HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

INT-777 (S-EMCA) is a potent TGR5 agonist with an EC50 of 0.82 μM. INT-777 (S-EMCA) inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3/cAMP/PKA signaling pathway after subarachnoid hemorrhage in rats.

Cytosporone B (Dothiorelone G) is a naturally occurring agonist for the nuclear receptor Nur77 (IC50 = 0.278 nM). Activation of Nur77 with cytosporone B induces the expression of Nur77-dependent genes, including the gene for Nur77 itself. Signaling through Nur77 induces apoptosis in cancer cells and retards xenograft tumor growth. It also induces genes related to gluconeogenesis and decreases atherosclerosis progression in mice fed a high fat and high cholesterol diet. Cytosporone B is brain penetrant and aggravates early brain injury in rats when given (13 mg/kg intraperitoneally) after experimentally-induced subarachnoid hemorrhage. Cytosporone B also has antibacterial properties.

Tirilazad, a nonglucocorticoid 21-aminosteroid, serves to inhibit lipid peroxidation. It mitigates the effects of trauma-induced brain or spinal cord injury, as well as damage resulting from stroke, ischemia, and reperfusion injury. Additionally, Tirilazad exhibits antiviral properties against nCoV and offers neuroprotection in cases of ischemic stroke. It is also utilized in subarachnoid hemorrhage research [1] [2] [3].

ML351 is a potent and selective inhibitor of human 15-lipoxygenase-1 (15 LOX)(IC50: 200 nM).

Tat-QFNP12 is a peptide that combines a transcriptional transactivator (Tat) transmembrane domain with an inhibitor targeting the interaction between N-Myc downstream regulated gene 2 (NDRG2) and protein phosphatase Mg2+/Mn2+ dependent 1A (PPM1A). This compound effectively mitigates blood-brain barrier endothelial tight junction disruption caused by elevated levels of matrix metalloproteinase-9 (MMP-9), alleviates cerebral edema, and promotes spontaneous activity along with symmetric limb movement in a mouse model of subarachnoid hemorrhage induced by endovascular puncture. These benefits are observed at a dosage of 20 mg/kg.

Methazolamide (CL 8490) is a carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.