Tofacitinib
Kinase inhibitor: JAK. Limits 'cytokine storm' in humans. Spinelli et al. Sci. Immunol., 5:eabc5367, May 2020, https://doi.org/10.1126/sciimmunol.abc5367.
- Datasheet: view or download
- Applications:"Cytokine storm" drug (approved, U.S.), in COVID-19 clinical trials
Biochemicals & reagents
540737-29-9
1) Jiang et al. (2008), Examining the chirality, confirmation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitril (CP-690,550); J. Mol. Chem., 51 8012 2) Cutolo and Meroni (2013), Clinical utility of the oral JAK inhibitor tofacitinib in the treatment of rheumatoid arthritis; J. Inflamm. Res., 6 129 3) Martina et al. (2016), Inhiition of JAK3 and PKC via Immunosuppressive Drugs Tofacitinib and Sotrastaurin Inhibits Proliferation of Human B Lymphocytes In Vitro; Transplant. Proc., 48 3046 4) Moisan et al. (2015), White-to-brown metabolic conversion of human adipocytes by JAK inhibition; Nat. Cell Biol., 17 57 5) Dowty et al. (2014), Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis; J. Pharmacol. Exp. Ther., 348 165
312.37
-20°C
Tofacitinib is a potent pan-JAK inhibitor with IC50s = 1, 20 and 112 nM for JAK3, JAK2 and JAK1 respectively (1). This compound displays potent antiinflammatory (2) and immunosuppressant (3) activities. It also promotes a white-to-brown metabolic metabolic conversion in human adipoctes (4) and is therapeutically used for rheumatoid arthritis (5).