Drug intelligence / Profile preview

CAY10526

Development stage
Preclinical
Lead developer
Cayman Chemical
Modality
Small Molecules
Administration
In Vitro (cell Culture), Animal Models (intraperitoneal)
01

Overview

CAY10526 is a **small molecule inhibitor** of **microsomal prostaglandin E synthase-1 (mPGES-1)**, selectively inhibiting the production of prostaglandin E2 (PGE2) without affecting the upstream cyclooxygenase-2 (COX-2)[1][5][9][10]. CAY10526 dose-dependently inhibits PGE2 synthesis in cell-based models and has shown significant suppression of tumor growth and increased apoptosis in melanoma xenografts[3][2][7][10]. Mechanistically, it downregulates anti-apoptotic proteins (BCL-2, BCL-XL), upregulates pro-apoptotic markers (BAX, BAK, cleaved caspase 3), and inhibits Y-box binding protein 1 (YB-1) phosphorylation, affecting cell survival and proliferation[3]. Additionally, CAY10526 acts as an **NF-κB pathway inhibitor**[7]. Its primary application is as a biochemical probe/research tool in cancer biology, inflammation, and prostanoid signaling; it is not approved for clinical use and is for research use only[2][7].

Other names
4-(benzo[b]thiophen-2-yl)-3-bromo-5-hydroxydihydrofuran-2(3H)-one4-Benzo[b]thiophen-2-yl-3-bromo-5-hydroxy-2(5H)-furanone4-Benzo[b]thien-2-yl-3-bromo-5-hydroxy-5H-furan-2-one
02

Targets

PTGES (Microsomal prostaglandin E synthase-1)NOS2 (Nitric Oxide Synthase 2)YBX1 (Y-box-binding protein 1)

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