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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.

Cat. No. Product Name CAS No. Information
H9542

Cabamiquine succinate

2444781-71-7

Cabamiquine succinate(DDD 498 succinate,M-5717 succinate) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7;DDD107498 inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2.

H9541

Cabamiquine

1469439-69-7

Cabamiquine(DDD 498,M-5717) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7;DDD107498 inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2.

H6040

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.

H6039

CaMKII-IN-1

1208123-85-6

A potent and highly selective CaMKII inhibitor with IC50 of 63 nM; no inhibitory effect for CaMKIV, MLCK, p38α, Akt1, PKC etc; shows 25-fold higher potency than KN-93.

H6042

STO-609

52029-86-4

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).

H6041

KN-62

127191-97-3

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.

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