I-BET762 (MOLIBRESIB) (GSK525762)

Background Information:

I-BET762 (Molibresib) (GSK525762) is a cell-permeable
benzodiazepine-based inhibitor of BET (bromodomain and extra terminal
domain) proteins, BRD2, BRD3 and BRD4, binds to the tandem bromodomains
of BET with Kd of 50.5–61.3 nM, displacing a tetra-acetylated H4 peptide
prebound to tandem bromodomains of BET with IC50 of 32.5–42.5 nM in
FRET analysis. I-BET-762 occupies the acetyl-lysine binding pocket of
BET proteins and inhibits binding of BET proteins to acetylated
histones, thus disrupts the formation of the chromatin complexes
essential for expression of inflammatory genes.

Reference:

1. Olivier Mirguet, et al., Discovery of Epigenetic Regulator
I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of
the BET Bromodomains, J. Med. Chem., 2013, 56 (19), pp 7501–7515.
2. A. Chaidos, et al., Potent antimyeloma activity of the novel
bromodomain inhibitors I-BET151 and I-BET762, Blood, 2014, vol. 123 no.
5, 697-705.
3. A product with the highest standard in every aspect, manifested by
HPLC-MS, Chiral HPLC, NMR and Quantitative Elemental Analysis.

APIM050335: I-BET762 (MOLIBRESIB) (GSK525762)

CAS No.: 1260907-17-2.
Molecular Formula: C₂₂H₂₂ClN₅O₂ ? 0.2H₂O.
Molecular Weight: 427.5.
Purity: ≥99.5% (HPLC at 214 and 254 nm), 100% optical purity (Chiral HPLC).
QC: HPLC-MS, ¹HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO, Ethanol.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.