IOX2 sodium

IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases[1][2].

Research Areas >> Cancer

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase

IC50: 22 nM (PHD2)[2]

IOX2 sodium (0、10、25 和 50 μM) 剂量依赖性地抑制胶原蛋白相关肽 (CRP；0.25μg/mL) 或凝血酶 (0.03 U/mL) 诱导的血小板聚集和 ATP 释放。 但 IOX2 不影响 P-选择素表达和糖蛋白 (GP)Ibα、GPVI 或 αIIbβ3 的表面水平[1]。 IOX2 sodium 还抑制血小板在纤维蛋白原或胶原蛋白上的扩散和凝块回缩[1]。 IOX2 sodium (50 μM；24 h) 增加正常人的表皮角质形成细胞 (NHEK) 和正常人真皮成纤维细胞 (NHDF) 在常氧和缺氧条件下生长时 VEGF-A 和 BNIP3 的转录水平[2]。

IOX2 sodium (10 mg/kg；腹腔注射；单剂量) 损害小鼠体内血小板的止血功能和动脉血栓形成[1]。 Animal Model: Mouse[1] Dosage: 10 mg/kg Administration: Intraperitoneal injection Result: Upregulated HIF-1α in platelets, decreased ROS generation, and downregulated NOX1 expression. Increased the phosphorylation level of VASP (Ser157/239), and inhibited the phosphorylation of p38 (Thr180/Tyr182), ERK1/2 (Thr202/Tyr204), AKT (Thr308/Ser473), and PKCδ (Thr505) in CRP- or thrombin-stimulated platelets.

[1]. Gu W, et al. Inhibition of Hypoxia-Inducible Factor Prolyl-Hydroxylase Modulates Platelet Function. Thromb Haemost. 2022 Oct;122(10):1693-1705.  

[2]. Deppe J, et al. Impairment of hypoxia-induced HIF-1α signaling in keratinocytes and fibroblasts by sulfur mustard is counteracted by a selective PHD-2 inhibitor. Arch Toxicol. 2016 May;90(5):1141-50.