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N-[6-(4-氯苯氧基)己基]-N'-氰基-N''-4-吡啶基胍

用途

GMX1778(CHS-828)是NAMPT高效抑制剂,可抑制剂NAD_addition_的生化合成,IC50值小于25nM。

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名称

[ CAS 号 ]:
200484-11-3

[ 中文名 ]:
N-[6-(4-氯苯氧基)己基]-N'-氰基-N''-4-吡啶基胍

[ 英文名 ]:
GMX1778

[英文别名 ]:

N-Cyano-N'-(4-nitrophenyl)thiourea
Thiourea,N-cyano-N'-(4-nitrophenyl)
GMX1778

生物活性

[ 描述 ]:

GMX1778(CHS-828)是NAMPT高效抑制剂,可抑制剂NAD_addition_的生化合成,IC50值小于25nM。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> NAMPT

研究领域 >> 癌症

[参考文献]

[1]. Watson M, et al. The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors. Mol Cell Biol. 2009 Nov;29(21):5872-88.

[2]. Cerna D, et al. Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by small molecule GMX1778 regulates reactive oxygen species (ROS)-mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner. J Biol Chem. 2012 Jun 22;287(26):22408-17.

[相关活性小分子]

(E)-Daporinad | P7C3 | STF-118804 | KPT-9274 | N-[[4-[(3,5-二氟苯基)磺酰基]苯基]甲基]咪唑并[1,2-A]吡啶-6-甲酰胺 | 2-羟基-2-甲基-N-[1,2,3,4-四氢-2-[2-(3-吡啶基氧基)乙酰基]-6-异喹啉基]-1-丙烷磺酰胺 | CB 300919 | CB30865

物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
526.9±58.0 °C at 760 mmHg

[ 分子式 ]:
C₁₉H₂₂ClN₅O

[ 分子量 ]:
371.864

[ 闪点 ]:
272.4±32.3 °C

[ 精确质量 ]:
371.151276

[ PSA ]:
82.33000

[ LogP ]:
4.95

[ 外观性状 ]:
white solid

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.587

[ 储存条件 ]:
-20℃

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P301 + P312 + P330-P305 + P351 + P338

[ 危险品运输编码 ]:
NONH for all modes of transport

文献

EIF2A-dependent translational arrest protects leukemia cells from the energetic stress induced by NAMPT inhibition.

BMC Cancer 15 , 855, (2015)

Nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme in NAD(+) biosynthesis from nicotinamide, is one of the major factors regulating cancer cells metabolism and is considered a pr...

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