Identification | Back Directory | [Name]
BC-1382 | [CAS]
1013753-99-5 | [Synonyms]
BC-1382 1-(benzenesulfonyl)-N-[(2S)-1-[(2-methoxyphenyl)methylamino]-1-oxopropan-2-yl]piperidine-4-carboxamide 4-Piperidinecarboxamide, N-[(1S)-2-[[(2-methoxyphenyl)methyl]amino]-1-methyl-2-oxoethyl]-1-(phenylsulfonyl)- | [Molecular Formula]
C23H29N3O5S | [MDL Number]
MFCD30470656 | [MOL File]
1013753-99-5.mol | [Molecular Weight]
459.56 |
Chemical Properties | Back Directory | [Melting point ]
163 - 164°C | [storage temp. ]
-20°C Freezer, Under inert atmosphere | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [color ]
White to Off-White |
Hazard Information | Back Directory | [Uses]
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity[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: | C57BL/6J mice were challenged intratracheally with PA103 (104 CFU per mouse) or LPS (3 mg/kg)[1] | 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.
Significantly decreased lavage cytokine levels in both models.
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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. DOI:10.1126/scitranslmed.aab3881 |
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