JQ1 is a potent BET bromodomain inhibitor. IC₅₀ = 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively (data for + isomer). Competitive binding by JQ1 displaces the BRD4 fusion oncoprotein from chromatin, prompting squamous differentiation and specific antiproliferative effects in BRD4-dependent cell lines and patient-derived xenograft models. Induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts. Blocks inflammation and bone loss in periodontitis⁴. Displays reversible contraceptive effects in male mice. Note this product is racemic (+/-) making the IC₅₀ nominally 2 fold greater than literature values for the (+) isomer.

Physical Properties: White powder

MW=457.0 C₂₃H₂₅ClN₄O₂S

Analysis: >98% (TLC); NMR (Conforms)

Solubilization: May be dissolved in DMSO (40 mg/ml); or ethanol (40 mg/ml)

Storage: Store desiccated as supplied at ambient temperature for up to 1 year. Store solutions at -20°C for up to two months.