Cat. No.: HY-P1290

PKA Inhibitor Fragment (6-22) amide

Name: PKA Inhibitor Fragment (6-22) amide
Brand: MedChemExpress
SKU: HY-P1290
Price: 85.00 USD
Availability: InStock
Rating: 5 (5 reviews)

(Synonyms: PKI-(6-22)-amide)

5 Cited Publications

Customer Review

Based on 5 publication(s) in Google Scholar

PKA Inhibitor Fragment (6-22) amide is a highly potent and specific competitive inhibitor of PKA, with K_i 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.

Purity : 98.00%
CAS No.: 121932-06-7
Formula: C₈₀H₁₃₀N₂₈O₂₄
Molecular Weight:1868.06

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)

PKA Inhibitor Fragment (6-22) amide Chemical Structure

CAS No.: 121932-06-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

PKA

2.8 nM (Ki)

All PKA Isoforms :

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.

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.

Chemical Information

CAS No. 121932-06-7
Appearance Solid
Molecular Weight 1868.06
Formula C₈₀H₁₃₀N₂₈O₂₄
Color White to off-white
Synonyms

PKI-(6-22)-amide
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)

Publications (5)

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Journal Impact Factor

Cell Mol Immunol

Chaperone- and PTM-mediated activation of IRF1 tames radiation-induced cell death and the inflammatory response. [Abstract]

2024 Aug;21(8):856-872. PMID: 38849539
Theranostics

Endogenous glutamate determines ferroptosis sensitivity via ADCY10-dependent YAP suppression in lung adenocarcinoma. [Abstract]

2021 Mar 24;11(12):5650-5674. PMID: 33897873
Acta Pharmacol Sin

Endothelial Gsα deficiency promotes ferroptosis and exacerbates atherosclerosis in apolipoprotein E-deficient mice via the inhibition of NRF2 signaling. [Abstract]

2025 May;46(5):1289-1302. PMID: 39806063
Chin Med

Grain-sized moxibustion activates dendritic cells to enhance the antitumor immunity of cancer vaccines. [Abstract]

2025 May 27;20(1):73. PMID: 40426190
Elife

Renal interstitial cells promote nephron regeneration by secreting prostaglandin E2. [Abstract]

2023 Jan 16:12:e81438. PMID: 36645741

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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Dalton G D, et al. Alterations in brain Protein Kinase A activity and reversal of morphine tolerance by two fragments of native Protein Kinase A inhibitor peptide (PKI)[J]. Neuropharmacology, 2005, 48(5): 648-657.

[2]. Katz BM, et al. Synthesis, characterization and inhibitory activities of (4-N3[3,5-3H]Phe10)PKI(6-22)amide and its precursors: photoaffinity labeling peptides for the active site of cyclic AMP-dependent protein kinase. Int J Pept Protein Res. 1989;33(6):439-445. [Content Brief]

[3]. Carmo J, et al. Uvaol Improves the Functioning of Fibroblasts and Endothelial Cells and Accelerates the Healing of Cutaneous Wounds in Mice. Molecules. 2020;25(21):4982. Published 2020 Oct 28. [Content Brief]

Calculators

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

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Dilution Calculator

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

PKA Inhibitor Fragment (6-22) amide

5 Cited Publications

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PKA Inhibitor Fragment (6-22) amide

Publications Citing Use of MedChemExpress (MCE) PKA Inhibitor Fragment (6-22) amide

All PKA Isoforms