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Background: (-)-JQ1 is the inactive stereoisomer of the potent, cell-permeable, small moleculebromodomain inhibitor (+)-JQ1 that competitively binds to acetyl-lysine recognition motifs. (+)-JQ1competitively binds to the bromodomain displacing the BRD4 fusion oncoprotein from chromatin,which induces squamous differentiation and specific anti-proliferative effect in BRD4-dependent celllines and patient-derived xenograft models. However, study results have shown that (-)-JQ1 fails tosignificantly interact with any bromodomain tested and exhibits inhibition against BRD4(1) with andIC50 of 10,000 nM.
Biological Activity: (-)-JQ1 showed no inhibition of BRD4-dependent NMC cells.
CAS Number: 1268524-71-5
Solubility: Soluble in DMSO or ethanol at 100 mM
Storage Stability: Store at or below -80°C. Stable for less than 6 months when stored as directed.
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: Filippakopoulos, P., et al. Nature. 2010 Dec 23;468(7327):1067-73.Application Reference:
1. BET bromodomain inhibitors block growth of pancreatic cancer cells in three-dimensional collagen (2014)
2. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology (2014)
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