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

Lb54 是一种 caspase-3 和 caspase-7 激活剂，对人 procaspase-3 的 EC50 为 660.9 nM。Lb54 可激活 caspase-3/7，后者在天冬氨酸残基 87 位点切割 Gasdermin D (GSDMD) 以产生 p10 片段，从而阻止 GSDMD 形成成孔型 p30 片段。Lb54 通过激活 caspase-3/7 抑制 GSDMD 介导的细胞焦亡 (pyroptosis)，进而减轻炎症反应并发挥脓毒症保护作用。Lb54 可减轻急性肺损伤，并通过抑制单核细胞来源树突状细胞的成熟来抑制全身炎症。Lb54 可用于脓毒症相关研究。

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Lb54

Lb54 Chemical Structure

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Lb54 相关抗体

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查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

Lb54 (compound 2) (1 μM; 3 h) 通过激活 caspase-3/7 抑制 THP-1 来源巨噬细胞的焦亡，caspase-3/7 会剪切 GSDMD 形成非成孔的 p10 片段而非介导焦亡的 p30 片段[1]。
Lb54 (5 μM；12 h) 可直接激活重组人 procaspase-3，其 EC50 为 0.6609 μM，且与该蛋白的结合 Kd 为 76.72 μM[1]。
Lb54 (1 μM) 通过在 LPS (HY-D10560)/Nigericin (HY-127019) 诱导的细胞焦亡过程中抑制促炎通路、上调代谢过程，来调控 THP-1 来源巨噬细胞的转录组[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Lb54 相关抗体:

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.
体内研究
(In Vivo)

Lb54 (compound 2) (2 mg/kg；i.p.；LPS 攻击前 24 h 和 4 h 各给药 1 次) 可通过降低炎症细胞因子水平、抑制 GSDMD 介导的细胞焦亡及减轻肺损伤，在小鼠模型中发挥抗 LPS 诱导脓毒性休克的作用，将小鼠存活率提升至约 42.9%[1]。
Lb54 (2 mg/kg; i.p.; 预处理) 可通过减少 GSDMD 阳性免疫细胞浸润和肺损伤，改善 盲肠结扎穿孔 (CLP) 小鼠脓毒症模型的小鼠存活率[1]。
Lb54 (2 mg/kg；腹腔注射；于 LPS 攻击前 24 h 和 4 h 各给药 1 次) 可在 LPS 诱导的急性肺损伤 (ALI) 小鼠模型中抑制单核细胞焦亡及向树突状细胞的成熟，从而减轻炎症免疫反应[1]。

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.
分子量

598.60

Formula

C27H22N2O10S2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Lb54 相关分类

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  • 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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