STO-609 acetate 

STO-609 acetate is a selective and cell-permeable inhibitor of the Ca²⁺/calmodulin-dependent protein kinase kinase (CaM-KK), with K_i values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 acetate inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC₅₀ ~0.02 g/ml.

STO-609 inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with K_i values of 80 and 15 ng/mL, respectively, and also inhibits their autophosphorylation activities. STO-609 is highly selective for CaM-KK without any significant effect on the downstream CaM kinases (CaM-KI and -IV), and the IC₅₀ value of the compound against CaM-KII is 10 μg/mL. STO-609 inhibits constitutively active CaM-KKα as well as the wild-type enzyme. In transfected HeLa cells, STO-609 suppresses the Ca²⁺-induced activation of CaM-KIV in a dose-dependent manner. STO-609 significantly reduces the endogenous activity of CaM-KK in SH-SY5Y neuroblastoma cells at a concentration of 1μg/mL (80% inhibitory rate)^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

374.35

C₂₁H₁₄N₂O₅

1173022-21-3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [2]. Kukimoto-Niino M, et al. Crystal structure of the Ca²⁺/calmodulin-dependent protein kinase kinase in complex with the inhibitor STO-609. J Biol Chem. 2011 Jun 24;286(25):22570-9.  [Content Brief]