2. Apoptosis Immunology/Inflammation
  3. Caspase Pyroptosis
  4. 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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Lb54

Lb54 Chemical Structure

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Lb54 Related Antibodies

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Description

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[1].

IC50 & Target[1]

Procaspase-3

660.9 nM (EC50)

Caspase-7

 

In Vitro

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.

Lb54 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: 1 μM
Incubation Time: 3 h
Result: Activated procaspase-3/7 while suppressing p30 fragment generation of GSDMD during
early pyroptosis induction.
In Vivo

Lb54 (compound 2) (2 mg/kg; i.p.; twice (24 h and 4 h before LPS challenge)) protects against LPS-induced septic shock in mice by reducing inflammatory cytokine levels, GSDMD-mediated pyroptosis, and lung injury, improving survival to ~42.9%[1].
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.

Animal Model: C57BL/6J (male, 25-30 g) injected with LPS[1]
Dosage: 2 mg/kg
Administration: i.p.; twice (24 h and 4 h before LPS challenge)
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%.
Animal Model: C57BL/6J (male, 25-30 g) bearing cecal ligation and puncture (CLP) sepsis[1]
Dosage: 2 mg/kg
Administration: i.p.; once
Result: Enhanced survival to 30% at 96 h; Reduced infiltration of GSDMD-positive neutrophils and monocytes in lung tissue; Significantly lowered lung injury score.
Animal Model: C57BL/6J (male, 25-30 g) bearing acute lung injury[1]
Dosage: 2 mg/kg
Administration: i.p.; twice (24 h and 4 h before LPS challenge)
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.
Molecular Weight

598.60

Formula

C27H22N2O10S2
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Lb54 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lb54Lb 54Lb-54CaspasePyroptosisTHP-1-derived macrophagesseptic shockGSDMDGasdermin Dmonocytessepsismonocyte-derived dendritic cellcaspase-3/7neutrophilslipopolysaccharideInhibitorinhibitorinhibit

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