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

PF-3644022 

Cat. No.: HY-107427
Handling Instructions

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
10 mM * 1 mL in DMSO USD 490 In-stock
Estimated Time of Arrival: December 31
1 mg USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 595 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1050 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • 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].

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].

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.

1276121-88-0

SMILES

O=C1C2=C(NC[[email protected]@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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PF-3644022PF3644022PF 3644022MAPKAPK2 (MK2)p38 MAPKMitogen-activated protein kinase activated protein kinase 2MAP kinase activated protein kinase 2MAPK activated protein kinase 2MAPKAP kinase 2Anti-inflammatorysafetyTNFαIL-6lipopolysaccharidemonocyticorallyefficaciousPRAKMK3Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
PF-3644022
Cat. No.:
HY-107427
Quantity:
MCE Japan Authorized Agent: