NEK7 degrader-3 is an orally active and brain-penetrant NEK7 molecular glue degrader with a DC 50 of 33.1 nM. NEK7 degrader-3 mediates interaction between NEK7 and E3 ligase cereblon , promoting proteasomal degradation of NEK7 and attenuating NLRP3 inflammasome-mediated inflammatory responses. NEK7 degrader-3 inhibits caspase-1 activity, cytokine release of IL-1β , IL-1α , and IL-18 , and pyroptosis -related plasma membrane permeabilization. NEK7 degrader-3 shows antiinflammatory activity in an LPS ( HY-D1056 )-induced neuroinflammation mouse model. NEK7 degrader-3 can be used for the research of neuroinflammation.
Products | Products > Disease Areas > Neurological, Eye or Ear Disease | Products > Disease Areas > Inflammation or Immune System Disease | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Cell Cycle/DNA Damage | Products > Signaling Pathways > Immunology/Inflammation | Products > Signaling Pathways > Apoptosis | Products > Research Areas > Neurological Disease | Products > Research Areas > Inflammation/Immunology | Products > Signaling Pathways > Interleukin Related | Products > Signaling Pathways > Pyroptosis | Products > Signaling Pathways > Molecular Glues | Products > Signaling Pathways > NEKs | Products > Signaling Pathways > NOD-like Receptor (NLR) | Products > Signaling Pathways > Caspase
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