HS-173

Description: HS-173 is a novel and potent PI3Kalpha (phosphatidylinositol 3-kinase) inhibitor (IC50 = 0.8 nM) with a potential to be used as an effective therapeutic agent for ameliorating liver fibrosis. HS-173 also has potential anticancer activity by promoting apoptosis and inhibiting angiogenesis. HS-173 blocked the PI3K/Akt signaling pathway in vitro and in vivo. It suppressed fibrotic responses such as cellproliferation and collagen synthesis by blocking PI3K/Akt signaling. HS-173 inhibited the PI3K signaling pathway, and showed anti-proliferative effects on cancer cells. Also, HS-173 induced cell cycle arrest at the G(2)/M phase and apoptosis. In addition, HS-173 decreased the expression HIF-1alpha and VEGF which play an important role in angiogenesis. This effect was confirmed by the suppression of tube formation and migration assay in vitro.

References: Cancer Lett. 2013 Jan 1; 328(1):152-9; Scientific Reports, 2013, 3, 3470.