NSD2/H3K36me2 modulator-1

NSD2/H3K36me2 modulator-1 is an orally active NSD2/H3K36me2 modulator. NSD2/H3K36me2 modulator-1 competitively binds to the SAM pocket of NSD2, potently inhibits NSD2 expression and suppresses H3K36me2 methylation. NSD2/H3K36me2 modulator-1 reverses epithelial-mesenchymal transition (EMT), inhibits cell migration, and induces G0/G1 phase arrest and apoptosis. NSD2/H3K36me2 modulator-1 induces decreased Mitochondrial membrane potential (MMP) and subsequent Reactive oxygen species (ROS) generation. NSD2/H3K36me2 modulator-1 can be used to research the NSD2-targeting epigenetic anticancer strategies for hepatocellular carcinoma (HCC) [1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Histone Methyltransferase; Reactive Oxygen Species (ROS)

Related Pathways

Apoptosis; Epigenetics; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

Field of Research

Cancer

Smiles

ClC1=CC(N(CC(N[C@@H]2C(C)(C)[C@@](CC[C@]3(C)[C@@]4([H])C[C@@H](O)[C@@]5([H])[C@@]3(C)CC[C@]5([H])[C@@]6(C)CCCC(C)(C)O6)(C)[C@]4(C)CC2)=O)C(C7=O)=O)=C7C=C1

Molecular Formula

C41H59ClN2O5

Molecular Weight

695.37

References & Citations

[1]Lv L, et al. Synthesis of amide-linked panaxadiol-indolinedione derivatives: A novel NSD2/H3K36me2 epigenetic modulator with significant antitumor efficacy. Eur J Med Chem. 2026 Jan 15;302 (Pt 1) :118275.