INDY

INDY is an ATP-competitive inhibitor of dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (DYRK1A; K_i = 180 nM; IC₅₀ = 240 nM).¹ It is selective for DYRK1A over monoamine oxidase (MAO) A and B at concentrations up to 100 μM. INDY inhibits DYRK1A phosphorylation of tau in COS-7 cells expressing EGFP-DYRK1A and EGFP-tau in a concentration-dependent manner. It also restores signaling through nuclear factory of activated T cells (NFAT) and NFAT-dependent transcription in HEK293 cells overexpressing DYRK1A. In vivo, INDY reverses developmental deformities induced by DYRK1A overexpression in X. laevis embryos. INDY also induces proliferation of human and rat β-cells and increases insulin secretion by human islets in vitro.²

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1. Ogawa, Y., Nonaka, Y., Goto, T., et al. Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A. Nat. Commun. 1:86, (2010).

2. Wang, P., Alvarez-Perez, J.C., Felsenfeld, D.P., et al. A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication. Nat. Med. 21(4), 383-388 (2015).