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PF-3644022 is an inhibitor of MAPK-activated protein kinase 2 (MK2, IC50 = 5.2 nM). It is selective for MK2 over MK3, MAPK-interacting protein kinase 1 (MNK-1), MNK-2, p90 ribosomal S6 kinase 1 (MSK1), MSK2, and p90 ribosomal S6 kinases 1-4 (RSK1-4, IC50s = 53, 3,000, 148, >1,000, >1,000, and >1,000 nM, respectively), as well as a panel of 200 other kinases at 1 µM, but also inhibits MK5/PRAK (IC50 = 5 nM). PF-3644022 inhibits LPS-induced TNF-alpha production in U937 cells and isolated human peripheral blood mononuclear cells (PBMCs) and whole blood (IC50s = 0.159, 0.16, and 1.97 µM, respectively) and reduces paw swelling in a rat model of arthritis induced by streptococcal cell wall peptidoglycan-polysaccharide complexes (ED50 = 20 mg/kg). It prevents decreases in motor function in a twy/twy mouse model of chronic cervical spinal cord compression when administered at a dose of 30 mg/kg. Peritumoral administration of PF-3644022 (30 µl of a 50 µM solution) enhances radiation-induced decreases in tumor volume and increases in survival in a patient-derived xenograft (PDX) mouse model of head and neck squamous cell carcinoma (HNSCC).Formal Name: (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 Formula: C21H18N4OS. Formula Weight: 374.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 3 mg/ml. lambdamax: 255, 287 nm. SMILES: CC1=CC=C(C2=CC=C(C(C(NC[C@@H](C)NC3=O)=C3S4)=C4C=C5)C5=N2)C=N1. InChi Code: InChI=1S/C21H18N4OS/c1-11-3-4-13(10-22-11)15-6-5-14-16(25-15)7-8-17-18(14)19-20(27-17)21(26)24-12(2)9-23-19/h3-8,10,12,23H,9H2,1-2H3,(H,24,26)/t12-/m1/s1. InChi Key: CMWRPDHVGMHLSZ-GFCCVEGCSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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