PD 169316

SKU: orb1226155

Description

A potent, selective p38 MAPK inhibitor with IC50 of 89 nM; displays >100-fold selectivity over ERK, PKA, PKCα; prevent p38 phosphorylation while promotes the phosphorylation of the pro-survival SAPK/JNK and ERK.

Key Properties

• CAS Number: 152121-53-4
• MW: 360.3412
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₃FN₄O₂
• SMILES: O=[N+](C1=CC=C(C2=NC(C3=CC=NC=C3)=C(C4=CC=C(F)C=C4)N2)C=C1)[O-]
• Target: p38 MAPK
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  PD169316 (1 mg/kg, intramuscular injection every day for 14 consecutive days) shows antiviral activity in a suckling mouse model. Animal model: EV71-challenged suckling mouse model (7-day-old Kunming mice). Dosage: 1 mg/kg. Administration: Intramuscular injection every day for 14 consecutive days. Result: Showed antiviral activity.
• 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. 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. 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. 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. Western blot analysis. Cell line: Ishikawa PRB or PRA cells. Concentration: 10 μM. Incubation time: 30 min. Result: Did not inhibit MEKK1-induced p38 phosphorylation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PD169316 | PD-169316

Quick Database Links

Gene Symbol

p38 MAPK