FB231
Based on 1 Customer Validation
FB231 is a Parkin activator. FB231 can induce mild mitochondrial stress, resulting in impaired mitochondrial function and activation of the integrated stress response. FB231 can lower the threshold for mitochondrial toxins to induce PINK1/Parkin-mediated mitophagy. FB231 can cause activation of the integrated stress response (ISR) and perturbation to iron-dependent pathways. FB231 can be used for the research of neurological disease, such as Parkinson’s disease.
For research use only. We do not sell to patients.
- Purity : 99.45%
- CAS No.: 2166045-37-8
- Formula: C24H21N5O2
- Molecular Weight:411.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
In Vitro
FB231 activates Parkin and enhances Parkin-mediated mitophagy induced by low-dose Oligomycin (HY-N6782)/Antimycin (O/A) (EC50 = 0.67 μM)[1].
FB231 (0.3125-20 μM, 6-24 h) reduces the threshold of O/A-induced mitophagy in YFP-Parkin/mt-Keima-expressing HeLa cells and SH-SY5Y cells with endogenous Parkin[1].
FB231 effectively chelates Fe2+ with an EC50 of 23.2 μM[1].
FB231 (6 h) increases mitochondrial oxygen consumption rate (OCR) and reduces cell sensitivity to the complex V inhibitor Oligomycin in WT HeLa cells[1].
FB231 (3.125-20μM, 24 h) reduces cell viability in HeLa and SH-SY5Y cells[1].
FB231 (10 μM, 16 h) induces the expression of ISR markers ATF3, ATF4, and IFRD1 in WT HeLa, YFP-Parkin HeLa, and PINK1-knockout HeLa cells [1].
FB231 (40 μM) stabilizes the HECT domain E3 ligase HERC4 and destabilizes the iron-responsive protein IREB2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:WT HeLa (no endogenous Parkin)
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Concentration:10 μM
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Incubation Time:16 h
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Result:Increased ATF3, ATF4, and IFRD1 levels Promoted the accumulation of the full-length form of mitochondrial protein DELE1.
Activated the DELE1-HRI-EIF2α pathway.
Chemical Information
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CAS No. 2166045-37-8
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Appearance Solid
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Molecular Weight 411.46
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Formula C24H21N5O2
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Color White to off-white
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SMILES
CC1=C(C=CC=C1)C(NC2=NN(C(NC(C3=C(C=CC=C3)C)=O)=N2)C4=CC=CC=C4)=O
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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
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (243.04 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)
In Vivo:
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 (6.08 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.
In Vivo Dissolution Calculator
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.
Protocols
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Mitochondrial membrane-potential fluorescent assay
Mitochondrial membrane potential fluorescent assays estimate ΔΨm in living cells using lipophilic cationic dyes such as TMRM, TMRE, rhodamine 123, and JC-1, which accumulate in mitochondria according to membrane polarization; loss of signal after FCCP or CCCP treatment is interpreted as mitochondrial depolarization. TMRM/TMRE and rhodamine 123 are commonly used for semi-quantitative live-cell microscopy or flow cytometry, while JC-1 can report a shift from red aggregate fluorescence to green monomer fluorescence during depolarization; interpretation requires controls because dye concentration, quenching mode, cell type, dye efflux, and mitochondrial mass can affect fluorescence independently of ΔΨm.
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Mitochondrial membrane-potential and mitochondrial mass staining
Mitochondrial membrane potential staining measures the electrochemical polarization across the mitochondrial inner membrane in live cells using lipophilic cationic fluorescent probes; early rhodamine-based work showed that selective mitochondrial dye accumulation is lost when the mitochondrial transmembrane potential is dissipated. JC-1 reports mitochondrial polarization by shifting from green monomer fluorescence to red J-aggregate fluorescence as dye concentration increases within energized mitochondria; therefore, the red/green fluorescence ratio is used as a relative readout of mitochondrial membrane potential. TMRE or TMRM staining provides a single-channel relative readout because these cationic rhodamine esters accumulate in polarized mitochondria, and lower fluorescence indicates reduced mitochondrial polarization when acquisition and dye-loading conditions are controlled. Mitochondrial mass staining is commonly performed with MitoTracker Green FM or related MitoTracker dyes as
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Mitophagy Solutions
Mitophagy is the selective autophagic degradation of mitochondria and functions as a mitochondrial quality-control pathway that removes damaged, depolarized, excess, or developmentally programmed mitochondria. The pathway links mitochondrial damage recognition, autophagosome recruitment, lysosomal delivery, and mitochondrial turnover to phenotypes such as mitochondrial homeostasis, oxidative-stress control, metabolic remodeling, differentiation, and neurodegeneration-related mitochondrial fidelity. The best-characterized damage-induced pathway is the PINK1-Parkin axis. Parkin is recruited selectively to impaired mitochondria and promotes their autophagic elimination, while mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, recruits Parkin, and activates Parkin-dependent mitophagy. PINK1 also phosphorylates ubiquitin to activate Parkin E3 ubiquitin ligase activity, and PINK1-driven ubiquitin phosphorylation creates a feed-forward signal for recruiting autophagy machi
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Research Protocol for Neurological Diseases
PINK1/Parkin-mediated mitophagy pathway is a mitochondrial quality-control signaling axis in which mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, activates Parkin recruitment and E3 ubiquitin ligase activity, promotes ubiquitination of outer mitochondrial membrane proteins, recruits selective autophagy adaptors, and drives lysosomal degradation of damaged mitochondria. In neurological disease research, this pathway is experimentally important because neurons, especially dopaminergic neurons, are highly dependent on mitochondrial integrity, and defective mitochondrial turnover can lead to mitochondrial dysfunction, oxidative stress, impaired neuronal survival, α-synuclein accumulation, and neuroinflammatory damage-associated signals. The genetic disease link is strongest in Parkinson’s disease because mutations in PRKN/parkin cause autosomal recessive juvenile parkinsonism, mutations in PINK1 cause hereditary early-onset Parkinson’s disease, and Drosophila studie
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.4304 mL | 12.1518 mL | 24.3037 mL | 60.7592 mL |
| 5 mM | 0.4861 mL | 2.4304 mL | 4.8607 mL | 12.1518 mL | |
| 10 mM | 0.2430 mL | 1.2152 mL | 2.4304 mL | 6.0759 mL | |
| 15 mM | 0.1620 mL | 0.8101 mL | 1.6202 mL | 4.0506 mL | |
| 20 mM | 0.1215 mL | 0.6076 mL | 1.2152 mL | 3.0380 mL | |
| 25 mM | 0.0972 mL | 0.4861 mL | 0.9721 mL | 2.4304 mL | |
| 30 mM | 0.0810 mL | 0.4051 mL | 0.8101 mL | 2.0253 mL | |
| 40 mM | 0.0608 mL | 0.3038 mL | 0.6076 mL | 1.5190 mL | |
| 50 mM | 0.0486 mL | 0.2430 mL | 0.4861 mL | 1.2152 mL | |
| 60 mM | 0.0405 mL | 0.2025 mL | 0.4051 mL | 1.0127 mL | |
| 80 mM | 0.0304 mL | 0.1519 mL | 0.3038 mL | 0.7595 mL | |
| 100 mM | 0.0243 mL | 0.1215 mL | 0.2430 mL | 0.6076 mL |