Bioactivity | IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.17 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1]. | ||||||||||||
Invitro | IRAK4-IN-21 (a 4-fold serial dilution from 10 µM; 1 h) decreases the levels of IL-23 (in THP-1 and DC cells), IL-6 (in HUVEC cells) and MIP-1β (in human whole blood)[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
In Vivo | IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production[1]. Animal Model: | ||||||||||||
Name | IRAK4-IN-21 | ||||||||||||
CAS | 2170694-04-7 | ||||||||||||
Formula | C28H28FN7O2 | ||||||||||||
Molar Mass | 513.57 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Chen Y, et al. Discovery of 5-Aryl-2,4-diaminopyrimidine Compounds as Potent and Selective IRAK4 Inhibitors. ACS Med Chem Lett. 2022 Apr 4;13(4):714-719. |