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101574-65-6

101574-65-6 structure
101574-65-6 structure
  • Name: GSK 4716
  • Chemical Name: 4-hydroxy-N-[(E)-(4-propan-2-ylphenyl)methylideneamino]benzamide
  • CAS Number: 101574-65-6
  • Molecular Formula: C17H18N2O2
  • Molecular Weight: 282.33700
  • Catalog: Research Areas Cancer
  • Create Date: 2018-12-20 13:23:19
  • Modify Date: 2024-01-05 18:17:49
  • GSK-4716 is a selective ERRβ/γ agonist.

Name 4-hydroxy-N-[(E)-(4-propan-2-ylphenyl)methylideneamino]benzamide
Synonyms GSK 4716
2gpp
QCR-163
GSK-4716
Description GSK-4716 is a selective ERRβ/γ agonist.
Related Catalog
Target

ERRβ/γ[1]

In Vitro Treatment of differentiated C2C12 cells with the ERRβ/γ agonist (relative to vehicle) over a 2 to 4 h time period reveals a reproducible and robust increase in the immunoreactivity of the GRα-D isoform. It is observed that MAO-A mRNA expression is significantly increased by treatment with the ERRβ/γ agonist, GSK4716. Furthermore, it is observed that GSK4716 induces the expression of the mRNAs encoding peroxisome proliferator-activated receptor-γcoactivator 1α (PGC-1α) and PGC-1β (key regulator of many metabolic genes) identified as direct coactivators for the ERR family. GSK4716 induces the expression of PGC-1 and genes involved in fatty acid oxidation in concordance with the characterized role of ERRγ in cardiac metabolism[1]. Treatment of primary mouse myotubes with GSK4716, an ERRβ/γ agonist, results in a concerted increase in the expression levels of Ppargc1a, Ppargc1b, and the Esrr genes. Furthermore,Cpt1b, Atp5b, and Idh3, genes in key mitochondrial pathways, are also induced by GSK4716. Additionally, GSK4716 increases citrate synthase activity and cytochrome c protein levels[2].
Cell Assay Proliferating mouse C2C12 myoblast are cultured and maintained in DMEM supplemented with 10% heat-inactivated serum supreme. Differentiation of myoblasts into post-mitotic, multi-nucleated myotubes are induced by mitogen withdrawal (DMEM supplemented with 2% horse serum) for 4 days. C2C12 myotubes are treated with either vehicle (DMSO) or ERRβ/γ agonist GSK4716 for 1 day and RNA collected and processed[1].
References

[1]. Wang SC, et al. An ERRbeta/gamma agonist modulates GRalpha expression, and glucocorticoid responsive gene expression in skeletal muscle cells. Mol Cell Endocrinol. 2010 Feb 5;315(1-2):146-52.

[2]. Rangwala SM, et al. Estrogen-related receptor gamma is a key regulator of muscle mitochondrial activity and oxidative capacity. J Biol Chem. 2010 Jul 16;285(29):22619-29.

Density 1.12g/cm3
Molecular Formula C17H18N2O2
Molecular Weight 282.33700
Exact Mass 282.13700
PSA 61.69000
LogP 3.67040
Index of Refraction 1.576
Storage condition 2-8℃
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H317-H410
Precautionary Statements P273-P280-P501
RIDADR UN 3077 9 / PGIII