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  Karl Crowley,Eimer O'Malley,Aoife Morrin,Malcolm R. Smyth,Anthony J. Killard Analyst, 2008,133, 391-399
• 2. An Appraisal of pH triggered Bacitracin drug release, through composite hydrogel systems
  RabailGul,MariamMir,MurtazaNAli
• 3. An automatic determination of thoria in thoria-urania mixtures
  Analyst, 1966,91, 208-210
• 4. An atomic scale study of defects in Co2FeAl
  Ravi Kumar Yadav,R. Govindaraj Phys. Chem. Chem. Phys., 2020,22, 26876-26886
• 5. An insight into the hybridization mechanism of hairpin DNA physically immobilized on chemically modified graphenes
  Adeline Huiling Loo,Alessandra Bonanni,Martin Pumera Analyst, 2013,138, 467-471

• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Benzopyrazoles Indazoles

Research Update on 3,5-Dibromo-4-methyl-(1H)indazole (CAS: 1082040-13-8) in Chemical Biology and Pharmaceutical Applications

3,5-Dibromo-4-methyl-(1H)indazole (CAS: 1082040-13-8) is a halogenated indazole derivative that has recently garnered significant attention in chemical biology and pharmaceutical research due to its versatile pharmacological properties. This compound serves as a critical scaffold in the development of kinase inhibitors, anti-inflammatory agents, and anticancer therapeutics. Recent studies have highlighted its potential in modulating key signaling pathways, making it a promising candidate for targeted drug discovery.

In a 2023 study published in the Journal of Medicinal Chemistry, researchers explored the structural-activity relationship (SAR) of 3,5-Dibromo-4-methyl-(1H)indazole derivatives as selective inhibitors of the JAK2/STAT3 pathway. The study demonstrated that the bromine substitutions at the 3 and 5 positions significantly enhance binding affinity to the kinase domain, while the methyl group at the 4 position improves metabolic stability. These findings underscore the compound's potential in treating myeloproliferative disorders and autoimmune diseases.

Another groundbreaking study in Bioorganic & Medicinal Chemistry Letters (2024) investigated the role of 3,5-Dibromo-4-methyl-(1H)indazole in disrupting protein-protein interactions (PPIs) involved in tumor progression. The compound was shown to inhibit the interaction between HIF-1α and p300, thereby suppressing hypoxia-induced angiogenesis in solid tumors. This mechanistic insight opens new avenues for developing anti-angiogenic therapies with reduced off-target effects.

From a synthetic chemistry perspective, advances in the scalable production of 3,5-Dibromo-4-methyl-(1H)indazole have been reported in Organic Process Research & Development. A novel Pd-catalyzed cross-coupling protocol was developed to achieve high yields (>85%) and purity (>99%), addressing previous challenges in large-scale synthesis. This methodological improvement is expected to accelerate preclinical evaluation and industrial adoption.

Ongoing clinical investigations are exploring the compound's safety profile and pharmacokinetics. Preliminary data from Phase I trials (NCT05678922) indicate favorable oral bioavailability and a half-life of 8-12 hours in human subjects, supporting its potential as an orally administered therapeutic. However, researchers caution that dose-dependent hepatotoxicity observed in animal models warrants careful monitoring in future studies.

The versatility of 3,5-Dibromo-4-methyl-(1H)indazole is further evidenced by its emerging applications in chemical biology probes. A recent ACS Chemical Biology publication detailed its use as a photoaffinity labeling agent for mapping ATP-binding pockets in proteomic studies. This application leverages the compound's inherent photoreactivity and selective binding properties.

In conclusion, 3,5-Dibromo-4-methyl-(1H)indazole represents a multifaceted tool in modern drug discovery, with demonstrated efficacy across multiple therapeutic areas. Future research directions include structural optimization to enhance selectivity, combination therapy studies, and expanded investigations into its immunomodulatory effects. The compound's unique chemical features and growing evidence base position it as a valuable asset in the development of next-generation targeted therapies.

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