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Background Information:
I-BET726 (GSK1324726A) is a potent and selective, tetrahydroquinoline-based small molecule ligand binding to BET proteins with IC50s (FRET) of 7.4, 7.1, 7.0, and 7.3 nM for BRD2, BRD3 BRD4 and BRDT, respectively (Ref. 2), showing no binding potency towards other proteins.
Reference:
1. A Wyce, et al, BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models, PLoS One, 2013 Aug 23; 8(8).
2. R. Gosmini, et al, The Discovery of I-BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor, J Med Chem. 2014 Oct 9, 57(19), 8111-31.
3. A product with the highest standard in every aspect, manifested by HPLC-MS, Chiral HPLC, NMR, the optical rotation and quantitative elemental analysis.
APIM050334: I-BET726 (GSK1324726A)
CAS No.: 1300031-52-0.
Molecular Formula: C25H23ClN2O3.
Molecular Weight: 434.9.
Purity: 99.5% chem purity (HPLC), 100% optical purity (Chiral HPLC), [α]20D = +375 o (c 0.21, EtOH).
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Quantitative Microanalysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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