Cercosporamide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种广谱天然抗真菌化合物，可作为选择性且高效的真菌 Pkc1 激酶抑制剂。

A broad-spectrum natural antifungal compound that acts as a selective and highly potent fungal Pkc1 kinase inhibitor; potent,y and ATP-competitively inhibits C. albicans Pkc (CaPkc1) kinase with IC50 of <40 nM, Ki of 7 nM; shows potent antifungal activity with MIC of 10 ug/ml against both C. albicans and A. fumigatus; also is a potent, selective, orally bioavailable Mnk inhibitor with IC50 of 116 nM and 11 nM for Mnk1 and Mnk2, respectively; blocks eIF4E phosphorylation in cancer cells, inducing apoptosis, suppressing proliferation, and reducing soft agar colonization; active in tumor xenograft model.

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. 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.

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.

-)-Cercosporamide

MAPK/ERK Signaling

MNK

MNK

Infection

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131436-22-1

331.2769

C16H13NO7

>98% (HPLC)

10 mM in DMSO

CC(=O)C1=C(C=C2C(C1=O)(C3=C(C=C(C(=C3O2)C(=O)N)O)O)C)O

4-Dibenzofurancarboxamide, 8-acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-, (9aS)-

(-20℃)

With Ice Pack

≥ 2 years