.64; F, 5.27; N, 15.55; O, 8.88
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| CAS # |
152121-53-4
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| Related CAS # |
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| Appearance |
white solid powder
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| SMILES |
C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)[N+](=O)[O-]
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| InChi Key |
BGIYKDUASORTBB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H13FN4O2/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(8-4-15)25(26)27/h1-12H,(H,23,24)
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| Chemical Name |
4-[4-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine
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| Synonyms |
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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 |
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| 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: ~14 mg/mL ( ~38.6 mM)
Water: Insoluble Ethanol: Insoluble |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (3.47 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: 1.25 mg/mL (3.47 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: ≥ 1.25 mg/mL (3.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%DMSO+40%PEG300+5%Tween 80+ 50%ddH2O: 0.7mg/ml (1.94mM) Solubility in Formulation 5: 5 mg/mL (13.88 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 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 |
*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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