I-BET 151 dihydrochloride

Name: I-BET 151 dihydrochloride
Brand: Tocris Bioscience
SKU: 4650
Rating: 5 (2 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 4650

(2)

Citations (9)

COA / SDS

BET bromodomain inhibitor; also promotes differentiation of hiPSCs into megakaryocytes

Key Product Details

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)
Molecular Weight:	488.37

View Full Technical Details for I-BET 151 dihydrochloride

Technical Data
Citations / Reviews (2)

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

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.

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 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 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	4.10 mL
10 mM	0.20 mL	1.02 mL	2.05 mL
50 mM	0.04 mL	0.20 mL	0.41 mL

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References for I-BET 151 dihydrochloride

References are publications that support the biological activity of the product.

Feng Scalable generation of universal platelets from human induced pluripotent stem cells. Stem Cell Reports 2014 PMID: 25418726
Shao Reprogramming by de-bookmarking the somatic transcriptional program through targeting of BET bromodomains. Cell Rep. 2016 PMID: 27653680
Dawson Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 2011 PMID: 21964340