产品
编 号:F054858
分子式:C14H24ClN3
分子量:269.81
产品类型
结构图
CAS No: 1172854-54-4
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产品详情
生物活性:
NS-3-008 hydrochloride is an orally active transcriptional inhibitor of G0/G1 switch 2 (G0s2) with an IC50 of 2.25 μM. NS-3-008 hydrochloride can be used for chronic kidney disease.
体内研究:
NS-3-008 (5 mg/kg; oral administration; daily; for 4 weeks; wild-type 5/6Nx mice) treatment results in decreased levels of G0s2 and Ccl2 mRNA in the kidneys. The phosphorylation of Stat5 and p65 protein is decreased, and SUN concentrations and renal caspase 3/7 activity decreased in 5/6Nx mice treated with NS-03-08. The F4/80-positive area and F4/80 protein levels are decreased in 5/6Nx mice treated with NS-3-008.
体外研究:
NS-3-008 binds to Hsd17b4; knockdown of Hsd17b4 decreased G0s2 mRNA levels, whereas overexpression of Hsd17b4 induced G0s2 mRNA expression. The inhibitory effects of NS-3-008 are blocked by knockdown of Hsd17b4 or deletion of the Stat5 binding site in the G0s2 promoter. NS-3-008 decreases the nuclear phosphorylation of Stat5.