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MedChemExpressModel BC-1382 - 1013753-99-5

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

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