Molecular structure of MK-2 Inhibitor III, CAS Number: 1186648-22-5
MK-2 Inhibitor III (CAS 1186648-22-5)
See product citations (3)
Alternate Names:
2-(2-quinolin-3-ylpyridin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
Application:
MK-2 Inhibitor III is a cell-permeable pyrrolopyridinyl compound that acts as a potent, selective, and ATP-biniding site-targeting MK-2/MAPKAP-K2 inhibitor
CAS Number:
1186648-22-5
Purity:
≥97%
Molecular Weight:
358.39
Molecular Formula:
C21H16N4O•H2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
MK-2 Inhibitor III is a cell-permeable pyrrolopyridinyl compound that acts as a potent, selective, and ATP-biniding site-targeting MK-2/MAPKAP-K2 inhibitor (IC50 = 8.5, 81, and 210 nM agaisnt MAPKAPK-2 (MK-2), PRAK(MK-5), and 3pK(MK-3), respectively), while exhibiting much less or no activity against 8 other studied kinases. The inhibition of MK-2 presents a strategic approach to controlling the production of pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-8. MK-2 Inhibitor III provides insights into how modulation of the p38 MAPK pathway can influence cell function and survival, particularly in the immune system and in cells exposed to environmental stressors.Shown to suppress LPS-induced TNF-alpha production in U937 cells (IC50 = 4.4 muM).
MK-2 Inhibitor III (CAS 1186648-22-5) References
- Arachidonic acid promotes phosphorylation of 5-lipoxygenase at Ser-271 by MAPK-activated protein kinase 2 (MK2). | Werz, O., et al. 2002. J Biol Chem. 277: 14793-800. PMID: 11844797
- Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). | Anderson, DR., et al. 2005. Bioorg Med Chem Lett. 15: 1587-90. PMID: 15745802
- Phosphorylation of HSF1 by MAPK-activated protein kinase 2 on serine 121, inhibits transcriptional activity and promotes HSP90 binding. | Wang, X., et al. 2006. J Biol Chem. 281: 782-91. PMID: 16278218
- CDC25B phosphorylation by p38 and MK-2. | Lemaire, M., et al. 2006. Cell Cycle. 5: 1649-53. PMID: 16861915
- Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). | Anderson, DR., et al. 2007. J Med Chem. 50: 2647-54. PMID: 17480064
- Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). | Trujillo, JI., et al. 2007. Bioorg Med Chem Lett. 17: 4657-63. PMID: 17570666
- First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. | Menichincheri, M., et al. 2009. J Med Chem. 52: 293-307. PMID: 19115845
- Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). | Lovering, F., et al. 2009. Bioorg Med Chem. 17: 3342-51. PMID: 19364658
- Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). | Lin, S., et al. 2009. Bioorg Med Chem Lett. 19: 3238-42. PMID: 19423344
- Inhibition of the protein kinase MK-2 protects podocytes from nephrotic syndrome-related injury. | Pengal, R., et al. 2011. Am J Physiol Renal Physiol. 301: F509-19. PMID: 21613416
- A computational study on thiourea analogs as potent MK-2 inhibitors. | Hao, M., et al. 2012. Int J Mol Sci. 13: 7057-7079. PMID: 22837679
- Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). | Lin, S., et al. 2015. Bioorg Med Chem Lett. 25: 5402-8. PMID: 26403928
- Ozone-related fluorescent compounds in mouse liver and lung. | Csallany, AS., et al. 1985. Environ Res. 37: 320-6. PMID: 4017987
Inhibitor of:
3pK, MAPKAPK-2, and PRAK.Activator of:
MK.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
MK-2 Inhibitor III, 5 mg | sc-221948 | 5 mg | $400.00 |