Chemical Name: 5-(2,6-Dichlorophenyl)-2-[2,4-difluorophenyl)thio]-6H-pyrimido[1,6-b]pyridazin-6-one
Biological ActivityVX 745 is a highly potent and selective p38α/MAPK14 inhibitor, also inhibits p38β (IC50 values are 10 nM and 220 nM respectively). VX 745 blocks TNFα production in LPS-stimulated HWB in vitro (IC50 = 51-180 nM). Also reduces phosphorylation of p38MAPKα and the downstream target Hsp27, leading to vasodilation, reduces IL-1β levels and amyloid plaques in cortex and hippocampus and lowers CSF tau levels in vivo.
External Portal InformationChemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of VX 745 is reviewed on the chemical probes website.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells.
Bagley et al.
Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
Goldstein et al.
Citations for VX 745
The citations listed below are publications that use Tocris products. Selected citations for VX 745 include:
2 Citations: Showing 1 - 2
Differential effect of p38 and MK2 kinase inhibitors on the inflammatory and toxicity biomarkers in vitro.
Authors: Singh Et al.
Hum Exp Toxicol 2018;37:521
The inflammatory kinase MAP4K4 promotes reactivation of Kaposi's sarcoma herpesvirus and enhances the invasiveness of infected endothelial cells.
Authors: Haas Et al.
PLoS Pathog 2013;9:e1003737
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