INDY

INDY is an ATP-competitive inhibitor of dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (DYRK1A, Ki = 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 beta-cells and increases insulin secretion by human islets in vitro.Formal Name: 1Z-(3-ethyl-5-hydroxy-2(3H)-benzothiazolylidene)-2-propanone. CAS Number: 1169755-45-6. Molecular Formula: C12H13NO2S. Formula Weight: 235.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml, Ethanol: slightly soluble. lambdamax: 216, 251, 365 nm. SMILES: OC1=CC=C2C(N(CC)/C(S2)=C/C(C)=O)=C1. InChi Code: InChI=1S/C12H13NO2S/c1-3-13-10-7-9(15)4-5-11(10)16-12(13)6-8(2)14/h4-7,15H,3H2,1-2H3/b12-6-. InChi Key: GCSZJMUFYOAHFY-SDQBBNPISA-N.