All Photos(2)
Synonym(s):
N-acetyl-Phe-Leu-Thr-Asp-chloromethylketone
Empirical Formula (Hill Notation):
C26H37ClN4O8
CAS Number:
Molecular Weight:
569.05
MDL number:
UNSPSC Code:
51111800
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥95% (HPLC)
form
(Powder or Lyophilized powder or film)
storage condition
desiccated
color
white to off-white
storage temp.
-10 to -25°C
Biochem/physiol Actions
Ac-FLTD-CMK is a selective gasdermin D (GSDMD) clevage inhibitor (IC50 = 46.7 nM, 329 nM, 1.49 μM, respectively, against GSDMD clevage by human caspase-1, -5, -4 in cell-free enzymatic assays) that suppresses pyroptosis downstream of both canonical and noncanonical inflammasomes, as well as reduces IL-1β release following activation of the NLRP3 inflammasome in macrophages (10 μM 4h post 200 ng/mL LPS and 0.5h before ATP or nigericin). Ac-FLTD-CMK selectively blocks GSDMD clevage by inflammatory caspases without affecting apoptotic caspases (caspase-3 IC50 >100 μM) or apoptosis.
Caution
Hygroscopic
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Jeanie Quach et al.
Mucosal immunology, 12(2), 323-339 (2018-10-27)
During invasion, Entamoeba histolytica (Eh) encounter macrophages and activate them to elicit tissue damaging pro-inflammatory responses. When Eh binds macrophages via the Gal-lectin, surface EhCP-A5 RGD sequence ligates α5β1 integrin to activate caspase-1 in a complex known as the NLRP3
Endothelial cell pyroptosis plays an important role in Kawasaki disease via HMGB1/RAGE/cathespin B signaling pathway and NLRP3 inflammasome activation
Cell Death & Disease, 10(10), 10(10)-10(10) (2019)
X X Tian et al.
International endodontic journal, 54(6), 916-925 (2020-12-31)
To explore the presence and function of NLRP6-caspase 4 inflammasome in human pulp tissue and human dental pulp cells (HDPCs). Pulp tissue was collected from freshly extracted human caries-free third molars and third molars with irreversible pulpitis. Quantitative real-time polymerase
Jie Yang et al.
Proceedings of the National Academy of Sciences of the United States of America, 115(26), 6792-6797 (2018-06-13)
The inflammasomes are signaling platforms that promote the activation of inflammatory caspases such as caspases-1, -4, -5, and -11. Recent studies identified gasdermin D (GSDMD) as an effector for pyroptosis downstream of the inflammasome signaling pathways. Cleavage of GSDMD by
Pengfei Wang et al.
Neuroreport, 32(3), 188-197 (2021-01-21)
Pyroptosis has been reported to contribute to the traumatic brain injury (TBI) process. Ac-FLTD-CMK is a newly synthesized pyroptosis inhibitor. However, whether Ac-FLTD-CMK inhibits pyroptosis and plays a neuroprotective role after TBI is unknown. The present study aimed to determine
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