2. Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Neuronal Signaling
  3. Pyk2 p38 MAPK Amyloid-β
  4. PF-719

PF-719 is a highly selective Pyk2 inhibitor with an IC50 value of 17 nM. PF-719 promotes the activation of LKB1 and p38 MAPK. PF-719 blocks synaptic deficits induced by Amyloid-beta oligomers and reverses the inhibition of long-term potentiation induced by β-amyloid oligomers. PF-719 can be used in research related to Alzheimer's disease and autoimmune diseases.

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PF-719

PF-719 Chemical Structure

CAS No. : 1404454-02-9

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PF-719 Related Antibodies

Top Publications Citing Use of Products

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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Description

PF-719 is a highly selective Pyk2 inhibitor with an IC50 value of 17 nM. PF-719 promotes the activation of LKB1 and p38 MAPK. PF-719 blocks synaptic deficits induced by Amyloid-beta oligomers and reverses the inhibition of long-term potentiation induced by β-amyloid oligomers. PF-719 can be used in research related to Alzheimer's disease and autoimmune diseases[1][2][3].

In Vitro

PF-719 (2 h) inhibits the activity of Pyk2 and significantly increases the phosphorylation levels of Tau at the S396/S404 and S202/T205 sites in mature iPSC-derived cortical neurons, without altering the activity of GSK3β[1].
Pretreatment of acute hippocampal slices from wild-type mice with PF-719 (500 nM; 30 min) completely reverses the β-amyloid oligomer-induced inhibition of long-term potentiation[2].
PF-719 is a highly selective inhibitor of purified Pyk2 kinase in vitro, with an IC50 value of 17 nM[3].
PF-719 (1 μM; 1 h pre-incubation, 3 h chemokinesis assay) inhibits CXCL13-induced chemotaxis of primary mouse splenic B-2 cells and marginal zone (MZ) B cells, as well as S1P-induced chemotaxis of MZ B cells at a concentration of 1 μM[3].

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

PF-719 Related Antibodies

Western Blot Analysis[3]

Cell Line: A20 murine B-lymphoma cells
Concentration: 0.5-2.5 μM
Incubation Time: 1 h (pre-incubation); 3 min (S1P stimulation)
Result: Completely inhibited S1P-induced tyrosine phosphorylation of Pyk2 at 1 μM.
Showed little to no effect on FAK tyrosine phosphorylation at 1 μM.
Blocked both Pyk2 and FAK tyrosine phosphorylation at 2.5 μM.
Molecular Weight

448.48

Formula

C22H27F3N6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1CC1)C2=CC=C(NC3=NC=C(C(F)(F)F)C(N[C@H]4[C@H](N(C)C)CCC4)=N3)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (111.49 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2298 mL 11.1488 mL 22.2975 mL
5 mM 0.4460 mL 2.2298 mL 4.4595 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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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

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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. 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
DMSO 1 mM 2.2298 mL 11.1488 mL 22.2975 mL 55.7438 mL
5 mM 0.4460 mL 2.2298 mL 4.4595 mL 11.1488 mL
10 mM 0.2230 mL 1.1149 mL 2.2298 mL 5.5744 mL
15 mM 0.1487 mL 0.7433 mL 1.4865 mL 3.7163 mL
20 mM 0.1115 mL 0.5574 mL 1.1149 mL 2.7872 mL
25 mM 0.0892 mL 0.4460 mL 0.8919 mL 2.2298 mL
30 mM 0.0743 mL 0.3716 mL 0.7433 mL 1.8581 mL
40 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3936 mL
50 mM 0.0446 mL 0.2230 mL 0.4460 mL 1.1149 mL
60 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9291 mL
80 mM 0.0279 mL 0.1394 mL 0.2787 mL 0.6968 mL
100 mM 0.0223 mL 0.1115 mL 0.2230 mL 0.5574 mL
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PF-719 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:

PF-7191404454-02-9PF719PF 719Pyk2p38 MAPKAmyloid-βProline-rich tyrosine kinase 2β-amyloid peptideAβAbetaamyloid-beta oligomerFAKiPSC-derived human cortical neuronsMAPK1TauLKB1B cellslong-term potentiationInhibitorinhibitorinhibit

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