| Size | Price | Stock | Qty |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 1.49 μM (MARK4)
MARK4 inhibitor 4 targets the ATP-binding pocket of microtubule affinity-regulating kinase 4 (MARK4). This compound is a selective MARK4 antagonist with an IC50 of 1.49 microM, designed to inhibit MARK4-mediated phosphorylation of microtubule-associated proteins, thereby modulating microtubule stability and cellular proliferation. |
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| ln Vitro |
Compound 23c, or MARK4 inhibitor 4, shows a notable suppression of Hela and U87MG cell growth with EC50 values of 2.16 and 3.51 μM [1]. It is administered at concentrations between 1 and 20 μM for a duration of 24 hours.
MARK4 inhibitor 4 demonstrates notable suppression of cell growth in human cancer cell lines, including HeLa and U87MG cells, with EC50 values of 2.16 microM and 3.51 microM, respectively. It inhibits MARK4 ATPase activity in biochemical assays, with activity confirmed in the micromolar concentration range at doses of 1-20 microM. |
| ln Vivo |
Not available. MARK4 inhibitor 4 has been studied in the context of cancer research and cow head lesions; however, specific in vivo efficacy data, including tumor growth inhibition in xenograft models or pharmacokinetic-pharmacodynamic relationships, are not provided in the available literature.
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| Enzyme Assay |
Standard MARK4 inhibition assays involve incubating recombinant MARK4 enzyme (5-50 ng/uL) with the inhibitor (1-20 uM) in kinase assay buffer (50 mM HEPES, pH 7.5, 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100) containing ATP (10-100 uM) and a peptide substrate (e.g., tau-derived peptide). The reaction is incubated at 30degC for 30-60 minutes, and kinase activity is measured using ADP-Glo or radioactive 33P-ATP incorporation assays. IC50 values are determined by fitting dose-response curves.
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| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: Hela, U87MG, U251, MDA-MB-435, HGFs cells Tested Concentrations: 1-20 μM Incubation Duration: 24 h Experimental Results: demonstrated obvious cytotoxicity in Hela and U87MG cell lines. Standard cell viability assays involve seeding HeLa, U87MG, or other cancer cells in 96-well plates, treating with MARK4 inhibitor 4 at concentrations ranging from 0-20 uM for 24 hours, and measuring cell viability using MTT, CCK-8, or CellTiter-Glo assays. EC50 values (2.16 uM for HeLa, 3.51 uM for U87MG) are calculated by fitting dose-response curves. |
| Animal Protocol |
Not available. For in vivo studies of MARK4 inhibitors, standard protocols involve administering the compound (typically 10-50 mg/kg) intraperitoneally or orally daily for 2-4 weeks in tumor-bearing mouse models, monitoring tumor volume and body weight twice weekly, and assessing target engagement and pharmacodynamic markers in tumor tissues at study endpoint.
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| ADME/Pharmacokinetics |
Not available. As a small-molecule kinase inhibitor, pharmacokinetic properties such as oral bioavailability, plasma half-life, volume of distribution, and metabolic stability would require experimental determination. These data are not available for MARK4 inhibitor 4 in the published literature.
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| Toxicity/Toxicokinetics |
Not available. Kinase inhibitors often exhibit manageable toxicity profiles at therapeutic doses, but specific toxicological data, including maximum tolerated dose, target organ toxicity, or safety margins, are not reported for MARK4 inhibitor 4. Preclinical safety studies have not been described.
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| References | |
| Additional Infomation |
MARK4 inhibitor 4 is a research-grade compound used to study MARK4 biology, microtubule dynamics, and the role of MARK4 in cancer and neurodegenerative diseases such as Alzheimer's disease. It has not progressed to clinical trials nor received regulatory approval for any therapeutic indication. This product is for laboratory research only.
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| Molecular Formula |
C33H27CLN4O3
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|---|---|
| Molecular Weight |
563.05
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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 | 1.7760 mL | 8.8802 mL | 17.7604 mL | |
| 5 mM | 0.3552 mL | 1.7760 mL | 3.5521 mL | |
| 10 mM | 0.1776 mL | 0.8880 mL | 1.7760 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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