Ac-FLTD-CMK

Ac-FLTD-CMK is a specific inhibitor for inflammatory caspases. Ac-FLTD-CMK inhibits gasdermin D (GSDMD) cleavage by caspases-1, -4, -5, and -11 in vitro. Ac-FLTD-CMK is effective against caspases-1, caspases-4 and caspases-5 with IC50 of 46.7 nM, 1.49 μM and 329 nM, respectively.

Ac-FLTD-CMK Chemical Structure

Ac-FLTD-CMK Chemical Structure

CAS No. 2376255-48-8

Purity & Quality Control

Ac-FLTD-CMK Related Products

Biological Activity

Description Ac-FLTD-CMK is a specific inhibitor for inflammatory caspases. Ac-FLTD-CMK inhibits gasdermin D (GSDMD) cleavage by caspases-1, -4, -5, and -11 in vitro. Ac-FLTD-CMK is effective against caspases-1, caspases-4 and caspases-5 with IC50 of 46.7 nM, 1.49 μM and 329 nM, respectively.
Targets
caspases-1 [1]
(Cell-free assay)
caspases-5 [1]
(Cell-free assay)
caspases-4 [1]
(Cell-free assay)
46.7 nM 329 nM 1.49 μM
In vitro
In vitro

A GSDMD-derived inhibitor, N-acetyl-Phe-Leu-Thr-Asp-chloromethylketone (Ac-FLTD-CMK), inhibits GSDMD cleavage in vitro and suppresses pyroptosis downstream of both canonical and noncanonical inflammasomes.[1]

Cell Research Cell lines BMDM cells
Concentrations 10 μM
Incubation Time 30 mins
Method

To observe ASC speck formation, BMDM cells expressing cerulean-ASC are plated at 2 x 104 /well in 96-well plates the day prior to experiment. Cells are primed with 200 ng/ml LPS for 4 hours before stimulating with either 5 mM ATP or 10 μM nigericin to activate the NLRP3 inflammasome, in the presence or absence of 10 μM z-VAD-FMK, Ac-FLTD-CMK, or MCC950. After 30 mins, the cerulean-ASC speck formation is observed with a Leica DMIL fluorescence microscopy.

In Vivo
In vivo

Ac-FLTD-CMK inhibits pyroptosis and exerts neuroprotective effect in a mice model of traumatic brain injury.[2]

Animal Research Animal Models 10–12 week-old male C57BL/6 mice
Dosages 0.5 μg for each mouse
Administration ICV

Chemical Information & Solubility

Molecular Weight 569.05 Formula

C26H37ClN4O8

CAS No. 2376255-48-8 SDF --
Smiles CC(C)CC(NC(=O)C(CC1=CC=CC=C1)NC(C)=O)C(=O)NC(C(C)O)C(=O)NC(CC(O)=O)C(=O)CCl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (175.73 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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