Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 7-(3,5-dimethyl-4-isoxazolyl)-2-(methoxymethyl)-1-[(1R)-1-phenylethyl]-8-[(3S)-3-pyrrolidinylmethoxy]-1H-imidazo[4,5-c]quinoline
Purity: ≥95%
Formula Markup: C30H33N5O3
Formula Weight: 511.6
CAS Number: 2451862-42-1
Notes: GSK778 is a bromodomain 1 (BD1) inhibitor.{69901} It selectively inhibits BD1 in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and bromodomain testis-specific protein (BRDT; IC50s = 79.43, 39.81, 39.81, and 158.49 nM, respectively, in time-resolved FRET assays) over BD2 in BRD2, BRD3, BRD4, and BRDT (IC50s = 3,162, 1,000, 6,309, and >10,000 nM, respectively, in time-resolved FRET assays). GSK778 inhibits LPS-induced increases in IL-6 and chemokine (C-C motif) ligand 2 (CCL2) secretion from primary human peripheral blood mononuclear cells (PBMCs; IC50s = 63.12 and 50.12 nM, respectively). It inhibits the proliferation of MV4-11 acute myeloid leukemia cells (IC50 = 200 nM).
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