C23H25ClN4O2S
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. Synonym(s): (R)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate Biological Activity: (-)-JQ1 showed no inhibition of BRD4-dependent NMC cells. 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. Reference(s):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)
Warning(s): Avoid freeze/thaw cycles. Scientific Category: Bromodomain Product Type: Inhibitor Data shown is lot-specific. Contact us for specific information on other lots.>>> 更多资讯详情请访问蚂蚁淘商城
