GSK4112
Based on 11 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 1216744-19-2
- Formula: C18H21ClN2O4S
- Molecular Weight:396.89
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK4112
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Pharmacol Res. 2023 Mar:189:106704. [Abstract]
- Int J Biol Macromol. 2025 Feb 15;305(Pt 1):141055. [Abstract]
- Free Radical Bio Med. 2019 Dec;145:312-320. [Abstract]
- J Orthop Translat. 2025 Jun 18:53:112-125. [Abstract]
- Cell Prolif. 2024 Jul 24:e13720. [Abstract]
- Heliyon. 2024 Nov 15;10(23):e40388. [Abstract]
- Mol Med Rep. 2025 Oct;32(4):270. [Abstract]
- Fish Physiol Biochem. 2020 Jun;46(3):891-907. [Abstract]
- Oncol Lett. 2018 Aug;16(2):1499-1506. [Abstract]
- SSRN. 2023 Oct 10.
Customer Validation & Images
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RT-PCR
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IF
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
2.3 μM
Compound: 1, GSK-4112/SR6452
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Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay
Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay
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[PMID: 22633688] |
GSK4112 (0-100 μM; 1 h) interacts with Rev-erbα with an EC50 value of 0.4 μM[1]. 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[1]. GSK4112 (10 μM; 16 h) reduces glucose output in murine hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cell line
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Concentration:10 μM
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Incubation Time:6 hours
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Result:Repressed mRNA levels of bmal1, G6 Pase, PEPCK and PGC1α.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice with Fas-induced acute hepatic damage[2]
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Dosage:25 mg/kg
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Administration:Intraperitoneal injection; 25 mg/kg; 0.5 h before Jo2 exposure
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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.
Chemical Information
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CAS No. 1216744-19-2
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Appearance Solid
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Molecular Weight 396.89
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Formula C18H21ClN2O4S
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Color White to off-white
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SMILES
ClC1=CC=C(CN(CC2=CC=C([N+]([O-])=O)S2)CC(OC(C)(C)C)=O)C=C1
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Synonyms
SR6452
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Pharmacol Res
m6A methylation-induced NR1D1 ablation disrupts the HSC circadian clock and promotes hepatic fibrosis. [Abstract]2023 Mar:189:106704. PMID: 36813093 -
Int J Biol Macromol
Dihydroartemisinin requires NR1D1 mediated Rab7 ubiquitination to regulate hepatic stellate cells lipophagy in liver fibrosis. [Abstract]2025 Feb 15;305(Pt 1):141055. PMID: 39956231 -
Free Radical Bio Med
2019 Dec;145:312-320. PMID: 31585206 -
J Orthop Translat
Inhibiting the REV-ERBα expression protects against mechanical overloading-induced cartilage clock disruption and osteoarthritis progression. [Abstract]2025 Jun 18:53:112-125. PMID: 40606845 -
Cell Prolif
Nuclear receptor Rev-erbα alleviates intervertebral disc degeneration by recruiting NCoR-HDAC3 co-repressor and inhibiting NLRP3 inflammasome. [Abstract]2024 Jul 24:e13720. PMID: 39045886 -
Heliyon
REV-ERBα inhibitor rescues MPTP/MPP+-induced ferroptosis of dopaminergic neuron through regulating FASN/SCD1 signaling pathway. [Abstract]2024 Nov 15;10(23):e40388. PMID: 39654780 -
Mol Med Rep
2025 Oct;32(4):270. PMID: 40709400 -
Fish Physiol Biochem
Nr1d1 affects autophagy in the skeletal muscles of juvenile Nile tilapia by regulating the rhythmic expression of autophagy-related genes. [Abstract]2020 Jun;46(3):891-907. PMID: 32072342
GSK4112 purchased from MedChemExpress. Usage Cited in: Fish Physiol Biochem. 2020 Jun;46(3):891-907. [Abstract]
Expression of autophagy and autophagy-related genes in tilapia skeletal muscle after GSK4112 treatment. The line represents the periodic sinusoidal function of gene expression in a circadian cycle constructed from the periodicity parameters calculated using COSINOR. The photoperiod regime is represented by the composite block. White, black, and gray, represent the light, dark, and light-dark transition phases, respectively.
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Oncol Lett
REV-ERBα reduction is associated with clinicopathological features and prognosis in human gastric cancer. [Abstract]2018 Aug;16(2):1499-1506. PMID: 30008829
GSK4112 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2018 Aug;16(2):1499-1506. [Abstract]
SGC 7901 and BGC 823 cells are treated with GSK4112 (20 and 40 μM) for 48 h. Hoechst33258 staining is performed to detect apoptotic cells that exhibit nuclear and cytoplasmic shrinkage, chromatin condensation and apoptotic bodies using UV fluorescence microscopy and are illustrated using red arrows.
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Solvent & Solubility
DMSO : 25 mg/mL (62.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.30 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Grant D, et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. ACS Chem Biol. 2010 Oct 15;5(10):925-932. [Content Brief]
[2]. Shao R, et al. REV-ERBα Agonist GSK4112 attenuates Fas-induced Acute Hepatic Damage in Mice. Int J Med Sci. 2021 Oct 25;18(16):3831-3838. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5196 mL | 12.5979 mL | 25.1959 mL | 62.9897 mL |
| 5 mM | 0.5039 mL | 2.5196 mL | 5.0392 mL | 12.5979 mL | |
| 10 mM | 0.2520 mL | 1.2598 mL | 2.5196 mL | 6.2990 mL | |
| 15 mM | 0.1680 mL | 0.8399 mL | 1.6797 mL | 4.1993 mL | |
| 20 mM | 0.1260 mL | 0.6299 mL | 1.2598 mL | 3.1495 mL | |
| 25 mM | 0.1008 mL | 0.5039 mL | 1.0078 mL | 2.5196 mL | |
| 30 mM | 0.0840 mL | 0.4199 mL | 0.8399 mL | 2.0997 mL | |
| 40 mM | 0.0630 mL | 0.3149 mL | 0.6299 mL | 1.5747 mL | |
| 50 mM | 0.0504 mL | 0.2520 mL | 0.5039 mL | 1.2598 mL | |
| 60 mM | 0.0420 mL | 0.2100 mL | 0.4199 mL | 1.0498 mL |
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