Bromodomain Inhibitor, (+)-JQ1

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Application
Blocking Reagent (BR), Inhibition Assay (InhA)
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Purpose A potent and highly specific BET inhibitor
Characteristics A potent and highly specific inhibitor for the BET (bromodomain and extra-terminal) family of bromodomains. (+)-JQ1 binds to BRD4 bromodomains 1 and 2 with kDavalues of approx. 50 and 90 nM, respectively. The binding is competitive with acetyl lysine. (+)-JQ1 can be a useful chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis.
Purity ≥ 98 % by HPLC
Chemical Name t-Butyl-2-((6S)-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
Formula C₂₃H₂₅ClN₄O₂S
Permeability Cell-permeable
Solubility DMSO (10 mM)
Molecular Weight 456.99 g/mol
CAS-No 1268524-70-4
Restrictions For Research Use only
Format Solid
Handling Advice Protect from air and moisture
Storage -20 °C
Expiry Date 24 months
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Product cited in: Gupta, Maetzig, Maertens, Sharif, Rothe, Weidner-Glunde, Galla, Schambach, Cherepanov, Schulz: "Bromo- and extraterminal domain chromatin regulators serve as cofactors for murine leukemia virus integration." in: Journal of virology, Vol. 87, Issue 23, pp. 12721-36, 2013 (PubMed).