BC-1382

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

BC-1382 是一种有效的泛素 E3 连接酶 HECTD2 抑制剂，可特异性破坏 HECTD2/PIAS1 相互作用（IC50 为 5 nM）。BC-1382 靶向 HECTD2 并减轻脂多糖 (LPS) 和铜绿假单胞菌诱导的肺部炎症。

BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction(IC50 of 5 nM).BC-1382, that targeted HECTD2 and attenuated lipopolysaccharide (LPS)- and Pseudomonas aeruginosa-induced lung inflammation.?

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).

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.

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Others

Other Targets

ubiquitin E3 ligase HECTD2

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1013753-99-5

459.56

C23H29N3O5S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (272.00 mM)

COc1ccccc1CNC(=O)[C@H](C)NC(=O)C1CCN(CC1)S(=O)(=O)c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years