8-Bromoadenosine 3',5'-cyclic monophosphate sodium salt 生物活性
描述
The cAMP/PKA signaling pathway regulates a wide range of cellular processes. 8-Bromo-cAMP is an activator of PKA with a Ka value of 0.05 μM[3]. Treatment of 0.1 and 0.5 mM 8-Bromo-cAMP significantly increased the number of NANOG positive ES cell-like colonies in human fibroblast cells compared to the negative control. The combination of 0.1 mM 8-Bromo-cAMP and 0.5 mM VPA inhibited the proliferation rates at day 3, 4 and 5 in HFF1 cells. The same co-treatment of 8-Bromo-cAMP and VPA in HFF1 cells also induced the upregulation of cytokine-related and inflammatory pathways at day 1, and down-regulated the p53, cell cycle and RB pathways[4]. In BEAS-2B cells, pretreatment of 100 μM 8-Bromo-cAMP for one hour significantly reduced HDE-induced release of IL-6 and IL-8 compared to cells only received 24-h treatment of 5% HDE with presence of 100 μM 8-Br-cAMP. Also in BEAS-2B cells, HDE (5%) significantly promoted the maximal PKC-ε activity at 6h, but pretreatment with 100 μM 8-Bromo-cAMP for hour blocked HDE-stimulated PKC-ε. The 1-h treatment with 8-Bromo-cAMP (0.1–10 μM) also significantly increased PKA activity in a dose-dependent manner[5]. In ddY mice, pretreatment with 8-Br-cAMP (i.p., 10 mg/kg) prior to LPS injection significantly inhibited LPS-induced dye leakage in the skin and the increase of serum TNF-α level[6].
作用机制
8-Bromo-cAMP is a brominated derivative of cAMP that functions as a cell-permeable analog of cAMP to activate cAMP-dependent protein kinase (PKA)[5].
8-Bromoadenosine 3',5'-cyclic monophosphate sodium salt 细胞实验
8-Br-cAMP upregulated vimentin and CD13 and downregulated CK and CD9, promoting the differentiation of WJ-MSCs into ESC-like cells.
Stem Cell Res Ther. 2017 Nov 2;8(1):246.
Human endometrial stromal (hES) cells
0.5 mM
2-4 days
Investigate the differential regulation of mTORC1 and mTORC2 during 8-Br-cAMP-induced decidualization. Results showed increased mTORC1 activity and decreased mTORC2 activity, leading to reduced Akt phosphorylation and activation of FOXO1, promoting the expression of decidualization markers PRL and IGFBP1.
Exp Mol Med. 2018 Oct 30;50(10):1-11.
Human esophageal cancer cell line Eca-109
20 µM
24 hours
To investigate the effects of 8-Br-cAMP on differentiation and apoptosis of Eca-109 cells. Results showed that the signals of wt p53 and iNOS were markedly stronger, while the signals of c-myc and EGFR were obviously weaker in E1 group (24-hour treatment).
World J Gastroenterol. 2005 Nov 7;11(41):6538-42.
JEG-3 cells
250 µM
36 hours
Induced trophoblastic differentiation and upregulated LGALS16 and CGB3/5 gene expression
Biomolecules. 2021 Dec 20;11(12):1909.
Human esophageal cancer cell line Eca-109
20 µM
48 hours
To investigate the effects of 8-Br-cAMP on differentiation and apoptosis of Eca-109 cells. Results showed that the signals of wt p53, iNOS, p38 kinase, and caspase-3 were significantly stronger, whereas the signals of bcl-2, c-myc, and Fas/FasL were markedly weaker in E2 group (48-hour treatment).
World J Gastroenterol. 2005 Nov 7;11(41):6538-42.
BeWo cells
250 µM
48 hours
Induced trophoblastic differentiation and upregulated LGALS16 and CGB3/5 gene expression
Biomolecules. 2021 Dec 20;11(12):1909.
Rat heart cells
10 µM
5 minutes
To evaluate the protective effects of 8-Br on the heart, results showed that 8-Br significantly reduced ventricular arrhythmias, improved hemodynamic function, and reduced infarct size
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