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PF-3644022
🥰Excellent
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).
PF-3644022
🥰Excellent
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).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $31 | In Stock | |
| 5 mg | $113 | In Stock | |
| 10 mg | $213 | In Stock | |
| 25 mg | $438 | In Stock | |
| 50 mg | $653 | In Stock | |
| 100 mg | $876 | In Stock | |
| 500 mg | $1,750 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $196 | In Stock |
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Purity:98.13%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| Molecular Weight | 374.46 |
| Formula | C21H18N4OS |
| Cas No. | 1276121-88-0 |
| Smiles | C[C@@H]1CNc2c(sc3ccc4nc(ccc4c23)-c2ccc(C)nc2)C(=O)N1 |
| Relative Density. | 1.298 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -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 | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Keywords
TNFαSerineProteaseSerine ProteasesafetyPRAKPF-3644022PF3644022PF 3644022p38MAPKp38 MAPKorallymonocyticMK3Mitogen-activated protein kinase activated protein kinase 2MAPKAPK2 (MK2)MAPKAP kinase 2MAPK activated protein kinase 2MAP kinase activated protein kinase 2lipopolysaccharideInhibitorinhibitIL-6efficaciousAnti-inflammatory
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