C-DIM 8 | Nur77 Antagonist

C-DIM 8 (151358-47-3) is an antagonist of the orphan nuclear receptor Nur77 (NR4A1, TR3).¹ Induces reactive oxygen species and ER stress in pancreatic cancer cells.² C-DIM 8 mimics the effect of Nur77 knockdown in non-small-cell lung cancer A549 and H460 cells, inhibiting cell growth and inducing apoptosis which was accompanied by decreased expression of survivin and inhibition of mTORC1 signaling.³ Inhibits the expression of β1- and β3-integrin and blocks integrin-dependent breast cancer cell migration.⁴ Decreases expression of the histone methyltransferase G9A (EHMT2) in a variety of cancer cell lines.⁵

References: Citations:

1. Chintharlapalli et al. (2005), Activation of Nur77 by selected 1,1-Bis(3’-indolyl)-1-(p-substituted phenyl)methanes induces apoptosis through nuclear pathways; J. Biol. Chem., 280 24903
2. Lee et al. (2014), The orphan nuclear receptor NR4A1 (Nur77) regulates oxidative and endoplasmic reticulum stress in pancreatic cancer cells; Mol. Cancer Res., 12 527
3. Lee et al. (2012), The nuclear receptor TR3 regulates mTORC1 signaling in lung cancer cells expressing wild-type p53; Oncogene, 31 3265
4. Hedrick et al. (2016), NR4A1 Antagonists Inhibit ß1-Integrin-Dependent Breast Cancer Cell Migration; Mol. Cell. Biol., 36 1383
5. Shrestha et al. (2021), The Histone Methyltransferase Gene G9A Is Regulated by Nuclear Receptor 4A1 in Alveolar Rhabdomyosarcoma Cells; Mol. Cancer Ther. 20 612