1. Apoptosis Immunology/Inflammation
  2. Caspase Pyroptosis
  3. Ac-DMLD-CMK TFA

Ac-DMLD-CMK TFA is a caspase 3 inhibitor and a GSDME inhibitor. Ac-DMLD-CMK TFA 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 TFA alleviates renal function deterioration, renal tubular epithelial cell injury, inflammatory cytokine secretion, pulmonary structural damage, and chemotherapy-induced nephrotoxicity.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Ac-DMLD-CMK TFA

Ac-DMLD-CMK TFA Chemical Structure

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Ac-DMLD-CMK TFA is a caspase 3 inhibitor and a GSDME inhibitor. Ac-DMLD-CMK TFA 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 TFA alleviates renal function deterioration, renal tubular epithelial cell injury, inflammatory cytokine secretion, pulmonary structural damage, and chemotherapy-induced nephrotoxicity[1][2][3].

IC50 & Target[1]

Caspase 3

 

In Vitro

Ac-DMLD-CMK TFA (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.

In Vivo

Ac-DMLD-CMK TFA (5 mg/kg/day; i.p.; single injection 1 hour prior to cisplatin administration) inhibits caspase 3 and Gsdme activation, alleviates kidney function deterioration, reduces renal tubular epithelial injury, and lowers inflammatory cytokine secretion in cisplatin-induced acute kidney injury in male C57BL/6 mice[1].
Ac-DMLD-CMK TFA (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.
Molecular Weight

681.08

Formula

C24H36ClF3N4O11S

Appearance

Solid

Color

White to off-white

Sequence

Ac-Asp-Met-Leu-{Asp-CMK}

Sequence Shortening

Ac-DML-{Asp-CMK}

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (146.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4683 mL 7.3413 mL 14.6826 mL
5 mM 0.2937 mL 1.4683 mL 2.9365 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4683 mL 7.3413 mL 14.6826 mL 36.7064 mL
5 mM 0.2937 mL 1.4683 mL 2.9365 mL 7.3413 mL
10 mM 0.1468 mL 0.7341 mL 1.4683 mL 3.6706 mL
15 mM 0.0979 mL 0.4894 mL 0.9788 mL 2.4471 mL
20 mM 0.0734 mL 0.3671 mL 0.7341 mL 1.8353 mL
25 mM 0.0587 mL 0.2937 mL 0.5873 mL 1.4683 mL
30 mM 0.0489 mL 0.2447 mL 0.4894 mL 1.2235 mL
40 mM 0.0367 mL 0.1835 mL 0.3671 mL 0.9177 mL
50 mM 0.0294 mL 0.1468 mL 0.2937 mL 0.7341 mL
60 mM 0.0245 mL 0.1224 mL 0.2447 mL 0.6118 mL
80 mM 0.0184 mL 0.0918 mL 0.1835 mL 0.4588 mL
100 mM 0.0147 mL 0.0734 mL 0.1468 mL 0.3671 mL
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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.

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Product Name:
Ac-DMLD-CMK TFA
Cat. No.:
HY-P10939A
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