產(chǎn)品目錄

規(guī)格	10mM*1mL in DMSO 5mg 10mg 25mg 50mg 100mg
CAS	52029-86-4
別名	N/A
化學(xué)名	N/A
分子式	C19H10N2O3
分子量	314.29
溶解度	DMSO: 5.6 mg/mL (17.82 mM and warming); H2O: < 0.1 mg/mL (insoluble)
儲存條件	Store 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 All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml. Ki: 80 ng/mL (CaM-KKα), 15 ng/mL (CaM-KKβ)[1]

STO-609 inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki 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].

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

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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