The Ca2+/calmodulin-dependent kinase (CaMK) family has been recognized as a key mediator in living organisms and various biological processes.
Calcium/calmodulin kinase II (CaMK II) is a multifunctional cytoplasmic calcium and calmodulin-dependent protein kinase that phosphorylates and alters the function of a variety of substrates. The CaMK II pathway has been found to regulate the RANKL-induced osteoclast formation via the cAMP-response element binding protein (CREB) pathway.
Among many signaling pathways of proliferation, intracellular calciumol/L has been extensively demonstrated to be very important. In cytoplasm, calciumol/L binds to calmodulin, and then activates the Ca2+/calmodulin (CaM) dependent kinases (CaMKs) which are a family of structurally related serine/threonine protein kinases including CaMKI-IV. CaMKII, a multi functional protein kinase, is ubiquitously involved in many physiological processes including control of cell cycle, apoptosis, gene expression, and neurotransmission.
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STO-609 is a selective and cell-permeable inhibitor of CaM-KK; inhibits recombinant CaM-KKα and CaM-KKβ with Ki of 80 and 15 ng/ml; without any significant effect on the downstream CaM kinases (CaM-KI and -IV, IC50 >10 ug); suppresses the Ca(2+)-induced activation of CaM-KIV in a dose-dependent manner in transfected HeLa cells; significantly reduces the endogenous activity of CaM-KK in SH-SY5Y neuroblastoma cells (1 ug/ml, 80% inhibition).
KN-62 is a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK II) with Ki of 900 nM for rat brain CaMK II; potently antagonizes ATP-stimulated Ba2+ influx into fura-2 loaded human lymphocytes with IC50 of 12.7 nM, inhibits ATP-stimulated ethidium+ uptake with IC50 of 13.1 nM; causes hypertension and tachycardia in rats, associated with the diminished rate of GABA release in cerebrospinal fluid.
CAMKK2 inhibitor 4t
CAMKK2 inhibitor 4t is a potent, selective, orally available, brain-penetrant CAMKK2 inhibitor with pIC50 of 8.5; potently inhibits AMPK phosphorylation in a hypothalamus-derived cell line with pIC50 of 6.3; reduces food intake in rodent models.
CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM; significantly high selectivity against CaMKIV, MLCK, p38a, Akt1, and PKC. IC50 value: 63 nM Target: CaMKII
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