IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively.

2021年4月23日 · IOX1 effectively downregulates tumour PD-L1 expression in vitro and in vivo. Simultaneously, it inhibits cancer cell’s multidrug resistance and promotes intracellular DOX accumulation, greatly...

We also identified that IOX1, a known histone demethylase inhibitor, significantly suppresses Wnt target gene transcription and CRC tumorigenesis. Mechanistically, IOX1 inhibits the enzymatic activity of KDM3 by binding to the Jumonji C domain and thereby preventing the demethylation of H3K9 on Wnt target gene promoters.

IOX1 was the most potent inhibitor against 8 of the 10 tested KDMs. IOX1 exhibited IC 50 values at 1 μM or lower against the KDM3, KDM4 and KDM6 subfamilies, and 5-25 μM against the KDM5 and KDM2/7 subfamilies.

2021年4月23日 · Here, we report a histone demethylase inhibitor, 5-carboxy-8-hydroxyquinoline (IOX1), which inhibits tumour histone demethylase Jumonji domain-containing 1A (JMJD1A) and thus downregulates its downstream β-catenin and subsequent PD-L1, providing an antibody-independent paradigm interrupting the PD-1/PD-L1 checkpoint.

IOX1 a broad-spectrum, cell permeable inhibitor of most 2OG oxygenases which does not require application in a pro-drug form [2]. It was discovered following a high throughput screening campaign against the JMJD2 (KDM4) family of 2-oxoglutarate-dependent …

IOX1 (5-Carboxy-8-hydroxyquinoline) is a broad spectrum inhibitor of 2-oxoglutarate (2OG) oxygenases, including Jumonji C domain (JmjC) demethylases. It is useful for the study of histone demethylation and hypoxic sensing and results in translocation …

The inhibition of JMJD2A by IOX1 suppressed the Ang II-induced cell proliferation, migration and cell cycle progression by inhibiting cyclin D1 expression and increasing p21 expression. The underlying mechanisms were related to the restoration …

2024年11月15日 · IOX1 is the most potent broad-spectrum inhibitor of the 2-ketoglutarate (2OG), and its potential targets include a variety of histone demethylases and DNA demethylases, with strong inhibitory effects on KDM3 and KDM4 [24], [25].