Cat. No. 5331
Chemical Name: (6S)-4-(4-Chlorophenyl)-2,3,9-trime
Biological ActivityBET bromodomain inhibitor. Downregulates Myc expression, causes G1 cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. Arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM). Also enhances the antitumor effect of rapamycin (Cat. No. 1292) in vitro and attenuates rapamycin induced Akt activation. Orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Wong et al (2014) The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors. Cell Death Dis. 5 e1450. PMID: 25299775.
King et al (2013) The ubiquitin ligase FBXW7 modulates leukemia-initiating cell activity by regulating MYC stability. Cell 153 1552. PMID: 23791182.
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Keywords: CPI 203, supplier, CPI203, BET, BRD4, domain, inhibitors, inhibits, (+)-JQ1, analogue, analog, 4499, Myc, G1, cell, cycle, arrest, antitumor, rapamycin, AKT, Tocris Bioscience, Bromodomain Inhibitor products
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