I-BET 151 dihydrochloride
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 ActivityI-BET 151 dihydrochloride is a 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. Also enhances fibroblast reprogramming to hiPSCs at low concentration.
For more information about how I-BET 151 dihydrochloride may be used, see our protocol: Transdifferentiating Fibroblasts into Neurons.
External Portal InformationChemicalprobes.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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
Dawson et al.
Scalable generation of universal platelets from human induced pluripotent stem cells.
Feng et al.
Stem Cell Reports, 2014;3:817
Reprogramming by de-bookmarking the somatic transcriptional program through targeting of BET bromodomains.
Shao et al.
Cell Rep., 2016;16:3138
Citations for I-BET 151 dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for I-BET 151 dihydrochloride include:
7 Citations: Showing 1 - 7
Epigenetic inactivation of the 5-methylcytosine RNA methyltransferase NSUN7 is associated with clinical outcome and therapeutic vulnerability in liver cancer.
Authors: Fernando Et al.
Mol Cancer 2023;22:83
CRISPR-based gene knockout screens reveal deubiquitinases involved in HIV-1 latency in two Jurkat cell models.
Authors: Pengfei Et al.
Sci Rep 2020;10:5350
BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication.
Authors: Bowry Et al.
Cell Rep 2018;25:2061
β-actin regulates a heterochromatin landscape essential for optimal induction of neuronal programs during direct reprograming.
Authors: Xie Et al.
PLoS Genet 2018;14:e1007846
Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and Lysosomal Function.
Authors: Scott W Et al.
Mol Cell 2017;66:517-532.e9
Reprogramming by De-bookmarking the Somatic Transcriptional Program through Targeting of BET Bromodomains.
Authors: Shao Et al.
Cell Rep 2016;16:3138
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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