BBC0403 is a selective BRD2 inhibitor, exhibiting dissociation constants (K d) of 7.64 μM for BRD2 (BD2) and 41.37 μM for BRD2 (BD1). It demonstrates greater binding specificity to BRD2 over BRD3 and BRD4, making it a potential candidate for research in osteoarthritis (OA).

BRD2 (BD2):7.64 μM (Kd), BRD2 (BD1):41.37 μM (Kd)

BBC0403, at concentrations of 5μM, 10μM, and 20μM over 12 hours, can reduce the expression of catabolic factors, the production of prostaglandin E2 (PGE2), and the degradation of the extracellular matrix (ECM). It prevents osteoarthritis (OA) by inhibiting NF-κB and MAPK signaling pathways [1].

BBC0403 (5-10 μg/kg; intra-articular injection; once per week; 6 weeks) effectively inhibits cartilage degradation in mice with osteoarthritis (OA) [1]. Animal Model: Male C57BL/6 mice (12 weeks old; 18-20 g) diagnosed with OA [1] Dosage: 5 μg/kg, 10 μg/kg Administration: Intra-articular (i.a.) injection once weekly for a duration of 6 weeks Outcome: Successfully prevented OA cartilage degradation in the subjects.