Adapalene

Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC₅₀s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity^[1][2][3]. IC50 & Target: AC50: 2.3 nM (RARβ), 9.3 nM (RARγ), and 22 nM (RARα)^[1] In Vitro: Adapalene (1-200 μM; 24 h) inhibits the viability of ES-2, HOV-7, MCF-7 , Hela, SW1990, HT1080, and MM-468 cells, with IC₅₀s of 10.36 μM, 10.81 μM, 12.00 μM, 19.08 μM, 19.52 μM, 21.70 μM, and 31.47 μM, respectively^[2].
Adapalene (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro^[2].
Adapalene (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells^[3].
Adapalene (1-200 μM) inhibits GOT1 activity, with an IC₅₀ of 21.79 μM^[2].
Adapalene (10^-6-10^-3 nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC₅₀ of 2.5 nM^[1]. In Vivo: Adapalene (15-100 mg/kg; p.o. daily for 21 days) inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice^[3].