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.
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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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related p38 MAPK Products |
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HWY336 is a selective, non-ATP competitive dual MKK4 and MKK7 inhibitor with IC50 values of 6 µM on MKK4 and 10 µM on MKK7 in vitro. HWY336 inhibits the phosphorylation of MKK4/MKK7 inside the activation loop or hinders the substrate to access the kinase. |
| BSJ-04-122
BSJ-04-122 is a covalent MKK4/7 dual inhibitor. BSJ-04-122 inhibits MKK4 and MKK7 with IC50 values of 4 nM and 181 nM, respectively. |
| OVA-E1 peptide TFA
OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). |
| MBP MAPK Substrate
MBP MAPK Substrate is used as an exogenous substrate for MAPK. |
| OVA-E1 peptide
OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). |
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