2. Immunology/Inflammation Apoptosis Cytoskeleton Cell Cycle/DNA Damage
  3. Interleukin Related TNF Receptor PAK
  4. PQA-18

PQA-18 is a unique PAK2 inhibitor (IC50: 10 nM). PQA-18 has immunosuppressing effects. PQA-18 suppresses IL2, IL4, IL6, and TNFα. PQA-18 inhibits the population of a subset of regulatory T cells and the immunoglobulin (Ig) production against T cell-dependent antigens as well as alleviates dermatitis in mice.

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PQA-18

PQA-18 Chemical Structure

CAS No. : 1604678-82-1

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PQA-18 Related Antibodies

Top Publications Citing Use of Products

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PQA-18 is a unique PAK2 inhibitor (IC50: 10 nM). PQA-18 has immunosuppressing effects. PQA-18 suppresses IL2, IL4, IL6, and TNFα. PQA-18 inhibits the population of a subset of regulatory T cells and the immunoglobulin (Ig) production against T cell-dependent antigens as well as alleviates dermatitis in mice[1].

IC50 & Target[1]

PAK2

10 nM (IC50)

IL-6

 

IL4

 

IL-2

 

In Vitro

PQA-18 (0.1-20 μM, 6-24 h) markedly inhibits ConA (HY-P2149)-induced production of IL2, IL4, IL6 and TNFα in human peripheral lymphocytes (IC50: 450, 650, 580 and 460 nM, respectively) and IL2 production at protein (IC50: 400 nM) and mRNA levels in Jurkat cells[1].
PQA-18 (10 μM) attenuates the phosphorylation of cofilin-1 and histone H4 by inhibiting the corresponding kinases[1].
PQA-18 (0.1 nM-1 μM) inhibits PAK2 kinase activity in a non-competitive and concentration-dependent manner by its autophosphorylation at Ser141(IC50 of 10 nM, Km of 2.1 μM)[1].

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

PQA-18 Related Antibodies

Real Time qPCR[1]

Cell Line: Jurkat cells cultured with ConA
Concentration: 1, 10, 20 μM
Incubation Time: 6 h
Result: Suppressed IL2 mRNA level in ConA-stimulated Jurkat cells.
Affected ∼50% of IL2 transcripts at a high dose (10 μM).
In Vivo

PQA-18 (0.5 mg/kg, i.p., three times a week) displays immunosuppressing activity in C57BL/6J mice immunized with NP-CGG, with inhibiting the population of a subset of regulatory T cells and the immunoglobulin (Ig) production against T cell-dependent antigens[1].
PQA-18 ointment (100 mg/mouse, contains 0.05%-0.1% PQA-18, three times a week, 17 weeks) improves dermatitis and IgE levels in Nc/Nga mice[1].

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

Animal Model: Male C57BL/6J mice (10 weeks old) immunized by intraperitoneal injection of 50 μg NP-CGG[1]
Dosage: 0.5 mg/kg
Administration: Intraperitoneal injection (i.p.); three times a week
Result: Suppressed the NP-specific responses (IgM, IgG1, and IgG3) in peripheral blood.
Significantly suppressed the number of Foxp3+CD4+CD25+ cells in spleens.
Molecular Weight

409.52

Formula

C25H31NO4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC2=C(OC/C=C(C)/C)C=CC=C2C(OC/C=C(C)/C)=C1)OC/C=C(C)\C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (48.84 mM; Need ultrasonic; 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 2.4419 mL 12.2094 mL 24.4188 mL
5 mM 0.4884 mL 2.4419 mL 4.8838 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 and light). 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

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Volume (start)

V1

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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 mg/mL (4.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (4.88 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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:

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
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).

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

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 (sealed storage, away from moisture and light). 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 2.4419 mL 12.2094 mL 24.4188 mL 61.0471 mL
5 mM 0.4884 mL 2.4419 mL 4.8838 mL 12.2094 mL
10 mM 0.2442 mL 1.2209 mL 2.4419 mL 6.1047 mL
15 mM 0.1628 mL 0.8140 mL 1.6279 mL 4.0698 mL
20 mM 0.1221 mL 0.6105 mL 1.2209 mL 3.0524 mL
25 mM 0.0977 mL 0.4884 mL 0.9768 mL 2.4419 mL
30 mM 0.0814 mL 0.4070 mL 0.8140 mL 2.0349 mL
40 mM 0.0610 mL 0.3052 mL 0.6105 mL 1.5262 mL
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PQA-18 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:

PQA-181604678-82-1PQA18PQA 18Interleukin RelatedTNF ReceptorPAKILTumor Necrosis Factor ReceptorTNFRp21 activated kinasesNc/NgaPeripheral lymphocytesJurkat cellsC57BL/6JImmunosuppressingDermatitis.Inhibitorinhibitorinhibit

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