Catalog #: 27401
Size: 1 mg
MW: 457.0 Da
CAS Registry #: 1268524-70-4
Formula: C23H25ClN4O2S
(+)-JQ1 is a specific inhibitor of the BET family of acetyl-lysine recognition motifs, including the BRD2, BRD3, BRD4 and BRDT bromodomains.
BET inhibitor, Bromodomain inhibitor

≥95% by HPLC

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.
Soluble in DMSO or ethanol; insoluble in water.
A crystalline solid.
Storage / Stability:
Store at or below +4°C. Stable at least 6 months from date of receipt, when stored as directed.

Filippakopoulos, P., et al., Nature. 468(7327):1067-73 (2011).

Application Reference(s): 
1. The polycomb group protein BMI-1 inhibitor PTC-209 is a potent anti-myeloma agent alone or in combination with epigenetic inhibitors targeting EZH2 and the BET bromodomains (2017)
2. Analysis of Chromatin Opening in Heterochromatic Non-Small cell Lung Cancer Tumor-Initiating Cells in Relation to DNA-Damaging Antitumor Treatment (2017)
3. Notch Inhibition Enhances Cardiac Reprogramming by Increasing MEF2C Transcriptional Activity (2017)
4. Panobinostat acts synergistically with ibrutinib in diffuse large B cell lymphoma cells with MyD88 L265 mutations (2017)
5. Erratum: BRD4 is a histone acetyltransferase that evicts nucleosomes from chromatin (2017)
6. Targeting BET proteins improves the therapeutic efficacy of BCL-2 inhibition in T-cell acute lymphoblastic leukemia (2017)
7. Uncovering BRD4 hyperphosphorylation associated with cellular transformation in NUT midline carcinoma (2017)
8. Deacetylase inhibitors repress STAT5-mediated transcription by interfering with bromodomain and extra-terminal (BET) protein function (2015) 
9. GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1 (2015) 
10. BET bromodomain inhibitors block growth of pancreatic cancer cells in three-dimensional collagen (2014) 
11. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology (2014) 
12. BET bromodomain protein inhibition is a therapeutic option for medulloblastoma (2013)

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