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| Targets |
IC50: 0.82 μM (MARK4)[1] Km:6.3×10 7[1]
MARK4 inhibitor 2 targets the ATP-binding pocket of microtubule affinity-regulating kinase 4 (MARK4). It is a selective MARK4 antagonist with an IC50 of 0.82 microM and a Km value of 6.3×10⁷, indicating high affinity for the enzyme and potent inhibition of MARK4-mediated phosphorylation of microtubule-associated proteins. |
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| ln Vitro |
In HeLa, U87MG, MDA-MB-435, U251, and HGFs cells, MARK4 inhibitor 2 (Compound 23a) (0-20 μM; 24 hours) suppresses cell proliferation with EC50 values ranging from 1.76 μM to 7.98 μM [1].
MARK4 inhibitor 2 (Compound 23a) inhibits the growth of multiple human cancer cell lines, including HeLa, U87MG, MDA-MB-435, and U251 cells. Treatment at concentrations of 0-20 microM for 24 hours suppresses cell proliferation with EC50 values ranging from 1.76 microM to 7.98 microM across different cell lines. |
| ln Vivo |
Not available. MARK4 inhibitor 2 inhibits the growth of human cells and can be used for cancer research; however, specific in vivo efficacy data, including tumor growth inhibition in animal xenograft models or survival studies, are not provided in the available literature. Pharmacodynamic markers have not been reported.
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| Enzyme Assay |
Standard MARK4 inhibition assays involve incubating recombinant MARK4 enzyme (5-20 ng/uL) with varying concentrations of inhibitor (0.1-20 uM) in kinase buffer (50 mM HEPES, pH 7.4, 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100) containing 10-100 uM ATP and a substrate peptide (e.g., biotinylated tau peptide). After 30-60 minutes at 30degC, kinase activity is quantified using a luminescent ADP detection kit or radioactive 33P-ATP incorporation, and IC50 values (0.82 uM) are determined.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HeLa, U87MG, MDA-MB-435, U251, HGFs cells Tested Concentrations: 0-20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited the growth of human cells with EC50 s of 2.13, 4.13, 1.76, 7.98, 3.55 μM for HeLa, U87MG, MDA-MB-435, U251, HGFs cells, respectively. diminished the proliferation of human cancer cells in the low micromolar range; also affects the non-cancerous HGF cells. Standard cell viability assays involve seeding HeLa, U87MG, MDA-MB-435, or U251 cells (5×103 per well) in 96-well plates, treating with MARK4 inhibitor 2 at 0-20 uM for 24 hours, then assessing viability using MTT, CCK-8, or CellTiter-Glo assays. EC50 values (1.76-7.98 uM) are calculated from dose-response curves fitted with four-parameter logistic regression. |
| Animal Protocol |
Not available. For in vivo evaluation of MARK4 inhibitors, standard protocols involve administering the compound (typically 10-100 mg/kg) by intraperitoneal or oral gavage once daily in mice bearing subcutaneous tumor xenografts, monitoring tumor volume and body weight every 2-3 days for 2-4 weeks, with plasma and tissue collection at endpoint for PK/PD analysis.
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| ADME/Pharmacokinetics |
Not available. As a small-molecule kinase inhibitor, pharmacokinetic properties such as bioavailability, clearance, half-life, and tissue distribution have not been reported for MARK4 inhibitor 2. Preclinical ADME (absorption, distribution, metabolism, excretion) studies are not available.
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| Toxicity/Toxicokinetics |
Not available. Specific toxicological data, including acute toxicity, subchronic toxicity, genotoxicity, or target organ effects, are not reported for MARK4 inhibitor 2. Inhibitors targeting ubiquitously expressed kinases carry risk of off-target effects, but safety data are not provided.
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| References | |
| Additional Infomation |
MARK4 inhibitor 2 is a research-grade compound used to study MARK4-dependent signaling pathways, cell cycle regulation, and the therapeutic potential of MARK4 inhibition in cancer and Alzheimer's disease. It has not entered clinical trials nor received regulatory approval. This product is for laboratory research only.
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| Molecular Formula |
C34H30N4O3
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| Molecular Weight |
542.63
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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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8429 mL | 9.2144 mL | 18.4288 mL | |
| 5 mM | 0.3686 mL | 1.8429 mL | 3.6858 mL | |
| 10 mM | 0.1843 mL | 0.9214 mL | 1.8429 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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