Catalog Number: 4650
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.
Technical Data
  • M.Wt:
    488.37
  • Formula:
    C23H21N5O3.2HCl
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol and to 100 mM in water
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    1883545-47-8
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline
Background References
  1. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
    Dawson et al.
    Nature, 2011;478:529
  2. Scalable generation of universal platelets from human induced pluripotent stem cells.
    Feng et al.
    Stem Cell Reports, 2014;3:817
Citations:

The citations listed below are publications that use Tocris products. Selected citations for I-BET 151 dihydrochloride include:

1 Citations: Showing 1 - 1

  1. GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1.
    Authors: Kumar Et al.
    Genes Dev 2015;5:9489

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