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| 25mg |
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Purity: ≥98%
FIN56 (FIN-56), a specific inducer of ferroptosis, causes the loss of GPX4 activity in cell lysates. Squalene synthase is additionally bound to and activated. It has been discovered that inhibiting the lipid-repair enzyme GPX4 causes ferroptosis. GPX4 was made to degrade faster by FIN56. Independent of the GPX4 degradation, FIN56 also binds to and activates the isoprenoid biosynthesis enzyme squalene synthase. Through a mechanism involving the control of GPX4 protein abundance, FIN56 causes ferroptosis. Overexpression of the GFP-GPX4 fusion protein prevents the cell death caused by FIN56. It binds to and activates squalene synthase, an enzyme involved in the synthesis of cholesterol, to suppress non-steroidogenic metabolites—likely coenzyme Q10—in the mevalonate pathway, increasing sensitivity to FIN56-induced ferroptosis.
| Targets |
Ferroptosis
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| ln Vitro |
FIN56 is a specific inducer of ferroptosis. The mechanism involves two distinct pathways: one leads to the degradation of GPX4, which necessitates the enzymatic activity of acetyl-CoA carboxylase, and the other activates squalene synthase, which depletes coenzyme Q10 without relying on the degradation of GPX4[1].
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| ln Vivo |
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| Enzyme Assay |
FIN56 causes the loss of GPX4 activity in cell lysates. FIN56-induced cell death is suppressed by GFP-GPX4 fusion protein overexpression. FIN56 triggers ferroptosis through a mechanism involving the regulation of GPX4 protein abundance.
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| Cell Assay |
In a 10-cm dish, 500,000 HT-1080 cells are seeded. For 16 hours, cells are grown at 37 °C. Cells are cotreated with 100 μM -tocopherol and either a vehicle (DMSO) or a ferroptosis inducer (10 μM erastin, 0.5 μM (1S, 3R)-RSL3, or 5 μM FIN56) on the day of the analysis, and then incubated for 10 h. Next, cells are trypsinized, pelleted, and given a single wash in 400 L of ice-cold PBS containing 1 mM EDTA. Both oxidized and reduced glutathione are quantified in technical triplicates in 120 μL of sample after the cell debris has been pelleted and eliminated. The protein concentration as determined by the Bradford assay is used to normalize the glutathione quantity.
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| References |
| Molecular Formula |
C25H31N3O5S2
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| Molecular Weight |
517.66
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| Exact Mass |
517.1705
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| Elemental Analysis |
C, 58.01; H, 6.04; N, 8.12; O, 15.45; S, 12.39
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| CAS # |
1083162-61-1
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1CCC(CC1)NS(=O)(=O)C2=CC3=C(C=C2)C4=C(C3=NO)C=C(C=C4)S(=O)(=O)NC5CCCCC5
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| InChi Key |
JLCFMMIWBSZOIS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H31N3O5S2/c29-26-25-23-15-19(34(30,31)27-17-7-3-1-4-8-17)11-13-21(23)22-14-12-20(16-24(22)25)35(32,33)28-18-9-5-2-6-10-18/h11-18,27-29H,1-10H2
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| Chemical Name |
2-N,7-N-dicyclohexyl-9-hydroxyiminofluorene-2,7-disulfonamide
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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 |
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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: 2.5 mg/mL (4.83 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 2.5 mg/mL (4.83 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (4.83 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 | 1.9318 mL | 9.6588 mL | 19.3177 mL | |
| 5 mM | 0.3864 mL | 1.9318 mL | 3.8635 mL | |
| 10 mM | 0.1932 mL | 0.9659 mL | 1.9318 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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ACC inhibitor prevents GPX4 protein degradationNat Chem Biol.2016 Jul;12(7):497-503 |
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