BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC 50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC)
In Vitro
BRD5529 has effective dose-dependent CARD9-TRIM62 inhibitory activity with an IC 50 value of 8.6 μM. BRD5529 directly binds CARD9, but not TRIM62, and disrupt its ubiquitinylation in vitro. BRD5529 (40 μM) produces dose-dependent inhibition of TRIM62-mediated CARD9 ubiquitinylation in vitro. BRD5529 (200 μM, 0-50 min; 200μM, 2-4 h) inhibits CARD9-dependent signaling in innate immune cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HEK293F cells Concentration: 40 μM Incubation Time: Result: Inhibited CARD9 ubiquitinylation reaction in vitro.
In Vivo
BRD5529 (i.p.; 0.1 or 1.0 mg/kg; daily, for 2 weeks) displays no inherent safety concerns in initial general safety and toxicology assessments. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Pneumocystis pneumonia (PCP) modelDosage: 0.1 or 1.0 mg/kg Administration: intraperitoneally (IP), daily, for 2 weeks Result: Resulted no significant changes in daily or final weight gain and proinflammatory cytokines showed no major differences. Showed no significant change of lung, liver, and kidney in pathology scoring.
