15854-08-7

aPKC-IN-2 is a small molecule inhibitor that inhibits aPKC activity. aPKC-IN-2 can effectively block vascular endothelial permeability in cell culture and in vivo experiments. aPKC-IN-2 shows biological activity in interfering with NFκB-driven gene transcription and is associated with inflammatory responses. aPKC-IN-2 has a significant inhibitory effect on vascular endothelial permeability induced by VEGF and TNF, and its EC50 value is in the low nanomolar range. The structural characteristics of aPKC-IN-2 reveal key elements of its inhibitory activity, providing the possibility for further development of small molecule aPKC inhibitors[1].

[1] Synthesis and structure-activity relationships of 2-amino-3-carboxy-4-phenylthiophenes as novel atypical protein kinase C inhibitors