Drug intelligence / Profile preview

bromosporine

Development stage
Preclinical
Lead developer
Structural Genomics Consortium
Modality
Small Molecules
Administration
Experimental (in Vitro Studies)
01

Overview

Bromosporine is a **broad-spectrum, non-selective inhibitor of bromodomains**, including the BET (bromodomain and extra-terminal) family. It acts through binding the acetyllysine recognition site of bromodomains, interfering with their ability to "read" epigenetic marks and thereby modulating expression of genes involved in processes such as cell proliferation, differentiation, and energy homeostasis. Bromosporine potently **reactivates latent HIV-1 from latency in cellular models**, likely by modulating CDK9 phosphorylation via Tat, and exhibits low cytotoxicity in primary T cells at relevant concentrations. It has been widely used as a chemical probe in epigenetics and cancer research[1][4][5][6][8].

Other names
ethyl N-[6-(3-methanesulfonamido-4-methylphenyl)-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-yl]carbamateCarbamic acid, N-[3-methyl-6-[4-methyl-3-[(methylsulfonyl)amino]phenyl]-1,2,4-triazolo[4,3-b]pyridazin-8-yl]-, ethyl esterethyl (3-methyl-6-(4-methyl-3-(methylsulfonamido)phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-8-yl)carbamateBSP
02

Targets

BPTF (Bromodomain PHD finger transcription factor)BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)BRD4 (Bromodomain-containing protein 4)BRD7 (Bromodomain-containing protein 7)BRD9 (Bromodomain-containing protein 9)CREBBP (CREB-binding protein)

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