Tyk2-IN-4(BMS986165)

Tyk2-IN-4 is a selective, potent, allosteric inhibitor of tyrosine kinase 2 (Tyk2).

Signaling Pathways >> Epigenetics >> JAK

Signaling Pathways >> JAK/STAT Signaling >> JAK

Signaling Pathways >> Stem Cell/Wnt >> JAK

Research Areas >> Inflammation/Immunology

Tyk2

Tyk2-IN-4 blocks receptor-mediated Tyk2 activation by stabilizing the regulatory pseudokinase domain of the protein[1].

Lupus-like disease is strongly inhibited in NZB/W mice treated with Tyk2-IN-4. Tyk2-IN-4 is safe and overall well-tolerated. There are no serious adverse events and the frequency of non-serious adverse events are similar in the active (75%) and placebo (76%) groups. After oral administration, Tyk2-IN-4 is rapidly absorbed and exhibits an apparent elimination half-life of 8-15 hours[1].

[1]. I Catlett, et al. SAT0226 A first-in-human, study of BMS-986165, a selective, potent, allosteric small molecule inhibitor of tyrosine kinase 2.

Baricitinib | Upadacitinib | Pacritinib | CYT387 | AZD1480 | Fedratinib(SAR302503,TG101348) | WP1066 | CHZ868 | AT9283 | GLPG0634 | Itacitinib | cerdulatinib | LY2784544 | SB1317 | Peficitinib