NS-3-008 HCl

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NS-3-008 HCl是一种转录G0/G1开关2 (G0s2)抑制剂(IC50为2.25 μM)。给予NS-3-008可抑制健康小鼠肝脏中G0s2的表达。

NS-3-008 HCl is a transcriptional G0/G1 switch 2 (G0s2) inhibitor( IC50 of 2.25 μM).Administration of NS-3-008 inhibited the expression of G0s2 in healthy mice liver.?In contrast, administration of NS-3-008 did not affect the MBP in wild-type sham and 5/6Nx mice.?NS-3-008 as a novel G0s2 inhibitor and showed that administration of this inhibitor ameliorated renal dysfunction in wild-type 5/6Nx mice.

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.

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.

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Others

Other Targets

G0s2

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1172854-54-4

269.81

C14H24ClN3

>98% (HPLC)

DMSO:120 mg/ml(444.76 mM; Need ultrasonic);H2O : 125 mg/mL (463.29 mM; Need ultrasonic)

Cl.CCCCCCNC(=N)NCc1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years