| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Caspase-3, Caspase-7
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| ln Vitro |
Ac-DEVD-CMK TFA (100 μM; 24 h) prevents apoptosis produced by IDB [3]. The human pharyngeal squamous cell carcinoma FaDu and Detroit 562 cell lines are resistant to citrate (10 mM)-induced p21 breakage and G2/M accumulation when exposed to Ac-DEVD-CMK TFA (10 μM; 36 h) [4].
In vitro, Ac-DEVD-CMK TFA (100 uM; 24 h) prevents apoptosis induced by various stimuli, including high glucose levels and 3,20-dibenzoate (IDB). It also inhibits p21 cleavage and G2/M accumulation induced by citrate in human pharyngeal squamous carcinoma FaDu and Detroit 562 cell lines. |
| ln Vivo |
Ac-DEVD-CMK TFA (inhibitor III for caspase-3; 25 mg/kg; intraperitoneal; single dose; three hours post-APAP) considerably reduces the liver damage (AILI) caused by acetaminophen (APAP; HY-66005) [5]. Ac-DEVD-CMK TFA (i.p.; single dose; 25 mg/kg) In sensitive Sdc1−/− mice, considerably reduced APAP-induced liver damage (AILI) [6].
In vivo, Ac-DEVD-CMK TFA has been shown to significantly reduce acetaminophen (APAP)-induced liver injury (AILI). At a dose of 25 mg/kg (i.p., single dose), it inhibits GSK-3beta or caspase-3 activity, mitigating liver damage in mouse models. It is used to study the role of caspase-3 in various disease models. |
| Enzyme Assay |
In a non-cellular enzymatic assay, purified recombinant caspase-3 is incubated in an assay buffer (e.g., 50 mM HEPES, pH 7.4, 100 mM NaCl, 0.1% CHAPS, 10 mM DTT, 1 mM EDTA) with a fluorogenic substrate, such as Ac-DEVD-AMC. Various concentrations of Ac-DEVD-CMK TFA are added to the reaction mixture. The reaction is initiated by adding the substrate, and fluorescence (Ex 355 nm, Em 460 nm) is measured continuously. The inhibitor's potency is determined by calculating the IC50 value.
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| Cell Assay |
Western Blot Analysis[4]
Cell Types: FaDu and Detroit 562 cell Tested Concentrations: 10 μM; with 10 mM citrate Incubation Duration: 36 h Experimental Results: Inhibited citrate to induce p21 cleavage. For in vitro cell studies, cells (e.g., FaDu, Detroit 562, or primary hepatocytes) are seeded in culture plates and allowed to attach overnight. The cells are then pre-treated with the caspase inhibitor (e.g., 10 uM) for 1 hour, followed by treatment with an apoptosis inducer (e.g., 10 mM citrate, or APAP). After incubation, cells are harvested and lysed. Apoptosis is quantified by measuring caspase-3 activity, or by Western blotting for cleaved caspase-3 and PARP. |
| Animal Protocol |
Animal/Disease Models: Sdc1−/− mice induced by APAP[6]
Doses: 25 mg/kg Route of Administration: IP; single dose, 3 hrs (hours) post-APAP Experimental Results: Inhibited GSK‐3β or caspase‐3 activity to mitigate liver damage. In a typical animal model, male C57BL/6 mice are injected with APAP (300 mg/kg, i.p.) to induce acute liver injury. One group of mice is treated with Ac-DEVD-CMK TFA (25 mg/kg, i.p.) 3 hours after APAP administration. The animals are sacrificed 24 hours post-APAP. Blood is collected for serum ALT/AST measurement. Liver tissues are collected for histological analysis (H&E staining) and for measuring GSK-3beta or caspase-3 activity. |
| ADME/Pharmacokinetics |
As a peptide-based caspase inhibitor, Ac-DEVD-CMK is expected to have a short in vivo half-life, likely in the range of minutes to a couple of hours. It is rapidly distributed throughout the body. The compound is metabolized by proteases and eliminated primarily through renal and biliary excretion. Its irreversible binding to the active site of caspase-3 also contributes to its clearance profile.
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| Toxicity/Toxicokinetics |
There are no comprehensive long-term toxicity studies for this research compound. At therapeutic doses (e.g., 25 mg/kg), it is well-tolerated. Potential toxicities are linked to its pharmacological action; complete inhibition of caspase-3 could prevent normal apoptosis, which is essential for development and immune function. It is for research use only.
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| References |
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| Additional Infomation |
Ac-DEVD is the optimal tetrapeptide recognition motif for caspase-3. The Chloromethyl Ketone (CMK) group forms an irreversible covalent bond with the catalytic cysteine in the caspase-3 active site. This inhibitor is widely used to study apoptosis in various contexts, including cancer, neurodegeneration, and liver disease. It is not a clinical drug.
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| Molecular Formula |
C23H32CLF3N4O13
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|---|---|
| Molecular Weight |
664.97
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| Related CAS # |
Ac-DEVD-CMK;285570-60-7
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~150.38 mM)
H2O :~50 mg/mL (~75.19 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5038 mL | 7.5191 mL | 15.0383 mL | |
| 5 mM | 0.3008 mL | 1.5038 mL | 3.0077 mL | |
| 10 mM | 0.1504 mL | 0.7519 mL | 1.5038 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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