ATN-224
Based on 6 publication(s) in Google Scholar
ATN-224 is an orally active Cu2+/Zn2+-superoxide dismutase 1 (SOD1) inhibitor. ATN-224 inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.0%
- CAS. Nr.: 649749-10-0
- Formel: C10H28MoN2O2S4
- Molecular Weight:432.56
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) ATN-224
More- Burns Trauma. 2025 Feb 17:13:tkaf007. [Abstract]
- Cell Death Discov. 2022 Feb 17;8(1):69. [Abstract]
- Br J Pharmacol. 2026 Aug;183(15):4471-4499. [Abstract]
- Anal Chem. 2018 Jan 16;90(2):1317-1324. [Abstract]
- Food Funct. 2021 May 11;12(9):3898-3918. [Abstract]
- Eur J Pharmacol. 2026 Jun 25:1030:179091. [Abstract]
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IF
Biologische Aktivität
IC50: 17.5±3.7 nM (SOD1, in endothelial cells)[1]
ATN-224 has a specific and high affinity for copper ions (108 mol/L-1) and shows no binding to calcium, iron, magnesium, zinc, or manganese ions at concentrations up to 1 mM as determined by isothermal titration calorimetry. ATN-224 inhibits the proliferation of both HUVEC (IC50=1.4±0.3 μM; n=5). ATN-224 is also able to inhibit the activity of purified bovine SOD1 with an IC50 of 0.33±0.03 μM after 24 hours of incubation. The SOD1 inhibition by ATN-224 is time dependent, reaching maximal inhibition at ~16 hours. ATN-224 seems to inhibit SOD1 by depleting the enzyme of copper. ATN-224 is able to inhibit SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM. ATN-224 inhibits FGF-2-induced ERK1/2 phosphorylation in a dose-dependent and time-dependent manner with an IC50 between 1.25 and 2.5 μM, consistent with the IC50 for the inhibition of proliferation[1]. ATN-224 is an orally-available inorganic small molecule that inhibits the copper/zinc-dependent enzyme, superoxide dismutase 1 (Cu/Zn-SOD1), in endothelial and tumor cells[2].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 649749-10-0
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Appearance Solid
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Molecular Weight 432.56
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Formel C10H28MoN2O2S4
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Color Pink to red
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SMILES
OCC[N+](C)(C)C.OCC[N+](C)(C)C.[S-][Mo]([S-])(=S)=S
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Synonyms
Bischolinetetrathiomolybdate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Burns Trauma
Flufenamic acid inhibits pyroptosis in ischemic flaps via the AMPK-TRPML1-Calcineurin signaling pathway. [Abstract]2025 Feb 17:13:tkaf007. PMID: 40655077 -
Cell Death Discov
Mitochondrial homeostasis regulates definitive endoderm differentiation of human pluripotent stem cells. [Abstract]2022 Feb 17;8(1):69. PMID: 35177589 -
Br J Pharmacol
A novel recombinant peptide, RGD-Latcripin-7A, targeting neovascularization in skin transplantation: Tissue regeneration and autophagy mechanism. [Abstract]2026 Aug;183(15):4471-4499. PMID: 42063339 -
Anal Chem
Visualizing the Regulation of Hydroxyl Radical Level by Superoxide Dismutase via a Specific Molecular Probe. [Abstract]2018 Jan 16;90(2):1317-1324. PMID: 29237269
ATN-224 purchased from MedChemExpress. Usage Cited in: Anal Chem. 2018 Jan 16;90(2):1317-1324. [Abstract]
Illumination of the ・OH release along the deactivation of SOD1 by enzyme inhibitor ATN-224. The RAW 264.7 cells are treated by 100 μM ATN-224 for 0, 2, 6, 18 h, and then incubated with 10 μM P2 for 30 min. Scale bar: 10 μm. Fluorescence intensity (F) is displayed as yellow bars.
