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A cell-permeable REV-ERB antagonist that inhibits REV-ERBα transcriptional repression activity (EC50 = 0.47 µM) in a REV-ERB target gene assay. It is also shown to block the ability of GSK4112 to enhance REV-ERB-&alpha-dependent repression (EC50 = 0.35 µM) in a co-transfection assay. Treatment of HepG2 cells with SR8278 at 10 µM results in a significant increase in the expression of either G6Pase and PEPCK mRNA expression, consistent with its antagonistic role against endogenous heme.
REV-ERBα Antagonist, SR8278 - CAS 101910-24-1 - Calbiochem 分析证书
标题
批号
554718
参考
参考信息概述
Kojetin, D., et al. 2010, Chem Bio in press
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
25-February-2020 JSW
Synonyms
SR8278
SR 8278
Description
A cell-permeable REV-ERB antagonist that inhibits REV-ERBα transcriptional repression activity (EC50 = 0.47 µM) in a REV-ERB target gene assay. It is also shown to block the ability of GSK4112 to enhance REV-ERB-&alpha-dependent repression (EC50 = 0.35 µM) in a co-transfection assay. Treatment of HepG2 cells with SR8278 at 10 µM results in a significant increase in the expression of either G6Pase and PEPCK mRNA expression, consistent with its antagonistic role against endogenous heme.
Form
White to yellow-brown solid or gum
Intert gas (Yes/No)
Packaged under inert gas
CAS number
101910-24-1
Chemical formula
C₁₈H₁₉NO₃S₂
Structure formula
Purity
>95% by HPLC
Solubility
DMSO (25 mg/ml)
Storage
Protect from light
-20°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to months at -20°C.