FMK 9a
Based on 2 publication(s) in Google Scholar
FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.
For research use only. We do not sell to patients.
- Purity: ≥98.0%
- CAS No.: 1955550-51-2
- Formula: C23H21FN2O3
- Molecular Weight:392.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) FMK 9a
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Biological Activity
IC50: 80 nM (autophagin-1, FRET assay); 73 nM (autophagin-1, LRA assay)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
>100 μM
Compound: 9a
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Inhibition of recombinant human cathepsin D (400 residues) expressed in CHO cells using 5-FAM/QXL 520 FRET peptide as substrate preincubated for 20 mins followed by substrate addition by fluorescence plate reader analysis
Inhibition of recombinant human cathepsin D (400 residues) expressed in CHO cells using 5-FAM/QXL 520 FRET peptide as substrate preincubated for 20 mins followed by substrate addition by fluorescence plate reader analysis
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[PMID: 27563406] |
| CHO | IC50 |
0.2 μM
Compound: 9a
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Inhibition of recombinant human cathepsin B (332 residues) expressed in CHO cells using Z-FR-AMC as substrate preincubated for 20 mins followed by substrate addition by fluorescence plate reader analysis
Inhibition of recombinant human cathepsin B (332 residues) expressed in CHO cells using Z-FR-AMC as substrate preincubated for 20 mins followed by substrate addition by fluorescence plate reader analysis
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[PMID: 27563406] |
| HEK-293T | CC50 |
>100 μM
Compound: 9a
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Cytotoxicity against HEK293T cells after 24 hrs
Cytotoxicity against HEK293T cells after 24 hrs
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[PMID: 27563406] |
ATG4B or autophagin-1 is a cysteine protease that cleaves ATG8 family proteins. ATG4B plays essential roles in the autophagosome formation and the autophagy pathway. FMK 9a shows strong inhibition of ATG4B, with IC50 values of 80 and 73 nM in the TR-FRET and cellular-based LRA assays, respectively. LC MS/MS study indicates that FMK 9a forms an irreversible covalent bond with the more reactive thiol group of Cys74 located at the catalytic site of ATG4B and thus inactivates ATG4B proteolytic activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1955550-51-2
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Appearance Solid
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Molecular Weight 392.42
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Formula C23H21FN2O3
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Color White to off-white
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SMILES
O=C(C1=C(C=CC=C2)C2=CC=C1)N[C@H](C(NCC(CF)=O)=O)CC3=CC=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Autophagy
Mitochondrial respiration supports autophagy to provide stress resistance during quiescence. [Abstract]2022 Oct;18(10):2409-2426. PMID: 35258392 -
Solvent & Solubility
DMSO : 100 mg/mL (254.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
FMK 9a is dissolved in DMSO. 5 μL of serial-diluted FMK 9a (1% DMSO) in assay buffer is added into 5 μL of purified ATG4B (final 0.1 nM) in 384-well plate, and the solution is incubated at room temperature (rt) for 30 min. Then, 5 μL of His-GATE-16-GST (final 20 nM) is added into the wells, and the solution is incubated for another 30 min. 5 μL of detection solution (final 2 nM of Eu-anti-His and 20 nM of Ulight-anti-GST) is added, and the resulting mixture is incubated at rt for 40 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5483 mL | 12.7415 mL | 25.4829 mL | 63.7073 mL |
| 5 mM | 0.5097 mL | 2.5483 mL | 5.0966 mL | 12.7415 mL | |
| 10 mM | 0.2548 mL | 1.2741 mL | 2.5483 mL | 6.3707 mL | |
| 15 mM | 0.1699 mL | 0.8494 mL | 1.6989 mL | 4.2472 mL | |
| 20 mM | 0.1274 mL | 0.6371 mL | 1.2741 mL | 3.1854 mL | |
| 25 mM | 0.1019 mL | 0.5097 mL | 1.0193 mL | 2.5483 mL | |
| 30 mM | 0.0849 mL | 0.4247 mL | 0.8494 mL | 2.1236 mL | |
| 40 mM | 0.0637 mL | 0.3185 mL | 0.6371 mL | 1.5927 mL | |
| 50 mM | 0.0510 mL | 0.2548 mL | 0.5097 mL | 1.2741 mL | |
| 60 mM | 0.0425 mL | 0.2124 mL | 0.4247 mL | 1.0618 mL | |
| 80 mM | 0.0319 mL | 0.1593 mL | 0.3185 mL | 0.7963 mL | |
| 100 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6371 mL |
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