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CAS No.: 1216744-19-2

GSK4112 Catalog No. CSN17576

Synonyms: SR6452

GSK4112 is an agonist of Rev-erbα with EC50 of 0.4 μM and it can be designed to mimic the action of heme.

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技术信息

生物活性

描述Rev-erbα (NR1D1) and Rev-erbβ (NR1D2) are heme sensors and atypical members of the nuclear receptor superfamily. Many of the Rev-erbα target genes play important roles in regulation of metabolic processes. In addition, Rev-erbα regulates the expression of proteins that comprise the core circadian clock in mammals. GSK4112 is a functional Rev-erbα agonist in liver cells to inhibit expression of the circadian target gene bmal1 with EC₅₀ value of 0.4 μM. In the presence of 0.5 μM hemin, recruitment of the NCoR1 ID1 peptide was reduced. In contrast, 10 μM GSK4112 increased the interaction of the receptor with the peptide above the basal level, consistent with the data from the chemical array screening. Following saturation of the receptor with hemin, the tertiary amine GSK4112 was able to reverse the suppression of the FRET (fluorescence resonance energy transfer) signal. The competitive actions of hemin and GSK4112 in the FRET assay strongly suggested that their binding as ligands to Rev-erbα was mutually exclusive. In the presence of 10 μM GSK4112, a statistically significant repression of bmal1 expression was observed. The mRNA for g6pc, pepck, and pgc1a were all repressed by 10 μM GSK4112 in HepG2 cells. A ChIP experiment in the same cells showed that a doubling of HDAC3 recruitment was observed in the presence of GSK4112 demonstrating that GSK4112 performed as a Rev-erbα agonist in cells to promote the formation of a transcriptional repressor complex with HDAC3 and repress target genes associated with the pathway of gluconeogenesis^[3].
参考文献

[1] Kojetin D, Wang Y, et al. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem Biol. 2011 Feb 18;6(2):131-4.
[2] Grant D, Yin L, et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. ACS Chem Biol. 2010 Oct 15;5(10):925-32.
[3] Grant D, Yin L, Collins JL, et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. ACS Chem Biol. 2010;5(10):925‐932

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5196 mL
- 12.5980 mL
- 25.1960 mL
- 5 mM
- 0.5039 mL
- 2.5196 mL
- 5.0392 mL
- 10 mM
- 0.2520 mL
- 1.2598 mL
- 2.5196 mL

技术信息

CAS号

1216744-19-2

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H21ClN2O4S

运输

蓝冰

分子量

396.89

别名

SR6452

溶解度

DMSO	133.0 mg/mL (335.1 mM)
Water	insoluble

动物实验配方

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