DCZ19931

DCZ19931 is a potent multi-targeting kinase inhibitor. DCZ19931 has anti-angiogenic effects on ocular neovascularization. DCZ19931 also inhibits ERK1/2-MAPK and p38-MAPK signaling[1].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK

Signaling Pathways >> MAPK/ERK Pathway >> ERK

Signaling Pathways >> Stem Cell/Wnt >> ERK

ERK1

ERK2

p38 MAPK

DCZ19931 (1 nM-10 μM; 24 h) 对人脐静脉内皮细胞 (HUVECs) 无明显的细胞毒性[1]。 DCZ19931 (500 nM; 24 h) 抑制 (10 ng/mL; 12 h) VEGFs 诱导的内皮细胞增殖、迁移和成管能力[1]。 DCZ19931 (500 nM; 24 h) 通过下调 ICAM-1，表达抑制血管通透性[1]。 DCZ19931 (500 nM; 24 h) 降低 HUVECs 中 p-ERK1/2、p-p38 和 p-JNK 的表达水平[1]。 DCZ19931 在小鼠脉络膜发芽试验中也显示出抗血管生成作用[1]。 Western Blot Analysis[1] Cell Line: Human umbilical vein endothelial cells (HUVECs) Concentration: 500 nM; with or without 50 ng/mL VEGF for 30 min Incubation Time: 24 hours Result: Decreased expression of phosphorylated ERK and phosphorylated p38.

DCZ19931 (1 μL, 1 μg/μL; 静脉注射; 单剂量) 抑制小鼠氧诱导视网膜病变 (OIR) 模型眼新生血管生成[1]. DCZ19931 (2 μL, 1 μg/μL; 静脉注射; 7 d) 无组织毒性，并抑制激光诱导脉络膜新生血管 (CNV) 模型小鼠的眼部新生血管生成[1]。 Animal Model: Laser-induced choroidal neovascularization (CNV) model in mice[1] Dosage: 2 μL, 1 μg/μL Administration: Intravitreal injection; single dose, monitored for 7 d following laser photocoagulation Result: Did not cause marked histopathological changes in retinal structures. Decreased the areas of CNV lesions, showed anti-angiogenic effect in vivo. Animal Model: Oxygen-induced retinopathy (OIR) model in mice[1] Dosage: 1 μL, 1 μg/μL Administration: Intravitreal injection; single dose Result: Further showed anti-angiogenic effect in vivo, inhibited ocular neovascularization.

[1]. Zhang H, et al. DCZ19931, a novel multi-targeting kinase inhibitor, inhibits ocular neovascularization. Sci Rep. 2022 Dec 13;12(1):21539.