Cat. No.: HY-107427

PF-3644022

2 Cited Publications

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PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC₅₀ of 5.2 nM and a K_i 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.

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Pureté: 99.91%
CAS No.: 1276121-88-0
Formule: C₂₁H₁₈N₄OS
Masse moléculaire:374.46

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PF-3644022 Chemical Structure

CAS No.: 1276121-88-0

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

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

Voir tous les produits spécifiques à Isoform p38 MAPK :

Cellular Effect

Cell Line	Type	Value	Description	References
MDCK	IC₅₀	7 μM Compound: 30; PF-3644022; PF022	Inhibition of MRP2 in MDCK cells after 15 mins by Calcein-AM assay Inhibition of MRP2 in MDCK cells after 15 mins by Calcein-AM assay	[PMID: 26502061]
PBMC	IC₅₀	0.16 μM Compound: PF-3644022	Inhibition of TNF alpha production in LPS induced human PBMC cells preincubated with compound for 1 hr followed by LPS induction and measured after 16 hrs by MSD analysis Inhibition of TNF alpha production in LPS induced human PBMC cells preincubated with compound for 1 hr followed by LPS induction and measured after 16 hrs by MSD analysis	[PMID: 20237073]
PBMC	IC₅₀	0.214 μM Compound: PF-3644022	Antiinflammatory activity in human PBMC cells assessed as inhibition of LPS induced TNF alpha production preincubated for 1 hr followed by LPS stimulation and measured after 16 hrs by MSD analysis Antiinflammatory activity in human PBMC cells assessed as inhibition of LPS induced TNF alpha production preincubated for 1 hr followed by LPS stimulation and measured after 16 hrs by MSD analysis	[PMID: 20237073]
PBMC	IC₅₀	1.26 μM Compound: PF-3644022	Inhibition of IL-6 production in LPS induced human PBMC cells preincubated with compound for 1 hr followed by LPS induction and measured after 16 hrs by MSD analysis Inhibition of IL-6 production in LPS induced human PBMC cells preincubated with compound for 1 hr followed by LPS induction and measured after 16 hrs by MSD analysis	[PMID: 20237073]
PBMC	IC₅₀	1.4 μM Compound: PF-3644022	Antiinflammatory activity in human PBMC cells assessed as inhibition of LPS induced IL-6 production preincubated for 1 hr followed by LPS stimulation and measured after 16 hrs by MSD analysis Antiinflammatory activity in human PBMC cells assessed as inhibition of LPS induced IL-6 production preincubated for 1 hr followed by LPS stimulation and measured after 16 hrs by MSD analysis	[PMID: 20237073]
PBMC	IC₅₀	2.09 μM Compound: PF-3644022	Inhibition of IL-8 production in LPS induced human PBMC cells preincubated with compound for 1 hr followed by LPS induction and measured after 16 hrs by MSD analysis Inhibition of IL-8 production in LPS induced human PBMC cells preincubated with compound for 1 hr followed by LPS induction and measured after 16 hrs by MSD analysis	[PMID: 20237073]
PBMC	IC₅₀	2.59 μM Compound: PF-3644022	Antiinflammatory activity in human PBMC cells assessed as inhibition of LPS induced IL-8 production preincubated for 1 hr followed by LPS stimulation and measured after 16 hrs by MSD analysis Antiinflammatory activity in human PBMC cells assessed as inhibition of LPS induced IL-8 production preincubated for 1 hr followed by LPS stimulation and measured after 16 hrs by MSD analysis	[PMID: 20237073]
PBMC	IC₅₀	2.71 μM Compound: PF-3644022	Antiinflammatory activity in human PBMC cells assessed as inhibition of LPS induced IL-1 beta production preincubated for 1 hr followed by LPS stimulation and measured after 16 hrs by MSD analysis Antiinflammatory activity in human PBMC cells assessed as inhibition of LPS induced IL-1 beta production preincubated for 1 hr followed by LPS stimulation and measured after 16 hrs by MSD analysis	[PMID: 20237073]
PBMC	IC₅₀	2.78 μM Compound: PF-3644022	Inhibition of IL-1 beta production in LPS induced human PBMC cells preincubated with compound for 1 hr followed by LPS induction and measured after 16 hrs by MSD analysis Inhibition of IL-1 beta production in LPS induced human PBMC cells preincubated with compound for 1 hr followed by LPS induction and measured after 16 hrs by MSD analysis	[PMID: 20237073]
Sf9	IC₅₀	7 μM Compound: 30; PF-3644022; PF022	Inhibition of human BSEP expressed in recombinant baculovirus infected insect Sf9 cell membrane vesicles assessed as [3H]-taurocholate transport preincubated for 5 mins followed by ATP or AMP addition measured after 5 mins by scintillation counting method Inhibition of human BSEP expressed in recombinant baculovirus infected insect Sf9 cell membrane vesicles assessed as [3H]-taurocholate transport preincubated for 5 mins followed by ATP or AMP addition measured after 5 mins by scintillation counting method	[PMID: 26502061]
U-937	IC₅₀	0.159 μM Compound: PF-3644022	Inhibition of TNF-alpha production in LPS-induced human U-937 cells preincubated with compound for 1 hr followed by LPS induction and measured after 4 hrs by MSD analysis Inhibition of TNF-alpha production in LPS-induced human U-937 cells preincubated with compound for 1 hr followed by LPS induction and measured after 4 hrs by MSD analysis	[PMID: 20237073]
U-937	IC₅₀	0.201 μM Compound: PF-3644022	Inhibition of MK2 activity in LPS induced human U937 cells preincubated with compound for 1 hr followed by LPS induction and measured after 30 mins by Western blot analysis Inhibition of MK2 activity in LPS induced human U937 cells preincubated with compound for 1 hr followed by LPS induction and measured after 30 mins by Western blot analysis	[PMID: 20237073]
U-937	IC₅₀	150 nM Compound: 30; PF-3644022; PF022	Inhibition of LPS-induced TNFalpha production in human U937 cells preincubated for 1 hr followed by LPS addition measured after 4 hrs by electro-chemiluminescence method Inhibition of LPS-induced TNFalpha production in human U937 cells preincubated for 1 hr followed by LPS addition measured after 4 hrs by electro-chemiluminescence method	[PMID: 26502061]
U-937	IC₅₀	201 nM Compound: 30; PF-3644022; PF022	Inhibition of MK2 in human U937 cells assessed as reduction in LPS-stimulated HSP27 phosphorylation at Ser82 preincubated for 1 hr followed by LPS addition measured after 30 mins by Western blot analysis Inhibition of MK2 in human U937 cells assessed as reduction in LPS-stimulated HSP27 phosphorylation at Ser82 preincubated for 1 hr followed by LPS addition measured after 30 mins by Western blot analysis	[PMID: 26502061]

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.

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.

Chemical Information

CAS No. 1276121-88-0
Appearance Solid
Masse moléculaire 374.46
Formule C₂₁H₁₈N₄OS
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Neurochem Int

SPP1 expression after spinal cord compression injury and its effects on glial cell activation. [Abstract]

2025 Nov:190:106063. PMID: 41015119
Research Square Preprint

2024 Apr 15.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Mourey RJ, et al. A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J Pharmacol Exp Ther. 2010 Jun;333(3):797-807 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

PF-3644022

2 Cited Publications

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PF-3644022

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Publications Citing Use of MedChemExpress (MCE) PF-3644022

Voir tous les produits spécifiques à Isoform p38 MAPK

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PF-3644022 Related Classifications

HY-107427 Related Classifications