Loading... Please wait...

Our Newsletter


GSK1210151A (I-BET 151) | BRD2/3/4 inhibitor

  • GSK1210151A (I-BET 151).jpg
  • GSK1210151A (I-BET 151), 400x400px, png
Price:
$109.00
Catalog #:
C4121-5
Quantity:


Product Description

GSK1210151A (I-BET151) is an orally-available, imidazolonoquinoline-based inhibitor of the BET family of bromodomains, active against BRD2, BRD3, and BRD4 at IC50s of 500, 250, and 800 nM, respectively. It is also a potent upregulator of ApoA1 with an EC170 of 100 nM. [1]

GSK1210151A was shown to have profoudn 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 partly due to the inhibition of transcrdiption of key genes (BCL2, C-MYC, and CDK6) through the displacement of BRD3/4, PAFc, and SEC components through chromatin. [2]

Because ApoA1 upregulation is often associated with anti-inflammatory properties in non hepatic cells, GSK1210151A was tested and shown to exhibit a dose-dependent inhibition of both IL-6 and TNFa production in LPS-stimulated human PBMCs. [3]


Technical information:

Chemical Formula:   C23H21N5O3
CAS #:   1300031-49-5
Molecular Weight:   415.44
Purity:   > 98%
Appearance:   White
Chemical Name:   7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one
Solubility:   Up to 22 mM in DMSO
Synonyms:   GSK-1210151A, GSK1210151A, I-BET151, I-BET 151, 1300031-49-5

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Seal et al., Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). Bioorg. Med. Chem. Lett. 2012, 22, 2968-2972. Pubmed ID: 22437115
2. Dawson et al., Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 2011, 478, 529-533. Pubmed ID: 21964340
3. Mirguet et al., From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151. Bioorg. Med. Chem. Lett. 2012, 22, 2963-2967. Pubmed ID: 22386529

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

Find Similar Products by Category

Write your own product review

Product Reviews

This product hasn't received any reviews yet. Be the first to review this product!

Add to Wish List

Click the button below to add the GSK1210151A (I-BET 151) | BRD2/3/4 inhibitor to your wish list.

You Recently Viewed...