JQ1 is a potent BET bromodomain inhibitor. IC₅₀ = 17.7, 32.6, 76.9 and 12942 nMrespectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) andCREBBP respectively (data for + isomer). Competitivebinding by JQ1 displaces the BRD4 fusion oncoprotein from chromatin, promptingsquamous differentiation and specific antiproliferative effects inBRD4-dependent cell lines and patient-derived xenograft models. Inducessquamous differentiation in NMC cell lines and inhibits tumor growth in NMCxenografts. Blocks inflammation and bone loss in periodontitis⁴.Displays reversible contraceptive effects in male mice. Note thisproduct is racemic (+/-) making the IC₅₀ nominally 2 fold greaterthan 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 assupplied at ambient temperature for up to 1 year. Store solutions at -20°C forup to two months.