GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 value of 0.4 μM. GSK4112 can be used as a chemical tool to probe the function of Rev-erbα in transcriptional repression, regulation of circadian biology, and metabolic pathways.
性状
Solid
体外研究(In Vitro)
GSK4112 (0-100 μM; 1 h) interacts with Rev-erbα with an EC50 value of 0.4 μM.
GSK4112 (10 μM; 6 h) represses expression of bmal1 and the target genes associated with the pathway of gluconeogenesis, recruits HDAC3 and modulates the effect of Rev-erbα on oscillation of hepatic gene expression.
GSK4112 (10 μM; 16 h) reduces glucose output in murine hepatocytes.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
RT-PCR
Cell Line:
HepG2 cell line
Concentration:
10 μM
Incubation Time:
6 hours
Result:
Repressed mRNA levels of bmal1, G6 Pase, PEPCK and PGC1α.
体内研究(In Vivo)
GSK4112 (25 mg/kg; i.p. 0.5 h before Jo2 exposure) attenuates Fas-induced hepatic damage.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male C57BL/6 mice with Fas-induced acute hepatic damage
Dosage:
25 mg/kg
Administration:
Intraperitoneal injection; 25 mg/kg; 0.5 h before Jo2 exposure
Result:
Obviously ameliorated the degree of liver damage, suppressed Jo2-induced ALT and AST increasing, improved the survival rate of mice and suppressed Fas-induced hepatocyte apoptosis.