RRx-001 是一种低氧选择性的表观遗传因子,被用作放射或化疗敏感剂,能诱发凋亡,克服骨髓瘤的耐药性。它是G6PD的有效抑制剂,具有抗疟、抗癌活性。它是免疫检查点的抑制剂,可下调CD47和SIRP-α。
产品描述
RRx-001 is a potent inhibitor ofglucose 6-phosphate dehydrogenase(G6PD) and with potent antimalarial activity
体外活性
RRx-001 inhibited the growth of colon cancer cells (HCT 116) and decreased levels of the DNA methyltransferases DNMT1 and DNMT3a in a time and dose-dependent manner. Treatment of HCT 116 cells with 0.5 μM RRx-001 for 24 h significantly increased transcripts of interferon (IFN)-responsive genes and this induction was sustained for up to 4 weeks after transient exposure to RRx-001. RRx-001 increased secretion of type I and III IFNs by HCT 116 cells, and these IFNs were confirmed to be bioactive. Transcription of endogenous retrovirus ERV-Fc2 and LTRs from the ERV-L family (MLT2B4 and MLT1C49) was induced by RRx-001[1].
Cas No.
925206-65-1
分子式
C5H6BrN3O5
分子量
268.02
别名
RRX-001
储存和溶解度
DMSO:100 mg/mL (373.11 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years