| CAS NO: | 1173022-21-3 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 374.35 |
| Cas No. | 1173022-21-3 |
| Formula | C19H10N2O3·C2H4O2 |
| Solubility | Soluble in DMSO |
| Chemical Name | 7-oxo-7H-benzo[de]benzo[4,5]imidazo[2,1-a]isoquinoline-3-carboxylic acid compound with acetic acid (1:1) |
| Canonical SMILES | O=C1N2C(C3=CC=C(C(O)=O)C4=CC=CC1=C34)=NC5=CC=CC=C25.OC(C)=O |
| 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。 |
STO-609 acetate is a specific inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), withKi values of 80 and 15 ng/ml against CaM-KKα and CaM-KKβ isoforms, respectively [1].
CaM-KKα and CaM-KKβ, highly expressed in the brain with the α isoform also expressed in various peripheral tissues such as thymus and spleen in mammals, belongs to Ca2+/calmodulin-dependent protein kinases, which are involved in many cellular responses mediated by an increase in the concentration of intracellular calcium [1].
STO-609 exhibited high selectivity for CaM-KK without significantly affecting the downstream CaM kinases (CaM-KI and -IV), and the IC50 value of STO-609 against CaM-KII was ~ 10 μg/ml. In transfected HeLa cells, STO-609 (0.01 ~ 10 μg/ml) suppressed the Ca2+-induced activation of CaM-KIV in a dose-dependent manner. In addition, in SH-SY5Y neuroblastoma cells, STO-609 at a concentration of 1 μg/ml significantly reduced the endogenous activity of CaM-KK [1].
In ovariectomized mice,in vivo administration of STO-609 (10 μM, 200 μl per mouse, i.p., thrice a week) resulted in increased osteoblasts and diminished osteoclasts, significantly protect adult mice from ovariectomy-induced osteoporosis [2].
References:
[1]. Tokumitsu H, Inuzuka H, Ishikawa Y, et al. STO-609, a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase. Journal of Biological Chemistry, 2002, 277(18): 15813-15818.
[2]. Cary R L, Waddell S, Racioppi L, et al. Inhibition of Ca2+/calmodulin-dependent protein kinase kinase 2 stimulates osteoblast formation and inhibits osteoclast differentiation. Journal of Bone and Mineral Research, 2013, 28(7): 1599-1610.
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