Drug intelligence / Profile preview

NJK14013

Development stage
Preclinical
Lead developer
Kyung Hee University College of Pharmacy
Modality
Small Molecules
Administration
Not Determined
01

Overview

NJK14013 is a **novel synthetic selective estrogen receptor modulator (SERM)** identified as bis(4-hydroxyphenyl)methanone-O-isopentyl oxime. It acts as an **agonist of estrogen receptor alpha (ERα)**, stimulating ER-dependent transcriptional activity and inducing ER phosphorylation, thereby enhancing the transcription of estrogen-responsive genes such as GREB1. Unlike endogenous estrogens, NJK14013 also **suppresses androgen receptor-dependent transcription** and exhibits anti-proliferative effects on a broad range of cancer cell lines, including both ER-positive and ER-negative breast cancer and endometrial cancer cells. Notably, NJK14013 induces apoptotic cell death in cancer cells while sparing non-cancerous endothelial cells, suggesting tumor-selective cytotoxicity. These properties highlight its potential for use in **anticancer therapy** or **hormone-replacement therapy** with a possibly reduced risk of carcinogenesis compared to conventional estrogens[1][3][5].

Other names
bis(4-hydroxyphenyl)methanone-O-isopentyl oxime
02

Targets

AR (Adrenergic receptors)ESR1 (ERα)

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