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Cercosporamide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cercosporamide图片
CAS NO:131436-22-1
包装与价格:
包装价格(元)
500 μg电议
1mg电议
5mg电议
10mg电议

产品名称
(-)-Cercosporamide
产品介绍
Cercosporamide 是一种高效的 ATP 竞争性Pkc1激酶抑制剂,IC50<50 nm,Ki<7 nm。cercosporamide 是一种独特的Mnk抑制剂。
生物活性

Cercosporamide is a highly potent, ATP-competitivePkc1kinase inhibitor, with anIC50of<50 nm and aKiof<7 nm. cercosporamide is a uniqueMnkinhibitor.

IC50& Target[1][2]

Pkc1

50 nM (IC50)

Pkc1

7 nM (Ki)

Mnk

 

体外研究
(In Vitro)

Cercosporamide is a broad-spectrum natural antifungal compound, is actually a selective and highly potent fungal Pkc1 kinase inhibitor[1]. Cercosporamide, an antifungal agent that is recently shown to act as a unique Mnk inhibitor, exhibits antileukemic properties. Cercosporamide is a potent inhibitor of phosphorylation of eIF4E at Ser209 in AML cells and results in potent inhibitory effects on primitive leukemic progenitors (CFU-L) from AML patients. To determine whether Cercosporamide exhibits negative regulatory effects on cell proliferation and viability of leukemia cells, MTT assays are conducted. When U937 cells are incubated in the presence or absence of the increasing doses of Cercosporamide, a dose-dependent suppression of cell growth is found. Similar experiments with comparable results are seen when the effects of Cercosporamide on MM6 and K562 cells are examined[2].

体内研究
(In Vivo)

Treatment with Cercosporamide or Ara-C alone significantly suppresses xenograft growth when compared with the respective vehicle (P<0.011 for 10 mg/kg twice-daily Cercosporamide; P<0.006 for Cercosporamide 20 mg/kg daily; P<0.0374 for Ara-C). The combination of Cercosporamide 10 mg/kg twice daily plus Ara-C is significantly more effective than either agent alone (P<0.0009 vs Cercosporamide; P=0.005 vs Ara-C; P<0.0001 vs either vehicle). Cercosporamide (20 mg/kg once daily) in combination with Ara-C shows similar effects, with significant inhibition of tumor growth vs captisol (P<0.0001) or water (P=0.0003), but does not show statistical significance vs Cercosporamide alone (20 mg/kg) or Ara-C alone[2].

分子量

331.28

性状

Solid

Formula

C16H13NO7

CAS 号

131436-22-1

中文名称

尾孢素酰胺

结构分类
  • Phenols
  • Polyphenols
  • Others
来源
  • Plants
  • Euphorbiaceae
  • Manihot esculentaCrantz

Cercosporidium fungus

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month