The present invention provides diacylhydrazine ligands and chiraldiacylhydrazine ligands for use with ecdysonereceptor-based inducible gene expression systems. Thus, the present inventionis useful for applications such as gene therapy, largescale production of proteins and antibodies, cell-based screening assays,functional genomics, proteomics, metabolomics, andregulation of traits in transgenic organisms, where control of gene expressionlevels is desirable. An advantage of the present inventionis that it provides a means to regulate gene expression and to tailorexpression levels to suit the user's requirements.