ZIP14-IN-1
Based on 1 Customer Validation
ZIP 14-IN-1 (PPTD) is a selective and orally active ZIP14 inhibitor. ZIP 14-IN-1 inhibits ZIP14 while sparing ZIP8 (SLC39A8). ZIP 14-IN-1 efficiently blocks ZIP14-mediated uptake of multiple divalent metals (zinc, iron, manganese and cadmium). ZIP 14-IN-1 binds to a pocket formed at the dimer interface of ZIP14, obstructing the metal transport pathway. ZIP 14-IN-1 effectively reverses the consequent elevation of reactive oxygen species (ROS) and lipid peroxidation, attenuating metal-induced cytotoxicity. ZIP 14-IN-1 can be uses for cancer cachexia research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.82%
- No. CAS: 1048-17-5
- Fòrmula: C21H25N3O
- Peso molecular:335.44
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
ZIP 14-IN-1 (compound 14) exhibits an IC50 of 8.1 μM for ZIP14-mediated zinc uptake in TREx-hZIP14, has no significant inhibition in TREx-hZIP8 cells at 37μM[1].
ZIP 14-IN-1 (0.03 to 50 µM) inhibits the uptake of all four metals (zinc, iron, manganese, and cadmium) with IC50s of 6.25μM and 6.06μM for Iron and Zinc, respectively, in TREx-cell lines and Xenopus laevis oocytes[1].
ZIP 14-IN-1 (0-50 μM, 24 h) blocks ZIP14-mediated metal influx and attenuated the associated cytotoxicity in TREx -hZIP14 cells and mouse myoblast cells[1].
ZIP 14-IN-1 (10 μM) suppresses ZIP14-mediated ROS and LPO production and inflammatory response in TREx-hZIP14 or TREx-hZIP8 cells[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:TREx-hZIP14 cells and mouse myoblast cells
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Concentration:0, 10 and 50 μM
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Incubation Time:24 h
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Result:Attenuated the sensitization of TREx-hZIP14 cells to zinc, iron, manganese, and cadmium induced by ZIP14 expression.
Reduced ZIP14 dependent metal uptake, elevated the generation of reactive oxygen species (ROS) and lipid peroxides (LPO) and attenuating cytotoxicity.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4T1 breast cancer cells(1 × 105 cells in 200 μL of 1:1 Matrigel/PBS)-induced female 456 BALB/cByJ mice (4 weeks)[1]
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Dosage:0.1 and 1.0 g/L
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Administration:p.o. in drinking water, daily for 10 days
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Result:Attenuated weight loss at both low and high doses and extended overall survival.
Significantly delayed the progression of cachexia-related symptoms, including ≥ 10% body weight loss and death.
Prevented structural deterioration in the skeletal muscles and inflammation responses.
Improved locomotor activity in the model.
Chemical Information
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No. CAS 1048-17-5
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Appearance Solid
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Peso molecular 335.44
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Fòrmula C21H25N3O
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Color White to off-white
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SMILES
O=C1NCN(C2=CC=CC=C2)C13CCN(CCC4=CC=CC=C4)CC3
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Synonyms
PPTD
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (298.12 mM; ultrasonic and warming and heat to 60°C; 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.
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.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hara T, et al. Matsukawa K, Ujihara S, Kawabe T, Taguchi H, Fujishiro H, Jenkitkasemwong S, Nunomura K, Lin B, Fukunaka A, Yoshigai E, Mishima K, Nakagawa S, Knutson MD, Imagawa H, Matsunaga N, Ohdo S, Hamachi I, Sakurai H, Fukada T. Discovery of a Selective Inhibitor of ZIP14 with Therapeutic Potential for Cancer-associated Cachexia. bioRxiv [Preprint]. 2025 Oct 23:2025.10.23.682519. [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 | 2.9812 mL | 14.9058 mL | 29.8116 mL | 74.5290 mL |
| 5 mM | 0.5962 mL | 2.9812 mL | 5.9623 mL | 14.9058 mL | |
| 10 mM | 0.2981 mL | 1.4906 mL | 2.9812 mL | 7.4529 mL | |
| 15 mM | 0.1987 mL | 0.9937 mL | 1.9874 mL | 4.9686 mL | |
| 20 mM | 0.1491 mL | 0.7453 mL | 1.4906 mL | 3.7264 mL | |
| 25 mM | 0.1192 mL | 0.5962 mL | 1.1925 mL | 2.9812 mL | |
| 30 mM | 0.0994 mL | 0.4969 mL | 0.9937 mL | 2.4843 mL | |
| 40 mM | 0.0745 mL | 0.3726 mL | 0.7453 mL | 1.8632 mL | |
| 50 mM | 0.0596 mL | 0.2981 mL | 0.5962 mL | 1.4906 mL | |
| 60 mM | 0.0497 mL | 0.2484 mL | 0.4969 mL | 1.2421 mL | |
| 80 mM | 0.0373 mL | 0.1863 mL | 0.3726 mL | 0.9316 mL | |
| 100 mM | 0.0298 mL | 0.1491 mL | 0.2981 mL | 0.7453 mL |
ZIP14-IN-1 Related Classifications
HY-179571 Related Classifications
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