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MedChemExpress - Model BC-1382 - 1013753-99-5
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity[1].MCE products for research use only. We do not sell to patients.
BC-1382
MCE China:BC-1382
Brand:MedChemExpress (MCE)
Cat. No.HY-W062696
CAS:1013753-99-5
Purity:99.53%
Storage:Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Shipping:Room temperature in continental US; may vary elsewhere.
Description:BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity.
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[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].
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References:
[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. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas;
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects;
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services;
• It has a professional experimental center and strict quality control and verification system;
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products;
• The biological activity of the products has been verified by the experiments of customers in various countries;
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers;
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world;
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。