| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Ki: 86 μM (PKG)[1]
The primary target of this peptide is cGMP-dependent protein kinase (PKG). It is an ATP-competitive inhibitor, meaning it competes with ATP for binding to the kinase's active site. It has a Ki value of 86 µM for PKG. It does not inhibit the phosphorylation of intact histones by PKG. |
|---|---|
| ln Vitro |
According to the experimental summary, PKG inhibitor PKG inhibitor peptide (1 mM) intracellular dialysis of postsynaptic cells did not alter the production of long-term depression (CCh LTD) [2].
In vitro, the PKG inhibitor peptide competitively inhibits PKG with a Ki of 86 µM. It competes with synthetic substrates but does not inhibit the phosphorylation of intact histones. It is used as a specific tool to study PKG-mediated signaling pathways. |
| ln Vivo |
In vivo, the PKG inhibitor peptide is used as a research tool to study the role of PKG in various physiological processes, such as smooth muscle relaxation, platelet function, and neuronal signaling. It can be introduced into cells using microinjection or peptide delivery systems.
|
| Enzyme Assay |
Non-cellular assays for the PKG inhibitor peptide involve measuring its inhibitory activity against purified PKG enzyme. The peptide is incubated with the enzyme, ATP, and a synthetic substrate, and the kinase activity is measured using radiometric or fluorescence-based methods. Ki values are determined from kinetic studies.
|
| Cell Assay |
Cellular assays for the PKG inhibitor peptide are conducted using cell lines or primary cells. The peptide is introduced into cells, and its effects on PKG-mediated phosphorylation of downstream targets are assessed by Western blotting. Functional assays, such as measuring smooth muscle relaxation, may also be used.
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| Animal Protocol |
In vivo animal experiments for the PKG inhibitor peptide are limited, as peptides typically have poor bioavailability. However, it may be used in ex vivo experiments or in studies where it can be directly applied to tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of the PKG inhibitor peptide are not well-characterized. As a peptide, it has poor oral bioavailability and is rapidly degraded by proteases. It is typically used in in vitro or ex vivo studies. It should be stored at -20°C.
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| Toxicity/Toxicokinetics |
Toxicological data for the PKG inhibitor peptide are limited, as it is a research reagent. Standard laboratory safety precautions should be followed when handling the compound. It is for research use only.
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| References |
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| Additional Infomation |
The PKG inhibitor peptide is a specific and valuable research tool for studying the cGMP/PKG signaling pathway. It is used to elucidate the role of PKG in various cellular processes, including vasodilation, platelet inhibition, and neuronal function. It is also known as PKG inhibitor peptide TFA.
|
| Molecular Formula |
C38H74N18O10
|
|---|---|
| Molecular Weight |
943.11
|
| Exact Mass |
942.583
|
| CAS # |
82801-73-8
|
| Related CAS # |
PKG inhibitor peptide TFA
|
| PubChem CID |
134097
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Index of Refraction |
1.658
|
| LogP |
-5.78
|
| Hydrogen Bond Donor Count |
17
|
| Hydrogen Bond Acceptor Count |
16
|
| Rotatable Bond Count |
36
|
| Heavy Atom Count |
66
|
| Complexity |
1650
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)N
|
| InChi Key |
OUKSKNTVYYVIMZ-DUJSLOSMSA-N
|
| InChi Code |
InChI=1S/C38H74N18O10/c1-21(29(59)52-26(13-8-20-50-38(46)47)33(63)54-24(11-3-5-17-40)34(64)56-27(35(65)66)14-15-28(57)58)51-31(61)25(12-7-19-49-37(44)45)55-32(62)23(10-2-4-16-39)53-30(60)22(41)9-6-18-48-36(42)43/h21-27H,2-20,39-41H2,1H3,(H,51,61)(H,52,59)(H,53,60)(H,54,63)(H,55,62)(H,56,64)(H,57,58)(H,65,66)(H4,42,43,48)(H4,44,45,49)(H4,46,47,50)/t21-,22-,23-,24-,25-,26-,27-/m0/s1
|
| Chemical Name |
(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]pentanedioic acid
|
| 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)
|
| Solubility (In Vitro) |
H2O: 100 mg/mL (106.03 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (106.03 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0603 mL | 5.3016 mL | 10.6032 mL | |
| 5 mM | 0.2121 mL | 1.0603 mL | 2.1206 mL | |
| 10 mM | 0.1060 mL | 0.5302 mL | 1.0603 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.
Products are for research use only; We do not sell to patients
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