Necrostatin-34 (Nec-34), a RIPK1 kinase inhibitor, stabilizes RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain.In Vitro: Necrostatin-34 (Nec-34) exhibits IC50 values of 667 nM and 134 nM for TNFα in FADD def-Jurkat cells and L939 cells, respectively.
Necrostatin-34 (Nec-34, 10?μM) inhibits the dimerization-induced RIPK1 activation as examined by phosphorylation of Ser166 (p-S166) of RIPK1, a biomarker for RIPK1 activation.
Necrostatin-34 (Nec-34) may block TNFα-induced complex II formation by inhibiting the activation of RIPK1 kinase.