Adapalene阿达帕林,106685-40-9

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Adapalene

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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