《An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains》 was published in Angewandte Chemie, International Edition in 2019. These research results belong to D’Ascenzio, Melissa; Pugh, Kathryn M.; Konietzny, Rebecca; Berridge, Georgina; Tallant, Cynthia; Hashem, Shaima; Monteiro, Octovia; Thomas, Jason R.; Schirle, Markus; Knapp, Stefan; Marsden, Brian; Fedorov, Oleg; Bountra, Chas; Kessler, Benedikt M.; Brennan, Paul E.. Product Details of 53085-52-2 The article mentions the following:
Bromodomain-containing proteins are epigenetic modulators involved in a wide range of cellular processes, from recruitment of transcription factors to pathol. disruption of gene regulation and cancer development. Since the druggability of these acetyl-lysine reader domains was established, efforts were made to develop potent and selective inhibitors across the entire family. Here we report the development of a small mol.-based approach to covalently modify recombinant and endogenous bromodomain-containing proteins by targeting a conserved lysine and a tyrosine residue in the variable ZA or BC loops. Moreover, the addition of a reporter tag allowed in-gel visualization and pull-down of the desired bromodomains. The experimental part of the paper was very detailed, including the reaction process of 6-Chloro-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-amine(cas: 53085-52-2Product Details of 53085-52-2)
6-Chloro-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-amine(cas: 53085-52-2) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Product Details of 53085-52-2
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem