| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg | |||
| Other Sizes |
| Targets |
hCA/Wnt/β-catenin-IN-1 targets human carbonic anhydrase isoforms hCA II, hCA IX, and hCA XII with Ki values of 33.6, 24.1, and 6.8 nM, respectively. This potent and selective inhibition of the tumor-associated isoforms IX and XII is a key feature of its mechanism. It also targets the Wnt/β-catenin signaling pathway by abrogating the association of β-catenin with TCF-4. Furthermore, it effectively reduces the activity of P-glycoprotein (P-gp), a membrane transporter that mediates multidrug resistance in cancer cells. This triple-targeting approach makes it a valuable tool for studying and potentially overcoming drug resistance.
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| ln Vitro |
In vitro, hCA/Wnt/β-catenin-IN-1 is a potent inhibitor of hCA II, IX, and XII. It has demonstrated significant inhibition of cancer cell viability, including in the NCI/ADR-RES doxorubicin-resistant cell line. This activity is attributed to its ability to reduce P-gp activity and suppress the Wnt/β-catenin signaling pathway. By inhibiting carbonic anhydrases, the compound can also affect the pH balance of the tumor microenvironment, which can further impair cancer cell survival and proliferation. Its ability to overcome multidrug resistance makes it particularly interesting for cancer research.
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| ln Vivo |
Specific in vivo activity data for hCA/Wnt/β-catenin-IN-1 are not detailed in the available literature. However, its potent in vitro activity against cancer cell lines, especially the multidrug-resistant NCI/ADR-RES line, and its ability to inhibit key cancer-related pathways strongly suggest that it would have significant efficacy in vivo. It is expected to be evaluated in mouse xenograft models of various cancers, including those that are resistant to conventional chemotherapy. Such studies would be essential to confirm its antitumor activity and to assess its pharmacokinetic and safety profiles.
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| Enzyme Assay |
Non-cellular enzyme assays are used to characterize the inhibitory activity of hCA/Wnt/β-catenin-IN-1 against human carbonic anhydrases. In these assays, the compound is incubated with the purified enzyme (hCA II, IX, or XII) and a suitable substrate, such as 4-nitrophenyl acetate. The inhibition of enzymatic activity is measured spectrophotometrically, and Ki values are calculated from the dose-response curves. These assays provide direct evidence of the compound's potency and selectivity for the different hCA isoforms.
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| Cell Assay |
In vitro cellular assays are used to evaluate the broader anti-cancer effects of hCA/Wnt/β-catenin-IN-1. Cancer cell lines, including the doxorubicin-resistant NCI/ADR-RES cells, are treated with the compound. Cell viability is assessed using standard assays such as MTT or CellTiter-Glo. The compound's effect on P-gp activity can be measured using fluorescent substrates that are effluxed by the transporter. Inhibition of the Wnt/β-catenin pathway is confirmed by measuring the expression of downstream target genes or by using reporter assays that measure β-catenin-dependent transcription.
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| Animal Protocol |
In vivo animal experiments for hCA/Wnt/β-catenin-IN-1 would typically be conducted in mouse xenograft models. Immunodeficient mice would be implanted with human cancer cells, particularly those that are multidrug-resistant. The compound would be administered via intraperitoneal (IP) or oral (PO) routes, and tumor growth inhibition would be the primary endpoint. Tumor tissues would be analyzed for hCA inhibition, P-gp activity, and Wnt/β-catenin signaling to confirm target engagement in vivo.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties for hCA/Wnt/β-catenin-IN-1 are not detailed in the available sources. As a small molecule with a molecular weight of 492.54, its PK would be influenced by factors such as solubility, metabolic stability, and permeability. Its properties would be characterized in preclinical studies, including parameters like half-life, clearance, volume of distribution, and oral bioavailability. The compound is stable as a powder when stored at -20°C for up to 3 years.
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| Toxicity/Toxicokinetics |
Toxicological data for hCA/Wnt/β-catenin-IN-1 are not provided in the available sources. As a research compound, its safety profile has not been extensively characterized. However, its inhibition of carbonic anhydrases and the Wnt/β-catenin pathway could have potential on-target toxicities, and comprehensive toxicological studies would be required for any therapeutic development.
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| References | |
| Additional Infomation |
hCA/Wnt/β-catenin-IN-1 has a molecular formula of C26H24N2O6S and a molecular weight of 492.54. Its CAS number is 3032826-63-1. It is a potent inhibitor of human carbonic anhydrases and also suppresses the Wnt/β-catenin signaling pathway and P-gp activity. It has demonstrated significant inhibition of cancer cell viability, including in multidrug-resistant cell lines. It is supplied for research purposes only.
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| Molecular Formula |
C26H24N2O6S
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| Molecular Weight |
492.54
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| Appearance |
White to off-white 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 | 2.0303 mL | 10.1515 mL | 20.3029 mL | |
| 5 mM | 0.4061 mL | 2.0303 mL | 4.0606 mL | |
| 10 mM | 0.2030 mL | 1.0151 mL | 2.0303 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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