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

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1. Thoma, G., Nuninger, F., Falchetto, R., et al. Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family. J. Med. Chem. 54(1), 284-288 (2011).

2. Tsujimoto, H., Araoka, T., Nishi, Y., et al. Small molecule TCS21311 can replace BMP7 and facilitate cell proliferation in in vitro expansion culture of nephron progenitor cells. Biochem. Biophys. Res. Commun. (2020).