Phone: 1-617-401-8149
Fax: 1-617-606-5019
Email: message@sydlabs.com
Or leave a message with a formal purchase
order (PO) Or credit card.
| Catalog No. | Product Name | Size | List Price (US$) | Quantity |
|---|
Price/availability/specifications subject to change without notice. Unless otherwise indicated, our catalog and customized products are for research use only and not intended for human or animal diagnostic or therapeutic use.
Phone: 1-617-401-8149
Fax: 1-617-606-5019
Email: message@sydlabs.com
Or leave a message with a formal purchase
order (PO) Or credit card.
Background Information:
The Bromodomain and Extra Terminal domain (BET), a family of four proteins that selectively recognize and bind to acetylated lysine residues in histone, plays a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. BET proteins stimulate transcription by recruiting specific types of proteins, for example the super elongation complex (SEC), to chromatin, leading to stimulation of transcriptional elongation of certain target genes including oncogenes and pro-inflammatory cytokines. Targeting BET proteins and displacing them could provide a method of inducing cell cycle arrest and even cell death of defectively programmed cells. I-BET151, a small molecule inhibitor that interacts with BRD4 and BRD3 BET proteins and displaces them from chromatin, has profound efficacy against human and murine MLL-fusion leukemic cell lines, through the induction of early cell cycle arrest and apoptosis. The mode of action is, at least in part, due to suppressing the transcription of key genes (BCL2, C-MYC and CDK6) that are critical for MLL-fusion leukemia maintenance (Ref. 1).
Reference:
1. M. A. Dawson, et al, Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia, Nature, 478, 529–533(27 October 2011).
2. All pharmacological parameters of this compound (I-BET151) are based on a single isomer (optically pure R-enantiomer), thus a compound with adequate optical purity (confirmed by Chiral HPLC) is required for an uncompromised high quality research. Buyer Beware: Partially racemized I-BET151 (up to 15% wrong isomer, thus give the optical purity as low as 85%), is being offered by many other vendors, who won’t report their optical purity (too poor to report).
APIM050333: I-BET151 (GSK1210151A) -- OPTICALLY PURE SOURCE
CAS No.: 1300031-49-5.
Molecular Formula: C23H21N5O3.
Molecular Weight: 415.4.
Purity: >99.5% (achiral HPLC at 214 and 254 nm), 100% optical purity (chiral HPLC).
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
Copyright © 2009-2022 sydlabs.com. All rights reserved.
Use of this website means that you have read, understood, and accepted the Syd Labs Privacy Policy and Terms & Conditions.