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CAS No. :
MCE 国际站:TH-6
产品活性:TH-6 是一种有效的 HDAC 抑制剂,对 HDAC1、HDAC2、HDAC3、HDAC6、HDAC8 的 IC50 分别为 0.115、0.135、0.242、0.138、2.120 µM。TH-6 抑制细胞迁移和侵袭。TH-6 诱导细胞凋亡 (apoptosis)和细胞周期停滞在 G2/M 期。TH-6 显示出抗肿瘤活性。
研究领域:Cell Cycle/DNA Damage | Epigenetics | Apoptosis | NF-κB | Metabolic Enzyme/Protease | Immunology/Inflammation
作用靶点:HDAC | Apoptosis | Reactive Oxygen Species
In Vitro: TH-6 (0-2 µM) shows antiproliferative activities in cancer cell lines and normal human lung cells.
TH-6 (0-10 µM) inhibits tubulin polymerization with an IC50 value of 4.06 µM.
TH-6 (0.03, 0.1, 0.3 1 µM; 24 h) increases the expression of Ac-α-Tubulin and AC-Histone H3 in HepG2 cells.
TH-6 (7.5, 15, 30 nM) induces apoptosis and cell cycle arrest at G2/M phase.
TH-6 (0-30 nM) decreases the MMP and increase ROS levels of HepG2 cells in a dose-dependent manner.
TH-6 (7.5, 15, 30 nM; 48 h) inhibits cell migration and invasion in MDA-MB-231 cells and suppress the migration of HUVECs in a concentration-dependent manner.
TH-6 shows favorable liver microsomal stability in vitro with t1/2 of 50.3 min.
In Vivo: TH-6 (10, 20 mg/kg; i.v.; daily for 21 days) shows anti-tumor activity in mouse.
TH-6 (20 mg/kg) shows antivascular activity and a good cardiovascular safety profile in mouse.
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