Sulfisoxazole

Sulfisoxazole (Sulfafurazole) is an orally active endothelin receptor antagonist with IC₅₀ values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A^[1][2]. In Vitro:Sulfisoxazole (0-100 μM) inhibits the secretion of sEV in three representative human breast cell lines: MCF10A (normal), MCF7 (weakly invasive), and MDA-MB231 (highly invasive)^[2].
Sulfisoxazole (200 μM, 48 h) together with αPD‐L1 recovers the activity of CD8+ cytotoxic T cells by inhibiting secretion of cancer cell (MDA-MB-231) exosomal PD‐L1^[3].
Sulfisoxazole (100 μM, 72 h) inhibits the LPS induced elevation of nitric oxide and the reduction in GABA-containing neurones in a primary rat retinal culture^[4].
In Vivo:Sulfisoxazole (p.o., 200 mg/kg, 14 days) inhibits tumor growth in mouse 4T1 breast cancer xenografts and female nude mice orthotopically implanted with MDA-MB231 cells^[2].
Sulfisoxazole (p.o., 200 mg/kg) together with αPD‐L1 (5 mg/kg, i.p.) reduces the tumor growth rate in CT26 tumor‐bearing mice, and boosts the antitumor effect of αPD‐1^[3].
Sulfisoxazole (5 μL of 400 μM, injected into the vitreous humour of the ischemic eye) shows neuroprotection effect to the retina of rats with ischemia/reperfusion^[4].