908112-37-8

908112-37-8 structure

Name: AT-533
Chemical Name: AT-533
CAS Number: 908112-37-8
Molecular Formula: C₂₃H₃₀N₄O₃
Molecular Weight: 410.51
Catalog: Signaling Pathways Anti-infection HSV
Create Date: 2023-04-04 14:33:09
Modify Date: 2024-01-06 07:20:41
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].

Name	AT-533

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)[1][2][3].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Anti-infection >> HSV Signaling Pathways >> Metabolic Enzyme/Protease >> HSP Research Areas >> Infection Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FAK Signaling Pathways >> PI3K/Akt/mTOR >> Akt Research Areas >> Inflammation/Immunology Signaling Pathways >> Cell Cycle/DNA Damage >> HSP Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR Signaling Pathways >> MAPK/ERK Pathway >> ERK Signaling Pathways >> Stem Cell/Wnt >> ERK
Target	HSP90 HSV-1 ERK1 ERK2 NF-κB Akt HIF-1α VEGF/VEGFR-2
In Vitro	AT-533 (0-1350 nM; 24 h 或 48 h) 抑制 20ng/mL VEGF 诱导的管形成、细胞迁移和 HUVEC侵袭[1]。 AT-533 (2 μM 或 75 μM; 24 h) 抑制缺氧诱导的乳腺癌细胞中 HIF-1α/VEGF 信号通路，抑制 Akt/mTOR/p70S6K, Erk1/2 和 FAK 磷酸化[1]。 AT-533 (10 nM, 50 nM; 48 h) 对绒毛膜 (CAM) 模型具有抗血管生成能力[1]。 AT-533 (0.5 μM; 2 h, 4 h) 降低 RAW264.7 和 BV2 细胞受 HSV-1 诱导引起 TNF-α、IL-1β 和 IL-6 的产生[2]。 Cell Viability Assay[1] Cell Line: Human umbilical vein endothelial cells (HUVECs): MCF-7 and MDA-MB-231 Concentration: 0, 5.6, 16.7, 50, 150, 450, and 1350 nM Incubation Time: 12 h, 24 h, 48 h, and 72 h Result: Inhibited cell viability at 48 h with an IC50 value of 50.1 nM. Western Blot Analysis[1] Cell Line: MCF-7 cells and MDA-MB-231 cells Concentration: 5 nM, 10 nM, 50 nM, and 75 nM Incubation Time: 24 h Result: Inhibited the phosphorylation of VEGF-2, Akt, mTOR, Erk1/2, FAK.
In Vivo	AT-533 (10 mg/kg; 腹腔注射; 每天 1 次，共 21 天) 抑制小鼠 MDA-MB-231 乳腺癌异种移植瘤模型中 HIF-1α/VEGF 信号通路相关蛋白的表达[1]。 AT-533 (1, 2, 4 mg/kg; 腹腔注射; 每天 1 次，共 30 天) 在 Sprague-Dawley 大鼠的亚急性毒性试验中，不引起死亡、食欲下降、体重下降、不良反应[3]。 Animal Model: Male C57BL/6 mice with MDA-MB-231 breast cancer xenografts[1] Dosage: 10 mg/kg; Administration: Intraperitoneal injection; once daily for 21 days Result: Significantly downregulated HIF-1α and VEGF expression.
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. [2]. Li F, et al. AT-533, a Hsp90 inhibitor, attenuates HSV-1-induced inflammation. Biochem Pharmacol. 2019 Aug;166:82-92. [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.

Molecular Formula	C₂₃H₃₀N₄O₃
Molecular Weight	410.51

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