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).
生物化学的/生理学的作用
Cell permeable: yes
Primary Target RORα/γ
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
再構成
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
その他情報
Wang, Y., et al. 2010. ACS Chem Biol.5, 1029. Wang, Y., et al. 2012. PLoS One.7, e34921.
法的情報
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
MYCN activation is a hallmark of advanced neuroblastoma (NB) and a known master regulator of metabolic reprogramming, favoring NB adaptation to its microenvironment. We found that the expression of the main regulators of the molecular clock loops is profoundly disrupted