Cercosporamide, Inhibitor

Cercosporamide

Cat. Num. AAA5752903

• Purity: 98.00%
• Synonyms: Cercosporamide; (-)-Cercosporamide; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• Formula: C16H13NO7
• SMILES: O=C(C1=C(C([C@@]23C)=C(O)C=C1O)OC2=CC(O)=C(C(C)=O)C3=O)N
• CAS Number: 131436-22-1
• Target & IC50: Mnk: ic50 50nM; Pkc1: ic50 7nM (ki)
• In Vitro: treatment with Cercosporamide or Ara-C alone significantly suppresses xenograft growth when compared with the respective vehicle (P<0.011 for 10mg/kg twice-daily Cercosporamide; P<0.006 for Cercosporamide 20mg/kg daily; P<0.0374 for Ara-C). The combination of Cercosporamide 10mg/kg twice daily plus Ara-C is significantly more effective than either agent alone. Cercosporamide (20mg/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 (20mg/kg) or Ara-C alone [2].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Cercosporamide, inhibitor

Cercosporamide is a ATP-competitive Pkc1 kinase inhibitor (IC50 <50nM; Ki <7nM). It also is a unique Mnk inhibitor.

References

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.
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.
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.