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抑制剂描述:

产品名称:LW6

产品别名:见爱必信官网

英文别名:LW6

靶点:HIF

CAS:934593-90-5

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

 LW6是hypoxia-inducible factor 1(HIF)抑制剂。在缺氧环境下,LW6能通过降解HIF-1α,从而有效地抑制HIF-1α的积累,不影响HIF-1α mRNA水平。在cell-based HRE-reporter gene assays中,LW6抑制缺氧诱导的HIF-1α转录活性的IC50为2.64 μM。

溶解性:DMSO:13 mg/mL (29.85 mM)
Ethanol:1 mg/mL (2.29 mM)

体外研究:

LW6 inhibits HIF-1α expression induced by hypoxia. It promotes apoptosis preferentially in hypoxic cells. Treatment with LW6 presents no additive effect on cell cycle arrest. LW6 induces ROS formation through the depolarization of MMP in hypoxic cells. Although LW6 increases mitochondrial ROS production, the combination with hypoxia induces a marked increase in ROS production and this high level is maintained up until 24 h. LW6 is also a specific inhibitor of MDH2. As MDH2 is known to serve a significant role in the citric acid cycle at the mitochondrial membrane, LW6 indirectly reduces the activity of the mitochondrial respiratory chain through the inhibition of MDH2. In MDCKII-BCRP cells overexpressing BCRP, LW6 enhances significantly (p . LW6 also down-regulates BCRP expression at concentrations of 0.1-10 μM. Furthermore, cells become more susceptible to the cytotoxicity of anticancer drugs in the presence of LW6.

体内研究:LW6 exerts marked anti-tumor efficacy in vivo and causes reductions in HIF-1α expression levels in mice carrying xeno-grafts of HCT116 cells. LW6 improves the cytotoxicity and bioavailability of anticancer drugs translocated by BCRP.

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