Drug intelligence / Profile preview

acetylshikonin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Acetylshikonin is a naturally occurring **acetate ester** and a **hydroxy-1,4-naphthoquinone** derivative found in plants such as Lithospermum erythrorhizon and Arnebia species[2][5][8]. It is characterized as a **small molecule** with prominent **anti-cancer** and **anti-inflammatory** properties. Mechanistically, acetylshikonin acts as a **microtubule-targeting agent (MTA)** by inhibiting tubulin polymerization, causing G2/M phase cell cycle arrest and promoting apoptosis in various cancer cell lines (including hepatocellular carcinoma, renal cell carcinoma, and others)[3][6]. It also inhibits cytochrome P450 2J2 (CYP2J2) activity and induces nuclear translocation of forkhead box protein O3 (FOXO3)[6]. These properties collectively position acetylshikonin as a promising preclinical lead for research in oncology[3][6].

Other names
Shikonin, acetylShikonin acetateO-Acetylshikonin(R)-acetyl shikoninRacemic Acetyl Shikonin Labeled d7
02

Targets

CYP2J2 (Cytochrome P450 family 2 subfamily J member 2)FOXO3 (Forkhead box protein O3)TUBB (Tubulin (alpha and beta subunits))

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