1169755-45-6

INDY is an ATP-competitive inhibitor of dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (DYRK1A; K_i = 180 nM; IC₅₀ = 240 nM). 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.

INDY is a dual-specificity tyrosine-(Y)-phosphorylation-regulated kinase 1A/B (DYRK1A/B) inhibitor (1,2).

DYRK1A; DYRK1B

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[1] YASUSHI OGAWA. Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A[J]. Nature Communications, 2010, 1 1: 1-9. DOI: 10.1038/ncomms1090
[2] PENG WANG. A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication[J]. Nature Medicine, 2015, 21 4: 383-388. DOI: 10.1038/nm.3820