| Identification | Back Directory | [Name]
4(3H)-Quinazolinone, 2-[3,5-dimethyl-4-(3-oxetanyloxy)phenyl]-5,7-dimethoxy- | [CAS]
2644662-83-7 | [Synonyms]
BBC0403
4(3H)-Quinazolinone, 2-[3,5-dimethyl-4-(3-oxetanyloxy)phenyl]-5,7-dimethoxy- | [Molecular Formula]
C21H22N2O5 | [MOL File]
2644662-83-7.mol | [Molecular Weight]
382.41 |
| Chemical Properties | Back Directory | [Boiling point ]
589.8±60.0 °C(predicted) | [density ]
1.33±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
5.27±0.20(predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. BBC0403 exhibitS higher binding specificity for BRD2 compared to BRD3 and BRD4. BBC0403 has the potential for osteoarthritis (OA) research[1]. | [in vivo]
BBC0403 (5-10 μg/kg; i.a.; once per week; 6 weeks) prevents OA cartilage degradation in mice[1]. | Animal Model: | Male C57BL/6 mice (12?weeks old; 18-20?g) bearing osteoarthritis (OA)[1] | | Dosage: | 5 μg/kg, 10 μg/kg | | Administration: | Intra-articular (i.a.) injection; once per week; 6 weeks | | Result: | Prevented OA cartilage degradation in mice. |
| [IC 50]
BRD2 (BD2): 7.64 μM (Kd); BRD2 (BD1): 41.37 μM (Kd) | [References]
[1] Hyemi Lee, et al. BRD2-specific inhibitor, BBC0403, inhibits the progression of osteoarthritis pathogenesis in osteoarthritis-induced C57BL/6 male mice. Br J Pharmacol. 2024 Apr 10. DOI:10.1111/bph.16359 |
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