BC-1382

• CAT Number: I023046
• CAS Number: 1013753-99-5
• Molecular Formula: C23H29N3O5S
• Molecular Weight: 459.56
• Purity: ≥95%
• Synonyms: 1-(benzenesulfonyl)-N-[(2S)-1-[(2-methoxyphenyl)methylamino]-1-oxopropan-2-yl]piperidine-4-carboxamide
• InChI: InChI=1S/C23H29N3O5S/c1-17(22(27)24-16-19-8-6-7-11-21(19)31-2)25-23(28)18-12-14-26(15-13-18)32(29,30)20-9-4-3-5-10-20/h3-11,17-18H,12-16H2,1-2H3,(H,24,27)(H,25,28)/t17-/m0/s1
• InChIKey: RCWXKFCEGKXUIN-KRWDZBQOSA-N
• SMILES: CC(C(=O)NCC1=CC=CC=C1OC)NC(=O)C2CCN(CC2)S(=O)(=O)C3=CC=CC=C3

BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity[1].
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].
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].

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.
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