NS-3-008hydrochloride是一种口服活性的G0s2转录抑制剂，IC50为2.25μM。NS-3-008hydrochloride可用于慢性肾脏疾病。
货号:ajcx31212
CAS:1172854-54-4
分子式:C14H24ClN3
分子量：269.81
溶解度:DMSO: 125 mg/mL (463.29 mM); H2O: 125 mg/mL (463.29 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[1].

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[1].

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[1].

[1]. Matsunaga N, et al. Inhibition of G0/G1 Switch 2 Ameliorates Renal Inflammation in Chronic Kidney Disease. EBioMedicine. 2016 Nov;13:262-273.