I-BET 151 dihydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 4650
BET bromodomain inhibitor; also promotes differentiation of hiPSCs into megakaryocytes
Key Product Details
Description
BET bromodomain inhibitor; also promotes differentiation of hiPSCs into megakaryocytes
Product Description
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. Used in protocol to differentiate fibroblasts directly into neurons (see below).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 GlaxoSmithKlineExternal 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.Product Specifications
Molecular Weight
488.37
Formula
C23H21N5O3.2HCl
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 48.84 | 100 | |
| DMSO | 41.54 | 100 | |
| Ethanol | 41.54 | 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for I-BET 151 dihydrochloride
For research use only
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