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Biological Activity:

MS436 is a potent and selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively. It effectively inhibits BRD4 activity in NF-κB-directed production of nitric oxide and proinflammatory cytokine interleukin-6 in murine macrophages without siginificanty inhibition on cell viability. MS436 represents a new class of bromodomain inhibitors to study the functional differences of the two bromodomains of BRD4

How to Use:

In vitro: MS436 was used at 10-100 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Zhang G, et al. Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. (2013) J Med Chem. 56(22):9251-64.