Bromosporine

Description: Bromosporine is a novel, potent and broad spectrum inhibitor against BET bromodomains with potential use as a chemical probe for bromodomain functional assays. It inhibits BRD2, BRD4, BRD9 and CECR2 with IC50s of 0.41 uM, 0.29 uM, 0.122 uM and 0.017 uM, respectively. Bromodomains (BRDs) are protein interaction modules that read epigenetic marks recognizing epsilon-N-lysine acetylation motifs. Bromodomains is a 110 amino acid protein domain which can recognize monoacetylated lysine residues and play a pivotal role in the targeting of chromatin-modifying enzymes to specific sites. It has been revealed that proteins contained BRDs involves in the development of many diseases, including cancers, inflammatory diseases and neurological diseases.

References: http://www.thesgc.org/chemical-probes/bromosporine

Synonym: Bromosporine

Ethyl (3-methyl-6-(4-methyl-3-(methylsulfonamido)phenyl)-[1, 2, 4]triazolo[4, 3-b]pyridazin-8-yl)carbamate

InChi Key: UYBRROMMFMPJAN-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H20N6O4S/c1-5-27-17(24)18-15-9-14(21-23-11(3)19-20-16(15)23)12-7-6-10(2)13(8-12)22-28(4, 25)26/h6-9, 22H, 5H2, 1-4H3, (H, 18, 24)

SMILES Code: O=C(OCC)NC1=CC(C2=CC=C(C)C(NS(=O)(C)=O)=C2)=NN3C1=NN=C3C