Lb54
Lb54 is a caspase-3 and caspase-7 activator with an EC50 of 660.9 nM for human procaspase-3. Lb54 activates caspase-3/7, which cleaves Gasdermin D (GSDMD) at aspartic acid residue 87 to generate a p10 fragment, preventing formation of the pore-forming p30 fragment of GSDMD. Lb54 suppresses GSDMD-mediated pyroptosis through caspase-3/7 activation, thereby attenuating inflammatory responses and conferring protection against sepsis. Lb54 alleviates acute lung injury, and inhibited systemic inflammation by restraining the maturation of monocyte-derived dendritic cells. Lb54 can be used for the research of sepsis.
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- Formule: C27H22N2O10S2
- Masse moléculaire:598.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Activité biologique
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Procaspase-3 660.9 nM (EC50) |
Caspase-7 |
Lb54 (compound 2) (1 μM; 3 h) inhibits pyroptosis in THP-1-derived macrophages by activating caspase-3/7, which cleaves GSDMD to form the non-pore-forming p10 fragment instead of the pyroptotic p30 fragment[1].
Lb54 (5 μM; 12 h) directly activates recombinant human procaspase-3 with an EC50 of 0.6609 μM and binds to it with a Kd of 76.72 μM[1].
Lb54 (1 μM) modulates the transcriptome of THP-1-derived macrophages by suppressing proinflammatory pathways and upregulating metabolic processes during LPS (HY-D10560)/Nigericin (HY-127019)-induced pyroptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells
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Concentration:1 μM
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Incubation Time:3 h
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Result:Activated procaspase-3/7 while suppressing p30 fragment generation of GSDMD during
early pyroptosis induction.
Lb54 (2 mg/kg; i.p.; pretreatment) improves survival in the cecal ligation and puncture (CLP) sepsis model by reducing GSDMD-positive immune cell infiltration and lung injury[1].
Lb54 (2 mg/kg; i.p.; twice (24 h and 4 h before LPS challenge)) inhibits monocyte pyroptosis and maturation into dendritic cells in LPS-induced acute lung injury mice, reducing inflammatory immune responses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 25-30 g) injected with LPS[1]
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Dosage:2 mg/kg
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Administration:i.p.; twice (24 h and 4 h before LPS challenge)
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Result:Improved survival to 42.9%; Significantly reduced serum levels of IL-1β, TNF-α, and IFN-γ at 12 h post-LPS; Attenuated GSDMD p30 cleavage in lung tissues; Reduced lung injury score; Decreased IL-1β and TNF-α positive areas in lung immunohistochemical staining; Reduced proportion of CD45+/GSDMD+ cells in lung tissue from 23.20% to 7.09%.
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Animal Model:C57BL/6J (male, 25-30 g) bearing cecal ligation and puncture (CLP) sepsis[1]
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Dosage:2 mg/kg
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Administration:i.p.; once
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Result:Enhanced survival to 30% at 96 h; Reduced infiltration of GSDMD-positive neutrophils and monocytes in lung tissue; Significantly lowered lung injury score.
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Animal Model:C57BL/6J (male, 25-30 g) bearing acute lung injury[1]
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Dosage:2 mg/kg
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Administration:i.p.; twice (24 h and 4 h before LPS challenge)
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Result:Suppressed LPS-induced systemic inflammation by inhibiting monocyte-derived dendritic cell (moDC) maturation; Reduced GSDMD expression in monocytes and neutrophils; Attenuated antigen-presenting capacity of monocytes; Suppressed monocyte maturation into dendritic cells; Downregulated key antigen presentation genes (H2-Ab1, Cd74, H2-Eb1, H2-Aa) and interferon response genes (Ifit1, Ifi206, Oasl2) in monocytes.
Chemical Information
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Masse moléculaire 598.60
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Formule C27H22N2O10S2
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SMILES
COC(C(OC1=C(O)C=CC2=C1)=C3)=CC=C3C(O[C@H]4C=COC=C([C@]54[H])[C@@H](O)[C@@](N5C([C@]6([C@H]2O)N7C)=O)(SS6)C7=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lb54 Related Classifications
HY-181168 Related Classifications
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