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NRX-0492

Product Specifications

CAS Number

2416130-57-7

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

Product Datasheet

https://www.targetmol.com/attachment/DataSheet/64416115505233965/T75133

Available Sizes

Curated Selection

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