I-BET 151 dihydrochloride

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Cat.No. 4650 - I-BET 151 dihydrochloride | C23H21N5O3.2HCl | CAS No. 1883545-47-8
Description: BET bromodomain inhibitor; also promotes differentiation of hiPSCs into megakaryocytes
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
Purity: ≥98% (HPLC)
Citations (4)
Reviews (2)
Protocols (1)
Literature (5)

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. Also enhances fibroblast reprogramming to hiPSCs at low concentration.

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.

Compound Libraries

I-BET 151 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 488.37
Formula C23H21N5O3.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1883545-47-8
PubChem ID 170320
Smiles O=C(N3[C@H](C)C4=NC=CC=C4)NC2=C3C1=CC(OC)=C(C5=C(C)ON=C5C)C=C1N=C2.Cl.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 41.54 100
ethanol 41.54 100
water 48.84 100

Preparing Stock Solutions

The following data is based on the product molecular weight 488.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

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Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.05 mL 10.24 mL 20.48 mL
5 mM 0.41 mL 2.05 mL 4.1 mL
10 mM 0.2 mL 1.02 mL 2.05 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References are publications that support the biological activity of the product.

Dawson et al (2011) Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 478 529 PMID: 21964340

Feng et al (2014) Scalable generation of universal platelets from human induced pluripotent stem cells. Stem Cell Reports 3 817 PMID: 25418726

Shao et al (2016) Reprogramming by de-bookmarking the somatic transcriptional program through targeting of BET bromodomains. Cell Rep. 16 3138 PMID: 27653680

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

View Related Products by Product Action

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Keywords: I-BET 151 dihydrochloride, I-BET 151 dihydrochloride supplier, I-BET151, epigenetics, bet, bromodomains, inhibits, inhibitors, chromatin, recruitment, readers, antileukemia, MLL, fusion, induces, apoptosis, Bromodomains, ESCs, and, iPSC, 4650, Tocris Bioscience

4 Citations for I-BET 151 dihydrochloride

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

Xie et al (2018) β-actin regulates a heterochromatin landscape essential for optimal induction of neuronal programs during direct reprograming. PLoS Genet 14 e1007846 PMID: 30557298

Shao et al (2016) Reprogramming by De-bookmarking the Somatic Transcriptional Program through Targeting of BET Bromodomains. Cell Rep 16 3138 PMID: 27653680

Bowry et al (2018) BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication. Cell Rep 25 2061 PMID: 30463005

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

Reviews for I-BET 151 dihydrochloride

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By Anonymous on 06/22/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: U2OS

I-BET151 (1 μM)

I used short treatments with I-BET151 in the presence of JQ1.

PMID: 30463005
review image

Reprogramming media with i-BET.
By Anonymous on 02/23/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: ipsc

100 nM

PMID: 27653680
review image

Protocols for I-BET 151 dihydrochloride

The following protocol features additional information for the use of I-BET 151 dihydrochloride (Cat. No. 4650).

Literature in this Area

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Cancer Research Product Guide

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Stem Cell

Stem Cell Research Product Guide

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Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.


Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.