Cercosporamide
Chemical Name: (9aS)-8-Acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-4-dibenzofurancaboxamide
Purity: ≥96%
Biological Activity
Cercosporamide is a potent inhibitor of MAP-kinase interacting kinase-2 (Mnk2) and JAK3 (IC50 values are 11, 31 and 116 nM for Mnk2, JAK3 and Mnk1 respectively). Blocks eIF4E phosphorylation; exhibits antiproliferative and proapoptotic activity in cancer cells in vitro. Also inhibits Pkc1. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia.
Wu H, Hu C, Wang A, Weisberg E, Chen Y, Yun C, Wang W, Liu Y, Liu X, Tian B, Wang J, Zhao Z, Liang Y, Li B, Wang L, Wang B, Chen C, Buhrlage S, Qi Z, Zou F, Nonami A, Li Y, Fernandes S, Adamia S, Stone R, Galinsky I, Wang X, Yang G, Griffin J, Brown J, Eck M, Liu J, Gray N, Liu Q
Leukemia, 2016;30(1):173-81. -
Translational control of PML contributes to TNFalpha-induced apoptosis of MCF7 breast cancer cells and decreased angiogenesis in HUVECs.
Hsu K, Guan B, Cheng X, Guan D, Lam M, Hatzoglou M, Kao H
Cell Death Differ, 2015;23(3):469-83. -
Cotargeting MNK and MEK kinases induces the regression of NF1-mutant cancers
J Clin Invest, 2016;0(0):. -
Discovery of cercosporamide, a known antifungal natural product, as a selective Pkc1 kinase inhibitor through high-throughput screening.
Sussman et al.
Eukaryot.Cell, 2004;3:932 -
Therapeutic inhibition of MAP kinase interacting kinase blocks eukaryotic initiation factor 4E phosphorylation and suppresses outgrowth of experimental lung metastases.
Konicek et al.
Cancer Res., 2011;71:1849 -
Targeting Mnks for cancer therapy.
Hou et al.
Oncotarget, 2012;3:118 -
CXCR7 promotes melanoma tumorigenesis via Src kinase signaling
S Xu, J Tang, C Wang, J Liu, Y Fu, Y Luo
Cell Death Dis, 2019;10(3):191.
Product Datasheets
Citation for Cercosporamide
The citations listed below are publications that use Tocris products. Selected citations for Cercosporamide include:
1 Citation: Showing 1 - 1
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Repeat-associated non-AUG translation in C9orf72-ALS/FTD is driven by neuronal excitation and stress.
Authors: Westergard Et al.
EMBO Mol Med 2019;11
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