A cell-permeable diaryl amide derived from T1317 (a known LXR agonist and retinoic acid receptor (ROR) inverse agonist) that acts as a highly selective agonist of RORα/γ and does not exhibit affinity for FXR, LXRa and LXRb. Shown to stabilize p53 in cancer cells and increase the expression of p21 and PUMA. Induces apoptosis in hepatocellular carcinoma (HepG2) cells in a RORα and p53-dependent process. Also reported to increase the expression of Sox4 and REV-ERBα in HepG2 cells. Exhibits suitable pharmacokinetic properties with sustained plasma levels even after 8 hours following a single i.p. injection. Exposure to SR1078 Induces expression of glucose-6-phosphatase and fibroblast growth factor 21 in murine models (10 mg/kg/i.p).
10 mg in Glass bottle
Packaged under inert gas
Cell permeable: yes
Toxicity: Standard Handling (A)
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Wang, Y., et al. 2010. ACS Chem Biol.5, 1029.
Wang, Y., et al. 2012. PLoS One.7, e34921.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany