化学性质:
规格 | 500ug 1mg 5mg |
CAS | 634207-53-7 |
别名 | N/A |
化学名 | sodium (4aR,6R,7R,7aR)-6-(6-amino-8-((4-chlorophenyl)thio)-9H-purin-9-yl)-7-methoxytetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-2-olate 2-oxide |
分子式 | C17H16ClN5O6PS.Na |
分子量 | 507.82 |
溶解度 | 0.5mg/mL in ethanol, 25mg/mL in DMSO, 30mg/mL in DMF |
储存条件 | Desiccate at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
8-CPT-2Me-cAMP, sodium salt is a selective agonist of EPAC [1].
Cyclic AMP guanine nucleotide exchange factors (EPACs) are intracellular sensors for cAMP and function as nucleotide exchange factors for the Ras GTPase homologues Rap1 and Rap2 [1].
8-CPT-2Me-cAMP, sodium salt is a selective EPAC agonist. 8-CPT-2Me-cAMP increased Rap1 activation by EPAC1. Meantime, light chain 2 (LC2) of the microtubule-associated protein MAP1A increased this response. In LC2- and EPAC1-transfected cells, 8-CPT-2Me-cAMP increased cell adhesion to laminin [1]. In Jurkat Tcells, 8-CPT-2Me-cAMP (100 μM) activated Rap1, which was not affected by H-89, a PKA inhibitor [2]. In 1-LN prostate cancer cells, 8-CPT-2Me-cAMP increased Epac1, p-AktS473 and p-AktT308 in a dose-dependent way. 8-CPT-2Me-cAMP increased p-AktS473 and AktS473 kinase activity by two-three fold. Also, 8-CPT-2Me-cAMP activated mTORC1 and mTORC2 [3].
In human prostate cancer cells, 8-CPT-2Me-cAMP increased the levels of p-cPLA2S505, COX-2 and PGE2. However, COX-2, EP4 or mTOR inhibitors inhibited this effect and reduced protein and DNA synthesis induced by Epac1. These results suggested Epac1 was a pro-inflammatory modulator and promoted cell proliferation [4].
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