中文名称:
2-CHLORO-N-(3,4-DIMETHOXYBENZYL)ACETAMIDE
中文同义词:
2-氯-N-((3,4-二甲氧苯基)甲基)乙酰胺;2-氯-N-(3,4-二甲氧基苄基)乙酰胺;2-氯-N-[(3,4-二甲氧苯基)甲基]乙酰胺;乙酰胺,2-氯-N-((3,4-二甲氧苯基)甲基)-;UBA5抑制剂(DKM 2-93);2-氯-N-((3;4-二甲氧苯基)甲基)乙酰胺
英文名称:
2-CHLORO-N-(3,4-DIMETHOXYBENZYL)ACETAMIDE
英文同义词:
2-CHLORO-N-(3,4-DIMETHOXYBENZYL)ACETAMIDE;CHEMBRDG-BB 9070724;2-Chloro-N-((3,4-dimethoxyphenyl)methyl)acetamide;Acetamide, 2-chloro-N-((3,4-dimethoxyphenyl)methyl)-;Brn 2857211;N-(Dimethoxy-3,4 benzyl)-chloroacetamide;N-(Dimethoxy-3,4 benzyl)-chloroacetamide [french];2-chloro-N-(3,4-dimethoxybenzyl)acetamide(SALTDATA: FREE)
熔点
116-118 °C(Solv: carbon tetrachloride (56-23-5))
沸点
425.7±45.0 °C(Predicted)
密度
1.194±0.06 g/cm3(Predicted)
酸度系数(pKa)
13.42±0.46(Predicted)
生物活性
DKM 2-93是相对选择性的UBA5抑制剂，IC50值为430 μM。
靶点
IC50: 430 μM (UBA5), 90 μM (PaCa2 cells), 30 μM (Panc1 cells)
体外研究
Ubiquitin-like modifier activating enzyme 5 (UBA5) is a novel pancreatic cancer therapeutic target. DKM 2-93 impairs pancreatic cancer cell survival through covalently modifying the catalytic cysteine of UBA5, thereby inhibiting its activity as a protein that activates the ubiquitin-like protein UFM1 to UFMylate proteins. DKM 2-93 inhibits PaCa2 and Panc1 cells survival with IC 50 s of 90 and 30 μM, respectively.
体内研究
DKM 2-93 daily treatment significantly impairs tumor growth of PaCa2 cells in vivo in tumor xenograft studies in immune-deficient mice without causing any weight loss or overt toxicity.
