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Purity: ≥98%
Z-FA-FMK, a novel and irreversible inhibitor of cysteine protease, also inhibits effector caspases. It is a control peptidic fluoromethylketone (boc-Thr-CH2F). Z-FA-FMK is capable of selectively inhibiting recombinant effector caspases 2, -3, -6, and -7 in addition to inhibiting caspase activity in vitro. Conversely, Z-FA-FMK only partially inhibits the apoptosome-associated caspase 9 in vitro, while purified initiator caspases 8 and 10 remain unaffected.
| Targets |
Cathepsin B; cathepsin L; Caspase-2; Caspase-3; Caspase-6; Caspase-7
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| ln Vitro |
Z-FA-FMK prevents fibroblasts and osteoclasts from breaking down fibrillar collagen. [2] Through the inhibition of NF-kappaB-dependent gene expression in macrophages, Z-FA-FMK suppresses the production of cytokines induced by LPS.[3] In vitro, Z-FA-FMK effectively inhibits T cell proliferation that is brought on by mitogens and IL-2.[4]
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| ln Vivo |
Z-FA-FMK dramatically increases the growth of pneumococci in the blood and lungs in a mouse model of intranasal pneumococcal infection.[4] For severe combined immunodeficiency mice, Z-FA-FMK prevents reovirus infection of host heart tissues and Ras oncogenic tumors.[5]
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| Cell Assay |
Through the incorporation of [³H]thymidine, T cell proliferation after mitogen stimulation is measured. PBMCs or purified T cells are seeded in a 96-well plate and stimulated with PHA (5 μg/ml), costimulated with 5 μg/ml anti-CD3 mAb and 2.5 μg/ml anti-CD28 mAb, or PMA plus ionomycin in the presence or absence of z-FA-FMK. [methyl-³H]thymidine (0.037 MBq) is pulsed into the cells for the final 16 hours of their 72-hour culture. Using a Tomtec automated multiwell harvester, the cells are collected onto glass fiber filter mats.
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| Animal Protocol |
SCID mice with HT1080 xenograft (6-8 weeks)
1 mg/kg Intratumor injection; every 2 days, for 27 days |
| References | |
| Additional Infomation |
See also: Z-FA-Fmk (annotation moved to).
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| Molecular Formula |
C21H23N2O4F
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|---|---|---|
| Molecular Weight |
386.42
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| Exact Mass |
386.164
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| Elemental Analysis |
C, 65.27; H, 6.00; F, 4.92; N, 7.25; O, 16.56
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| CAS # |
197855-65-5
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| Related CAS # |
(S,S)-Z-FA-FMK;105637-38-5
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| PubChem CID |
6915837
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
630.5±55.0 °C at 760 mmHg
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| Flash Point |
335.1±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.549
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| LogP |
3.67
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
28
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| Complexity |
517
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FCC(C(C)N([H])C([C@H](CC1C=CC=CC=1)N([H])C(=O)OCC1C=CC=CC=1)=O)=O
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| InChi Key |
ASXVEBPEZMSPHB-PKHIMPSTSA-N
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| InChi Code |
InChI=1S/C21H23FN2O4/c1-15(19(25)13-22)23-20(26)18(12-16-8-4-2-5-9-16)24-21(27)28-14-17-10-6-3-7-11-17/h2-11,15,18H,12-14H2,1H3,(H,23,26)(H,24,27)/t15?,18-/m0/s1
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| Chemical Name |
benzyl N-[(2S)-1-[(4-fluoro-3-oxobutan-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5879 mL | 12.9393 mL | 25.8786 mL | |
| 5 mM | 0.5176 mL | 2.5879 mL | 5.1757 mL | |
| 10 mM | 0.2588 mL | 1.2939 mL | 2.5879 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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