Z-FA-FMK

Catalog No.S7391 Batch:S739102

Technical Data

Formula	C₂₁ H₂₃ F N₂ O₄
Molecular Weight	386.42	CAS No.	197855-65-5
Solubility (25°C)*	In vitro	DMSO	77 mg/mL (199.26 mM)
		Ethanol	48 mg/mL (124.21 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Z-FA-FMK ((1S)-Z-FA-FMK) is an irreversible cysteine protease inhibitor, and also inhibits effector caspases.

Targets

cysteine protease ^[1]

In vitro

Z-FA-FMK inhibits the degradation of fibrillar collagen by fibroblasts and osteoclasts. ^[2] Z-FA-FMK inhibits LPS-induced cytokine production via inhibition of NF-kappaB-dependent gene expression in macrophages. ^[3] Z-FA-FMK efficiently blocks T cell proliferation induced by mitogens and IL-2 in vitro. ^[4]

In vivo

Z-FA-FMK significantly increases pneumococcal growth in both lungs and blood in a mouse model of intranasal pneumococcal infection. ^[4] Z-FA-FMK blocks reovirus infection of Ras oncogenic tumours and host heart tissues in severe combined immunodeficiency mice. ^[5]

Protocol (from reference)

Cell Assay:^{^[4]}	Cell lines PBMCs Concentrations ~100 μM Incubation Time 72 hours Method T cell proliferation following mitogen stimulation is determined using [³H]thymidine incorporation. In brief, PBMCs or purified T cells are seeded in a 96-well plate and stimulated with either PHA (5 μg/ml), costimulated with anti-CD3 mAb (5 μg/ml) and anti-CD28 mAb (2.5 μg/ml) or PMA plus ionomycin in the presence or absence of z-FA-FMK. The cells are cultured for 72 h with the last 16 h pulsed with [methyl-³H]thymidine (0.037 MBq). The cells are harvested onto glass fiber filter mats using a Tomtec automated multiwell harvester.

Cell Assay:^{^[4]}

Cell lines
PBMCs
Concentrations
~100 μM
Incubation Time
72 hours
Method
T cell proliferation following mitogen stimulation is determined using [³H]thymidine incorporation. In brief, PBMCs or purified T cells are seeded in a 96-well plate and stimulated with either PHA (5 μg/ml), costimulated with anti-CD3 mAb (5 μg/ml) and anti-CD28 mAb (2.5 μg/ml) or PMA plus ionomycin in the presence or absence of z-FA-FMK. The cells are cultured for 72 h with the last 16 h pulsed with [methyl-³H]thymidine (0.037 MBq). The cells are harvested onto glass fiber filter mats using a Tomtec automated multiwell harvester.

References

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Selleck's Z-FA-FMK has been cited by 10 publications

Pharmacological targeting of TFIIH suppresses KRAS mutant pancreatic ductal adenocarcinoma and synergizes with TRAIL [ Cancer Res, 2022, can.21.4222]	PubMed: 35819261
Potential drug discovery for COVID-19 treatment targeting Cathepsin L using a deep learning-based strategy [ Comput Struct Biotechnol J, 2022, 20:2442-2454]	PubMed: 35602976
Targeting multiple cell death pathways extends the shelf life and preserves the function of human and mouse neutrophils for transfusion [ Sci Transl Med, 2021, 13(604)eabb1069]	PubMed: 34321317
Design of modular autoproteolytic gene switches responsive to anti-coronavirus drug candidates [ Nat Commun, 2021, 12(1):6786]	PubMed: 34811361
SARS-CoV-2 requires cholesterol for viral entry and pathological syncytia formation [ Elife, 2021, 10e65962]	PubMed: 33890572
Development of a Cell-Based Luciferase Complementation Assay for Identification of SARS-CoV-2 3CLpro Inhibitors [ Viruses, 2021, 13(2)173]	PubMed: 33498923
Autophagy Participates in Lysosomal Vacuolation-Mediated Cell Death in RGNNV-Infected Cells [ Front Microbiol, 2020, 30;11:790]	PubMed: 32425913
Ferroptosis Is Involved in Alcohol-Induced Cell Death in vivo and in vitro [ Biosci Biotechnol Biochem, 2020, 18;1-8]	PubMed: 32419644
[ Oncogene, 2018, ]	PubMed: 29326439
The Tumor Suppressor p53 Limits Ferroptosis by Blocking DPP4 Activity [ Cell Rep, 2017, 20(7):1692-1704]	PubMed: 28813679

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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