Highly potent JAK1 and JAK2 inhibitor; also inhibits JAK3 and Tyk2
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
(Kd 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
| Marque | Tocris |
|---|---|
| Réf. B-LABO | BL-RE-125874 |
| Réf. fabricant | 18706006 |
| Nom chimique ou matériau | 1-(Ethylsulfonyl)-3-[4-(7 H-pyrrolo[2,3-d]pyrimidin-4-yl)-1 H-pyrazol-1-yl]-3-azetidineacetonitrile |
| CAS | 1187594-09-7 |
| Quantité | 50 mg |
| Cible | JAK Kinase Inhibitors |
| Formule moléculaire | C<sub>16</sub>H<sub>17</sub>N<sub>7</sub>O<sub>2</sub>S |
| Pureté | 0.98 |
