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PF-3644022

PF-3644022
PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) (IC50s: 53 nM and 5.0 nM, respectively).
Catalog No. T16501Cas No. 1276121-88-0
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Purity:98.13%
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PF-3644022

Purity: 98.13%
Catalog No. T16501Cas No. 1276121-88-0

PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) (IC50s: 53 nM and 5.0 nM, respectively).
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Pack SizePriceAvailabilityQuantity
1 mg$31In Stock
5 mg$113In Stock
10 mg$213In Stock
25 mg$438In Stock
50 mg$653In Stock
100 mg$876In Stock
500 mg$1,750In Stock
1 mL x 10 mM (in DMSO)$196In Stock
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Product Introduction

Bioactivity
Description
PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated
Targets&IC50
PRAK:5.0 nM, MK2:(ki)3 nM, MK2:5.2 nM, MK3:53 nM
In vitro
PF-3644022 potently inhibits TNFα production with similar activity (IC50 of 160 nM), in the human U937 monocytic cell line or peripheral blood mononuclear cells. PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood (IC50: 1.6 and 10.3 μM, respectively). 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 vivo
PF-3644022 (3-100 mg/kg; oral gavage; twice daily for 12 days; Lewis rats) treatment exhibits dose-dependent inhibition of chronic paw swelling, measured on day 21 post-treatment (ED50: 20 mg/kg)[1].
Chemical Properties
Molecular Weight374.46
FormulaC21H18N4OS
Cas No.1276121-88-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 41.67 mg/mL (111.28 mM), Sonication and heating to 80℃ are recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6705 mL13.3526 mL26.7051 mL133.5256 mL
5 mM0.5341 mL2.6705 mL5.3410 mL26.7051 mL
10 mM0.2671 mL1.3353 mL2.6705 mL13.3526 mL
20 mM0.1335 mL0.6676 mL1.3353 mL6.6763 mL
50 mM0.0534 mL0.2671 mL0.5341 mL2.6705 mL
100 mM0.0267 mL0.1335 mL0.2671 mL1.3353 mL

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