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≈ 5 nM)。具有抗炎活性。

BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC 50 ≈ 5 nM).Anti-inflammatory activity.

Solid

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).
has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[1]. Tiffany A Coon, et al. The proinflammatory role of HECTD2 in innate immunity and experimental lung injury. Sci Transl Med. 2015 Jul 8;7(295):295ra109.

In Vitro: DMSO : 125 mg/mL (272.00 mM; Need ultrasonic)配制储备液