PD169316, a p38 MAPK inhibitor. When at 5 μM or higher,it can block TGFβ signaling activity and thus caution must be used when attributing cellular activities exclusively to p38 MAPK signaling when these inhibitors are used experimentally. PD169316 attenuated apoptosis in potassium-deprived cells in a dose dependent manner significantly . PD169316 rescued the inhibitory effect of sphingosine on the formation of inositol phosphates by PGF(2alpha) or NaF in osteoblast-like MC3T3-E1 cells.
|Source||Oncol Lett (2018). Figure 7. PD169316|
|Cell Lines||NB4 cells|
|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.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 10 mg/mL|
The p38 MAPK inhibitor, PD169316, inhibits transforming growth factor beta-induced Smad signaling in human ovarian cancer cells.
Fu Y, et al. Biochem Biophys Res Commun. 2003 Oct 17;310(2):391-7. PMID: 14521923.
Inhibition of p38 kinase mimics survival signal-linked protection against apoptosis in rat cerebellar granule neurons.
Nath R, et al. Cell Mol Biol Lett. 2001;6(2):173-84. PMID: 11544639.
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SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.
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