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  3. GSK4112

GSK4112  (Synonyms: SR6452)

Cat. No.: HY-14414 Purity: ≥98.0%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 61 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 99 In-stock
Estimated Time of Arrival: December 31
50 mg USD 396 In-stock
Estimated Time of Arrival: December 31
100 mg USD 715 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK4112 purchased from MCE. 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.

    GSK4112 purchased from MCE. 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.
    • Biological Activity

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    • 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].

    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].

    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.
    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (62.99 mM; Need ultrasonic)

    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
    10 mM 0.2520 mL 1.2598 mL 2.5196 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.30 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation
    References
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    Help & FAQs
    • 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.:
    HY-14414
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