BBC0403 is a selective BRD2 inhibitor with Kd of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. BBC0403 has higher selectivity for BRD2 than BRD3 and BRD4. BBC0403 has potential for osteoarthritis (OA) research.

Physicochemical Properties

Molecular Formula	C21H22N2O5
Molecular Weight	382.41
CAS #	2644662-83-7
Appearance	Solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	BRD2 (BD2) 7.64 μM (Kd) BRD2 (BD1) 41.37 μM (Kd)
ln Vitro	BBC0403 (5μM, 10μM and 20μM, 12 hours) reduces the expression of catabolic factors, the production of prostaglandin E2 (PGE2) and the degradation of the extracellular matrix (ECM). BBC0403 prevents OA by inhibiting NF-κB and MAPK signaling[1].
ln Vivo	BBC0403 (5-10 μg/kg; intra-articular injection; once a week; 6 weeks) prevents cartilage degradation in OA mice [1].
Animal Protocol	Animal/Disease Models:Male C57BL/6 mice (12 weeks old; 18-20 g) bearing osteoarthritis (OA)[1] Doses: 5 μg/kg, 10 μg/kg Route of Administration: Intra-articular (i.a.) injection; once per week; 6 weeks Experimental Results: Prevented OA cartilage degradation in mice.
References	[1]. BRD2-specific inhibitor, BBC0403, inhibits the progression of osteoarthritis pathogenesis in osteoarthritis-induced C57BL/6 male mice. Br J Pharmacol. 2024 Apr 10.

Solubility Data

Solubility (In Vitro)

DMSO : 25 mg/mL (65.37 mM; with sonication (<60°C))

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.54 mM)(Saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then add 450 μL saline to make it 1 mL. *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.54 mM)(saturation unknown) in 10% DMSO 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6150 mL	13.0750 mL	26.1499 mL
	5 mM	0.5230 mL	2.6150 mL	5.2300 mL
	10 mM	0.2615 mL	1.3075 mL	2.6150 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.