I-BET726 (GSK1324726A)

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: C₂₅H₂₃ClN₂O_3.
Molecular Weight: 434.9.
Purity: 99.5% chem purity (HPLC), 100% optical purity (Chiral HPLC), [α]²⁰_D = +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.