BRD4 Inhibitor-38 (Compound 25) is an orally active BRD4 inhibitor with IC50 values of 3.64 μM and 0.12 μM for BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-38 has anti-inflammatory activity with an IC50 value of 1.98 μM for nitric oxide (NO) production.

Physicochemical Properties

Molecular Formula	C19H18N2O4
Molecular Weight	338.36
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	BRD4 BD1 3.64 μM (IC50); BRD4 BD2 0.12 μM (IC50)
ln Vitro	BRD4 Inhibitor-38 (Compound 25) (2.5-20 μM; 2 h) exhibits anti-inflammatory activity in Raw 264.7 and THP-1 cells [1].
ln Vivo	BRD4 Inhibitor-38 (Compound 25) (25-100 mg/kg; po; single dose) exhibits anti-inflammatory activity in a mouse model of acute inflammation induced by LPS (10 mg/kg; Single dose) [1].
Cell Assay	Real Time qPCR[1] Cell Types: Raw 264.7, THP-1 Tested Tested Concentrations: 2.5, 5, 10, 20 μM Incubation Duration: 2 h (stimulated with LPS (1 μg/mL) and LPS (100 ng/mL) + IFN-γ (20 ng/mL) for 6 h. note: Compound 25 were pre-treated for 2 h before stimulating with LPS for 6 h.) Experimental Results: Inhibited the mRNA expression of LPS-induced IL-6 and TNF-α in a dependent manner.
Animal Protocol	Animal/Disease Models: LPS-induced mouse model of acute inflammation[1]. Doses: 25, 50, 100 mg/kg Route of Administration: Oral administration (p.o.)，single dose. After LPS treatment (10mg/kg; Single dose) Experimental Results: Significantly inhibited the increase of inflammatory genes IL-6 and TNF-α at doses of 50 and 100 mg/kg. Alleviated lung tissue edema, damage, and lung hemorrhage. Mitigated kidney damage, significantly increased the proportion of normal renal tubules, improved the internal brush border structure, reduced renal interstitial inflammatory cell infiltration, and decreased the number of interstitial vacuoles at a dose of 100 mg/kg.
References	[1]. Marine natural product-inspired discovery of novel BRD4 inhibitors with anti-inflammatory activityJ. European Journal of Medicinal Chemistry, 2024: 117193.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.9554 mL	14.7772 mL	29.5543 mL
	5 mM	0.5911 mL	2.9554 mL	5.9109 mL
	10 mM	0.2955 mL	1.4777 mL	2.9554 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.