H151 - STING inhibitor

STING inhibitor

H-151 is a potent, irreversible, and selective small-molecule inhibitor of STING [1], a key sensor of cytosolic nucleic acids STING is a transmembrane protein found in the endoplasmic reticulum. Upon activation, it functions as a signaling hub, orchestrating immune responses to pathogenic, tumoral, or self-DNA detected in the cytoplasm[2].

Mode of action:

H-151 exerts its inhibitory action by covalently binding to STING at the transmembrane cysteine residue at position 91. This synthetic indole-derivative blocks STING palmitoylation and clustering, two essential steps for STING signaling. In models of autoinflammatory disease, H-151 blocks STING‑induced expression of pro-inflammatory cytokines and reduces inflammation [1].

Key features:

• H-151 potently inhibits both human and murine STING, in vitro and in vivo (mouse models)
• H-151 strongly reduces STING-mediated but not RIG-I-mediated Interferon-β production
• H-151 blocks the activity of all STING variants tested
• InvitroFit™ grade: each lot is highly pure (≥95%) and functionally tested

Read our review: Follow the path to STING

References:

1. Haag S.M. et al., 2018. Targeting STING with covalent small-molecule inhibitors. Nature 559:269-73.
2. Ishikawa H. & Barber G.N. 2008. STING is an endoplasmic reticulum adaptor that facilitates innate immune signalling. Nature 455:674-8.