| Bioactivity | BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity[1]. | |||||||||
| Invitro | 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[1].BC-1382 drastically increases PIAS1 protein level in a nonstimulus condition with IC50≈100 nM[1].BC-1382 improves PIAS1 protein stability by increasing its t1/2[1].BC-1382 suppresses LPS-induced PIAS1 degradation and restores PIAS1 protein levels at 800 nM[1].BC-1382 suppresses LPS-induced proinflammatory cytokines released by human peripheral blood mononuclear cells (PBMCs)[1]. | |||||||||
| In Vivo | 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[1]. Animal Model: | |||||||||
| Name | BC-1382 | |||||||||
| CAS | 1013753-99-5 | |||||||||
| Formula | C23H29N3O5S | |||||||||
| Molar Mass | 459.56 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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. |