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).
Biochem/physiol Actions
Cell permeable: yes
Primary Target RORα/γ
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Wang, Y., et al. 2010. ACS Chem Biol.5, 1029. Wang, Y., et al. 2012. PLoS One.7, e34921.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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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
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