KG-501

KG-501 (CAS No.: 18228-17-6) is a small-molecule inhibitor belonging to the class of naphthalene-2-carboxanilides, a group of compounds characterized by an aniline-substituted carboxamide framework, and is widely used in biomedical research as a modulator of transcriptional signaling. It functions primarily as an inhibitor of cAMP response element-binding protein (CREB)-mediated transcription by disrupting the protein–protein interaction between CREB and the KIX domain of CREB-binding protein (CBP), thereby interfering with transcriptional coactivator recruitment and downstream gene expression. In addition to its effects on CREB signaling, KG-501 has been shown to inhibit interactions involving the transcription factor Myb with KIX domains of CBP and p300, highlighting its broader impact on transcriptional regulatory networks. The compound exhibits biological activity in the low micromolar range, with reported inhibition of CREB-dependent transcription and cancer cell proliferation, as well as modulation of gene expression and induction of differentiation in leukemia cell models. These properties make KG-501 a valuable tool for investigating transcription factor–coactivator interactions, epigenetic regulation, and oncogenic signaling pathways, and it is commonly applied in cell-based assays and early-stage drug discovery efforts where experimental concentrations are adjusted according to specific study designs.