| Bioactivity | BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 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)[1][2]. | ||||||||||||
| Target | IC50: 8.6 μM (CARD9-TRIM62) | ||||||||||||
| Invitro | BRD5529 has effective dose-dependent CARD9-TRIM62 inhibitory activity with an IC50 value of 8.6 μM[1].BRD5529 directly binds CARD9, but not TRIM62, and disrupt its ubiquitinylation in vitro[1].BRD5529 (40 μM) produces dose-dependent inhibition of TRIM62-mediated CARD9 ubiquitinylation in vitro[1].BRD5529 (200 μM, 0-50 min; 200μM, 2-4 h) inhibits CARD9-dependent signaling in innate immune cells[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| 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[2]. Animal Model: | ||||||||||||
| Name | BRD5529 | ||||||||||||
| CAS | 1358488-78-4 | ||||||||||||
| Formula | C25H31N5O4 | ||||||||||||
| Molar Mass | 465.54 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Leshchiner ES, et al. Small-molecule inhibitors directly target CARD9 and mimic its protective variant in inflammatorybowel disease. Proc Natl Acad Sci U S A. 2017 Oct 24;114(43):11392-11397. [2]. Theodore J Kottom, et al. Preclinical and Toxicology Studies of BRD5529, a Selective Inhibitor of CARD9. Drugs R D. 2022 Jun;22(2):165-173. |