jak1-dependent

Delgocitinib (JTE-052) is a specific JAK (Janus kinase) inhibitor with IC50 values of 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2 respectively. Delgocitinib is involved in various inflammatory and autoimmune diseases through JAK-dependent cytokines and can effectively suppress multiple cytokine signaling while inhibiting itching caused by cytokines. It is widely used to treat various inflammatory diseases, including autoimmune diseases and hypersensitivity reactions.

JAK3-IN-1 is an orally active, selective and potent JAK3 inhibitor that can be used to study immune system diseases.

VVD-118313 (compound 5a), a potent, selective JAK1 inhibitor, targets an isoform-restricted allosteric cysteine to inhibit JAK1-dependent trans-phosphorylation and cytokine signaling. This compound is utilized in cancer research [1].

Oclacitinib maleate (PF-03394197 maleate) is a novel inhibitor of JAK family members, with IC50 values ranging from 10 to 99 nM, and JAK1-dependent cytokines, with IC50 ranging from 36 to 249 nM, while not inhibiting a panel of 38 non-JAK kinases.

Upadacitinib is a potent and selective JAK inhibitor. Upadacitinib is approximately 74 fold selective for Jak1 over Jak2 in cellular assays dependent on specific, relevant cytokines. Upadacitinib demonstrates efficacy in rat arthritis models.