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Food Funct
Hesperetin ameliorates hepatic oxidative stress and inflammation via the PI3K/AKT-Nrf2-ARE pathway in oleic acid-induced HepG2 cells and a rat model of high-fat diet-induced NAFLD. [Abstract]2021 May 11;12(9):3898-3918. PMID: 33977953 -
Eur J Pharmacol
Bergapten promotes angiogenesis by enhancing endothelial autophagy and reducing pyroptosis in ischemic skin flap. [Abstract]2026 Jun 25:1030:179091. PMID: 42349817
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (115.59 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.78 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 (5.78 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.
Protokoll
Cells are plated in a six-well format (100-300,000 per well) and incubated with ATN-224 at indicated concentrations and for indicated times. Cells are then stimulated with 10 ng/mL FGF-2 for various times and lysed. Lysates are subjected to Western blot analysis using an antibody specific for phosphorylated p44/42 mitogen-activated protein kinase (Thr202/Tyr204) with appropriate signal correction using an antibody specific for p44/42 mitogen-activated protein kinase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Human umbilical vein endothelial cells (HUVEC) are maintained in M200/LSGS medium and cells are used between passages 2 and 4 for all experiments. For proliferation assay, cells are plated at 3,000 per well on 0.1% gelatin in M200/2% FBS for 4 hours and then stimulated with 2 ng/mL FGF-2 in the presence or absence of ATN-224 up to 48 hours. HUVEC proliferation is determined using either the Alamar Blue or the MTT assay. Multiple myeloma MM1S cells are grown in RPMI 1640 with 10% fetal bovine serum and 2 mM L-glutamine. HL-60 promyelocytic leukemia cells and MOLT-4 acute myeloblastic leukemia cells are plated at 400,000/mL in T-75 flasks and incubated for 48 to 96 hours for proliferation assays. MMS1 cell proliferation is determined using calcein AM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Cold Matrigel (500 μL) is mixed with 800 ng/mL FGF-2 or 300 ng/mL VEGF and heparin (50 μg/mL). Negative control plugs did not contain the proangiogenic factors. The Matrigel mixture is injected s.c. into 4- to 8-week-old female BALB/c nude mice. In some experiments, either ATN-224 (94 μM) with or without Mn-TBAP (100 μM) or water is added directly to the Matrigel plug in the treated and negative control groups, respectively. Alternatively, mice are treated by oral gavage either with distilled water or ATN-224 everyday from Monday to Friday. Animals are sacrificed and the plugs are recovered 5 days after plug injection. The plugs are then minced and homogenized with a tissue homogenizer, and hemoglobin levels in the plugs are determined using Drabkin's solution.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (279 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)
Verweise
[1]. Juarez JC, et al. Copper binding by tetrathiomolybdate attenuates angiogenesis and tumor cell proliferation through the inhibition of superoxide dismutase 1. Clin Cancer Res. 2006 Aug 15;12(16):4974-82. [Content Brief]
[2]. Lin J, et al. A non-comparative randomized phase II study of 2 doses of ATN-224, a copper/zinc superoxide dismutase inhibitor, in patients with biochemically recurrent hormone-na?ve prostate cancer. Urol Oncol. 2013 Jul;31(5):581-8. [Content Brief]
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 | 2.3118 mL | 11.5591 mL | 23.1182 mL | 57.7955 mL |
| 5 mM | 0.4624 mL | 2.3118 mL | 4.6236 mL | 11.5591 mL | |
| 10 mM | 0.2312 mL | 1.1559 mL | 2.3118 mL | 5.7795 mL | |
| 15 mM | 0.1541 mL | 0.7706 mL | 1.5412 mL | 3.8530 mL | |
| 20 mM | 0.1156 mL | 0.5780 mL | 1.1559 mL | 2.8898 mL | |
| 25 mM | 0.0925 mL | 0.4624 mL | 0.9247 mL | 2.3118 mL | |
| 30 mM | 0.0771 mL | 0.3853 mL | 0.7706 mL | 1.9265 mL | |
| 40 mM | 0.0578 mL | 0.2890 mL | 0.5780 mL | 1.4449 mL | |
| 50 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1559 mL | |
| 60 mM | 0.0385 mL | 0.1927 mL | 0.3853 mL | 0.9633 mL | |
| 80 mM | 0.0289 mL | 0.1445 mL | 0.2890 mL | 0.7224 mL | |
| 100 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5780 mL |
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