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Description
Overview
A cell-permeable thieno[2,3-d]pyrimidine compound that acts as a selective inhibitor of MAP kinase-interacting kinases 1 and 2 (Mnk1 and 2: IC50 = 23 and 16 nM for MNK1 and MNK2, respectively). Displays much reduced activity against several other protein kinases and does not affect the phosphorylation of ERK, Akt, mTORC1, and ribosomal S6 kinase. Shown to strongly inhibit eIF4E phosphorylation (~1 µM) and abolished the activity completely at higher concentration in MDA-MB-231 and SSC25 cancer cell (~ 1 µM). Shown to be much more effective Mnk inhibitor than CGP57380 (Cat. No. 454861). Reported to inhibit the migration of mouse embryonic fibroblasts and MDA-MB-231 and SCC25 cells, but does not affect their viability and proliferation.
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
28-July-2017 JSW
Synonyms
MNK1 Inhibitor, Mnk-I1
Description
A cell-permeable thieno[2,3-d]pyrimidine compound that acts as a selective inhibitor of MAP kinase-interacting kinases 1 and 2 (Mnk1 and 2: IC50 = 23 and 16 nM for MNK1 and MNK2, respectively). Displays much reduced activity against several other protein kinases and does not affect the phosphorylation of ERK, Akt, mTORC1, and ribosomal S6 kinase. Shown to strongly inhibit eIF4E phosphorylation (~1 µM) and abolished the activity completely at higher concentration in MDA-MB-231 and SSC25 cancer cell (~ 1 µM). Shown to be much more effective Mnk inhibitor than CGP57380 (Cat. No. 454861). Reported to inhibit the migration of mouse embryonic fibroblasts and MDA-MB-231 and SCC25 cells, but does not affect their viability and proliferation.
Form
Light beige solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₂H₂₇F₂N₅O₂S
Purity
≥98% by HPLC
Solubility
DMSO (25 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
