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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-NAMPT-GMX1778
GMX1778

Chemical Structure : GMX1778

CAS No.: 200484-11-3

GMX1778 (CHS-828;GMX-1778)

货号: PC-42257Not For Human Use, Lab Use Only.

GMX1778 (CHS-828) is a potent, specific, competitive NAMPT inhibitor with Kd of 120 nM, enzyme IC50 of <25 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GMX1778 (CHS-828) is a potent, specific, competitive NAMPT inhibitor with Kd of 120 nM, enzyme IC50 of <25 nM.
GMX1778 blocks the NAD+ biosynthesis and results in tumor cell death, furthermore, phosphoribosylated by NAMPT, increases its cellular retention.
GMX1778 also induces ROS in cancer cells, but not in normal cells.
The prodrug of GMX1778, GMX1777, shows antitumor activity in vivo combined with nicotinic acid.

物理化学性质&存储条件

分子量 371.8639
分子式 C19H22ClN5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 39 mg/mL

Chemical Name/SMILES

Guanidine, N-[6-(4-chlorophenoxy)hexyl]-N'-cyano-N''-4-pyridinyl-

参考文献

1. Watson M, et al. Mol Cell Biol. 2009 Nov;29(21):5872-88.

2. Jonsson E, et al. Cancer Lett. 2001 Jan 26;162(2):193-200.

3. Hjarnaa PJ, et al. Cancer Res. 1999 Nov 15;59(22):5751-7.

4. Cerna D, et al. J Biol Chem. 2012 Jun 22;287(26):22408-17.

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