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Table 1 Hits from the epigenetic modifier screen

From: BET bromodomain inhibitors and agonists of the beta-2 adrenergic receptor identified in screens for compounds that inhibit DUX4 expression in FSHD muscle cells

Compound

% inhibition of ZSCAN4 reporter

% inhibition of Renilla luciferase

Mechanism

(+)-JQ1

99 (1 μMa)

27 (1 μMa)

BET bromodomain inhibitor

PFI-1

89 (1 μMa)

0 (1 μMa)

BET bromodomain inhibitor

SGC-CBP30

75 (1 μMa)

24 (1 μMa)

CBP/p300 bromodomain inhibitor

Bromosporine

92 (2 μMa)

9 (2 μMa)

Pan-bromodomain inhibitor

  1. aConcentration of compound used in the assay