| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
IC50:0.164μM(potent peroxiredoxin 1,PRDX1)[1]
PRDX1-IN-1 specifically targets Peroxiredoxin 1 (PRDX1), a member of the peroxiredoxin family of antioxidant enzymes. By inhibiting PRDX1, this compound disrupts the cellular redox balance, leading to an accumulation of reactive oxygen species (ROS). This oxidative stress results in the inhibition of cancer cell proliferation, invasion, migration, and the induction of apoptosis. |
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| ln Vitro |
PRDX1-IN-1 (compound 7e) inhibits the growth of human lung cancer cell A549, human breast cancer cell line MDA-MB-231, human liver cancer cell line SK Activity-Hep-1, and human lung cancer cell lines LETP-a-2 and H1975; the IC50 values are 1.92 μM, 2.93 μM, 1.99 μM, 2.67 μM, and 2.42 μM, respectively [1]. Inhibiting cancer cell growth, invasion, and migration, PRDX1-IN-1 (2 μM or 4 μM, 24 h) increases intracellular ROS buildup [1]. Inducing apoptosis in A549 cells, PRDX1-IN-1 (2 μM or 4 μM, 24 h) [1]. PRDX1-IN-1 (2 μM or 4 μM, 6 h) stimulates the production of apoptosis-related proteins (cleaved caspase-3/8 and cleaved PARP) and inhibits important signaling pathways (AKT and ERK) in A549 cells [1].
In vitro, PRDX1-IN-1 is a selective inhibitor of PRDX1 with an IC50 value of 0.164 microM. Treatment with PRDX1-IN-1 (0.5-10 microM) induces intracellular ROS accumulation and inhibits the proliferation, invasion, and migration of cancer cells, as well as promoting apoptosis. It has potential anti-inflammatory and anticancer activity for the study of breast and esophageal cancer. |
| ln Vivo |
In a mouse lung cancer model, PRDX1-IN-1 (0.5 or 1 mg/kg, ip, daily for 19 days) suppresses tumor growth [1].
In vivo, PRDX1-IN-1 is designed to inhibit PRDX1, leading to the accumulation of ROS within cells. This mechanism has the potential to suppress tumor growth in animal models by inducing oxidative stress and apoptosis in cancer cells. It can be used in research related to cancer, particularly in models of breast and esophageal cancer. |
| Enzyme Assay |
A cell-free enzyme inhibition assay for PRDX1-IN-1 uses purified recombinant human PRDX1 protein. The assay buffer contains HEPES (pH 7.0), DTT, and EDTA. A substrate such as H2O2 or a small organic peroxide is used in a coupled assay with a detection agent (e.g., Amplex Red/horseradish peroxidase). The decrease in fluorescence (ex/em = 560/590 nm) is measured to calculate the IC50.
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| Cell Assay |
Proliferation assay[1]
Cell Types: lung cancer cell lines(LTEP-a-2 and H1975), human breast cancer cell line(MDA-MB-231), human hepatoma cell line(SK-Hep-1) Tested Concentrations: 0.5– 10 μM Incubation Duration: 48 h Experimental Results: Inhibited the proliferation activities of cancer cells A549, LTEP-a-2, H1975, MDA-MB-231, SK-Hep-1. Apoptosis assay [1] Cell Types: human lung cancer cells A549 Tested Concentrations: 2 μM or 4 μM Incubation Duration: 24 h Experimental Results: Increased the ratio of the total number of early(annexin-V+/PI− ) and late(annexin-V+/PI+) apoptotic cells Dramatically. WB assay[1] Cell Types: A549 cell Tested Concentrations: 2 μM or 4 μM Incubation Duration: 6 h Experimental Results: diminished the phosphorylation levels of PI3K, AKT, C-RAF and ERK. Matrigel invasion assay[1] Cell Types: A549 cell Tested Concentrations: 2 μM or 4 μM Incubation Duration: 24 - 48 h Experimental Results: Inhibited the cell matrix and invasion. Breast or esophageal cancer cells are seeded in 96-well plates in appropriate medium. After overnight incubation, cells are treated with PRDX1-IN-1 at varying concentrations (0.5-10 microM) for 24-72 hours. Cell viability is measured by MTT or CellTiter-Glo assay. Intracellular ROS levels are measured using a fluorescent dye (e.g., DCFH-DA). Invasion and migration are assessed using Transwell or scratch wound assays. |
| Animal Protocol |
Animal/Disease Models: C57BL/6J male mice injected with Lewis cell (lung cancer)[1]
Doses: 0.5 or 1 mg/kg Route of Administration: intraperitoneal (ip)injection, every day for 19 days. Experimental Results: Inhibited tumor growth, with the tumor growth inhibition (TGI) values of 77.47% and 69.89% in the groups of 1 mg/kg and 0.5 mg/kg, respectively. Induced the changes in morphological characteristics of tumor cells, including cell agglutination, contraction, and nuclear chromatin marginalization. A standard in vivo animal protocol for PRDX1-IN-1 would involve a mouse xenograft model. Female BALB/c nude mice are implanted subcutaneously with breast (e.g., MDA-MB-231) or esophageal cancer cells. When tumors reach 100-150 mm3, mice are randomized and treated intraperitoneally (i.p.) with PRDX1-IN-1 (10-50 mg/kg). Tumor volume is measured regularly, and ROS levels in the tumor are measured via fluorescent probes. |
| ADME/Pharmacokinetics |
PRDX1-IN-1 has a molecular weight of 713.95 and the formula C46H55N3O4. The product is a powder that should be stored at -20degC for up to 3 years. In solution, it is stable for 6 months at -20degC. Specific PK data are not available. The compound is soluble in DMSO. For in vivo use, it would require formulation in a vehicle such as 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for PRDX1-IN-1 have been reported. As a research chemical, standard laboratory safety precautions should be followed. Since it induces ROS, it may have potential for off-target effects, but these have not been extensively characterized. Standard safety protocols for handling research chemicals apply.
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| References | |
| Additional Infomation |
PRDX1-IN-1 is a research-grade chemical and is not approved for clinical use. It is a selective and potent inhibitor of PRDX1 with an IC50 of 0.164 microM. It is a valuable tool for studying the role of PRDX1 in cancer biology, particularly in breast and esophageal cancer, and for exploring the therapeutic potential of targeting the cellular antioxidant system. It is for research use only.
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| Molecular Formula |
C46H55N3O4
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| Molecular Weight |
713.95
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| Appearance |
Light yellow to yellow solid powder
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4007 mL | 7.0033 mL | 14.0066 mL | |
| 5 mM | 0.2801 mL | 1.4007 mL | 2.8013 mL | |
| 10 mM | 0.1401 mL | 0.7003 mL | 1.4007 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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