Category: 53085-52-2

Winter-Holt, Jon J.; Bardelle, Catherine; Chiarparin, Elisabetta; Dale, Ian L.; Davey, Paul R. J.; Davies, Nichola L.; Denz, Christopher; Fillery, Shaun M.; Guerot, Carine M.; Han, Fujin; Hughes, Samantha J.; Kulkarni, Meghana; Liu, Zhaoqun; Milbradt, Alexander; Moss, Thomas A.; Niu, Huijun; Patel, Joe; Rabow, Alfred A.; Schimpl, Marianne; Shi, Junjie; Sun, Dongqing; Yang, Dejian; Guichard, Sylvie published an article on February 24 ,2022. The article was titled 《Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models》, and you may find the article in Journal of Medicinal Chemistry.Related Products of 53085-52-2 The information in the text is summarized as follows:

ATAD2 is an epigenetic bromodomain-containing target which is overexpressed in many cancers and has been suggested as a potential oncol. target. While several small mol. inhibitors have been described in the literature, their cellular activity has proved to be underwhelming. In this work, we describe the identification of a novel series of ATAD2 inhibitors by high throughput screening, confirmation of the bromodomain region as the site of action, and the optimization campaign undertaken to improve the potency, selectivity, and permeability of the initial hit. The result is compound 5 (AZ13824374)(I), a highly potent and selective ATAD2 inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models.6-Chloro-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-amine(cas: 53085-52-2Related Products of 53085-52-2) was used in this study.

6-Chloro-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-amine(cas: 53085-52-2) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Related Products of 53085-52-2

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Li, Xin; Wu, Yizhe; Tian, Gaofei; Jiang, Yixiang; Liu, Zheng; Meng, Xianbin; Bao, Xiucong; Feng, Ling; Sun, Hongyan; Deng, Haiteng; Li, Xiang David published an article in Journal of the American Chemical Society. The title of the article was 《Chemical Proteomic Profiling of Bromodomains Enables the Wide-Spectrum Evaluation of Bromodomain Inhibitors in Living Cells》.Name: 6-Chloro-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-amine The author mentioned the following in the article:

Bromodomains, epigenetic “”readers”” of lysine acetylation marks, exist in different nuclear proteins with diverse biol. functions in chromatin biol. Malfunctions of bromodomains are associated with the pathogenesis of human diseases, such as cancer. Bromodomains have therefore emerged as therapeutic targets for drug discovery. Given the high structural similarity of bromodomains, a critical step in the development of bromodomain inhibitors is the evaluation of their selectivity to avoid off-target effects. While numerous bromodomain inhibitors have been identified, new methods to evaluate the inhibitor selectivity toward endogenous bromodomains in living cells remain needed. Here we report the development of a photoaffinity probe, photo-bromosporine (photo-BS), that enables the wide-spectrum profiling of bromodomain inhibitors in living cells. Photo-BS allowed light-induced crosslinking of recombinant bromodomains and endogenous bromodomain-containing proteins (BCPs) both in vitro and in living cells. The photo-BS-induced labeling of the bromodomains was selectively competed by the corresponding bromodomain inhibitors. Proteomics anal. revealed that photo-BS captured 28 out of the 42 known BCPs from the living cells. Assessment of the two bromodomain inhibitors, bromosporine and GSK6853, resulted in the identification of known as well as previously uncharacterized bromodomain targets. Collectively, we established a chem. proteomics platform to comprehensively evaluate bromodomain inhibitors in terms of their selectivity against endogenous BCPs in living cells. 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: 53085-52-2Name: 6-Chloro-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-amine)

6-Chloro-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-amine(cas: 53085-52-2) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Name: 6-Chloro-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-amine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

《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