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CAS No. : 106685-40-9
MCE 国际站:Adapalene
产品活性:Adapalene (CD271) 是第三代合成类视黄醇,局部应用于痤疮。Adapalene 是一种有效的 RAR 激动剂,对 RARβ、RARγ、RARα 的 AC50 值分别为 2.3 nM、9.3 nM 和 22 nM。Adapalene 还以非竞争性方式抑制 GOT1 的酶活性。Adapalene 具有抗肿瘤活性。
研究领域:Metabolic Enzyme/Protease | Vitamin D Related/Nuclear Receptor | Autophagy | Apoptosis
作用靶点:RAR/RXR | Autophagy | Apoptosis
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.
Adapalene (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro.
Adapalene (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells.
Adapalene (1-200 μM) inhibits GOT1 activity, with an IC50 of 21.79 μM.
Adapalene (10-6-10-3 nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC50 of 2.5 nM.
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.
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货号: HY-B0091
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