2. Anti-infection MAPK/ERK Pathway Epigenetics TGF-beta/Smad
  3. Fungal MNK PKC
  4. Cercosporamide

Cercosporamide  (Synonyms: 尾孢素酰胺; (-)-Cercosporamide)

目录号: HY-16982 纯度: ≥99.0%
COA 产品使用指南 技术支持

Cercosporamide 是一种高效的 ATP 竞争性 PKC 激酶抑制剂，靶向 PKC1，IC50<50 nM，Ki<7 nM。Cercosporamide 是一种独特的 Mnk 抑制剂。

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Cercosporamide Chemical Structure

Cercosporamide Chemical Structure

CAS No. : 131436-22-1

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规格 价格 是否有货 数量
500 μg ￥9500
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Cercosporamide 相关抗体

Top Publications Citing Use of Products

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cercosporamide is a highly potent, ATP-competitive PKC kinase inhibitor targeting to PKC1, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.

IC50 & Target[1][2]

Pkc1

50 nM (IC50)

Pkc1

7 nM (Ki)

Mnk

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
KMS-11 EC50
> 10 μM
Compound: Cercosporamide
Antiproliferative activity against luciferase expressing human KMS11 cells after 5 days by CellTiter-Glo luminescent assay
Antiproliferative activity against luciferase expressing human KMS11 cells after 5 days by CellTiter-Glo luminescent assay
[PMID: 27002243]
Sf9 IC50
0.044 μM
Compound: 1
Inhibition of Candida albicans Pkc1 expressed in insect Sf9 cells by scintillation proximity assay
Inhibition of Candida albicans Pkc1 expressed in insect Sf9 cells by scintillation proximity assay
[PMID: 19109017]
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cercosporamide 相关抗体:
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

331.28

Formula

C16H13NO7
CAS 号
性状

固体

颜色

White to yellow

中文名称

尾孢素酰胺
结构分类
初始来源

Cercosporidium fungus
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 1 mg/mL (3.02 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0186 mL 15.0930 mL 30.1859 mL
5 mM --- --- ---
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

COA (295 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

U937, MM6, and K562 cells are incubated for 5 days in the presence or absence of the indicated doses of Cercosporamide (1, 10, and 20μM) . Cell proliferation is assessed by an MTT assay[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
MV4-11 cells are implanted at a density of 5×106 cells per mouse. Tumors are measured by caliper and tumor volume is calculated. Once tumors reach a group mean of 100 mm3, animals are randomized to the following treatment groups: Ara-C (20 mg/kg daily dosed intraperitoneally), Cercosporamide (10 mg/kg twice daily, 20 mg/kg daily dosed orally by gavage), Ara-C plus Cercosporamide combinations (as above), or the relative vehicle controls (captisol for Cercosporamide and water for Ara-C)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Cercosporamide 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0186 mL 15.0930 mL 30.1859 mL 75.4649 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cercosporamide131436-22-1(-)-Cercosporamide尾孢素酰胺FungalMNKPKCMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseProtein kinase CInhibitorinhibitorinhibit

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