Cercosporamide
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.
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- CAS No.: 131436-22-1
- 화학식: C16H13NO7
- 분자량:331.28
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Pkc1 50 nM (IC50) |
Pkc1 7 nM (Ki) |
Mnk |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
<3 μM
Compound: CERCO
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Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
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[PMID: 29853332] |
| KMS-11 | EC50 |
>10 μM
Compound: Cercosporamide
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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
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[PMID: 27002243] |
| Sf9 | IC50 |
0.044 μM
Compound: 1
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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
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[PMID: 19109017] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 131436-22-1
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Appearance Solid
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분자량 331.28
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화학식 C16H13NO7
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Color White to yellow
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SMILES
O=C(C1=C(C([C@@]23C)=C(O)C=C1O)OC2=CC(O)=C(C(C)=O)C3=O)N
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Synonyms
(-)-Cercosporamide
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 1 mg/mL (3.02 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (281 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Sussman A, et al. Discovery of Cercosporamide, a known antifungal natural product, as a selective Pkc1 kinase inhibitor through high-throughput screening. Eukaryot Cell. 2004 Aug;3(4):932-43. [Content Brief]
[2]. Altman JK, et al. Inhibition of Mnk kinase activity by Cercosporamide and suppressive effects on acute myeloid leukemia precursors. Blood. 2013 May 2;121(18):3675-81. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.0186 mL | 15.0930 mL | 30.1859 mL | 75.4649 mL |
Cercosporamide Related Classifications
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