| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PKMζ[1]
ZIP targets protein kinase Mζ (PKMζ), a constitutively active atypical PKC isozyme that plays a critical role in the maintenance of long-term potentiation (LTP) and memory. By inhibiting PKMζ, ZIP disrupts synaptic plasticity and memory maintenance. The peptide is derived from the pseudosubstrate region of PKCζ and acts as a competitive inhibitor. |
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| ln Vitro |
ZIP demonstrates potent in vitro inhibition of PKMζ activity. As a cell-permeable peptide, it can enter cells and specifically inhibit PKMζ, blocking its kinase activity. The compound's activity is typically assessed in kinase assays using purified PKMζ or in cell-based assays measuring PKMζ-mediated phosphorylation of substrates.
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| ln Vivo |
In vivo activity of ZIP has been demonstrated in animal models, where injections of ZIP can block the impairment in morphine conditioned place preference. ZIP is widely used in neuroscience research to study the role of PKMζ in synaptic plasticity, memory maintenance, cell polarity, and signal transduction.
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| Enzyme Assay |
In vitro enzyme assays for ZIP involve measuring its inhibition of PKMζ kinase activity. The assay typically uses purified PKMζ enzyme and a peptide substrate, with kinase activity measured by detecting phosphorylation using radioactive ATP or fluorescence-based methods. IC50 values can be determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for ZIP involve treating neuronal cell lines or primary neurons with the peptide and measuring PKMζ activity, synaptic protein phosphorylation, or electrophysiological responses. The peptide's cell permeability allows for direct application to cultured cells.
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| Animal Protocol |
In vivo animal experiments for ZIP involve administering the peptide to animal models (e.g., via intracranial injection) and evaluating effects on memory, learning, and synaptic plasticity. Behavioral tests such as conditioned place preference or Morris water maze are used to assess the functional consequences of PKMζ inhibition.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for ZIP are limited. The peptide has a molecular weight of 1928.38 Da and a molecular formula of C90H154N30O17. Purity is >95%. The peptide is soluble in water at up to 1 mg/mL. It should be stored desiccated at -20°C. Its ADME properties have not been characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for ZIP are limited. As a research peptide, comprehensive toxicological studies have not been reported. The compound is intended for research use only and is not for human therapeutic application. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
ZIP (CAS#: 863987-12-6) has the molecular formula C90H154N30O17 and a molecular weight of 1928.38 Da. Its sequence is Myr-Ser-Ile-Tyr-Arg-Arg-Gly-Ala-Arg-Arg-Trp-Arg-Lys-Leu-OH. ZIP is a cell-permeable inhibitor of PKMζ used in neuroscience research to study synaptic plasticity and memory. Purity is >95%.
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| Molecular Formula |
C90H154N30O17
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|---|---|
| Molecular Weight |
1928.38
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| Exact Mass |
403.022
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| CAS # |
863987-12-6
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| Related CAS # |
ZIP TFA
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| PubChem CID |
16156119
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| Appearance |
White to off-white solid powder
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| LogP |
2.735
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| Hydrogen Bond Donor Count |
33
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| Hydrogen Bond Acceptor Count |
23
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| Rotatable Bond Count |
76
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| Heavy Atom Count |
137
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| Complexity |
3810
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| Defined Atom Stereocenter Count |
13
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| SMILES |
CCCCCCCCCCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC2=CNC3=CC=CC=C32)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O
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| InChi Key |
CRKARHQCXWSUMV-HOHDCHNJSA-N
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| InChi Code |
InChI=1S/C90H154N30O17/c1-7-9-10-11-12-13-14-15-16-17-18-36-71(123)110-70(52-121)83(134)120-73(54(5)8-2)84(135)118-67(48-56-37-39-58(122)40-38-56)81(132)115-64(33-25-44-104-88(96)97)77(128)112-61(31-23-42-102-86(92)93)75(126)108-51-72(124)109-55(6)74(125)111-63(32-24-43-103-87(94)95)76(127)114-66(35-27-46-106-90(100)101)79(130)117-68(49-57-50-107-60-29-20-19-28-59(57)60)82(133)116-65(34-26-45-105-89(98)99)78(129)113-62(30-21-22-41-91)80(131)119-69(85(136)137)47-53(3)4/h19-20,28-29,37-40,50,53-55,61-70,73,107,121-122H,7-18,21-27,30-36,41-49,51-52,91H2,1-6H3,(H,108,126)(H,109,124)(H,110,123)(H,111,125)(H,112,128)(H,113,129)(H,114,127)(H,115,132)(H,116,133)(H,117,130)(H,118,135)(H,119,131)(H,120,134)(H,136,137)(H4,92,93,102)(H4,94,95,103)(H4,96,97,104)(H4,98,99,105)(H4,100,101,106)/t54-,55-,61-,62-,63-,64-,65-,66-,67-,68-,69-,70-,73-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[2-[[(2S)-5-carbamimidamido-2-[[(2S)-5-carbamimidamido-2-[[(2S)-3-(4-hydroxyphenyl)-2-[[(2S,3S)-2-[[(2S)-3-hydroxy-2-(tetradecanoylamino)propanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]pentanoyl]amino]pentanoyl]amino]acetyl]amino]propanoyl]amino]pentanoyl]amino]pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]pentanoyl]amino]hexanoyl]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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : 25 mg/mL (12.96 mM)
H2O : 6.25 mg/mL (3.24 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5186 mL | 2.5928 mL | 5.1857 mL | |
| 5 mM | 0.1037 mL | 0.5186 mL | 1.0371 mL | |
| 10 mM | 0.0519 mL | 0.2593 mL | 0.5186 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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