Ac-DMLD-CMK
Ac-DmLD-CMK is a caspase 3 inhibitor and a GSDME inhibitor. Ac-DmLD-CMK binds directly to the catalytic domain of caspase-3, blocks caspase-3-mediated cleavage of GSDME, inhibits the activation of caspase 3 and Gsdme in the caspase 3-Gsdme signaling pathway, and reduces the levels of pyroptosis and apoptosis as well as the expression of LDH, IL-6, IL-1β and IL-18. Ac-DmLD-CMK alleviates renal function deterioration, renal tubular epithelial cell injury, inflammatory cytokine secretion, pulmonary structural damage, and chemotherapy-induced nephrotoxicity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2588354-33-8
- Formel: C22H35ClN4O9S
- Molecular Weight:567.05
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Alle Caspase Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
|
Caspase 3 |
Ac-DMLD-CMK (5 μM; 6 h pre-incubation) inhibits simvastatin-induced pyroptosis and cell viability reduction in MGC-803 human gastric cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ac-DMLD-CMK (5 mg/kg; i.p.; single dose 3 h pre-CLP) significantly reduces CLP-induced acute lung injury in male C57BL/6 J mice by inhibiting caspase-3/GSDME-mediated pyroptosis and apoptosis, as evidenced by reduced lung injury scores, inflammatory mediator levels, and cell death markers[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (male, 6-8 weeks old, 20-25 g, cisplatin-induced)[1]
-
Dosage:5 mg/kg/day
-
Administration:i.p.; single injection 1 hour prior to cisplatin administration
-
Result:Reduced serum creatinine and blood urea nitrogen levels compared to cisplatin-only treated mice.
Alleviated renal tubular epithelial cell death.
Reduced levels of cleaved mouse Gsdme (Gsdme-N) and cleaved caspase 3, with no significant effect on full-length mouse Gsdme (Gsdme-FL).
Suppressed renal mRNA expression of Ngal, Il6,Tnfa, and Il1b; did not affect Kim1 expression.
-
Animal Model:C57BL/6 J (male, 6-8 weeks old, CLP-induced sepsis model)[2]
-
Dosage:5 mg/kg
-
Administration:i.p.; single dose (3 h before CLP surgery)
-
Result:Reduced lung coefficient relative to CLP group.
Improved lung histopathology, with reduced alveolar wall thickening, congestion, bleeding, and inflammatory cell infiltration, and decreased lung injury score relative to CLP group.
Attenuated ultrastructural lung damage, including reduced type II alveolar epithelial cell edema, mitochondrial structural damage, and lamellar body vacuolization relative to CLP group.
Decreased protein expression of GSDME-N and cleaved-caspase-3 in lung tissue relative to CLP group.
Reduced mean fluorescence intensity of GSDME in lung tissue relative to CLP group.
Decreased caspase-3 activity in lung tissue relative to CLP group.
Reduced serum lactate dehydrogenase (LDH) and interleukin-6 (IL-6) levels relative to CLP group.
Decreased proportion of TUNEL-positive cells in lung tissue relative to CLP group.\nDecreased protein expression of cleaved-PARP in lung tissue relative to CLP group
nDecreased protein expression of IL-18 and IL-1β in lung tissue relative to CLP group.
Decreased lung tissue levels of pro-caspase-1, caspase-1, pro-IL-1β, and IL-1β relative to CLP group.
Chemical Information
-
CAS. Nr. 2588354-33-8
-
Molecular Weight 567.05
-
Formel C22H35ClN4O9S
-
Sequence
Ac-Asp-Met-Leu-{Asp-CMK}
-
Sequence Shortening
Ac-DML-{Asp-CMK}
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Shen X, et al. Caspase 3/GSDME-dependent pyroptosis contributes to chemotherapy drug-induced nephrotoxicity. Cell Death Dis. 2021;12(2):186. Published 2021 Feb 15. [Content Brief]
[2]. Qin H, et al. Inhibiting caspase-3/GSDME-mediated pyroptosis ameliorates septic lung injury in mice model. Mol Immunol. 2024;172:96-104. [Content Brief]
[3]. Xia Y, et al. Antitumor Effect of Simvastatin in Combination With DNA Methyltransferase Inhibitor on Gastric Cancer via GSDME-Mediated Pyroptosis. Front Pharmacol. 2022;13:860546. Published 2022 Apr 20. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)