BC-1382

SKU: orb1219927

Description

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.

Key Properties

• CAS Number: 1013753-99-5
• MW: 459.56
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₉N₃O₅S
• SMILES: COc1ccccc1CNC(=O)[C@H](C)NC(=O)C1CCN(CC1)S(=O)(=O)c1ccccc1
• Target: ubiquitin E3 ligase HECTD2
• Solubility: In Vitro: DMSO : 125 mg/mL (272.00 mM)

Bioactivity

• 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. 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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• In Vitro:
  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).
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

ubiquitin E3 ligase HECTD2