TGX-221

TGX-221 is a potent, cell-permeable, and highly selective small molecule inhibitor of the Phosphoinositide 3-kinase (PI3K) catalytic subunit p110β. As an ATP-competitive inhibitor, it exhibits an IC50 of approximately 5-10 nM and demonstrates approximately 1000-fold selectivity for the p110β isoform over p110α. The compound effectively blocks the PI3K/Akt signaling pathway, which is a major driver of cell growth, survival, and tumorigenesis. TGX-221 has been extensively studied in preclinical research for its efficacy in treating PTEN-deficient tumors, including prostate cancer, glioblastoma, and gastric cancer. It has also shown particular promise in clear cell renal cell carcinoma (ccRCC) characterized by VHL and SETD2 mutations. Beyond oncology, TGX-221 has investigated for its anti-thrombotic properties, as it can inhibit platelet aggregation without significantly impacting bleeding time.