Cayman TCS 21311

TCS 21311 is an inhibitor of JAK3 (IC₅₀ = 8 nM in an enzyme assay).¹ It is selective for JAK3 over JAK1, JAK2, and tyrosine kinase 2 (TYK2; IC₅₀s = 1,017, 2,550, and 8,055 nM, respectively) but does inhibit glycogen synthase kinase 3β (GSK-3β), PKCα, and PKCθ (IC₅₀s = 13, 68, and 3 nM, respectively). TCS 21311 inhibits cytokine-induced STAT5 phosphorylation, a JAK3-dependent activity, in CTLL and M-07 cells (IC₅₀s = 1,294 and 525 nM, respectively) and inhibits TCR/CD28-mediated T cell activation, a PCK-dependent activity, in Jurkat cells (IC₅₀ = 689 nM). It also increases proliferation of mouse embryonic nephron progenitor cells (NPCs) and NPCs derived from human induced pluripotent stem cells (iPSCs) in the absence of bone morphogenic protein 7 (BMP7) when used at a concentration of 0.3 µM.²

WARNING This product is not for human or veterinary use.