Chemical structure of (+)-JQ1.
(+)-JQ1 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 1.09 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Store lyophilized at room temperature, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 2 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Molecular Weight: 457.0 g/mol
Molecular Formula: C23H25ClN4O2S
Solubility: Soluble in DMSO at 60 mg/ml or ethanol at 46 mg/ml.
(+)-JQ1 is a potent BET bromodomain inhibitor with IC50 values of 77 nM and 33 nM for BRD4 bromodomain 1 and BRD4 bromodomain 2, respectively. This small molecule competitively binds to the acetyl-lysine recognition pocket of BET bromodomains, which in turn displaces BET proteins from chromatin (1). The BET family of proteins are associated in many different cellular processes, including mitosis, viral/host interaction, and inflammatory gene expression (2-4). Studies have shown that (+)-JQ1 induced autophagy through LKB1/AMPK pathway activation can inhibit bladder cancer (BC) cell proliferation (5).
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