Product Name :
Cercosporamide
Description:
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
CAS:
131436-22-1
Molecular Weight:
331.28
Formula:
C16H13NO7
Chemical Name:
(1S)-12-acetyl-3, 5, 11-trihydroxy-1-methyl-13-oxo-8-oxatricyclo[7.4.0.0, ]trideca-2, 4, 6, 9, 11-pentaene-6-carboxamide
Smiles :
CC(=O)C1C(=O)[C@@]2(C)C3=C(OC2=CC=1O)C(C(N)=O)=C(O)C=C3O
InChiKey:
GEWLYFZWVLXQME-MRXNPFEDSA-N
InChi :
InChI=1S/C16H13NO7/c1-5(18)10-7(20)4-9-16(2,14(10)22)12-8(21)3-6(19)11(15(17)23)13(12)24-9/h3-4,19-21H,1-2H3,(H2,17,23)/t16-/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥360 days if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of Product information|CAS Number: 131436-22-1|Molecular Weight: 331.28|Formula: C16H13NO7|Synonym:|(-)-Cercosporamide|Chemical Name: (1S)-12-acetyl-3, 5, 11-trihydroxy-1-methyl-13-oxo-8-oxatricyclo[7.4.0.0, ]trideca-2, 4, 6, 9, 11-pentaene-6-carboxamide|Smiles: CC(=O)C1C(=O)[C@@]2(C)C3=C(OC2=CC=1O)C(C(N)=O)=C(O)C=C3O|InChiKey: GEWLYFZWVLXQME-MRXNPFEDSA-N|InChi: InChI=1S/C16H13NO7/c1-5(18)10-7(20)4-9-16(2,14(10)22)12-8(21)3-6(19)11(15(17)23)13(12)24-9/h3-4,19-21H,1-2H3,(H2,17,23)/t16-/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{DOTMA} web|{DOTMA} Metabolic Enzyme/Protease|{DOTMA} Biological Activity|{DOTMA} Formula|{DOTMA} supplier|{DOTMA} Epigenetics} |Shelf Life: ≥360 days if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Cercosporamide is a broad-spectrum natural antifungal compound, is actually a selective and highly potent fungal Pkc1 kinase inhibitor. 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.{{Anti-Mouse IFNAR1 Antibody (MAR1-5A3)} web|{Anti-Mouse IFNAR1 Antibody (MAR1-5A3)} IFNAR|{Anti-Mouse IFNAR1 Antibody (MAR1-5A3)} Epigenetics|{Anti-Mouse IFNAR1 Antibody (MAR1-5A3)} Purity & Documentation|{Anti-Mouse IFNAR1 Antibody (MAR1-5A3)} Purity|{Anti-Mouse IFNAR1 Antibody (MAR1-5A3)} supplier} To determine whether Cercosporamide exhibits negative regulatory effects on cell proliferation and viability of leukemia cells, MTT assays are conducted.PMID:32701010 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.|In Vivo:|Treatment with Cercosporamide or Ara-C alone significantly suppresses xenograft growth when compared with the respective vehicle (PReferences:|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.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.Products are for research use only. Not for human use.|
