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. 2023 Nov 3;83(2):139–160. doi: 10.1136/ard-2023-223850

Table 2.

In vitro selectivity of common JAKinibs for the major families of type I/II cytokines

Type I cytokine receptor Type II cytokine receptor
Receptor family GP-130 family IL-2R CGC family IL-12/23 family CβC family IL-10 family Type I IFNs Type II IFNs
Cytokine ligands IL-6, 11, 27, LIF, OSM IL-2, 4, 7, 9, 15, 21 IL-12, 23 IL-3, IL-5, GM-CSF IL-10, 19, 20, 22, 26 IFNα, β IFNγ
Asc JAKs JAK1, JAK2, TYK2 JAK1, JAK3 JAK2, TYK2 JAK2 JAK1, JAK2, TYK2 JAK1, TYK2 JAK1, JAK2
Downstream STATs STAT1, 3, 5 STAT1, 3, 5, (6) STAT3, 4 STAT5 STAT1, 3, 5 STAT1, 2, 3 STAT1, 3, 5
Inhibitors in increasing order of selectivity Tofacitinib +++ +++ +++ +++ +++ +++ +++
Peficitinib +++ +++ ++ ++ +++ +++ +++
Baricitinib +++ +++ +++ +++ +++ +++ +++
Upadacitinib +++ +++ ++ + +++ +++ +++
Filgotinib +++ +++ + + +++ +++ +++
Abrocitinib +++ +++ +++ +++ +++

The degree of inhibition is normalised against the ability of each JAKinib to inhibit JAK1 as measured by the IC50 value in nM.

+++=IC50 of the most inhibited associated JAK for a given cytokine family is lower than or equal to the IC50 for JAK1.

++=IC50 of the most inhibited associated JAK for a given cytokine family is onefold to twofold higher than the IC50 for JAK1.

+=IC50 of the most inhibited associated JAK for a given cytokine family is 2-fold to 10-fold higher than the IC50 for JAK1.

–=IC50 of the most inhibited associated JAK for a given cytokine family is >10 times higher than the IC50 for JAK1.

GM-CSF, granulocyte macrophage colony-stimulating factor; IFN, interferon; IL, interleukin; JAK, Janus kinase; STAT, signal transducer and activator of transcription.