2373065-59-7
Chemical Structure
DS12881479
- CAS No.: 2373065-59-7
- Formula:C16H19N3OS
- Molecular Weight:301.41
IUPAC Name: N-(5-(tert-butyl)isoxazol-3-yl)-2-(4-((6-(4-(methylsulfonyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)phenyl)acetamide
InChIKey: BTZKRRFKIKIADV-UHFFFAOYSA-N
SMILES: O=C(C1CCN(C)CC1)NC2=NC=C(C3=CC=CC=C3)S2
Biological Activity: DS12881479 is a selective non-ATP-competitive MNK1 inhibitor with an IC50 value of 387 nM. DS12881479 stabilizes MNK1 in its autoinhibited DFD-out conformation, blocks eIF4E phosphorylation, suppresses tumor cell proliferation and induces weak apoptosis. DS12881479 also inhibits FLT3 and DYRK1a kinase activity at high concentrations. DS12881479 can be used for the research of cancer, such as leukemia[1][2].
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DS12881479 | 99.63% | DS12881479 is a selective non-ATP-competitive MNK1 inhibitor with an IC50 value of 387 nM. DS12881479 stabilizes MNK1 in its autoinhibited DFD-out conformation, blocks eIF4E phosphorylation, suppresses tumor cell proliferation and induces weak apoptosis. DS12881479 also inhibits FLT3 and DYRK1a kinase activity at high concentrations. DS12881479 can be used for the research of cancer, such as leukemia. | ||||||||||||||||||||
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- [1]. Yang Z, et al. Discovery of P11-2: A Potent First-in-Class MNK1-Targeting PROTAC Degrader for the Treatment of Cancer. J Med Chem. 2025;68(10):10092-10110. [Content Brief]
- [2]. Matsui Y, et al. A novel inhibitor stabilizes the inactive conformation of MAPK-interacting kinase 1. Acta Crystallogr F Struct Biol Commun. 2018;74(Pt 3):156-160. [Content Brief]
Keywords
