Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H13FN4O2 |
| Molecular Weight | 360.3412 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[O-][N+](=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(F)C=C4
InChI
InChIKey=BGIYKDUASORTBB-UHFFFAOYSA-N
InChI=1S/C20H13FN4O2/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(8-4-15)25(26)27/h1-12H,(H,23,24)
DescriptionCurator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/22913737
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/22913737
PD-169316 is a selective inhibitor of p38 MAPK. It inhibits p38 MAPK with an IC50 of 89 nM. PD169316, inhibits transforming growth factor beta-induced Smad signaling in human ovarian cancer cells. In an amyloid β (Aβ) rat model of Alzheimer's disease it was demonstrated that caspase-3 and Bax/Bcl-2 ratio, two marks of apoptosis, were significantly decreased in the rats pre-treated with PD169316 intracerebroventricularly.This study suggested the potential neuroprotective role of PD 169316 against the neuronal toxicity induced by Aβ.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| MEK and p38MAPK inhibitors potentiate TNF-alpha induced apoptosis in U937 cells. | 2001 Jan-Feb |
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| Tumor promoter arsenite stimulates histone H3 phosphoacetylation of proto-oncogenes c-fos and c-jun chromatin in human diploid fibroblasts. | 2003 Apr 11 |
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| Involvement of p38 mitogen-activated protein kinase in heat shock protein 27 induction in human neutrophils. | 2003 Apr 18 |
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| Rosiglitazone and retinoic acid induce uncoupling protein-1 (UCP-1) in a p38 mitogen-activated protein kinase-dependent manner in fetal primary brown adipocytes. | 2003 Jan 3 |
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| All-trans retinoic acid potentiates Taxotere-induced cell death mediated by Jun N-terminal kinase in breast cancer cells. | 2004 Jan 15 |
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| A p38 inhibitor allows to dissociate differentiation and apoptotic processes triggered upon LIF withdrawal in mouse embryonic stem cells. | 2004 Mar |
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| Role of cell signaling in B[a]P-induced apoptosis: characterization of unspecific effects of cell signaling inhibitors and apoptotic effects of B[a]P metabolites. | 2005 Jan 15 |
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| Calcium-activated RAF/MEK/ERK signaling pathway mediates p53-dependent apoptosis and is abrogated by alpha B-crystallin through inhibition of RAS activation. | 2005 Sep |
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| p38 mitogen-activated protein kinase activity commits embryonic stem cells to either neurogenesis or cardiomyogenesis. | 2006 May |
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| N-(4-hydroxyphenyl)retinamide-induced apoptosis triggered by reactive oxygen species is mediated by activation of MAPKs in head and neck squamous carcinoma cells. | 2006 May 4 |
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| Up-regulation of cyclooxygenase-2 by cobalt chloride-induced hypoxia is mediated by phospholipase D isozymes in human astroglioma cells. | 2007 Dec |
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| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. | 2007 Dec 18 |
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| Dissecting the signaling pathway of nicotine-mediated neuroprotection in a mouse Alzheimer disease model. | 2007 Jan |
|
| The role of p38 MAPK and JNK in Arsenic trioxide-induced mitochondrial cell death in human cervical cancer cells. | 2008 Oct |
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| 15-Deoxy-Delta-Prostaglandin J(2) Upregulates the Expression of LPS-Induced IL-8/CXCL8 mRNA in Vascular Smooth Muscle Cells from Spontaneously Hypertensive Rats. | 2009 Apr |
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| Heparin binding epidermal growth factor-like growth factor and PD169316 prevent apoptosis in mouse embryonic stem cells. | 2009 Feb |
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| Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. | 2011 Oct 30 |
|
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. | 2013 Apr 15 |
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| Quinoline compound KM11073 enhances BMP-2-dependent osteogenic differentiation of C2C12 cells via activation of p38 signaling and exhibits in vivo bone forming activity. | 2015 |
|
| A Role for p38 Mitogen-activated Protein Kinase-mediated Threonine 30-dependent Norepinephrine Transporter Regulation in Cocaine Sensitization and Conditioned Place Preference. | 2015 Apr 24 |
Patents
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GX3Y2V80CV
Created by
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4712
Created by
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DTXSID8042684
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152121-53-4
Created by
admin on Sat Dec 16 08:09:02 GMT 2023 , Edited by admin on Sat Dec 16 08:09:02 GMT 2023
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SUBSTANCE RECORD
