1043812-24-3
Chemical Structure
eEF2K Degrader-3
- CAS No.: 1043812-24-3
- Formula:C28H32N4O5
- Molecular Weight:504.58
InChIKey: NYBAOZRKGXFCLD-UHFFFAOYSA-N
SMILES: O=C(C1CN(C(C2=NN(C3=CC=C(C)C(C)=C3)C(N(CC4=CC=CC(C)=C4)C2=O)=O)=O)CCC1)OCC
Biological Activity: eEF2K Degrader-3 is an eEF2K molecular glue degrader (Kd = 0.831 μM) that recruits βTRCP to mediate ubiquitin-proteasome degradation. eEF2K Degrader-3 triggers rapid downregulation of eEF2K and produces a durable effect. eEF2K Degrader-3 inhibits TNBC cell proliferation, migration, and invasion, suppresses tumor growth and lung metastasis in mouse models, decreases vimentin and increases E-cadherin in organoids, and downregulates AURKA and SOX8 downstream of eEF2K degradation. eEF2K Degrader-3 can be used for research on triple-negative breast cancer (TNBC)[1].
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eEF2K Degrader-3 | eEF2K Degrader-3 is an eEF2K molecular glue degrader (Kd = 0.831 μM) that recruits βTRCP to mediate ubiquitin-proteasome degradation. eEF2K Degrader-3 triggers rapid downregulation of eEF2K and produces a durable effect. eEF2K Degrader-3 inhibits TNBC cell proliferation, migration, and invasion, suppresses tumor growth and lung metastasis in mouse models, decreases vimentin and increases E-cadherin in organoids, and downregulates AURKA and SOX8 downstream of eEF2K degradation. eEF2K Degrader-3 can be used for research on triple-negative breast cancer (TNBC). | |||||||||||||||||||||
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