HS-1371 is a potent and ATP-competitive receptor-interacting protein kinase 3 (RIP3) inhibitor with an IC50 of 20.8 nM[1].
HS1371 is a potent RIP3 kinase inhibitor with IC50 of 20.8 nM. It binds to the ATP-binding region of RIP3, thereby preventing ATP binding, inhibiting the enzymatic activity of RIP3 in vitro.
HS1371 inhibits autorenal phosphorylation of RIP3 at S227. In HT-29 cells, it has full inhibitory activity on TNF-induced necroptosis signaling and is inactive on the phosphorylation of RIP3 and MLKL. It protects cells from RIP3-dependent necrotic cell death but does not affect apoptotic cell death.
| Target | Value |
RIP3 kinase
() | 20.8 nM |
[1] Park HH, et al. HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis. Exp Mol Med. 2018 Sep 20;50(9):125. DOI:
10.1038/s12276-018-0152-8
