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.
|Related p38 MAPK Products|
Dilmapimod (also known as SB-681323 and GW-681323) is a p38 MAPK inhibitor that potentially suppresses inflammation in COPD.
Pamapimod is a novel p38 mitogen-activated protein kinase inhibitor, inhibited p38alpha and p38beta enzymatic activity, with IC50 values of 0.014 +/- 0.002 and 0.48 +/- 0.04 microM, respectively.
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.
SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po). IC50 value: 170 nM Target: p38MAPK
SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes.
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