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Submit ReviewI-BET 151 dihydrochloride
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)
Biological Activity for I-BET 151 dihydrochloride
I-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.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
External Portal Information for I-BET 151 dihydrochloride
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 for I-BET 151 dihydrochloride
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 for I-BET 151 dihydrochloride
| M. Wt | 488.37 |
| Formula | C23H21N5O3.2HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1883545-47-8 |
| PubChem ID | 170320 |
| InChI Key | IQOJZZHRYSSFJM-UHFFFAOYSA-N |
| 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 for I-BET 151 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.54 | 100 | |
| ethanol | 41.54 | 100 | |
| water | 48.84 | 100 |
Preparing Stock Solutions for I-BET 151 dihydrochloride
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.
| 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 for I-BET 151 dihydrochloride
References for I-BET 151 dihydrochloride
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.
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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
7 Citations for I-BET 151 dihydrochloride
Citations are publications that use Tocris products. Selected citations for I-BET 151 dihydrochloride include:
Scott W et al (2017) Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and Lysosomal Function. Mol Cell 66 517-532.e9 PMID: 28525743
Bowry et al (2018) BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication. Cell Rep 25 2061 PMID: 30463005
Pengfei et al (2020) CRISPR-based gene knockout screens reveal deubiquitinases involved in HIV-1 latency in two Jurkat cell models. Sci Rep 10 5350 PMID: 32210344
Shao et al (2016) Reprogramming by De-bookmarking the Somatic Transcriptional Program through Targeting of BET Bromodomains. Cell Rep 16 3138 PMID: 27653680
Fernando et al (2023) Epigenetic inactivation of the 5-methylcytosine RNA methyltransferase NSUN7 is associated with clinical outcome and therapeutic vulnerability in liver cancer. Mol Cancer 22 83 PMID: 37173708
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
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? Please let us know.
Reviews for I-BET 151 dihydrochloride
Average Rating: 5 (Based on 2 Reviews.)
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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.
Reprogramming media with i-BET.
By
Anonymous on 02/23/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: ipsc
100 nM
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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Stem Cell Research Product Guide
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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.
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