| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
MARK Substrate targets Microtubule Affinity-Regulating Kinases (MARKs), a family of serine/threonine kinases including MARK1, MARK2, MARK3, and MARK4. These kinases are involved in the regulation of microtubule dynamics by phosphorylating microtubule-associated proteins (MAPs). The peptide serves as a substrate for MARK kinases, particularly MARK2. Through its phosphorylation by MARKs, the peptide can be used to measure kinase activity and to screen for MARK inhibitors. Dysregulation of MARKs is implicated in neurodegenerative disorders and cancer.
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| ln Vitro |
In vitro studies have validated MARK Substrate as a robust substrate for determining the inhibitory potency of compounds against MARK2. The peptide is phosphorylated by MARK kinases, and the extent of phosphorylation is used to measure kinase activity. The peptide's sequence (NVKSKIGSTENLK) contains the consensus phosphorylation site for MARK kinases. MARK Substrate is widely used in kinase activity assays and inhibitor screening studies. Its utility as a research tool has been confirmed in multiple applications studying MARK family kinases and their roles in microtubule dynamics and disease.
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| ln Vivo |
In vivo studies of MARK Substrate are not applicable, as it is a peptide substrate used for in vitro kinase assays rather than a therapeutic compound. The peptide is designed for biochemical research applications to study MARK kinase activity and to screen for MARK inhibitors. Its role in vivo would be limited to its use as a research tool in ex vivo assays using tissue lysates or cell extracts. The compound is not intended for therapeutic use and is not administered to animals for pharmacological studies.
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| Enzyme Assay |
The in vitro kinase assay for MARK Substrate involves incubating the peptide with purified MARK kinase (MARK1, MARK2, MARK3, or MARK4) in the presence of ATP and a radioactive or non-radioactive phosphate donor. The reaction is carried out in a suitable buffer at physiological pH and temperature. Phosphorylation of the substrate is measured using methods such as scintillation counting for radiolabeled assays, or using phospho-specific antibodies or mass spectrometry for non-radioactive assays. Kinetic parameters including Km and Vmax are determined from initial velocity measurements at various substrate concentrations. Inhibition studies can be performed by adding MARK inhibitors to the reaction.
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| Cell Assay |
In vitro cellular assays for MARK Substrate are limited, as the peptide is primarily used as a biochemical substrate rather than a cellular probe. For studies involving MARK kinases in cells, cell lysates expressing MARKs are incubated with the peptide substrate to measure kinase activity. Cells are treated with modulators of MARK activity, lysed, and the lysates are used in kinase assays with MARK Substrate. The extent of substrate phosphorylation reflects cellular MARK activity. Alternatively, the peptide can be used in immunoprecipitation kinase assays where MARKs are immunoprecipitated from cell lysates and assayed with the substrate.
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| Animal Protocol |
In vivo animal studies for MARK Substrate are not applicable as it is an in vitro research tool. The peptide is not administered to animals for pharmacological studies. Its use is limited to biochemical and cell-based assays to study MARK kinase activity. For research applications, the peptide is used in ex vivo assays with tissue samples or in vitro with purified kinases or cell lysates. Standard protocols for MARK kinase activity measurement employ MARK Substrate as a reliable and validated substrate for determining kinase activity and inhibitor potency.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for MARK Substrate are not applicable, as it is a peptide substrate used for in vitro research rather than a therapeutic compound. The peptide has a molecular weight of 1417.61 g/mol and a molecular formula of C60H108N18O21. For in vitro use, the peptide is typically dissolved in aqueous buffers. Solubility: in vitro, it is soluble in H2O at 100 mg/mL (70.54 mM). It is not intended for in vivo administration, so pharmacokinetic parameters are not relevant. The peptide should be stored under appropriate conditions to maintain stability.
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| Toxicity/Toxicokinetics |
Toxicology data for MARK Substrate are not applicable, as it is a peptide substrate used for in vitro research rather than a therapeutic compound. The peptide is not administered to animals or humans, so toxicological assessments are not relevant. For laboratory use, standard safety precautions for handling peptides should be followed. The compound is intended for research use only and is not for human or therapeutic applications. No specific toxicity data are available.
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| Additional Infomation |
MARK Substrate is a synthetic peptide substrate for Microtubule Affinity-Regulating Kinases (MARKs) with the sequence Asn-Val-Lys-Ser-Lys-Ile-Gly-Ser-Thr-Glu-Asn-Leu-Lys (NVKSKIGSTENLK). It has a molecular formula of C60H108N18O21 and a molecular weight of 1417.61 g/mol. The peptide is used as a robust substrate for determining the inhibitory potency of compounds against MARK2 and other MARK family members (MARK1-4). MARKs are serine/threonine kinases involved in microtubule dynamics regulation. The peptide is a research tool for kinase activity assays and inhibitor screening.
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| Exact Mass |
1416.793
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|---|---|
| CAS # |
847991-34-8
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| PubChem CID |
170907780
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
-12.1
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| Hydrogen Bond Donor Count |
23
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| Hydrogen Bond Acceptor Count |
25
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| Rotatable Bond Count |
52
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| Heavy Atom Count |
99
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| Complexity |
2710
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| Defined Atom Stereocenter Count |
14
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| SMILES |
CC[C@H](C)[C@@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(=O)N)N
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| InChi Key |
FRMPKKOKFUPGCO-UCASNNTISA-N
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| InChi Code |
InChI=1S/C60H108N18O21/c1-8-31(6)47(77-52(90)35(16-10-13-21-62)69-55(93)41(28-80)75-50(88)34(15-9-12-20-61)70-58(96)46(30(4)5)76-49(87)33(64)24-42(65)82)57(95)67-26-44(84)68-40(27-79)56(94)78-48(32(7)81)59(97)71-36(18-19-45(85)86)51(89)74-39(25-43(66)83)54(92)73-38(23-29(2)3)53(91)72-37(60(98)99)17-11-14-22-63/h29-41,46-48,79-81H,8-28,61-64H2,1-7H3,(H2,65,82)(H2,66,83)(H,67,95)(H,68,84)(H,69,93)(H,70,96)(H,71,97)(H,72,91)(H,73,92)(H,74,89)(H,75,88)(H,76,87)(H,77,90)(H,78,94)(H,85,86)(H,98,99)/t31-,32+,33-,34-,35-,36-,37-,38-,39-,40-,41-,46-,47-,48-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[2-[[(2S,3S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2,4-diamino-4-oxobutanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-4-carboxybutanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]hexanoic acid
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O : ~100 mg/mL (~70.54 mM)
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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.) |
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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