I-BET 151 dihydrochloride

Cat. No. 4650

I-BET 151 dihydrochloride C23H21N5O3.2HCl [1883545-47-8]

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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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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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.

If you know of a relevant reference for I-BET 151 dihydrochloride please let us know.

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.

Do you know of a great paper that uses I-BET 151 dihydrochloride from Tocris? If so please let us know.

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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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