| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Autocamtide-2-related inhibitory peptide, myristoylated targets calmodulin-dependent protein kinase II (CaMKII). It acts as a substrate-competitive inhibitor, binding to the kinase active site and preventing the phosphorylation of natural substrates. The myristoyl group facilitates membrane association and intracellular delivery, making it a potent tool for studying CaMKII function in cells.
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| ln Vitro |
In vitro, Autocamtide-2-related inhibitory peptide demonstrates potent inhibition of CaMKII with an IC50 of 40 nM. It is highly specific for CaMKII and does not significantly inhibit other protein kinases. The peptide acts as a competitive inhibitor with respect to the substrate autocamtide-2, effectively blocking CaMKII-mediated phosphorylation events in biochemical assays.
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| ln Vivo |
In vivo activity data for this myristoylated peptide are not extensively detailed in the available sources. However, the myristoylated form is designed to improve cell permeability and is used in cellular and potentially in vivo studies to inhibit CaMKII activity. It can be used to investigate the role of CaMKII in various physiological and pathological processes, including synaptic plasticity, cardiac function, and cancer.
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| Enzyme Assay |
The in vitro enzyme assay for this peptide typically involves measuring the inhibition of CaMKII activity using a radioactive or fluorescent phosphorylation assay. Recombinant CaMKII or immunoprecipitated kinase is incubated with a substrate peptide (e.g., autocamtide-2) in the presence of ATP and varying concentrations of the inhibitor. The IC50 is determined by quantifying the reduction in substrate phosphorylation.
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| Cell Assay |
Cellular assays involve treating cultured cells (e.g., neurons, cardiomyocytes) with the myristoylated peptide to allow intracellular delivery. After treatment, CaMKII activity is assessed by Western blotting using phospho-specific antibodies against CaMKII substrates or by measuring downstream signaling events. The myristoyl group enhances peptide uptake, enabling functional studies in intact cells.
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| Animal Protocol |
In vivo animal studies with myristoylated Autocamtide-2-related inhibitory peptide are not specifically described in the provided sources. The peptide is primarily used as a research tool to study CaMKII function in vitro and in cell-based assays. For in vivo applications, the peptide may be administered via injection, but specific animal models and dosing regimens are not detailed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Autocamtide-2-related inhibitory peptide, myristoylated are not available in the provided sources. As a peptide, it is likely to have poor oral bioavailability and a short half-life in circulation. The myristoyl group may improve membrane permeability but does not necessarily enhance systemic pharmacokinetics. The compound is typically used in research settings rather than as a therapeutic agent.
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| Toxicity/Toxicokinetics |
Toxicity information for this peptide is not reported in the available sources. As a tool compound used in research, it is not intended for therapeutic use and is generally considered to have low toxicity in in vitro assays at concentrations used for CaMKII inhibition. Specific toxicological data are not available.
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| References | |
| Additional Infomation |
Autocamtide-2-related inhibitory peptide, myristoylated is a widely used research tool for studying CaMKII-dependent signaling pathways. It is available as a reagent from various suppliers and is not an approved therapeutic drug. The peptide is used in neuroscience, cardiovascular research, and cancer biology to investigate the role of CaMKII in cellular processes.
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| Molecular Formula |
C78H142N22O20
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|---|---|
| Molecular Weight |
1708.0974984169
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| Exact Mass |
1707.077
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| CAS # |
201422-04-0
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| Related CAS # |
Autocamtide-2-related inhibitory peptide, myristoylated TFA
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| PubChem CID |
121513908
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| Appearance |
White to off-white solid powder
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| LogP |
-3.6
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| Hydrogen Bond Donor Count |
23
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| Hydrogen Bond Acceptor Count |
24
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| Rotatable Bond Count |
67
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| Heavy Atom Count |
120
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| Complexity |
3340
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| Defined Atom Stereocenter Count |
13
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| SMILES |
O=C([C@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([C@]([H])(C([H])([H])[H])N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O)N([H])[H])=O)=O)=O)N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])[H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])[H])C(N([H])[C@]([H])(C(=O)O[H])C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)=O)C([H])([H])C(=O)O[H])=O)C([H])(C([H])([H])[H])C([H])([H])[H])=O)=O)C([H])([H])C([H])([H])C(=O)O[H])=O)C([H])([H])C([H])([H])C(N([H])[H])=O)=O)C([H])([H])C([H])([H])C([H])([H])/N=C(\N([H])[H])/N([H])[H])=O)C([H])([H])C([H])([H])C([H])([H])/N=C(\N([H])[H])/N([H])[H]
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| InChi Key |
QKOOKZWMKXOQRL-YJDHHEDVSA-N
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| InChi Code |
InChI=1S/C78H142N22O20/c1-11-12-13-14-15-16-17-18-19-20-21-32-60(102)86-38-25-23-28-50(80)67(110)92-51(29-22-24-37-79)68(111)89-47(8)64(107)97-56(41-44(2)3)74(117)94-53(31-27-40-88-78(84)85)70(113)93-52(30-26-39-87-77(82)83)71(114)95-54(33-35-59(81)101)72(115)96-55(34-36-61(103)104)69(112)90-49(10)66(109)100-63(46(6)7)75(118)98-57(43-62(105)106)73(116)91-48(9)65(108)99-58(76(119)120)42-45(4)5/h44-58,63H,11-43,79-80H2,1-10H3,(H2,81,101)(H,86,102)(H,89,111)(H,90,112)(H,91,116)(H,92,110)(H,93,113)(H,94,117)(H,95,114)(H,96,115)(H,97,107)(H,98,118)(H,99,108)(H,100,109)(H,103,104)(H,105,106)(H,119,120)(H4,82,83,87)(H4,84,85,88)/t47-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-,58-,63-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-amino-6-(tetradecanoylamino)hexanoyl]amino]hexanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-oxopentanoyl]amino]-4-carboxybutanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-4-methylpentanoic 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 |
| 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 | 0.5854 mL | 2.9272 mL | 5.8545 mL | |
| 5 mM | 0.1171 mL | 0.5854 mL | 1.1709 mL | |
| 10 mM | 0.0585 mL | 0.2927 mL | 0.5854 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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