Chemical Name: 4-Acetyl-N-[5-[(diethylamino)sulfonyl]-2-hydroxyphenyl]-3-ethyl-5-methyl-1H-pyrrole-2-carboxamide
Biological ActivityBET bromodomain inhibitor (Kd values are 160, 170, 380, 490, 830 and 850 nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2) respectively). Also inhibits BRDT(1), CBP, p300 and BRDT(2) (Kd values are 1.2, 1.6, 2.6 and 3.7 μM respectively). Attenuates proliferation of HL-60 leukemia cells in vitro.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
4-Acyl pyrroles: mimicking acetylated lysines in histone code reading.
Lucas et al.
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