Drug intelligence / Profile preview

ESE-15-ol

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

ESE-15-ol is a *synthetic estradiol analogue* with demonstrated **antimitotic and anticancer activity** in vitro, particularly against tumorigenic and metastatic breast cancer cells (e.g., MCF-7 and MDA-MB-231). It selectively inhibits **carbonic anhydrase IX** (CAIX), a tumor-associated enzyme involved in pH regulation and metastatic adaptation, more potently than wild-type CAII[1][3]. ESE-15-ol exerts its effects by blocking cells in the G2/M phase of the cell cycle, disrupting *mitotic spindle apparatus*, inducing cell death via *mitochondrial membrane depolarization*, and promoting apoptosis through the intrinsic pathway with involvement of Bcl-2 and PUMA/BBC3 upregulation. It also appears to increase reactive oxygen species (ROS), interfere with chromatin remodeling, and impede the cell cycle checkpoint[1][3][5]. Developed primarily as a research compound, its main explored indication is cancer, especially breast cancer[1][3].

Other names
2-ethyl-3-O-sulphamoyl-estra-1,3,5(10),15-tetraen-17-ol
02

Targets

CA9 (Carbonic anhydrase IX)BCL-2 (BCL-2 family)CA2 (Carbonic Anhydrase 2)

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