STO-609 - CaMK 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESTO-609Cat. No.: HY-19805CAS No.: 52029-86-4分式: CHNO分量: 314.29作靶点: CaMK; AMPK作通路: Neuronal Signaling; Epigenetics; PI3K/Akt/mTOR储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 5.6 mg/mL (17

2、.82 mM; Need ultrasonic and warming)H2O : 0.1 mg/mL (insoluble)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1818 mL 15.9089 mL 31.8177 mL5 mM 0.6364 mL 3.1818 mL 6.3635 mL10 mM 0.3182 mL 1.5909 mL 3.1818 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 STO-609是选择性和细胞可渗透的

3、CaM-KK 抑制剂，对重 组 CaM-KK 和 CaM-KK 的Ki值分别为 80 和 15ng/mL。STO-609 抑制 Hela 细胞溶解物中的 AMP 活化蛋激酶激酶 (AMPKK) 活性，IC50 值为 0.02 g/ml。IC50 & Target Ki: 80 ng/mL (CaM-KK), 15 ng/mL (CaM-KK) 1体外研究STO-609 inhibits the activities of recombinant CaM-KK and CaM-KK isoforms, with Ki values of 80 and 151/2 Master of Small

4、Molecules 您边的抑制剂师www.MedChemEng/mL, respectively, and also inhibits their autophosphorylation activities. STO-609 is highly selective forCaM-KK without any significant effect on the downstream CaM kinases (CaM-KI and -IV), and the IC50 valueof the compound against CaM-KII is 10 g/mL. STO-609 inhibit

5、s constitutively active CaM-KK as well as thewild-type enzyme. In transfected HeLa cells, STO-609 suppresses the Ca2+-induced activation of CaM-KIVin a dose-dependent manner. STO-609 significantly reduces the endogenous activity of CaM-KK in SH-SY5Yneuroblastoma cells at a concentration of 1g/mL (80

6、% inhibitory rate) 1.PROTOCOLKinase Assay 2 CaM-KI (2.5 g/mL), CaM-KII (0.75 g/mL), CaM-KIV (9 g/mL), and mLCK (0.6 g/mL) are incubated with40 M syntide-2 or 50 M mLC peptide (for mLCK) at 30 C for 5 min in a solution (25 L) containing 50 mMHEPES (pH 7.5), 10 mM Mg(Ac)2, 1 mM DTT, 50 M -32PATP (4500

7、 cpm/pmol) with variousconcentrations of STO-609 (010 g/mL)in Me2SO at a final concentration of 4%) in the presence of 1 mMCaCl2, 2 M CaM. Protein kinase activity is measured by the phosphocellulose filter method. Specificactivities of CaM-KI, CaM-KII, CaM-KIV, and mLCK in the absence of STO-609 are

8、 calculated 1. STO-609is bound in the ATP-binding pocket of the CaMKK KD. The inhibition mechanism of STO-609 is ATP-competitive 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 EBioMedicine. 2019 Jun.See more customer validations on HYPERL

9、INK / www.MedChemEREFERENCES1. Tokumitsu H, et al. STO-609, a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase. J Biol Chem. 2002 May3;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.McePdfHeightCaution: Product has not been fully validated for me