BRD5529

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BRD5529 是一种小分子抑制剂，可破坏 CARD9-E3 泛素连接酶 TRIM62 的相互作用，IC50 为 8.6 uM。

BRD5529 is a small-molecule inhibitor that disrupts the interaction of CARD9-E3 ubiquitin ligase TRIM62 with IC50 of 8.6 uM; directly and selectively bind CARD9, disrupts TRIM62 recruitment, inhibits TRIM62-mediated ubiquitinylation of CARD9, and demonstrates cellular activity and selectivity in CARD9-dependent pathways, selectively inhibits Dectin-1-mediated CARD9 activation, while leaving LPS-activated signaling intact.

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. Western Blot Analysis Cell Line:HEK293F cells Concentration:40 μM Incubation Time:Result:Inhibited CARD9 ubiquitinylation reaction in vitro.

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. Animal Model:Pneumocystis pneumonia (PCP) model Dosage: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.

BRD-5529 | BRD 5529

Proteasome/Ubiquitin

E3 Ubiquitin Ligase

E3 Ubiquitin Ligase

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1358488-78-4

465.554

C25H31N5O4

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (268.51 mM)

O=C(O)C1=C(N2CCC(N3CCCCC3)(C(N)=O)CC2)N=CC(NC(C4=CC=C(C)C=C4)=O)=C1

2-(4'-carbamoyl-[1,4'-bipiperidin]-1'-yl)-5-(4-methylbenzamido)nicotinic acid

(-20℃)

With Ice Pack

≥ 2 years