产品
编 号:F005884
分子式:C23H29N3O5S
分子量:459.56
产品类型
结构图
CAS No: 1013753-99-5
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产品详情
生物活性:
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity.
体内研究:
BC-1382 (10 mg/kg; intraperitoneal injection) significantly decreases lavage protein concentrations, lavage cell counts, and cell infiltrates in both PA103-stimulated and LPS-stimulated mice. BC-1382 significantly decreases lavage cytokine levels in both models.Animal Model:C57BL/6J mice were challenged intratracheally with PA103 (104 CFU per mouse) or LPS (3 mg/kg)
Dosage:10 mg/kg
Administration:Given through intraperitoneal injection
Result:Significantly decreased lavage protein concentrations, lavage cell counts, and cell infiltrates in both PA103-stimulated and LPS-stimulated mice.Significantly decreased lavage cytokine levels in both models.
体外研究:
BC-1382 targets HECTD2 and attenuates lipopolysaccharide (LPS)– and Pseudomonas aeruginosa-induced lung inflammation. HECTD2 is an ubiquitin E3 ligase. BC-1382 reduces the severity of cytokine-driven lung inflammation.BC-1382 drastically increases PIAS1 protein level in a nonstimulus condition with IC50≈100 nM.BC-1382 improves PIAS1 protein stability by increasing its t1/2.BC-1382 suppresses LPS-induced PIAS1 degradation and restores PIAS1 protein levels at 800 nM.BC-1382 suppresses LPS-induced proinflammatory cytokines released by human peripheral blood mononuclear cells (PBMCs).