Dimethylcurcumin

Dimethylcurcumin (ASC-J9, ASCJ 9) is a selective androgen receptor degrader (SARD). It promotes the degradation of androgen receptors, resulting in decreased expression of androgenic genes.

It has been investigated as a treatment for prostate cancer  and is currently undergoing phase II trials as a topical acne treatment.

Mechanism of action


Dimethylcurcumin has two proposed mechanisms which contribute to its disruption of AR activity:
 * It promotes dissociation of the AR-AR dimer from its coregulators ARA55 (TGFB1I1) and ARA70 (NCOA4), which prevents transcription of AR-regulated genes and leads to degradation of AR.  See diagram on right.
 * It directly promotes selective degradation of the AR.

Dimethylcurcumin is a curcumin analogue, but the latter mechanism of action appears to be unique to dimethylcurcumin :[Supplementary Fig. 1] (however, see Research warning below). Curcumin has been used in traditional medicine as a treatment for hirsutism, an androgen sensitive condition, but its efficacy has not been extensively studied.

Research warning
Curcumin is well known to yield false positives on bioassays, so results for curcumin analogues based purely on in vitro assays should be treated with skepticism.