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PF-3644022

SKU: orb1307895

Description

PF-3644022 is a potent and selective ATP-competitive inhibitor of MAPKAPK2 (MK2) with an IC50 of 5.2 nM. It also inhibits MK3 and PRAK and suppresses TNFα production, demonstrating anti-inflammatory effects in cellular assays. This compound is a valuable research tool for studying p38 MAPK signaling in inflammation and related disease models.

Research Area

Protein Biochemistry, Signal Transduction

Images & Validation

Key Properties

CAS Number1276121-88-0
MW374.46
Purity99.12%
FormulaC21H18N4OS
SMILESC[C@@H]1CNc2c(sc3ccc4nc(ccc4c23)-c2ccc(C)nc2)C(=O)N1
Targetp38 MAPK,MAPK,Serine Protease
SolubilityDMSO:41.67 mg/mL (111.28 mM)

Bioactivity

Target IC50
PRAK:5.0 nM|MK3:53 nM|MK2:(ki)3 nM|MK2:5.2 nM
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).
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Anti-inflammatory, MAP kinase activated protein kinase 2, MAPK activated protein kinase 2, MAPKAP kinase 2, MAPKAPK2 (MK2), Inhibitor, efficacious, Mitogen-activated protein kinase activated protein kinase 2, MK2, MK3, orally, lipopolysaccharide, inhibit, IL-6, monocytic, TNFα, Serine Protease, SerineProtease, PF 3644022, PRAK, PF3644022, PF-3644022, p38MAPK, p38 MAPK, safety
Quality Guarantee

Quality Guarantee

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Key Properties

No computed properties available.

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Protocol Information

PF-3644022 (orb1307895)

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Available Sizes

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1 mg
$ 80.00
5 mg
$ 160.00
1 ml x 10 mM (in DMSO)
$ 240.00
10 mg
$ 260.00
25 mg
$ 480.00
50 mg
$ 700.00
100 mg
$ 920.00
500 mg
$ 1,790.00
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