Molecular structure of PF-3644022, CAS Number: 1276121-88-0
PF-3644022 (CAS 1276121-88-0)
Alternate Names:
(10R)-9,10,11,12-Tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one
CAS Number:
1276121-88-0
Molecular Weight:
374.46
Molecular Formula:
C21H18N4OS
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
PF-3644022 is an exceedingly powerful inhibitor that effectively competes with ATP to target mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) with remarkable potency (IC50 = 5.2 nM Ki = 3 nM). This compound demonstrates the ability to inhibit the production of tumor necrosis factor α (TNFα) in both U937 monocytic cells and peripheral blood mononuclear cells (PBMCs) with a notable efficacy (IC50 = 160 nM).
PF-3644022 (CAS 1276121-88-0) References
- 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. | Mourey, RJ., et al. 2010. J Pharmacol Exp Ther. 333: 797-807. PMID: 20237073
- MAPKAP kinases MK2 and MK3 in inflammation: complex regulation of TNF biosynthesis via expression and phosphorylation of tristetraprolin. | Ronkina, N., et al. 2010. Biochem Pharmacol. 80: 1915-20. PMID: 20599781
- Microwave-assisted synthesis of 3-aminobenzo[b]thiophene scaffolds for the preparation of kinase inhibitors. | Bagley, MC., et al. 2015. Org Biomol Chem. 13: 6814-24. PMID: 26013834
- Suppression of the senescence-associated secretory phenotype (SASP) in human fibroblasts using small molecule inhibitors of p38 MAP kinase and MK2. | Alimbetov, D., et al. 2016. Biogerontology. 17: 305-15. PMID: 26400758
- Role of MK2 signaling pathway in the chronic compression of cervical spinal cord. | Song, H., et al. 2015. Am J Transl Res. 7: 2355-63. PMID: 26807183
- Deciphering the true antiproliferative target of an MK2 activation inhibitor in glioblastoma. | Brennan, PE. 2016. Cell Death Dis. 7: e2069. PMID: 26821065
- Targeting p38 or MK2 Enhances the Anti-Leukemic Activity of Smac-Mimetics. | Lalaoui, N., et al. 2016. Cancer Cell. 29: 145-58. PMID: 26859455
- Coordination of stress signals by the lysine methyltransferase SMYD2 promotes pancreatic cancer. | Reynoird, N., et al. 2016. Genes Dev. 30: 772-85. PMID: 26988419
- Mesenchymal MAPKAPK2/HSP27 drives intestinal carcinogenesis. | Henriques, A., et al. 2018. Proc Natl Acad Sci U S A. 115: E5546-E5555. PMID: 29844172
- MAPKAPK2 (MK2) inhibition mediates radiation-induced inflammatory cytokine production and tumor growth in head and neck squamous cell carcinoma. | Berggren, KL., et al. 2019. Oncogene. 38: 7329-7341. PMID: 31417185
- Phosphorylated Hsp27 prevents LPS-induced excessive inflammation in THP-1 cells via suppressing ROS-mediated upregulation of CBP. | Bi, X., et al. 2020. Cell Biol Int. 44: 253-267. PMID: 31483551
- Resveratrol inhibits IL-33-mediated mast cell activation by targeting the MK2/3-PI3K/Akt axis. | Nakajima, S., et al. 2019. Sci Rep. 9: 18423. PMID: 31804564
- A tumor-specific modulation of heterogeneous ribonucleoprotein A0 promotes excessive mitosis and growth in colorectal cancer cells. | Konishi, H., et al. 2020. Cell Death Dis. 11: 245. PMID: 32303675
- Role of MK2 signaling pathway mediating microglia/macrophages polarization in chronic compression injury of cervical spinal cord. | Yu, L., et al. 2021. Ann Palliat Med. 10: 1304-1312. PMID: 33040559
- MKL1 fuels ROS-induced proliferation of vascular smooth muscle cells by modulating FOXM1 transcription. | Wu, T., et al. 2023. Redox Biol. 59: 102586. PMID: 36587486
Inhibitor of:
β-Arrestin-1, CaMKKα, IL-25, MAPKAPK-2, MIP-1γ, MSK1, Sam 68, TSSK 6, and YAP.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PF-3644022, 5 mg | sc-478487 | 5 mg | $367.00 | |||
PF-3644022, 25 mg | sc-478487A | 25 mg | $2856.00 |