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

PF-3644022 

Cat. No.: HY-107427 Purity: 99.93%
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
Solution
10 mM * 1 mL in DMSO USD 490 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 490 In-stock
Estimated Time of Arrival: December 31
Solid
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
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Based on 1 publication(s) in Google Scholar

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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].

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

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].

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.
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)

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
10 mM 0.2671 mL 1.3353 mL 2.6705 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References
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Product Name:
PF-3644022
Cat. No.:
HY-107427
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