| 产品描述: | TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity. |
| 靶点: |
HDAC1:0.115 μM (IC50); HDAC2:0.135 μM (IC50); HDAC3:0.242 μM (IC50); HDAC6:0.138 μM (IC50); HDAC8:2.120 μM (IC50) |
| 体外研究: |
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. |
| 体内研究: |
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. |
| 参考文献: |
1. Zhu H, et al. Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects. J Med Chem. 2022 Aug 4. |
| 保存条件: |
-80°C 6个月; -20°C 1个月,避光 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.329 ml |
11.643 ml |
23.286 ml |
| 5 mM |
0.466 ml |
2.329 ml |
4.657 ml |
| 10 mM |
0.233 ml |
1.164 ml |
2.329 ml |
| 50 mM |
0.047 ml |
0.233 ml |
0.466 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |