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Chemical Structure : ETC-168
Catalog No.: PC-72233Not For Human Use, Lab Use Only.
ETC-168 (ETC168) is a potent, selective MNK kinase inhibitor with biochemical IC50 of 23 and 43 nM against MNK1 and MNK2, respectively.
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ETC-168 (ETC168) is a potent, selective MNK kinase inhibitor with biochemical IC50 of 23 and 43 nM against MNK1 and MNK2, respectively.
ETC-168 acts as a MNK2-biased, dual-MNK inhibitor in cells.
ETC-168 induced dose-dependent growth suppression and inhibited 50% of cell viability at 5 uM in LPS141 and MESSA, ETC-168 treatment elicited a consistent increase of cells in G0/G1 phase among LPS141, LP6, and MESSA cells in a dose-dependent manner. ETC-168 decreased cells of S and G2/M phases, while no significant induction of sub-G1 cells.
Inhibition of MNK1/2 by ETC-168 elevated the expression of MNK1/2 at both transcript and protein levels in soft tissue sarcoma (STS) cells.
ETC-168 effectively suppressed both p-4E and cell viability in MESSA cells, but not CGP57380 and eFT508.
ETC-168 suppresseed phosphorylation of ribosomal protein S6 (RPS6) in sensitive STS cell, decreased expression of E2F1, FOXM1, and WEE1.
Inhibition of MCL1 via S63845 synergizes with ETC-168 against STS cells.
| M.Wt | 409.449 | |
| Formula | C24H19N5O2 | |
| Appearance | Solid | |
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1. Haiyan Yang, et al. J Med Chem. 2018 May 24;61(10):4348-4369.
2. Xin-Yu Ke, et al. Oncogene. 2021 Mar;40(10):1851-1867.
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