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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C27H22N2O10S2
- 分子量:598.60
-
保管条件:
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]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
Caspase アイソフォーム固有の製品をすべて表示
More
生物活性
|
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.
-
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.
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.
化学情報
-
分子量 598.60
-
分子式 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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Lb54 関連分類
HY-181168 関連分類
Powered by Bioz