2. Stem Cell/Wnt TGF-beta/Smad
  3. PKA
  4. PKA Inhibitor Fragment (6-22) amide

PKA Inhibitor Fragment (6-22) amide  (Synonyms: PKI-(6-22)-amide)

Cat. No.: HY-P1290 Purity: 98.00%
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PKA Inhibitor Fragment (6-22) amide is a highly potent and specific competitive inhibitor of PKA, with Ki values of 1.7 nM and 1.6 nM against human and bovine PKA catalytic subunits, respectively. The IC50 of PKA Inhibitor Fragment (6-22) amide targeting bovine PKA is 8.6 nM. PKA Inhibitor Fragment (6-22) amide effectively abolishes PKA activity in mouse brain and spinal cord, and exerts in vivo efficacy via intracerebroventricular administration. PKA Inhibitor Fragment (6-22) amide significantly reverses low-dose morphine analgesic tolerance in mice and blocks photoaffinity labeling of cAMP-dependent protein kinase. PKA Inhibitor Fragment (6-22) amide can be applied to research in fields related to the mechanism of morphine analgesic tolerance and skin wound healing.

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

Custom Peptide Synthesis

PKA Inhibitor Fragment (6-22) amide

PKA Inhibitor Fragment (6-22) amide Chemical Structure

CAS No. : 121932-06-7

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Based on 5 publication(s) in Google Scholar

Other Forms of PKA Inhibitor Fragment (6-22) amide:

PKA Inhibitor Fragment (6-22) amide Related Antibodies

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PKA PKAR PKACα

  • Biological Activity

  • Purity & Documentation

  • References

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Description

PKA Inhibitor Fragment (6-22) amide is a highly potent and specific competitive inhibitor of PKA, with Ki values of 1.7 nM and 1.6 nM against human and bovine PKA catalytic subunits, respectively. The IC50 of PKA Inhibitor Fragment (6-22) amide targeting bovine PKA is 8.6 nM. PKA Inhibitor Fragment (6-22) amide effectively abolishes PKA activity in mouse brain and spinal cord, and exerts in vivo efficacy via intracerebroventricular administration. PKA Inhibitor Fragment (6-22) amide significantly reverses low-dose morphine analgesic tolerance in mice and blocks photoaffinity labeling of cAMP-dependent protein kinase. PKA Inhibitor Fragment (6-22) amide can be applied to research in fields related to the mechanism of morphine analgesic tolerance and skin wound healing[1][2][3].

IC50 & Target

PKA

2.8 nM (Ki)

In Vitro

PKA Inhibitor Fragment (6-22) amide (10 μM; 20 min) potently inhibits nearly all basal and total cytosolic and particulate PKA activity in vitro in thalamus, PAG, medulla, and LSC fractions from drug-naïve mouse brain and spinal cord[1].
PKA Inhibitor Fragment (6-22) amide (500 μM; 10 min pre-incubation, 3 min UV irradiation) specifically binds to the active site of the bovine heart type II cAMP-dependent protein kinase catalytic subunit[2].
PKA Inhibitor Fragment (6-22) amide (10 µM; 1 h pre-incubation, 24 h co-incubation with uvaol) inhibits uvaol (HY-N1109)-induced migration of NIH3T3 fibroblasts by 25% in a scratch wound healing assay[3].
PKA Inhibitor Fragment (6-22) amide (10 µM; 1 h pre-incubation, 24 h co-incubation with uvaol) inhibits uvaol-induced migration of tEnd.1 endothelial cells by 27% in a scratch wound healing assay[3].

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

PKA Inhibitor Fragment (6-22) amide Related Antibodies

Cell Migration Assay [3]

Cell Line: NIH3T3 fibroblast cell line, tEnd.1 endothelial cell line
Concentration: 10 µM
Incubation Time: 1 h (pre-incubation); 24 h (co-incubation with uvaol)
Result: Reduced uvaol-induced NIH3T3 fibroblast migration towards the scratched area by 25%.
Reduced uvaol-induced tEnd.1 endothelial cell migration towards the scratched area by 27%.
In Vivo

PKA Inhibitor Fragment (6-22) amide (2.5 nmol; i.c.v.; single dose) partially reverses low-level morphine antinociceptive tolerance in male Swiss Webster mice, reducing the morphine ED50 by ~78% in tolerant animals[1].
PKA Inhibitor Fragment (6-22) amide (3.75 nmol; i.c.v.; single dose) significantly inhibits cytosolic PKA activity in the thalamus, periaqueductal gray, and lumbar spinal cord of drug-naïve male Swiss Webster mice[1].
PKA Inhibitor Fragment (6-22) amide (3.75 nmol; i.c.v.; single dose) significantly inhibits total cytosolic PKA activity in the thalamus of morphine-tolerant male Swiss Webster mice[1].

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

Animal Model: Swiss Webster (male, 25-30 g, morphine pellet implantation for 72 h to induce tolerance)[1]
Dosage: 2.5 nmol
Administration: i.c.v.; single dose
Result: Did not alter morphine antinociceptive potency in placebo-pelleted mice, with an ED50 of 4.0 mg/kg and a potency ratio of 1.0 vs. controls.
Reduced the morphine ED50 from 41.0 mg/kg to 9.2 mg/kg in morphine-pelleted tolerant mice, with a potency ratio of 2.4 vs. controls, but did not completely reverse morphine tolerance.
Reduced the morphine ED50 by ~78% in tolerant animals.
Molecular Weight

1868.06

Formula

C80H130N28O24
CAS No.
Appearance

Solid

Color

White to off-white

Sequence Shortening

TYADFIASGRTGRRNAI-NH2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

Solvent & Solubility
In Vitro: 

H2O

Peptide Solubility and Storage Guidelines:

1.  Calculate the length of the peptide.

2.  Calculate the overall charge of the entire peptide according to the following table:

  Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.  Recommended solution:

Overall charge of peptide Details
Negative (<0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, add NH4OH (<50 μL).
3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
Purity & Documentation
References
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PKA Inhibitor Fragment (6-22) amide Related Classifications

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The molarity calculator equation

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

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The dilution calculator equation

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

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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:

PKA Inhibitor Fragment (6-22) amide121932-06-7PKI-(6-22)-amidePKAProtein kinase Aprotein kinase AtEnd.1 endothelial cellsperiaqueductal graymouse braincAMP-dependent protein kinase catalytic subunitbovine heart type II cAMP-dependent protein kinasemouse spinal cordNIH3T3 fibroblastsmale Swiss Webster micemorphine antinociceptive toleranceInhibitorinhibitorinhibit

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