Ac-DEVD-CHO TFA

Ac-DEVD-CHO TFA is the trifluoroacetate salt form of Ac-DEVD-CHO (CAS No.: 169332-60-9). Ac-DEVD-CHO (full name: acetyl-aspartic acid-glutamic acid-valine-aspartic aldehyde, Acetyl-Asp-Glu-Val-Asp-aldehyde) is a selective caspase-3 (DEVDase) inhibitor that targets caspase-3 in animal cells and caspase-3-like proteases (DEVDase) in plant cells, inhibiting both; the biological pathways it participates in regulating include the downstream programmed cell death (PCD) pathway of plant S-RNase-mediated self-incompatibility, where it can block PCD processes triggered by DEVDase activation, such as pollen tube DNA degradation, disruption of cytoplasmic structure, and formation of Golgi bodies, as well as the cigarette smoke-induced airway inflammation and mucus hypersecretion pathway in animals, where it can inhibit caspase-3-mediated inflammatory responses downstream of the NLRP3 inflammasome and downregulate the expression of pro-inflammatory factors and mucins. Existing studies have not reported its precise IC₅₀ or EC₅₀ quantitative parameters: in the petunia self-incompatibility system, 0.25 mM is an effective working concentration, and stigma treatment 2 h before pollination can completely inhibit self-incompatibility-induced pollen tube PCD, allowing pollen tubes to grow normally to the ovary and complete fertilization and fruit set; a concentration of 1 mM significantly inhibits the growth of all pollen tubes, and a concentration of 1.99 mM is toxic to pistil tissues. Animal experiments were all therapeutic applications in disease models, using a cigarette smoke-induced chronic obstructive pulmonary disease model in C57BL/6J mice, with a dosing regimen of 3 mg/kg by intraperitoneal injection once every two days, which significantly reduced serum IL-1β and IL-8 levels, decreased the content of mucin Muc5ac in bronchoalveolar lavage fluid, and alleviated inflammatory cell infiltration in the airways, but did not show a significant improvement in emphysematous lesions.

References:

[1] He M, Zhang G, Shen F, Li X. Effects of Z-VaD-Ala-Asp-Fluoromethyl Ketone (Z-VAD-FMK) and Acetyl-Asp-Glu-Val-Asp-Aldehyde(Ac-DEVD-CHO) on Inflammation and Mucus Secretion in Mice Exposed to Cigarette Smoke. Int J Chron Obstruct Pulmon Dis. 2023 Feb 5;18:69-78. doi: 10.2147/COPD.S385748. PMID: 36777242; PMCID: PMC9910210.

[2] Zakharova EV, Demyanchuk IS, Sobolev DS, Golivanov YY, Baranova EN, Khaliluev MR. Ac-DEVD-CHO (caspase-3/DEVDase inhibitor) suppresses self-incompatibility-induced programmed cell death in the pollen tubes of petunia (Petunia hybrida E. Vilm.). Cell Death Discov. 2024 Jan 30;10(1):59. doi: 10.1038/s41420-024-01821-x. PMID: 38287001; PMCID: PMC10825214.