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Biological Activity: (+)-JQ1 has been shown to inhibit BRD4 (BD1) with a Kd of 50 nM, and BRD4 (BD2) with a Kd of 90 nM.
CAS Number: 1268524-70-4
Description: (+)-JQ1 is a specific inhibitor of the BET family of acetyl-lysine recognition motifs, including the BRD2, BRD3, BRD4 and BRDT bromodomains.
Format: A crystalline solid
Purity: ≥95% by HPLC
Solubility: Soluble in DMSO or ethanol; insoluble in water.
Storage Stability: Store at or below +4°C. Stable at least 6 months from date of receipt, when stored as directed.
Biosafety Level: Not applicable (BSL-1)
References: Filippakopoulos P., et al. Nature. 468(7327):1067-73 (2011).Application Reference:1. Pinz, S., et al. Nucleic Acids Res. 2015 Apr 20;43(7):3524-45. "Deacetylase inhibitors repress STAT5-mediated transcription by interfering with bromodomain and extra-terminal (BET) protein function"
2. GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1 (2015)
3. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology (2014)
4. BET bromodomain protein inhibition is a therapeutic option for medulloblastoma (2013)
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