TGX-221

TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment. IC50 & Target: IC50: 8.5 nM (p110β), 211 nM (p110δ)^[5] In Vitro: TGX-221, BL05 and BL05-HA show selective cytotoxicity to LNCaP cells, which may be due to the deficiency of PTEN in this cell line and the accumulation of PIP3 in the cells^[1]. TGX-221 (1 μM) does not affect the expression and phosphorylation of AMPK in C2C12 myoblasts^[2]. TGX221 (0.1, 1, 10 µM) induces IL-6 release from ASM cells^[2]. TGX-221 does not affect neurotensin-stimulated Akt phosphorylation when used alone, but it further suppresses neurotensin-stimulated phosphorylation of Akt when combined with gefitinib. TGX-221 abolishes the neurotensin-stimulated phosphorylation of Akt in Panc-1 cells^[3]. In Vivo: TGX-221 (TGX221, 2.5 mg/kg i.v.) abolishes cyclic flow reductions in a Folts-like carotid artery stenosis preparation of thrombosis, without changing bleeding time, heart rate, blood pressure or carotid vascular conductance^[4].