I-BET151 (GSK1210151A)

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I-BET151 (GSK1210151A)

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).

Catalog NO:	CT-BET151
Synonym:	GSK1210151A
CAS NO:	1300031-49-5
Mol. Formula:	C₂₃H₂₁N₅O₃
MW:	415.4

** in vivo Quality Material. The Optically pure source (ref 3). 99% by Achiral and Chiral HPLCs. Hydrate, validated by a spot-on quantitative elemental analysis. Bulk Stock! Prompt

Pricing and OrderingTechnical Data

QC & Certificates

References

NO	Size	Price	In Stock
1	10 mg	$100.00	YES
2	50 mg	$280.00	YES
3	100 mg	$450.00	YES
4	200 mg	$750.00	YES

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Solubility : Soluble in DMSO

Storage : Store at 0 °C (short term), -20 °C (long term), desiccated

Purity : >99% by Achiral and Chiral HPLCs

Original QC Data : HPLC-MS, ¹H-NMR, Chiral HPLC, and Quantitative Elemental Analysis Report

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I-BET151, Lot 06, Certificate of Analysis.pdf

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)

3*. 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 10-15% wrong isomer, thus gives the optical purity as low as 80-70%), is being offered by many other vendors, who won’t report their optical purity (too poor to report).