1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Apoptosis
  2. REV-ERB Apoptosis
  3. GSK4112

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.

GSK4112 Chemical Structure

GSK4112 Chemical Structure

CAS No. : 1216744-19-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 99 In-stock
50 mg USD 396 In-stock
100 mg USD 715 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1].

    In Vitro

    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.

    RT-PCR[1]

    Cell Line: HepG2 cell line
    Concentration: 10 μM
    Incubation Time: 6 hours
    Result: Repressed mRNA levels of bmal1, G6 Pase, PEPCK and PGC1α.
    In Vivo

    GSK4112 (25 mg/kg; i.p. 0.5 h before Jo2 exposure) attenuates Fas-induced hepatic damage[2].

    MedChemExpress (MCE) 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[2]
    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.
    Molecular Weight

    396.89

    Formula

    C18H21ClN2O4S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=CC=C(CN(CC2=CC=C([N+]([O-])=O)S2)CC(OC(C)(C)C)=O)C=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5196 mL 12.5979 mL 25.1959 mL
    5 mM 0.5039 mL 2.5196 mL 5.0392 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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
    References

    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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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    GSK4112
    Cat. No.:
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