MedChemExpress LLC (MCE)

MedChemExpress - Model AT-533 - 908112-37-8

AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs)[1][2][3].

AT-533

MCE China：AT-533

Brand：MedChemExpress (MCE)

Cat. No.HY-148877

CAS：908112-37-8

Purity：98.86%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

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

In Vitro：AT-533 (0-1350 nM; 24 h or 48 h) inhibits 20 ng/mL VEGF-induced tube formation, cell migration, and invasion of HUVECs[1]. AT-533 (2 μM or 75 μM; 24 h) inhibits the HIF-1α/VEGF signaling pathway in hypoxia-induced breast cancer cells, as well as inhibiting Akt/mTOR/p70S6K, Erk1/2, and FAK phosphorylation[1]. AT-533 (10 nM, 50 nM; 48 h) shows anti-angiogenic ability in chorioallantoic membrane (CAM) model[1]. AT-533 (0.5 μM; 2 h, 4 h) decreases TNF-α, IL-1β and IL-6 production in RAW264.7 and BV2 cells induced by HSV-1[2].

In Vivo：AT-533 (10 mg/kg; i.p.; once daily for 21 d) suppresses the expression of the HIF-1α/VEGF signaling pathway-related proteins in MDA-MB-231 breast cancer xenografts tumor model in mouse[1]. AT-533 (1, 2 and 4 mg/kg; i.p.; once daily for 30 d) has no mortality, loss of appetite and body weight, adverse reactions in Sprague-Dawley rats in subacute toxicity test[3].

IC50 & Target：HSP90 HSV-1 ERK1 ERK2 NF-κB Akt HIF-1α VEGF/VEGFR-2

References：

[1]. Zhang PC, et al. AT-533, a novel Hsp90 inhibitor, inhibits breast cancer growth and HIF-1α/VEGF/VEGFR-2-mediated angiogenesis in vitro and in vivo. Biochem Pharmacol. 2020 Feb;172:113771. [Content Brief]

[2]. Li F, et al. AT-533, a Hsp90 inhibitor, attenuates HSV-1-induced inflammation. Biochem Pharmacol. 2019 Aug;166:82-92. [Content Brief]

[3]. Wu Y, et al. Subacute toxicological evaluation of AT-533 and AT-533 gel in Sprague-Dawley rats. Exp Ther Med. 2021 Jun;21(6):632. [Content Brief]

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