NRX-0492

• Target:

  BTK|||Others|||PROTACs

• Related Pathways:

  Others|||Tyrosine Kinase/Adaptors|||PROTAC|||Angiogenesis

• Bioactivity:

  NRX-0492 is an orally administered compound that efficiently degrades Bruton's 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 [1].

• Smiles:

  O=C1C=2C (C (=O) N1C3C (=O) NC (=O) CC3) =CC=C (C2) N4C[C@H] (CN5CCC (CC5) C6=CC=C (NC7=NC (=CN=C7C (N) =O) N8C[C@@H] (CCC8) N9CCN (C) C9=O) C=C6) CC4

• Molecular Formula:

  C43H51N11O6

• Molecular Weight:

  817.94

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  2416130-57-7