In vitro: Z-FA-FMK inhibits the degradation of fibrillar collagen by fibroblasts and osteoclasts. Z-FA-FMK inhibits LPS-induced cytokine production via inhibition of NF-kappaB-dependent gene expression in macrophages. Z-FA-FMK efficiently blocks T cell proliferation induced by mitogens and IL-2 in vitro.
In vivo: Z-FA-FMK significantly increases pneumococcal growth in both lungs and blood in a mouse model of intranasal pneumococcal infection. Z-FA-FMK blocks reovirus infection of Ras oncogenic tumours and host heart tissues in severe combined immunodeficiency mice.
|Preparation 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.|
|Incubation time||72 h|
|Animal models||SCID mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||77 mg/mL in DMSO|
Suppression of Human T Cell Proliferation Mediated by the Cathepsin B Inhibitor, z-FA-FMK Is Due to Oxidative Stress.
Rajah T, et al. PLoS One. 2015 Apr 27;10(4):e0123711. PMID: 25915766.
Z-FA-FMK as a novel potent inhibitor of reovirus pathogenesis and oncolysis in vivo.
Kim M, et al. Antivir Ther. 2010;15(6):897-905. PMID: 20834102.
|GJ103 sodium salt
GJ103 sodium salt is an active analog of the read-through compound GJ072.
Tubercidin (7-Deazaadenosine) is an adenosine analog, is an antibiotic obtained from Streptomyces tubercidicus.
ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM) and TRPC6 channel (IC50>10 μM).
Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
Apoptozole is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
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