AT-533 is a potent inhibitor of Hsp90 and HSV. AT-533 blocks the HIF-1α/VEGF/VEGFR-2 signaling pathway, leading to suppress tumor growth and angiogenesis. AT-533 also inhibits the activation of the downstream pathways, including Erk1/2, FAK, Akt/mTOR/p70S6K,. AT-533 inhibits the cell migration, invasion, and the tube formation of human umbilical vein endothelial cells (HUVECs).

AT-533 (0-1350 nM; 24h or 48h) inhibits 20ng/mL VEGF induced tube formation, cell migration and HUVEC invasion. AT-533 (2 μ M or 75 μ M; 24 h) inhibits HIF-1 α/ VEGF in hypoxia induced breast cancer cells signaling pathway and inhibits Akt/mTOR/p70S6K, Erk1/2, and FAK phosphorylation. AT-533 (10 nM, 50 nM; 48 h) exhibits anti angiogenic ability on the chorionic villus (CAM) model [1]. AT-533 (0.5 μ M; 2 hours, 4 hours) reduces TNF induced by HSV-1 in RAW264.7 and BV2 cells- α、 IL-1 β and the production of IL-6 [2].

AT-533 (10 mg/kg; intraperitoneal injection; once a day for 21 days) inhibited the expression of HIF-1 α/ VEGF signaling pathway related proteins in mouse MDA-MB-231 xenograft model of breast cancer [1]. AT-533 (1, 2, 4 mg/kg; intraperitoneal injection; once a day for 30 days) did not cause death, appetite loss, weight loss, or adverse reactions in subacute toxicity tests of Sprague Dawley rats [3].