The stress-activated protein kinase (SAPK) p38 isoforms are mitogen-activated protein kinase (MAPK) family members. MAPKs act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development. The well reported isoforms of p38 MAPKs include p38α, p38β and others.
VX-702 is a selective inhibitor of p38α MAPK. VX-702 inhibited the activation of platelet MAPK-activated protein kinase-2, the substrate of p38α MAPK with IC50s ranging from 4 – 20 nM[3]. In an ex vivo blood assay primed with LPS, VX-702 dose-dependently inhibited the production of IL-6, IL-1β and TNFα with IC50s of 59, 122 and 99 ng/ml, respectively [4].
In collagen-induced mouse arthritis model, VX-702 dosed at 0.1 mg/kg twice daily or 5 mg/kg twice daily were of equivalent therapeutic effects to methotrexate or prednisolone at the same doses, as measured by the percentage inhibition of wrist joint erosion and an inflammation score[4]. In a rat model of ischemia-reperfusion injury, VX-702 orally administrated at the doses of 5 or 50 mg/kg dose-dependently reduced the increase of phosphor MK2 in the ischemic zone tissue, and the MI/AAR ratio was significantly reduced in the 50 mg/kg VX-702 treated group[4].
VX-702 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
HOP-62 cell
Growth inhibition assay
Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.01543 μM
SANGER
human A2780 cell
Growth inhibition assay
Inhibition of human A2780 cell growth in a cell viability assay, IC50=21.8225 μM
SANGER
human A388 cell
Growth inhibition assay
Inhibition of human A388 cell growth in a cell viability assay, IC50=7.80384 μM
SANGER
human A4-Fuk cell
Growth inhibition assay
Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=6.43662 μM
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