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GSK4112 (Synonyms: SR6452)

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

GSK4112 is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.

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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 432 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Customer Review

Based on 3 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.

    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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    Description

    GSK4112 is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. IC50 value: 0.4 μM (EC50) Target: Rev-erbα in vitro: GSK4112 profiled as a Rev-erb agonist in cells to inhibit expression of the circadian target gene bmal1. In addition, GSK4112 repressed the expression of gluconeogenic genes in liver cells and reduced glucose output in primary hepatocytes. Therefore, GSK4112 is useful as a chemical tool to probe the function of Rev-erb in transcriptional repression, regulation of circadian biology, and metabolic pathways. Additionally, GSK4112 may serve as a starting point for design of Rev-erb chemical probes with in vivo pharmacologicalm activity.

    Molecular Weight

    396.89

    Formula

    C₁₈H₂₁ClN₂O₄S

    CAS No.

    1216744-19-2

    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)

    H2O : < 0.1 mg/mL (insoluble)

    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 provided by MCE.
    References
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    Product Name:
    GSK4112
    Cat. No.:
    HY-14414
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