481908
烟酰胺磷酸核糖转移酶抑制剂，FK866
The Nicotinamide Phosphoribosyltransferase Inhibitor, FK866, also referenced under CAS 658084-64-1, controls the biological activity of Nicotinamide Phosphoribosyltransferase. This small molecule/inhibitor is primarily used for Neuroscience applications.
别名:
烟酰胺磷酸核糖转移酶抑制剂，FK866, APO866，NAMPTase抑制剂I，PBEF抑制剂I，Visfatin抑制剂I，NAPRT抑制剂，（E）-N-（4-（1-苯甲酰基哌啶-4-基）丁基）-3-（吡啶-3-基）丙烯酰胺，NAMPT抑制剂
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所有图片(1)
About This Item
推荐产品
质量水平
方案
≥97% (HPLC)
表单
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
yellow
溶解性
DMSO: 100 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
N2(CCC(CC2)CCCCNC(=O)\C=C\c3cnccc3)C(=O)c1ccccc1
InChI
1S/C24H29N3O2/c28-23(12-11-21-8-6-15-25-19-21)26-16-5-4-7-20-13-17-27(18-14-20)24(29)22-9-2-1-3-10-22/h1-3,6,8-12,15,19-20H,4-5,7,13-14,16-18H2,(H,26,28)/b12-11+
InChI key
KPBNHDGDUADAGP-VAWYXSNFSA-N
一般描述
一种可渗透细胞的吡啶基丙烯酰胺化合物，可作为选择性的变构NAPRT/NAMPT（烟酰胺磷酸核糖基转移酶）抑制剂（酶/底物复合物的Ki=0.4 nM；游离酶的Ki′=0.3 nM），同时对NPRT（烟酸磷酸核糖基转移酶）活性（K-562提取物中10 nM时NAPRT活性抑制82%，而1 µM时NPRT活性无抑制）没有影响。已显示FK866治疗可通过消耗HepG2和NIH-3T3培养物（在10 nM FK866治疗24小时后减少>95%）中的NAD+ （目录号481911 & 481915）来诱导细胞死亡，同样，已证明添加外源NAD+可从FK866诱导的NAD+消耗和细胞死亡中挽救NIH-3T3和SH-SY5Y。
一种可渗透细胞的吡啶基丙烯酰胺化合物，可作为选择性的变构NAPRT/NAMPT（烟酰胺磷酸核糖基转移酶）抑制剂（酶/底物复合物的Ki=0.4 nM；游离酶的Ki′=0.3 nM），同时对NPRT（烟酸磷酸核糖基转移酶）活性（K-562提取物中10 nM时NAPRT活性抑制82%，而1 µM时NPRT活性无抑制）没有影响。已显示FK866治疗可通过消耗HepG2和NIH-3T3培养物（在10 nM FK866治疗24小时后减少>95%）中的NAD+（目录号481911 & 481915）来诱导细胞死亡，同样，已证明添加外源NAD+可从FK866诱导的NAD+消耗和细胞死亡中挽救NIH-3T3和SH-SY5Y。
包装
用惰性气体包装
警告
毒性：标准处理（A）
外形
以50 mM（2 mg/102.17 µl）DMSO溶液提供。
其他说明
Formentini, L., et al. 2009.Biochem.Pharmacol.77, 1612.
Nakahata, Y., et al. 2009.Science324, 654.
Ramsey.K.M., et al. 2009.Science324, 651.
Billington, R.A., et al. 2008.J. Biol. Chem.283, 6367.
Hasmann, M. and Schemainda, I., 2003.Cancer Res.63, 7436.
Nakahata, Y., et al. 2009.Science324, 654.
Ramsey.K.M., et al. 2009.Science324, 651.
Billington, R.A., et al. 2008.J. Biol. Chem.283, 6367.
Hasmann, M. and Schemainda, I., 2003.Cancer Res.63, 7436.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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Several enzymes of intermediary metabolism have been identified to bind RNA in cells, with potential consequences for the bound RNAs and/or the enzyme. In this study, we investigate the RNA-binding activity of the mitochondrial enzyme malate dehydrogenase 2 (MDH2), which
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Xiangguo Shi et al.
Science advances, 7(30) (2021-07-23)
Metabolic dysregulation underlies malignant phenotypes attributed to cancer stem cells, such as unlimited proliferation and differentiation blockade. Here, we demonstrate that NAD+ metabolism enables acute myeloid leukemia (AML) to evade apoptosis, another hallmark of cancer stem cells. We integrated whole-genome
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The metabolism of different cells within the same microenvironment can differ and dictate physiological or pathological adaptions. Current single-cell analysis methods of metabolism are not label-free. The study introduces a label-free, live-cell analysis method assessing endogenous fluorescence of NAD(P)H and
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