| CAS NO: | 142439-96-1 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 419.1 |
| Cas No. | 142439-96-1 |
| Formula | C12H10Cl2N2O5PS·Na |
| Synonyms | Sp-5,6-DCI-cBIMPS |
| Solubility | ≤167mg/ml in ethanol;167mg/ml in DMSO;167mg/ml in dimethyl formamide |
| Chemical Name | 5,6-dichloro-1-[3,5-O-[(S)-mercaptophosphinylidene]-β-D-ribofuranosyl]-1H-benzimidazole, monosodium salt |
| Canonical SMILES | [S-][P@]1(OC[C@]2([H])[C@@]([C@@H](O)[C@H](N3C(C=C(Cl)C(Cl)=C4)=C4N=C3)O2)([H])O1)=O.[Na+] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Ki: 30 nM
Sp-5,6-dichloro-cBIMPS is a PKA activator.
In cell biology, protein kinase A (PKA) is a family of enzymes whose activity is dependent on cellular levels of cyclic AMP. PKA is also known as cAMP-dependent protein kinase. PKA has several functions in the cell, such as regulation of sugar, glycogen, and lipid metabolism.
In vitro: Sp-5,6-dichloro-cBIMPS was found to be both a potent and specific activator of purified cAMP-PK and of cAMP-PK in platelet membranes, whereas 8-pCPT-cAMP proved to be a potent activator of cAMP-PK and cyclic-GMP-dependent protein kinase both as purified enzymes and in platelet membranes. Moreover, it was found that Sp-5,6-dichloro-cBIMPS was not significantly hydrolysed by three types of cyclic nucleotide phosphodiesterases, whereas 8-pCPT-cAMP was hydrolysed to a significant extent by the Ca2+/calmodulin-dependent phosphodiesterase and by the cGMP-inhibited phosphodiesterase. The apparent lipophilicity of Sp-5,6-dichloro-cBIMPS was higher than that of 8-pCPT-cAMP. Extracellular application of Sp-5,6-dichloro-cBIMPS to intact human platelets could reproduce the pattern of protein phosphorylation that was induced by prostaglandin E1. Additionally, in intact platelets, Sp-5,6-dichloro-cBIMPS was also more effective than 8-pCPT-cAMP in inducing quantitative phosphorylation of vasodilator-stimulated phosphoprotein, a major substrate of cAMP-PK in platelets. As demonstrated by prostaglandin E1, pretreatment of human platelets with Sp-5,6-DCl-cBiMPS Sp-5,6-dichloro-cBIMPS was able to prevent the aggregation induced by thrombin [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Sandberg, M. ,Butt, E.,Nolte, C., et al. Characterization of Sp-5,6-dichloro-1-β-D-ribofuranosylbenzimidazole-3',5'-monophosphorothioate (Sp-5,6-DCl-cBiMPS) as a potent and specific activator of cyclic-AMP-dependent protein kinase in cell extracts and intact cells. Biochemistry Journal 279, 521-527 (1991).
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