| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
MARK-IN-1 targets microtubule affinity-regulating kinases (MARK1, MARK2, MARK3, and MARK4). These kinases phosphorylate microtubule-associated proteins such as tau and MAP2, regulating microtubule stability and dynamics. Inhibition of MARK activity affects cell polarity, migration, and cytoskeletal organization.
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|---|---|
| ln Vitro |
MARK-IN-1 (compound 25) is a strong MARK inhibitor. One promising strategy to prevent neurofibrillary tangle pathology in Alzheimer's disease is to inhibit MARK [1].
In vitro, MARK-IN-1 inhibits MARK kinase activity, leading to reduced phosphorylation of microtubule-associated proteins. This affects microtubule dynamics and cellular processes such as cell polarity and migration. Detailed IC50 values against specific MARK isoforms are available in the primary literature describing the compound. |
| ln Vivo |
In vivo activity data for MARK-IN-1 are limited. As a MARK inhibitor, it may have effects on neuronal development and cancer cell migration in animal models. Specific in vivo efficacy data have not been extensively reported in the available literature.
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| Enzyme Assay |
In vitro enzyme assays for MARK-IN-1 are performed using purified recombinant MARK kinases. The compound is incubated with the kinase, ATP, and a peptide substrate in a kinase buffer. MARK activity is measured by detecting phosphorylated substrate using luminescence-based (e.g., ADP-Glo) or fluorescence-based methods. IC50 values are determined from dose-response curves generated with serial dilutions.
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| Cell Assay |
Cellular assays for MARK-IN-1 are conducted using cell lines such as neurons or cancer cells. Cells are treated with serial dilutions of the compound (0.1 nM to 10 uM) for 24-72 hours. MARK substrate phosphorylation (e.g., tau phosphorylation) is assessed by Western blot. Microtubule dynamics are evaluated by immunofluorescence staining. Cell migration is assessed by scratch or Transwell assays. Cell viability is measured by MTT assay.
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| Animal Protocol |
In vivo animal studies for MARK-IN-1 are not well-established in the literature. As a research compound, it could potentially be evaluated in mouse models of cancer or neurodegenerative diseases. Specific protocols and efficacy data have not been reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MARK-IN-1 have not been extensively characterized. The compound is a research-use small molecule typically stored as a powder at -20degC. Solubility and bioavailability data are available in the primary literature. No specific PK parameters have been reported.
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| Toxicity/Toxicokinetics |
Toxicological data for MARK-IN-1 are limited. As a research compound, standard safety assessments would include evaluation of cytotoxicity in cell-based assays and acute toxicity in animal models. No significant toxicity has been reported in the available literature. The compound is for research use only.
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| References | |
| Additional Infomation |
MARK-IN-1 is a research-use compound not approved for clinical therapeutic applications. It serves as a chemical probe for studying the role of MARK kinases in cell polarity, neuronal development, and cancer. The compound is valuable for investigating microtubule dynamics and the therapeutic potential of MARK inhibition.
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| Molecular Formula |
C22H23N7OF2S
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|---|---|
| Molecular Weight |
471.52612
|
| Exact Mass |
471.165
|
| CAS # |
1109283-93-3
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| PubChem CID |
25141108
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| Appearance |
Light yellow to yellow solid powder
|
| LogP |
4.502
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
33
|
| Complexity |
733
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC1=C(C=C(S1)C(=O)N[C@@H]2[C@@H](CCCC2(F)F)N)C3=C4N=CC(=CN4N=C3)C5=CN(N=C5)C
|
| InChi Key |
SFILVHFYISPBOI-IEBWSBKVSA-N
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| InChi Code |
InChI=1S/C22H23F2N7OS/c1-12-15(6-18(33-12)21(32)29-19-17(25)4-3-5-22(19,23)24)16-9-28-31-11-13(7-26-20(16)31)14-8-27-30(2)10-14/h6-11,17,19H,3-5,25H2,1-2H3,(H,29,32)/t17-,19-/m1/s1
|
| Chemical Name |
N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-methyl-4-[6-(1-methylpyrazol-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]thiophene-2-carboxamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO: ~100 mg/mL (~212.1 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1208 mL | 10.6038 mL | 21.2076 mL | |
| 5 mM | 0.4242 mL | 2.1208 mL | 4.2415 mL | |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1208 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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