1. Stem Cell/Wnt Anti-infection Epigenetics TGF-beta/Smad
  2. Epigenetic Reader Domain Flavivirus PKA
  3. PKI 14-22 amide,myristoylated

PKI 14-22 amide, myristoylated is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated can prevent the development of morphine analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated can be used in research fields such as opioid tolerance mechanisms and antiviral drugs.

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Kundenspezifische Peptidsynthese

PKI 14-22 amide,myristoylated

PKI 14-22 amide,myristoylated Chemische Struktur

CAS. Nr. : 201422-03-9

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Based on 3 publication(s) in Google Scholar

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Beschreibung

PKI 14-22 amide, myristoylated is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated can prevent the development of morphine analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated can be used in research fields such as opioid tolerance mechanisms and antiviral drugs[1][2][3].

IC50 & Target

Zika virus

 

In Vitro

PKI 14-22 amide,myristoylated (20-40 μM; 72 h) significantly inhibits Zika virus replication in HUVEC and astrocytes, reducing viral titers by more than 85% without causing significant cytotoxicity[2].
PKI 14-22 amide,myristoylated (10-40 μM; 4-24 h) inhibits viral structural protein (capsid/NS1) expression and positive and negative strand RNA synthesis[2].

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

Western Blot Analysis[2]

Cell Line: HUVEC
Concentration: 10 μM, 20 μM, 40 μM
Incubation Time: 48-72 h
Result: Significantly reduced expression of viral capsid and NS1 proteins in a dose-dependent manner.
At 40 μM, protein levels were undetectable by 72 hpi, while 10 μM showed partial inhibition.
In Vivo

PKI 14-22 amide, myristoylated (5 nmol/mouse; intracerebroventricular injection; 3 times: 1 time/1 hour before surgery + 2 times/24 and 48 hours after surgery) completely preventes the development of Morphine analgesic tolerance in the mouse morphine tolerance model, without affecting the withdrawal reaction induced by Naloxone (HY-17417A)[3].

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

Animal Model: Male Swiss Webster mice (25-30 g, 6 weeks), morphine tolerance model via 75 mg pellet implantation[3]
Dosage: 5 nmol/mouse
Administration: 1 dose (1 h before pellet implantation) + 2 additional doses at 24 h and 48 h post-implantation, total 3 doses over 3 days.
Result: In the tail immersion test, morphine-pelleted mice pre-treated with PKI showed no tolerance to morphine’s antinociceptive effect, with ED50 values comparable to naive mice (6.2 vs. 6.6 mg/kg, non-significant difference).
Molekulargewicht

1209.49

Formel

C53H100N20O12

CAS. Nr.
Appearance

Solid

Color

White to off-white

Sequence Shortening

Myristoyl-GRTGRRNAI-NH2

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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)

Lösungsmittel & Löslichkeit
In Vitro: 

H2O : 50 mg/mL (41.34 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8268 mL 4.1340 mL 8.2679 mL
5 mM 0.1654 mL 0.8268 mL 1.6536 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). 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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 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).
Reinheit & Dokumentation
Verweise

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). 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 0.8268 mL 4.1340 mL 8.2679 mL 20.6699 mL
5 mM 0.1654 mL 0.8268 mL 1.6536 mL 4.1340 mL
10 mM 0.0827 mL 0.4134 mL 0.8268 mL 2.0670 mL
15 mM 0.0551 mL 0.2756 mL 0.5512 mL 1.3780 mL
20 mM 0.0413 mL 0.2067 mL 0.4134 mL 1.0335 mL
25 mM 0.0331 mL 0.1654 mL 0.3307 mL 0.8268 mL
30 mM 0.0276 mL 0.1378 mL 0.2756 mL 0.6890 mL
40 mM 0.0207 mL 0.1033 mL 0.2067 mL 0.5167 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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  • 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.

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