AGN 192403

AGN 192403 (BRD4780) is a potent and selective imidazoline-1 receptor antagonist with a K_i value of 42 nM. AGN 192403 is also a TMED9 inhibitor. AGN 192403 shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 can be used for glioma tumor and neurological diseases research^[1][2]. In Vitro: AGN 192403 (10-100 μM, 24 h) inhibits the former lysosomal destabilization and the subsequent decrease in mitochondrial potential in astrocytes exposed to Naphthazarin (HY-N7526)^[1].
AGN 192403 (10-100 μM, 24 h) inhibits the Antimycin A- and Rotenone (HY-B1756)-induced decrease in mitochondrial potential, cytochrome c release, caspase-9 activation, and eventually LDH release in astrocytes^[1].
AGN 192403 (4-25 μM, 14 days) exerts a remarkable inhibitory effect on glioma stem cells (GSC)s self-renewal, demonstrating almost complete inhibition of self-renewal at the highest concentration applied^[2].
AGN 192403 (0-25 μM, 18-48 h) targets TMED9, reduces the stemness, reduces GSC migration, and inhibits GSC tumorigenic functions^[2].
AGN 192403 (4-25 μM, 0-8 days) induces cell death in a dose dependent manner in patient-derived GSCs^[2].
AGN 192403 (4-25 μM, 48 h-8 days) inhibits TMED9 and exerts anti-tumor effects in diffuse intrinsic pontine glioma (DIPG) cells^[2]. In Vivo: AGN 192403 (3000 μg/kg, i.v., single dose pretreat) can bloack imidazoline-1 receptor without modifying the baseline values of heart rate and blood pressure in rats^[3].