NS-3-008|CAS 1172854-54-4|DC Chemicals

Cas No.:	1172854-54-4
Chemical Name:	1-benzyl-3-hexylguanidine hydrochloride
Synonyms:	NS-3-008 HCl; NS-3-008 hydrochloride; NS-3-008; NS 3-008; NS3-008; NS-3008; NS 3008; NS3008
SMILES:	N=C(NCC1=CC=CC=C1)NCCCCCC.[H]Cl
Formula:	C₁₄H₂₄ClN₃
M.Wt:	269.817
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	https://www.thelancet.com/journals/ebiom/article/PIIS2352-3964(16)30463-7/fulltext

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).
Target:	IC50: 2.25 μM (G0s2)[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].
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].
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.

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NS-3-008 HCl