PF-3644022
Based on 3 publication(s) in Google Scholar
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.
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- Purity : 99.91%
- CAS No.: 1276121-88-0
- 화학식: C21H18N4OS
- 분자량:374.46
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PF-3644022
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In Vivo Efficacy Study
Biological Activity
제품 설명
IC50 & Target
IC50: 5.2 nM (MK2), 5.0 nM (PRAK) and 53 nM (MK3)[1].
Ki: 3 nM (MK2)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDCK | IC50 |
7 μM
Compound: 30; PF-3644022; PF022
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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
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[PMID: 26502061] |
| PBMC | IC50 |
0.16 μM
Compound: PF-3644022
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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
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[PMID: 20237073] |
| PBMC | IC50 |
0.214 μM
Compound: PF-3644022
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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
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[PMID: 20237073] |
| PBMC | IC50 |
1.26 μM
Compound: PF-3644022
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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
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[PMID: 20237073] |
| PBMC | IC50 |
1.4 μM
Compound: PF-3644022
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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
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[PMID: 20237073] |
| PBMC | IC50 |
2.09 μM
Compound: PF-3644022
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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
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[PMID: 20237073] |
| PBMC | IC50 |
2.59 μM
Compound: PF-3644022
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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
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[PMID: 20237073] |
| PBMC | IC50 |
2.71 μM
Compound: PF-3644022
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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
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[PMID: 20237073] |
| PBMC | IC50 |
2.78 μM
Compound: PF-3644022
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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
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[PMID: 20237073] |
| Sf9 | IC50 |
7 μM
Compound: 30; PF-3644022; PF022
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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
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[PMID: 26502061] |
| U-937 | IC50 |
0.159 μM
Compound: PF-3644022
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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
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[PMID: 20237073] |
| U-937 | IC50 |
0.201 μM
Compound: PF-3644022
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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
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[PMID: 20237073] |
| U-937 | IC50 |
150 nM
Compound: 30; PF-3644022; PF022
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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
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[PMID: 26502061] |
| U-937 | IC50 |
201 nM
Compound: 30; PF-3644022; PF022
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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
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[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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Lewis rats (125-140 g) injected with streptococcal cell wall[1]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg
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Administration:Oral gavage; twice a day; for 12 days
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Result:Showed dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing.
Chemical Information
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CAS No. 1276121-88-0
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Appearance Solid
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분자량 374.46
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화학식 C21H18N4OS
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Color Light yellow to yellow
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SMILES
O=C1C2=C(NC[C@@H](C)N1)C3=C(C=CC4=NC(C5=CN=C(C)C=C5)=CC=C34)S2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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PF-3644022 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jul 13:e76141.
CFAST detects the binding of the MK2 probe in lysates of MK2-expressing HEK293T cells treated with DMSO and PF-3644022, following heating at various temperatures.
PF-3644022 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jul 13:e76141.
Dose-response CETSA Western blot analysis of MK2 and ACTB was performed on MK2-expressing HEK293T cells treated with DMSO and PF-3644022 under heating at 54°C.
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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
PF-3644022 purchased from MedChemExpress. Usage Cited in: Neurochem Int. 2025 Nov:190:106063. [Abstract]
The combined use of AVV9-SPP1 and PF-3644022 (30 mg/kg) exacerbated myelin damage in spinal cord tissue. We performed Western blot analysis to evaluate the expression levels of GAP43 and NeuN proteins.
PF-3644022 purchased from MedChemExpress. Usage Cited in: Neurochem Int. 2025 Nov:190:106063. [Abstract]
The MK2 inhibitor PF-3644022 (30 mg/kg) was administered in combination with AAV9-SPP1. We performed BBB scoring on days 3, 7, 14, 21, and 28 post-surgery.
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용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
순도&문서
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Data Sheet (275 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
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