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.
