产品信息
抗原名称
G6PD；Nrf2-ARE
商品描述
RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.
分子量
268.02
纯度
98%
可溶性
DMSO : ≥ 100 mg/mL (373.11 mM)
外观
Off-white solid
In vitro(体外研究)
RRx-001 exerts its anti-proliferative effect, at least partially, through interference with glucose 6 phosphate dehydrogenase (G6PD), a key enzyme in the pentose phosphate pathway, responsible for maintaining adequate levels of the major cellular reductant, NADPH. RRx-001 affects glucose and G6PD enzyme activity in three different cancer cell lines namely Hep G2, CACO-2, and HT-29. RRx-001 induced G6PD inhibition and increased glucose consumption in a concentration dependent fashion. RRx-001 induces p53 and PARP-1 via generation of ROS/RNS. It exerts anticancer activity, at least in part, by interfering with 3 crucial metabolic demands of rapidly proliferating cells: bioenergetics, macromolecular biosynthesis, and manipulation of cellular cytosolic redox homeostasis. RRx-001 mediates nuclear translocation of Nrf2 and the activation of expression of its downstream enzymes HO-1 and NQO1 in tumor cells. Apart from epigenetic alterations, RRx-001 acts via pleiotropic mechanisms including redox signaling and redox-induced dysregulation of many different signal pathways such as Nrf2, p53, PARP cleavage, HIF1 alpha, and G6PD activity. It also triggers p53 and p21 activity in response to double-stranded DNA breaks as well as deregulates cancer cellular energetics and metabolism. RRx-001 is a potent activator of the Nrf2-ARE signaling pathway via ROS/RNS generation.
In vivo(体内研究)
RRx-001 shows promise for short-term blood flow redistribution in tumors with a pericyte- and α-SMA-rich vasculature. RRx-001 monotherapy is well tolerated, with no dose-limiting toxicities. It not only facilitates nuclear translocation of Nrf2, but also upregulates endogenous Nrf2 expression in SCC VII tumors in mice.
背景
分子式
C5H6BrN3O5
CAS号
925206-65-1
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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