PKI 14-22 amide,myristoylated TFA 

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

PKI 14-22 amide,myristoylated TFA (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 TFA (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.

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) TFA 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.

1323.51

C₅₅H₁₀₁F₃N₂₀O₁₄

Solid

White to off-white

Myristoyl-GRTGRRNAI-NH2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

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

* 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.

• [1]. L Ydrenius, et al. Activation of cAMP-dependent protein kinase is necessary for actin rearrangements in human neutrophils during phagocytosis. J Leukoc Biol. 2000 Apr;67(4):520-8.  [Content Brief]

  [2]. Cheng F, et al. Suppression of Zika Virus Infection and Replication in Endothelial Cells and Astrocytes by PKA Inhibitor PKI 14-22. J Virol. 2018 Jan 30;92(4):e02019-17.  [Content Brief]

  [3]. Gabra BH, et al. Pre-treatment with a PKC or PKA inhibitor prevents the development of morphine tolerance but not physical dependence in mice. Brain Res. 2008 Jun 27;1217:70-7.  [Content Brief]