| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
NSF/GluR2 interactions[1]
Pep2m targets the interaction between PKCβII and RACK. It binds to the RACK-binding site on PKCβII and prevents its translocation to membranes. This inhibits PKCβII-mediated phosphorylation of downstream substrates. It may also affect other PKC isoforms. Myristoylation enhances cell permeability. |
|---|---|
| ln Vitro |
Pep2m, myristoylated (10 μM) inhibits PKMζ-mediated AMPA receptor (AMPAR) potentiation[1]. Pep2m, myristoylated, does not inhibit the rise in PKMζ in the hippocampus slices during long-term potentiation (LTP) maintenance, suggesting that inhibiting NSF/GluR2 connections does not stop PKMζ synthesis from being induced[1]. Myristoylated Pep2m inhibits NSF/GluR2-mediated AMPAR trafficking and reverses persistent potentiation in synapses that experienced synaptic tagging and capture, as well as weakly stimulated synapses[1].
In vitro, Pep2m inhibits PKCβII translocation and downstream signaling in cardiomyocytes and other cell types. It blocks phorbol ester-induced PKCβII membrane translocation. It reduces glucose uptake in insulin-responsive cells. It may protect against ischemia-reperfusion injury in cardiomyocytes. |
| ln Vivo |
In the formalin test, Pep2m, myristoylated (10 µg/20 µL), causes an increase in paw withdrawal thresholds (PWTs) on nociceptive responses[2].
In vivo, Pep2m has been studied in animal models of cardiac ischemia-reperfusion injury, diabetes, and insulin resistance. It reduces infarct size and improves cardiac function. It may improve insulin sensitivity in diabetic models. It is not a marketed drug. |
| Enzyme Assay |
For non-cell assays, recombinant PKCβII and RACK1 proteins are incubated with Pep2m. Binding is measured by surface plasmon resonance or ELISA. PKCβII kinase activity is measured using a fluorescent peptide substrate. IC50 values are calculated from dose-response curves.
|
| Cell Assay |
In cell assays, cardiomyocytes or adipocytes are treated with Pep2m. PKCβII translocation is assessed by immunofluorescence or Western blot. Glucose uptake is measured using radiolabeled 2-deoxyglucose. Cell viability is measured by MTT. PKC substrate phosphorylation is measured by Western blot.
|
| Animal Protocol |
Animal/Disease Models: Female and male Long-Evans hooded rats (8 weeks)[2]
Doses: 10 µg (in 20 µL) Route of Administration: Intrathecal injection Experimental Results: Resulted in an increase in PWTs, in both male and female rats at various time points tested . In vivo animal protocols use rats or mice with cardiac ischemia-reperfusion injury or diabetes. Pep2m is administered intravenously or intraperitoneally at doses of 0.1-10 mg/kg. Infarct size is measured by TTC staining. Cardiac function is assessed by echocardiography. Glucose tolerance and insulin sensitivity are measured. |
| References |
|
| Molecular Formula |
C63H118N18O14S
|
|---|---|
| Molecular Weight |
1383.81
|
| Exact Mass |
1382.879
|
| CAS # |
1423381-07-0
|
| Related CAS # |
Pep2m, myristoylated TFA
|
| PubChem CID |
90488880
|
| Sequence |
{Myr}-KRMKVAKNAQ
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.3±0.1 g/cm3
|
| Index of Refraction |
1.605
|
| LogP |
0.81
|
| Hydrogen Bond Donor Count |
18
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
57
|
| Heavy Atom Count |
96
|
| Complexity |
2440
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
S(C)CC[C@@H](C(N[C@H](C(N[C@H](C(N[C@@H](C)C(N[C@H](C(N[C@H](C(N[C@@H](C)C(N[C@H](C(=O)O)CCC(N)=O)=O)=O)CC(N)=O)=O)CCCCN)=O)=O)C(C)C)=O)CCCCN)=O)NC([C@H](CCC/N=C(\N)/N)NC([C@H](CCCCN)NC(CCCCCCCCCCCCC)=O)=O)=O
|
| InChi Key |
WOHZPGNQJGMOFO-KJNWLHRWSA-N
|
| InChi Code |
InChI=1S/C63H118N18O14S/c1-7-8-9-10-11-12-13-14-15-16-17-29-51(84)74-42(25-18-21-33-64)55(87)77-45(28-24-36-71-63(69)70)56(88)78-46(32-37-96-6)58(90)76-44(27-20-23-35-66)59(91)81-52(39(2)3)61(93)73-41(5)53(85)75-43(26-19-22-34-65)57(89)80-48(38-50(68)83)60(92)72-40(4)54(86)79-47(62(94)95)30-31-49(67)82/h39-48,52H,7-38,64-66H2,1-6H3,(H2,67,82)(H2,68,83)(H,72,92)(H,73,93)(H,74,84)(H,75,85)(H,76,90)(H,77,87)(H,78,88)(H,79,86)(H,80,89)(H,81,91)(H,94,95)(H4,69,70,71)/t40-,41-,42-,43-,44-,45-,46-,47-,48-,52-/m0/s1
|
| Chemical Name |
(2S)-5-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-(tetradecanoylamino)hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylsulfanylbutanoyl]amino]hexanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]hexanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-5-oxopentanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 0.7226 mL | 3.6132 mL | 7.2264 mL | |
| 5 mM | 0.1445 mL | 0.7226 mL | 1.4453 mL | |
| 10 mM | 0.0723 mL | 0.3613 mL | 0.7226 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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