An agonist of the heme-dependent nuclear receptor REV-ERBα
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GSK4112

Item No. 11931

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl]-glycine, 1,1-dimethylethyl ester
CAS Number
1216744-19-2
Molecular Formula
C18H21ClN2O4S
Formula Weight
396.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 10 mg/mlEthanol: 1 mg/ml
λmax
219, 325 nm
SMILES
ClC(C=C1)=CC=C1CN(CC(OC(C)(C)C)=O)CC2=CC=C([N+]([O-])=O)S2
InChi Code
InChI=1S/C18H21ClN2O4S/c1-18(2,3)25-17(22)12-20(10-13-4-6-14(19)7-5-13)11-15-8-9-16(26-15)21(23)24/h4-9H,10-12H2,1-3H3
InChi Key
WYSLOKHVFKLWOU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $72

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    10 mg

    $134

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    25 mg

    $315

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    50 mg

    $556

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    Product Description

    GSK4112 is a synthetic agonist for REV-ERBα (EC50 = 0.4 μM) that was designed to mimic the action of heme.1,2 At 10 μM, GSK4112 can reset the circadian rhythm in a phasic manner by inhibiting expression of the circadian target gene bmal1 and reduce glucose output by 30% in mouse primary hepatocytes by repressing the expression of several gluconeogenic genes.1 GSK4112 has been used to investigate the function of REV-ERBα in the coordination of circadian rhythm and metabolism in rat ovaries.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Grant, D., Yin, L., Collins, J.L., et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. ACS Chem. Biol. 5(10), 925-932 (2010).

    2. Kojetin, D., Wang, Y., Kameneck, T.M., et al. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem. Biol. 6(2), 131-134 (2011).

    3. Chen, H., Chu, G., Zhao, L., et al. Rev-erbα regulates circadian rhythms and StAR expression in rat granulosa cells as identified by the agonist GSK4112. Biochem. Biophys. Res. Commun. 420(2), 374-379 (2012).