C101248

C101248 is a first-in-class, selective small-molecule inhibitor of the tandem pore domain halothane-inhibited K+ channel 1 (THIK-1), also known as KCNK13. Identified by Cerevance using their proprietary NETSseq platform, the compound targets THIK-1, a potassium channel primarily expressed in microglia that is upregulated in the brains of patients with Alzheimer's disease. By inhibiting THIK-1, C101248 modulates microglial function, specifically preventing the NLRP3-dependent release of the pro-inflammatory cytokine IL-1β and reducing microglial motility. This mechanism suggests potential therapeutic utility in treating neuroinflammatory conditions, particularly Alzheimer's disease, by mitigating chronic neuroinflammation and its associated neurotoxicity.

Other names

CAS 361368-24-3CAS361368-24-3CAS-361368-24-3