STO-609 acetate

Description: STO-609 acetate is a novel, potent, specific and cell-permeable inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKalpha and CaM-KKbeta isoforms with Ki values of 80 and 15 ng/ml, respectively, it also inhibits their autophosphorylation activities. STO-609 inhibits the activities of recombinant CaM-KK alpha and CaM-KK beta isoforms, with K(i) values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. Comparison of the inhibitory potency of the compound against various protein kinases revealed that STO-609 is highly selective for CaM-KK without any significant effect on the downstream CaM kinases (CaM-KI and -IV), and the IC(50) value of the compound against CaM-KII is approximately 10 microg/ml. STO-609 inhibits constitutively active CaM-KK alpha (glutathione S-transferase (GST)-CaM-KK-(84-434)) as well as the wild-type enzyme.

References: J Biol Chem. 2002 May 3; 277(18):15813-8; J Bone Miner Res. 2013 Jul; 28(7):1599-610.

Related CAS#: 52029-86-4 (free base)