An isoxazole class pan-BET family inhibitor

I-BET151 – 10 mg

Brand:
Cayman
CAS:
1300031-49-5
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

The bromodomain and extra terminal domain (BET) family of proteins including BRD2, BRD3, and BRD4 play 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.{26201} I-BET151 is an isoxazole class pan-BET family inhibitor, blocking BRD2, BRD3, and BRD4 with IC50 values of 0.5, 0.25, and 0.79 µM, respectively.{20183,25295,22883,28490} Through this action, it blocks the growth of leukemic cell lines driven by mixed lineage leukemia (MLL) fusions at nanomolar concentrations, whereas tyrosine kinase activated cells were much less sensitive.{20182} Specifically, I-BET151 induces apoptosis via reduced expression of BCL2 or triggers G0/G1 cell cycle arrest in MLL-fusion cell lines.{20182} I-BET151 is effective in vivo, suppressing MLL leukemia progression in two different mouse models.{20182}  

 

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SKU: 11181 - 10 mg Category:

Description

An isoxazole class pan-BET family inhibitor, blocking BRD2, BRD3, and BRD4 with IC50 values of 0.5, 0.25, and 0.79 µM, respectively); induces apoptosis or triggers G0/G1 cell cycle arrest in MLL-fusion cell lines; effective in vivo, suppressing MLL leukemia progression in two different mouse models

Formal name: 7,3,5-dimethyl-4-isoxazolyl-1,3-dihydro-8-methoxy-1-[1R-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one

Synonyms:  GSK1210151A

Molecular weight: 415.5

CAS: 1300031-49-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Chromatin Reader Interactions||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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