CAS NO: | 52029-86-4 |
生物活性 | STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), withKivalues 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 anIC50~0.02 g/ml. | ||||||||||||||||
IC50& Target | Ki: 80 ng/mL (CaM-KKα), 15 ng/mL (CaM-KKβ)[1] | ||||||||||||||||
体外研究 (In Vitro) | STO-609 inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Kivalues 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 IC50value 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]. | ||||||||||||||||
分子量 | 314.29 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H10N2O3 | ||||||||||||||||
CAS 号 | 52029-86-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 6.25 mg/mL(19.89 mM;ultrasonic and warming and heat to 80℃) DMF : 5.56 mg/mL(17.69 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液
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