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PD 169316 is a cell-permeable, potent and selective p38 MAP kinase inhibitor that indirectly activates proteasome activity and has antiviral activity against Enterovirus71 with an IC50 value 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. 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.
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Source | Oncol Lett (2018). Figure 7. PD169316 |
| Method | CCK‑8 assay | |
| Cell Lines | NB4 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h | |
| Results | The results of the CCK‑8 assay showed that PD169316 could partially reverse the growth inhibition induced by lapatinib treatment. |
| Molecular Weight | 360.34 |
| Formula | C20H13FN4O2 |
| CAS Number | 152121-53-4 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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BIRB 796 (Doramapimod) is a protein kinase inhibitor of p38 MAPK with Kd of 100pM. |
| Adezmapimod
Adezmapimod (SB203580) is a P38 MAPK inhibitor with an IC50 of 0.3-0.5 μM, which is 10 times less selective than SAPK3(106T) and SAPK4(106T), and inhibits PKB phosphorylation with an IC50 of 3-5 μM. |
| SB 202190
SB 202190 is a highly selective, potent and cell permeable inhibitor of p38 MAP kinase with IC50 values of 50 and 100 nM inhibiting p38α and p38β, respectively. |
| PH-797804
PH-797804 is a highly selective and potent inhibitor of p38 MAP kinase with IC50 of 26 nM. |
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