STO-609 是一种特异性和细胞渗透性的 Ca2+/钙调蛋白依赖性蛋白激酶激酶抑制剂,用于重组 CaM-KKα 和 CaM-KKβ,Ki值分别为 80 和 15 ng/mL。它抑制 Hela 细胞溶解物中的 AMP 活化蛋白激酶激酶活性,IC50值约为 0.02 g/ml。
产品描述
STO-609 is a specific and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK) for recombinant CaM-KKα/KKβ (Ki: 80/15 ng/mL).
体外活性
STO-609 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 dose-dependently suppresses the Ca2+-induced activation of CaM-KIV. STO-609 (1μg/mL) significantly reduces the endogenous activity of CaM-KK in SH-SY5Y neuroblastoma cells (80%).
Cas No.
52029-86-4
分子式
C19H10N2O3
分子量
314.3
别名
STO 609
储存和溶解度
DMSO:5.6 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years