I-BET762 - Molibresib | GSK525762

Based on 212 reference(s) in Google Scholar 8 10 212

Axon 4134

CAS [1260907-17-2]

MF C22H22ClN5O2
MW 423.90

  • Purity: 99%
  • Optical purity: >99% e.e.
  • Soluble in DMSO



I-BET762 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.

Keywords: I-BET762 | Supplier | BET bromodomain inhibitor | Molibresib | GSK525762 | I-BET 762 | I-BET-762 | GSK-525762 | GSK 525762 | CT-BET762 | CAS [1260907-17-2] | Histone | BET (BRD) | Inhibitor | Proteins

The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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