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:

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

Reference:

Other Information:

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