Bioactivity | NRX-0492 is an orally active and potent degrader of BTK. NRX-0492 catalyzes ubiquitylation and proteasomal degradation of BTK with DC50≤0.2 nM and DC90≤0.5 nM, respectively. NRX-0492 inhibits B-cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion. Moreover, NRX-0492 also links a noncovalent BTK-binding domain to Cereblon. Cereblon is an adaptor protein of the E3 ubiquitin ligase complex[1]. |
Name | NRX-0492 |
CAS | 2416130-57-7 |
Formula | C43H51N11O6 |
Molar Mass | 817.94 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Zhang D, et al. NRX-0492 degrades wild-type and C481 mutant BTK and demonstrates in vivo activity in CLL patient-derived xenografts. Blood. 2023 Mar 30;141(13):1584-1596. |