Z-FA-FMK

Catalog No.S7391

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

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Z-FA-FMK Chemical Structure

Z-FA-FMK Chemical Structure
Molecular Weight: 386.42

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description 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]
Features

Protocol(Only for 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.

Animal Study: [4]

Animal Models Mouse model of pneumococcal disease
Formulation
Dosages ~25 mg/kg
Administration i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Rasnick D. Anal Biochem. 1985, 149(2), 461-465.

[2] van Noorden CJ, et al. Biochem Biophys Res Commun. 1991, 178(1), 178-184.

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Chemical Information

Download Z-FA-FMK SDF
Molecular Weight (MW) 386.42
Formula

C21 H23 F N2 O4

CAS No. 197855-65-5
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 77 mg/mL (199.26 mM)
Ethanol 34 mg/mL warming (87.98 mM)
Water <1 mg/mL
In vivo
* <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.
Chemical Name Carbamic acid,N-[(1S)-2-[(3-fluoro-1-methyl-2-oxopropyl)amino]-2-oxo-1-(phenylmethyl)ethyl]-,phenylmethyl ester

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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