Baricitinib

Biological Activity

Baricitinib is a highly potent JAK1 and JAK2 inhibitor (IC₅₀ values are 5.9 and 5.7 nM, respectively). Also inhibits Tyk2 (IC₅₀ = 53 nM). Displays >100-fold selectivity for JAK1/2 over JAK3 (IC₅₀ = 53 nM for JAK3). Binds AAK1, BIKE, GAK and MPSK1 in vitro (K_d values are 17.2, 39.8, 134.4 and 68.5 nM, respectively). Inhibits IL-6-induced STAT phosphorylation and subsequent pro-inflammatory chemokine (MPC-1) and cytokine (IL-17 and IL-22) production in PBMCs and T-cells. Displays anti-inflammatory and disease modifying effects in the rat adjuvant arthritis model. In silico modelling predicts inhibition of SARS-CoV-2 cell entry.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Family-wide structural analysis of human numb-associated protein kinases.
   Sorrell et al.
   Structure., 2016;24:401
2. Baricitinib as potential treatment for 2019-nCoV acute respiratory disease.
   Richardson et al.
   Lancet., 2020;395:e30
3. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.
   Fridman et al.
   J.Immunol., 2010;184:5298

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