GNE-617 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GNE-617 hydrochloride是有效的烟酰胺磷酸核糖转移酶(NAMPT)竞争性抑制剂,其IC50值为5 nM[1].
GNE-617 hydrochloride是一种有效的NAMPT抑制剂.在缺乏NAPRT1和富含NAPRT1的细胞系中,GNE-617 hydrochloride减少了超过95%的NAD水平,其EC50值范围为0.54 nM ~ 4.69 nM.在体外ADME研究中,GNE-617 hydrochloride显示出最优的体外代谢稳定性\MDCK渗透性以及蛋白结合.此外,GNE-617 hydrochloride对各种细胞系显示出有效的抗增殖作用,对U251\HT1080\PC3\MiaPaCa2和HCT116细胞系的IC50值分别为1.8 nM\2.1 nM\2.7 nM\7.4 nM和2 nM.在U251人胶质瘤细胞异种移植小鼠中,GNE-617 hydrochloride也具有显著的抗肿瘤作用,而且对体重减轻无明显影响[1,2].
参考文献:
[1] Zheng X, Bauer P, Baumeister T, et al. Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors. Journal of medicinal chemistry, 2013, 56(16): 6413-6433.
[2] O'Brien T, Oeh J, Xiao Y, et al. Supplementation of Nicotinic Acid with NAMPT Inhibitors Results in Loss of In Vivo Efficacy in NAPRT1-Deficient Tumor Models. Neoplasia, 2013, 15(12): 1314-IN3.
Storage | Store at -20°C |
M.Wt | 463.88 |
Formula | C21H16ClF2N3O3S |
Solubility | Soluble in DMSO |
Chemical Name | (Z)-N-(4-((3,5-difluorophenyl)sulfonyl)benzyl)imidazo[1,2-a]pyridine-6-carbimidic acid hydrochloride |
SDF | Download SDF |
Canonical SMILES | FC1=CC(F)=CC(S(C2=CC=C(C/N=C(O)/C3=CN4C=CN=C4C=C3)C=C2)(=O)=O)=C1.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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