STO-609

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Chemical Structure| 52029-86-4 同义名 : -
CAS号 : 52029-86-4
货号 : A210855
分子式 : C19H10N2O3
纯度 : 98%
分子量 : 314.29
MDL号 : MFCD30685721
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(95.45 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 5 mg/mL(15.91 mM)，配合低频超声助溶
生物活性
靶点

  • CaMKKβ

    CaM-KKβ, Ki:47 nM

  • CaMKKα

    CaM-KKα, Ki:0.25 μM
描述 STO-609 suppresses the functionality of both recombinant CaM-KKα and CaM-KKβ isoforms, exhibiting Ki measurements of 80 and 15 ng/mL for each, respectively, and hampers their self-phosphorylation processes. It demonstrates a pronounced selectivity towards CaM-KK, showing negligible influence on the subsequent CaM kinases (CaM-KI and -IV), with the IC50 against CaM-KII being 10 μg/mL. Both the constitutively active and the wild-type variants of CaM-KKα are inhibited by STO-609. It also curtails the Ca2+-prompted activation of CaM-KIV within HeLa cells that have undergone transfection, operating in a concentration-dependent fashion. Moreover, at a dose of 1μg/mL, STO-609 markedly lowers the inherent activity of CaM-KK in SH-SY5Y neuroblastoma cells, achieving an inhibition rate of 80% [1].
作用机制 STO-609 permeates cells and competes with ATP to bind to the ATP-binding pocket on CaM-KK, thereby preventing them from activating the phosphorylation of CaM kinases.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.18mL

0.64mL

0.32mL

15.91mL

3.18mL

1.59mL

31.82mL

6.36mL

3.18mL
参考文献

[1]Tokumitsu H, et al. STO-609, a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase. J Biol Chem. 2002 May 3;277(18):15813-8.