| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
This peptide targets cGMP-dependent protein kinase (PKG) as a selective substrate. PKG is a serine/threonine kinase that plays a key role in the nitric oxide/cGMP signaling pathway, regulating vascular smooth muscle relaxation, platelet function, and neuronal signaling. The peptide is phosphorylated by PKG at the serine residue within the recognition sequence.
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|---|---|
| ln Vitro |
The incorporation of [33P]ATP into the synthetic peptide PKG substrate RKRSRAE is measured. PKG Iα gatekeeper mutants' kinase activity is inhibited by N6-benzyl-ATP, but WT is not affected. After being released from neuronal exocytosis, serotonin is reabsorbed by the serotonin transporter (SERT). Several mechanisms, including as the cyclic GMP signaling cascade involving PKG, guanylyl cyclase, and nitric oxide synthase, control SERT [1].
In vitro, this peptide serves as a selective substrate for PKG. It is phosphorylated by PKG in the presence of ATP and cGMP. The peptide is used to measure PKG activity in kinase assays and to study the regulation of the cGMP signaling pathway. |
| ln Vivo |
In vivo, this peptide is used as a tool to study PKG activity and cGMP signaling in tissues. It may be introduced into cells or tissues to assess PKG function or to compete with endogenous substrates. However, the primary use of this peptide is in in vitro biochemical assays.
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| Enzyme Assay |
Kinase assays for this peptide typically involve incubating the peptide with purified PKG, ATP, and cGMP. Phosphorylation of the peptide is detected using radiolabeled ATP (32P or 33P) or by using phospho-specific antibodies. The extent of phosphorylation is quantified by scintillation counting or ELISA.
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| Cell Assay |
Cellular assays for this peptide may involve introducing the peptide into cells using cell-permeable delivery methods or using lysates from cells treated with cGMP-elevating agents. PKG activity is measured by assessing phosphorylation of the peptide substrate.
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| Animal Protocol |
In vivo studies with this peptide are limited, as it is primarily used as an in vitro substrate. When used in vivo, it is typically delivered via microinjection or using cell-penetrating peptide technology. Tissues are harvested and PKG activity is assessed ex vivo.
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| ADME/Pharmacokinetics |
As a peptide, this compound is expected to have a short half-life due to proteolytic degradation. The peptide should be stored as a lyophilized powder at -20degC. Standard peptide handling and storage procedures apply.
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| Toxicity/Toxicokinetics |
Toxicity data for this peptide are limited. Peptide research compounds are generally well-tolerated at the concentrations used in biochemical assays. Standard safety precautions for laboratory handling should be followed.
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| References | |
| Additional Infomation |
This peptide is a research-use compound and is not approved for therapeutic applications. It is also known as PKG Substrate [RKRSRAE]. The peptide is used as a substrate for measuring PKG activity in kinase assays and to study cGMP-dependent signaling pathways. It is available from multiple research suppliers.
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| Molecular Formula |
C35H67N17O11
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|---|---|
| Molecular Weight |
902.013780000001
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| Exact Mass |
901.521
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| CAS # |
81187-14-6
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| PubChem CID |
57358765
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| Appearance |
White to off-white solid powder
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| LogP |
0.421
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| Hydrogen Bond Donor Count |
17
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
33
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| Heavy Atom Count |
63
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| Complexity |
1600
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)N
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| InChi Key |
BVKSYBQAXBWINI-LQDRYOBXSA-N
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| InChi Code |
InChI=1S/C35H67N17O11/c1-18(26(56)51-23(32(62)63)11-12-25(54)55)47-28(58)21(9-5-15-45-34(40)41)50-31(61)24(17-53)52-30(60)22(10-6-16-46-35(42)43)49-29(59)20(8-2-3-13-36)48-27(57)19(37)7-4-14-44-33(38)39/h18-24,53H,2-17,36-37H2,1H3,(H,47,58)(H,48,57)(H,49,59)(H,50,61)(H,51,56)(H,52,60)(H,54,55)(H,62,63)(H4,38,39,44)(H4,40,41,45)(H4,42,43,46)/t18-,19-,20-,21-,22-,23-,24-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxypropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]propanoyl]amino]pentanedioic 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 (~110.86 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (110.86 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 | 1.1086 mL | 5.5432 mL | 11.0864 mL | |
| 5 mM | 0.2217 mL | 1.1086 mL | 2.2173 mL | |
| 10 mM | 0.1109 mL | 0.5543 mL | 1.1086 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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