1172854-54-4

1172854-54-4 structure

Name: NS-3-008 hydrochloride
Chemical Name: NS-3-008
CAS Number: 1172854-54-4
Molecular Formula: C₁₄H₂₄ClN₃
Molecular Weight: 269.817
Catalog: Research Areas Inflammation/Immunology
Create Date: 2020-01-11 13:10:54
Modify Date: 2024-04-08 04:45:17
NS-3-008 is a novel small-molecule transcriptional inhibitor of G0s2 (G0/G1 switch 2) with IC50 of 2.25 uM; decreases levels of G0s2 and Ccl2 mRNA in the kidneys (5 mg/kg, p.o.); decreases the phosphorylation of Stat5 and p65 protein and suppresses renal inflammation in 5/6Nx mice, ameliorates renal dysfunction in mouse model of chronic kidney disease (CKD).

Name	NS-3-008

Description	NS-3-008 is a novel small-molecule transcriptional inhibitor of G0s2 (G0/G1 switch 2) with IC50 of 2.25 uM; decreases levels of G0s2 and Ccl2 mRNA in the kidneys (5 mg/kg, p.o.); decreases the phosphorylation of Stat5 and p65 protein and suppresses renal inflammation in 5/6Nx mice, ameliorates renal dysfunction in mouse model of chronic kidney disease (CKD).
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Inflammation/Immunology
Target	IC50: 2.25 μM (G0s2)[1]
In Vitro	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].
In Vivo	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].
References	[1]. Matsunaga N, et al. Inhibition of G0/G1 Switch 2 Ameliorates Renal Inflammation in Chronic Kidney Disease. EBioMedicine. 2016 Nov;13:262-273.