TAS1440

TAS1440 is a highly selective, histone H3-competitive inhibitor of purified recombinant human LSD1, with an IC₅₀ of 4.8 nM and no significant activity against LSD2, MAO-A, MAO-B, or a broad panel of other epigenetic enzymes^[1].
TAS1440 (0-7500 nM; 8 days) selectively inhibits proliferation of SCLC-A cell lines, with the greatest potency in NCI-H1417, NCI-H510A, NCI-H146, and COR-L51 cells, and exhibits stronger antiproliferative activity than covalent LSD1 inhibitors in these sensitive models^[1].
TAS1440 (300 nM; 1-7 days) induces transcriptional reprogramming in SCLC cell lines, activating tumor-suppressive TGF-β and NOTCH pathways and suppressing neuroendocrine gene expression, with the most pronounced changes in TAS1440-sensitive SCLC-A cell lines^[1].
TAS1440 (300 nM; 30 min-5 days) activates TGF-β and NOTCH signaling in SCLC-A cell lines by inducing SMAD2 phosphorylation, NOTCH1 upregulation, and nuclear accumulation of active pathway components, while also disrupting INSM1-LSD1 and SMAD2-LSD1 protein complexes more effectively than covalent LSD1 inhibitors^[1].
TAS1440 (300 nM; 5 days) induces global epigenetic reprogramming in SCLC-A cell lines, increasing active histone marks (H3K4me1, H3K4me2, H3K27ac) at TSSs and promoting INSM1 and SMAD2 binding to tumor-suppressive NOTCH and TGF-β pathway gene promoters^[1].
TAS1440 (100-3,000 nM; 7 days) antiproliferative and transcriptional effects in SCLC-A cell lines depend on LSD1 expression and catalytic activity, while its ability to disrupt INSM1/SMAD2-LSD1 complexes is independent of LSD1 catalytic function^[1].
TAS1440 (300 nM; 2 h-10 days) requires INSM1 for its antiproliferative effects, transcriptional reprogramming, and activation of TGF-β/NOTCH signaling in SCLC-A cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.