BRD5529
目录号: PL02261 纯度: ≥98%
CAS No. :1358488-78-4
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中文名称
BRD5529
英文名称
BRD5529
英文别名
BRD5529;methylbenzamido)nicotinic acid;2-(4-carbamoyl-4-piperidin-1-ylpiperidin-1-yl)-5-[(4-methylbenzoyl)amino]pyridine-3-carboxylic acid;2-(4'-Carbamoyl-[1,4'-bipiperidin]-1'-yl)-5-(4-
Cas No.
1358488-78-4
分子式
C25H31N5O4
分子量
465.54
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
BRD5529 是一种有效的剂量依赖性 CARD9-TRIM62 蛋白-蛋白相互作用 (PPI) 抑制剂,IC50 值为 8.6 μM。BRD5529 在体外对 CARD9 泛素化具有有效和完全的抑制作用,还具有良好的溶解性。BRD5529 可用于克罗恩病(CD)和溃疡性结肠炎(UC)等炎症性肠病(IBD)的研究。
生物活性
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).
性状
Solid
IC50 & Target[1][2]
IC50: 8.6 μM (CARD9-TRIM62)
体外研究(In Vitro)
BRD5529 has effective dose-dependent CARD9-TRIM62 inhibitory activity with an IC50 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 125 mg/mL (268.51 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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