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GSK4112
CAS No. 1216744-19-2
GSK4112( SR6452 | GSK-4112 | GSK 4112 | SR-6452 | SR 6452 )
Catalog No. M10812 CAS No. 1216744-19-2
A potent and selective small molecule Rev-erbα agonist with EC50 of 0.4 uM in biochemical assay.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 29 | In Stock |
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| 10MG | 44 | In Stock |
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| 25MG | 93 | In Stock |
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| 50MG | 166 | In Stock |
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| 100MG | 297 | In Stock |
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| 200MG | 427 | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameGSK4112
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NoteResearch use only, not for human use.
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Brief DescriptionA potent and selective small molecule Rev-erbα agonist with EC50 of 0.4 uM in biochemical assay.
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DescriptionA potent and selective small molecule Rev-erbα agonist with EC50 of 0.4 uM in biochemical assay; mediates the repression of Rev-erbα target gene bmal1 in liver cells, and inhibits and shifts the phase of gluconeogenesis in primary mouse hepatocytes.
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In VitroGSK4112 (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. 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.
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In VivoGSK4112 (25 mg/kg; i.p. 0.5 h before Jo2 exposure) attenuates Fas-induced hepatic damage. 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.
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SynonymsSR6452 | GSK-4112 | GSK 4112 | SR-6452 | SR 6452
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PathwayAutophagy
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TargetAutophagy
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RecptorRev-ErbBα
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Research AreaMetabolic Disease
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Indication——
Chemical Information
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CAS Number1216744-19-2
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Formula Weight396.8883
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Molecular FormulaC18H21ClN2O4S
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESO=C(OC(C)(C)C)CN(CC1=CC=C(Cl)C=C1)CC2=CC=C([N+]([O-])=O)S2
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Chemical NameGlycine, N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl]-, 1,1-dimethylethyl ester
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Grant D, et al. ACS Chem Biol. 2010 Oct 15;5(10):925-32.
2. Trump RP, et al. J Med Chem. 2013 Jun 13;56(11):4729-37.
3. Chandra V, et al. Autophagy. 2015 Nov 2;11(11):1987-1997.
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