SR 8278

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Description: Rev-Erbα antagonist
Chemical Name: 1,2,3,4-Tetrahydro-2-[[5-(methylthio)-2-thienyl]carbonyl]-3-isoquinolinecarboxylic acid ethyl ester
Purity: ≥99% (HPLC)
Citations (4)

Biological Activity for SR 8278

SR 8278 is a Rev-Erbα antagonist; inhibits Rev-Erbα transcriptional repression (EC50 = 0.47 μM). Blocks activity of Rev-Erbα agonist GSK 4112 (Cat. No. 3663) in HEK293 cells. Increases expression of glucose-regulating genes, G6Pase and PEPCK in HepG2 cells.

Compound Libraries for SR 8278

SR 8278 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SR 8278

M. Wt 361.48
Formula C18H19NO3S2
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1254944-66-5
PubChem ID 53393127
Smiles CCOC(=O)C1CC2=CC=CC=C2CN1C(=O)C1=CC=C(SC)S1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for SR 8278

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 36.15 100
ethanol 18.07 50

Preparing Stock Solutions for SR 8278

The following data is based on the product molecular weight 361.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.77 mL 13.83 mL 27.66 mL
5 mM 0.55 mL 2.77 mL 5.53 mL
10 mM 0.28 mL 1.38 mL 2.77 mL
50 mM 0.06 mL 0.28 mL 0.55 mL

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Product Datasheets for SR 8278

Certificate of Analysis / Product Datasheet
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References for SR 8278

References are publications that support the biological activity of the product.

Kojetin et al (2011) Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem. Biol. 6 131 PMID: 21043485

If you know of a relevant reference for SR 8278, please let us know.

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Keywords: SR 8278, SR 8278 supplier, SR8278, REV-ERB, heme, nuclear, receptors, antagonists, inhibits, glucose, regulation, circadian, Rev-Erb, Receptors, 4463, Tocris Bioscience

4 Citations for SR 8278

Citations are publications that use Tocris products. Selected citations for SR 8278 include:

Ning et al (2023) Nuclear receptor modulators inhibit osteosarcoma cell proliferation and tumour growth by regulating the mTOR signaling pathway. Cell Death Dis 14 51 PMID: 36681687

Parker et al (2017) Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell 168 527 PMID: 28111073

Hyun Ok et al (2022) Sinapic Acid Ameliorates REV-ERB α Modulated Mitochondrial Fission against MPTP-Induced Parkinson's Disease Model. Biomol Ther (Seoul) 30 409-417 PMID: 35611585

Hanne M et al (2022) Co-alterations of circadian clock gene transcripts in human placenta in preeclampsia. Sci Rep 12 17856 PMID: 36284122

Do you know of a great paper that uses SR 8278 from Tocris? Please let us know.

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