Ac-YVAD-CMK (Synonyms: N-Ac-Tyr-Val-Ala-Asp-CMK) |
| Catalog No.GC42721 |
Ac-YVAD-CMK is a selective irreversible inhibitor of caspase-1 (Ki=0.8nM), which can prevent the proinflammatory cytokine IL-1β activation. Ac-YVAD-CMK can reduce the inflammatory response and induce a long-lasting neuroprotective effect.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 178603-78-6
Sample solution is provided at 25 µL, 10mM.
Ac-YVAD-CMK is a selective irreversible inhibitor of caspase-1 (Ki=0.8nM), which can prevent the proinflammatory cytokine IL-1β activation. Ac-YVAD-CMK can reduce the inflammatory response and induce a long-lasting neuroprotective effect[1,2,3].
Ac-YVAD-CMK reduced the expression of IL-1β and IL-18 in activated microglia in vitro[3]. Ac-YVAD-CMK(40μM) decreased the rapid cell (PAMs, 3D4/21 cells and the endothelial cell line) death induced by ApxⅠ[4]. Ac-YVAD-CMK attenuated the inhibitory effects of berberine on the viability, migration and invasion of HepG2 cells[5].
AC-YVAD-CMK treatment significantly alleviated sepsis-induced acute kidney injury, with decreased histological injury in renal tissues, suppressed the accumulation of neutrophils and macrophages in renal tissues, and decreased sCR and BUN level[6]. Ac-YVAD-CMK protected the brain against ICH-induced injury, and the neuroprotective effect may result from anti-inflammation-induced blood–brain barrier protection[7]. Pretreatment of rats with Ac-YVAD-CMK (12.5mM/kg) significantly reduced endotoxin-induced mortality from 83% to 33% using Log Rank analysis[8].
References:
[1] Wang F, Li G, et al. Alcohol accumulation promotes esophagitis via pyroptosis activation. Int J Biol Sci. 2018;14(10):1245-1255. Published 2018 Jul 13.
[2] Rabuffetti M, Sciorati C, et al. Inhibition of caspase-1-like activity by Ac-Tyr-Val-Ala-Asp-chloromethyl ketone induces long-lasting neuroprotection in cerebral ischemia through apoptosis reduction and decrease of proinflammatory cytokines. J Neurosci. 2000;20(12):4398-4404.
[3] Liang H, Sun Y, et al. Ac-YVAD-cmk improves neurological function by inhibiting caspase-1-mediated inflammatory response in the intracerebral hemorrhage of rats. Int Immunopharmacol. 2019;75:105771.
[4] Hernandez-Cuellar E, Guerrero-Barrera AL, et al. An in vitro study of ApxI from Actinobacillus pleuropneumoniae serotype 10 and induction of NLRP3 inflammasome-dependent cell death. Vet Rec Open. 2021;8(1):e20. Published 2021 Oct 4.
[5] Chu Q, Jiang Y, et al. Pyroptosis is involved in the pathogenesis of human hepatocellular carcinoma. Oncotarget. 2016;7(51):84658-84665.
[6] Yang M, Fang JT, et al. Caspase-1-Inhibitor AC-YVAD-CMK Inhibits Pyroptosis and Ameliorates Acute Kidney Injury in a Model of Sepsis. Biomed Res Int. 2021;2021:6636621.
[7] Wu B, Ma Q, et al. Ac-YVAD-CMK Decreases Blood-Brain Barrier Degradation by Inhibiting Caspase-1 Activation of Interleukin-1β in Intracerebral Hemorrhage Mouse Model. Transl Stroke Res. 2010;1(1):57-64.
[8] Mathiak G, Grass G, et al. Caspase-1-inhibitor ac-YVAD-cmk reduces LPS-lethality in rats without affecting haematology or cytokine responses. Br J Pharmacol. 2000;131(3):383-386.
| Cell experiment [1]: | |
Cell lines | Microglia cells |
Preparation Method | Microglia cells (1×105) were stimulated with the caspase-1 inhibitor Ac-YVAD-CMK (dissolved by DMSO) for 1h. Thrombin was added at a final concentration of 10U/mL to activate the microglia cells for 24h. |
Reaction Conditions | 40μmol/L or 80μmol/L |
Applications | High level Ac-YVAD-CMK treatment (40μmol/L or 80μmol/L) significantly decreased the mRNA levels of IL-1β/IL-18. The 40μmol/L dose of Ac-YVAD-CMK significantly reduced the protein levels of caspase-1 (p20) and mature IL-1β/IL-18 compared with the thrombin-activated microglia group. |
| Animal experiment [2]: | |
Animal models | Male Sprague Dawley rats,weighing 250-275g |
Preparation Method | Ac-YVAD-CMK (300ng/rat in 3mL) was injected intracerebroventricularly 10 min after permanent middle cerebral artery occlusion in the rat. |
Dosage form | 300ng/rat in 3mL, intracerebroventricular injection |
Applications | Ac-YVAD-CMK treatment induced a significant reduction of infarct volume not only 24 h after ischemia but also 6d later. Ac-YVAD-CMK treatment resulted in a reduction not only of caspase-1 but also of caspase-3 activity at 24h and led to a parallel decrease of apoptosis as measured by nucleosome quantitation. Likewise, brain levels of the proinflammatory cytokines IL-1b and TNF-a were reduced at 24h. |
References: | |
| Cas No. | 178603-78-6 | SDF | |
| Synonyms | N-Ac-Tyr-Val-Ala-Asp-CMK | ||
| Chemical Name | N-acetyl-L-tyrosyl-L-valyl-N-[(1S)-1-(carboxymethyl)-3-chloro-2-oxo-propyl]-L-alaninamide | ||
| Canonical SMILES | ClCC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)Cc1ccc(O)cc1)C(C)C | ||
| Formula | C24H33ClN4O8 | M.Wt | 541 |
| Solubility | 20mg/mL in DMSO, 10mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8484 mL | 9.2421 mL | 18.4843 mL |
| 5 mM | 0.3697 mL | 1.8484 mL | 3.6969 mL |
| 10 mM | 0.1848 mL | 0.9242 mL | 1.8484 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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