Chemical Name: 7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydroxy-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one dihydrochloride
Biological Activity BET bromodomain inhibitor; blocks recruitment of BET to chromatin. Induces apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic cell lines in vitro (IC50 values are 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively); reduces BCL2 expression in NOMO1 cells. Improves survival in two rodent models of MLL-fusion leukemia in vivo. Enhances differentiation of human iPSC into megakaryocytes.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of I-BET 151 is reviewed on the chemical probes website.
Soluble to 100 mM in DMSO and to 100 mM in ethanol and to 100 mM in water
Store at -20°C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
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Sold for research purposes under agreement from GlaxoSmithKline
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