I-BET 151 dihydrochloride
Cat. No. 4650
Chemical Name: 7-(3,5-Dimethyl-4-isoxazolyl)-1,3-d
Biological ActivityBET 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.
Licensing InformationSold for research purposes under agreement from GlaxoSmithKline
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.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Feng et al (2014) Scalable generation of universal platelets from human induced pluripotent stem cells. Stem Cell Reports 3 817. PMID: 25418726.
Dawson et al (2011) Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 478 529. PMID: 21964340.
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Citations are publications that use Tocris products. Selected citations for I-BET 151 dihydrochloride include:
Kumar et al (2015) GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1. Genes Dev 5 9489. PMID: 25807524.
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Keywords: I-BET 151 dihydrochloride, supplier, I-BET151, epigenetics, bet, bromodomains, inhibits, inhibitors, chromatin, recruitment, readers, antileukemia, MLL, fusion, induces, apoptosis, Tocris Bioscience, Bromodomain Inhibitor products
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