2. MAPK/ERK Pathway
  3. MAPKAPK2 (MK2) p38 MAPK
  4. PF-3644022

PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.

For research use only. We do not sell to patients.

PF-3644022 Chemical Structure

PF-3644022 Chemical Structure

CAS No. : 1276121-88-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 396 In-stock
Solution
10 mM * 1 mL in DMSO USD 396 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 140 In-stock
10 mg USD 260 In-stock
25 mg USD 530 In-stock
50 mg USD 857 In-stock
100 mg USD 1372 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

PF-3644022 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PF-3644022

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK p38α p38β MAPK13 p38δ p38γ

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  • Purity & Documentation

  • References

  • Customer Review

Description

PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect[1].

IC50 & Target

IC50: 5.2 nM (MK2), 5.0 nM (PRAK) and 53 nM (MK3)[1].
Ki: 3 nM (MK2)[1]
In Vitro

The inhibitory activity of PF-3644022 against other MAPKAP kinase family members is evaluated. Other than MNK2 with an IC50 of 148 nM, other family members are largely not inhibited, showing at least several hundred-fold selectivity versus MK2[1].
In the human U937 monocytic cell line or peripheral blood mononuclear cells, PF-3644022 potently inhibits TNFα production with similar activity (IC50 of 160 nM). PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC50 values of 1.6 and 10.3 μM, respectively. Inhibition of TNFα in U937 cells and blood correlates closely with inhibition of phospho-heat shock protein 27, a target biomarker of MK2 activity[1].

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

PF-3644022 Related Antibodies
In Vivo

PF-3644022 (3-100 mg/kg; oral gavage; twice a day; for 12 days; Lewis rats) treatment shows dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing, with ED50 value of 20 mg/kg[1].

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

Animal Model: Female Lewis rats (125-140 g) injected with streptococcal cell wall[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral gavage; twice a day; for 12 days
Result: Showed dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing.
Molecular Weight

374.46

Formula

C21H18N4OS
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(NC[C@@H](C)N1)C3=C(C=CC4=NC(C5=CN=C(C)C=C5)=CC=C34)S2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (111.28 mM; ultrasonic and warming and heat to 80°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 2.6705 mL 13.3526 mL 26.7051 mL
5 mM 0.5341 mL 2.6705 mL 5.3410 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)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (5.55 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 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 (20.8 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:

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).
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

Purity: 99.65%

COA (249 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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 2.6705 mL 13.3526 mL 26.7051 mL 66.7628 mL
5 mM 0.5341 mL 2.6705 mL 5.3410 mL 13.3526 mL
10 mM 0.2671 mL 1.3353 mL 2.6705 mL 6.6763 mL
15 mM 0.1780 mL 0.8902 mL 1.7803 mL 4.4509 mL
20 mM 0.1335 mL 0.6676 mL 1.3353 mL 3.3381 mL
25 mM 0.1068 mL 0.5341 mL 1.0682 mL 2.6705 mL
30 mM 0.0890 mL 0.4451 mL 0.8902 mL 2.2254 mL
40 mM 0.0668 mL 0.3338 mL 0.6676 mL 1.6691 mL
50 mM 0.0534 mL 0.2671 mL 0.5341 mL 1.3353 mL
60 mM 0.0445 mL 0.2225 mL 0.4451 mL 1.1127 mL
80 mM 0.0334 mL 0.1669 mL 0.3338 mL 0.8345 mL
100 mM 0.0267 mL 0.1335 mL 0.2671 mL 0.6676 mL
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PF-3644022 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-36440221276121-88-0PF3644022PF 3644022MAPKAPK2 (MK2)p38 MAPKMitogen-activated protein kinase activated protein kinase 2MAP kinase activated protein kinase 2MAPK activated protein kinase 2MAPKAP kinase 2Anti-inflammatorysafetyTNFαIL-6lipopolysaccharidemonocyticorallyefficaciousPRAKMK3Inhibitorinhibitorinhibit

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