2. Stem Cell/Wnt
  3. PKG
  4. PKG Substrate

PKG Substrate is a selective substrate for cGMP-dependent protein kinase (PKG).

For research use only. We do not sell to patients.

Custom Peptide Synthesis

PKG Substrate Chemical Structure

PKG Substrate Chemical Structure

CAS No. : 81187-14-6

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5 mg USD 390 In-stock
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Based on 1 publication(s) in Google Scholar

PKG Substrate Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PKG Substrate is a selective substrate for cGMP-dependent protein kinase (PKG).

IC50 & Target

PKG[1]
In Vitro

Incorporation of [33P]ATP into the synthetic peptide PKG substrate RKRSRAE is measured. N6-benzyl-ATP inhibits kinase activity of PKG Iα gatekeeper mutants but not WT. The serotonin transporter (SERT) is responsible for reuptake of serotonin (5-hydroxytryptamine) after its exocytotic release from neurons. SERT is regulated by several processes, including a cyclic GMP signaling pathway involving nitric oxide synthase, guanylyl cyclase, and PKG[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PKG Substrate Related Antibodies
Molecular Weight

902.01

Formula

C35H67N17O11
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Arg-Lys-Arg-Ser-Arg-Ala-Glu
Sequence Shortening

RKRSRAE
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (110.86 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (110.86 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References
Kinase Assay
[1]

Kinase activity is measured by determining the amount of 33P radioactivity incorporated from [33P]ATP or [33P]N6-benzyl-ATP into a PKG specific peptide substrate (RKRSRAE). The standard 75 μL assay mixture contains 0.15 μCi of [33P]ATP, 10 μM ATP, 15 μM PKG peptide substrate, 2 μM PKI (a synthetic peptide inhibitor of cAMP-dependent protein kinase), 1 μg of purified kinase, and 100 μM 8-Br-cGMP in 50 mM HEPES buffer, pH 7.4, containing 10 mM MgCl2, 0.1% Tween 20, and 1 mM DTT. After incubation at 30°C for 2 min, the reaction is immediately put on ice, and 20 μL of the assay mixture is spotted onto P81 phosphocellulose paper and then quenched in 0.42% H3PO4. The paper is further washed three times in 0.42% H3PO4 for 10 min with gentle agitation and rinsed once with acetone. After air drying, radioactivity on the paper is measured with a Beckman LS6500 liquid scintillation counter. For measuring the effect of N6-benzyl-ATP on the activity of PKG I utilizing ATP as a co-substrate, unlabeled N6-benzyl-ATP is added to each reaction at the indicated concentrations. Saturation kinetic analyses for Km and Vmax with ATP or N6-benzyl-ATP are performed over a concentration range (0.0015-100 μM) by adding unlabeled ATP or N6-benzyl-ATP to a given amount of [33P]ATP or [33P]N6-benzyl-ATP, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.1086 mL 5.5432 mL 11.0864 mL 27.7159 mL
5 mM 0.2217 mL 1.1086 mL 2.2173 mL 5.5432 mL
10 mM 0.1109 mL 0.5543 mL 1.1086 mL 2.7716 mL
15 mM 0.0739 mL 0.3695 mL 0.7391 mL 1.8477 mL
20 mM 0.0554 mL 0.2772 mL 0.5543 mL 1.3858 mL
25 mM 0.0443 mL 0.2217 mL 0.4435 mL 1.1086 mL
30 mM 0.0370 mL 0.1848 mL 0.3695 mL 0.9239 mL
40 mM 0.0277 mL 0.1386 mL 0.2772 mL 0.6929 mL
50 mM 0.0222 mL 0.1109 mL 0.2217 mL 0.5543 mL
60 mM 0.0185 mL 0.0924 mL 0.1848 mL 0.4619 mL
80 mM 0.0139 mL 0.0693 mL 0.1386 mL 0.3464 mL
100 mM 0.0111 mL 0.0554 mL 0.1109 mL 0.2772 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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PKG Substrate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PKG Substrate81187-14-6PKGInhibitorinhibitorinhibit

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