NRX-0492 is an orally administered compound that efficiently degrades Brutons tyrosine kinase (BTK) by catalyzing its ubiquitylation and subsequent proteasomal degradation, achieving half-maximal degradation concentrations (DC50) of 0.2 nM and 90% degradation concentrations (DC90) of 0.5 nM. Additionally, NRX-0492 suppresses B-cell receptor (BCR) signaling, transcriptional activities, and chemokine production by linking a noncovalent BTK-binding domain to Cereblon, an adaptor protein within the E3 ubiquitin ligase complex.
Molekulargewicht:
817.94
CAS Nummer:
[2416130-57-7]
Formel:
C43H51N11O6
Target-Kategorie:
Others,BTK
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