2. シグナル伝達
  3. Neuronal Signaling
  4. CaMK
  5. CaMK II Isoform

CaMK II

CaMKII is a Ca2+/calmodulin-dependent serine/threonine kinase that converts intracellular calcium signals into phosphorylation-dependent cellular responses[1]. In excitatory synapses, CaMKII is central to synaptic plasticity, learning, and memory, where it phosphorylates synaptic proteins that regulate receptor trafficking, localization, activity, actin dynamics, translation, and transcription[1]. Mechanistically, Ca2+/calmodulin binding activates the regulatory domain, and CaMKII tools now support studies across cell types and cellular functions[2]. In disease-relevant models, CaMKIIδ expression increases in human heart failure, and CaMKII inhibition acutely improves contractility by reducing sarcoplasmic-reticulum Ca2+ leak and increasing Ca2+ load[3]. Compared with related isoforms, CaMKIIα and CaMKIIβ are largely brain-specific, whereas CaMKIIγ and CaMKIIδ show broader tissue expression[4]. The α and β isoforms mediate synaptic functions underlying learning, memory, and cognition, but CaMKIIβ has high-affinity F-actin binding that distinguishes it from CaMKIIα[4]. Structural comparison of α, β, γ, and δ isoforms documented shared holoenzyme architecture with measurable enzymatic differences among gene products[5]. For experimental applications, KN-93 inhibits CaMKII activity by binding Ca2+/calmodulin, supporting its use as a mechanistic inhibitor with target-engagement considerations[6].

CaMK II 関連製品 (39):

製品番号 製品名 製品効果 純度
  • HY-15465
    KN-93 Inhibitor 99.42%
    KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
  • HY-15465B
    KN-93 phosphate Inhibitor 99.72%
    KN-93 phosphate is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
  • HY-N6732
    K-252a Inhibitor 99.45%
    K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
  • HY-13290
    KN-62 Inhibitor 99.00%
    KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
  • HY-108599
    DCP-LA Activator 98.0%
    DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. DCP-LA activates Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulate AMPA receptor exocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-induced apoptosis.
  • HY-W720917
    Junicedric acid Activator
    Junicedric acid is a diterpenoid compound that can be isolated from the resin of the Araucaria araucana tree. Junicedric acid exerts neuroprotective activity by increasing intracellular calcium levels in hippocampal neurons, activating PKC and calcium/calmodulin-dependent protein kinase (CaMKII), and preventing Amyloid-β oligomer-induced synaptic protein loss, apoptosis, and long-term potentiation (LTP) inhibition. Junicedric acid can be used in the study of the pathological mechanisms of neurodegenerative diseases such as Alzheimer's disease.
  • HY-180951
    CaMKII-IN-3 Inhibitor
    CaMKII-IN-3 (Example 321) is a CaMKII inhibitor with an IC50 of less than 10 nM. CaMKII-IN-3 can be used for the study of heart diseases.
  • HY-18271
    CaMKII-IN-1 Inhibitor 98.63%
    CaMKII-IN-1 is a highly selective inhibitor of CaMKII with an IC50 value of 63nM. It has almost no effect on CaMKIV, MLCK, p38a, Akt1, and PKC.
  • HY-P10638
    TAT-CN21 Inhibitor 99.38%
    TAT-CN21 is a potent CaMKII inhibitor with an IC50 of 77.2 nM. TAT-CN21 inhibits both calcium/calmodulin-dependent and autonomously activated CaMKII, blocks glutamate-induced translocation of CaMK IIα, and reverses the enhanced phosphorylation of CaMKII at Thr286 following excitotoxic injury. TAT-CN21 shows application potential in studies related to ischemic stroke by reducing neuronal excitotoxicity and exacerbating pre-existing long-term neuronal death prior to injury. TAT-CN21 improves definitive behaviors in rats with residual nerve injury without altering indicators such as mechanical/thermal hyperalgesia or spatial memory. TAT-CN21 can also be used in studies related to neuropathic pain.
  • HY-N1916
    Coniferyl ferulate Inhibitor 98.73%
    Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC50 = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus.
  • HY-15465A
    KN-93 hydrochloride Inhibitor 99.64%
    KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
  • HY-P1029
    MLCK inhibitor peptide 18 Inhibitor 98.04%
    MLCK inhibitor peptide 18 is a myosin light chain kinase (MLCK) inhibitor with an IC50 of 50 nM, and inhibits CaM kinase II only at 4000-fold higher concentrations.
  • HY-173117
    RA306 Inhibitor 99.74%
    RA306 is an orally active CaMKIIδ/γ inhibitor with IC50 values of 15, 25, 61, and 420 nM against CaMKIIδ, γ, α, and β isoforms, respectively. RA306 reduces the serine/threonine phosphorylation level of PEAK1, inhibits PEAK1-mediated cancer cell migration and invasion, and attenuates the growth and metastasis of cancer xenografts. RA306 can be used in research related to triple-negative breast cancer and dilated cardiomyopathy.
  • HY-137506
    XST-14 Inhibitor 99.26%
    XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.
  • HY-P0214A
    Autocamtide-2-related inhibitory peptide TFA Inhibitor 99.20%
    Autocamtide-2-related inhibitory peptide (TFA) is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM.
  • HY-Z0478
    (-)-Limonene Inhibitor 99.42%
    (-)-Limonene ((S)-(-)-Limonene) is orally active and can cause mild bronchoconstriction. (-)-Limonene alleviates cytosolic and mitochondrial oxidative stress by inhibiting the increase of calcium ions (Ca2+) and Ca2+/calmodulin-dependent protein kinase II (CaMKII). It also exerts anti-stress effects by inhibiting the activity of the hypothalamic-pituitary-adrenal (HPA) axis. Additionally, (-)-Limonene can be used as an antibacterial agent in aquaculture.
  • HY-P0215
    Autocamtide-2-related inhibitory peptide, myristoylated Inhibitor 98.68%
    Autocamtide-2-related inhibitory peptide, myristoylated is the myristoylated Autocamtide-2-related inhibitory peptide. Autocamtide-2-related inhibitory peptide is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM.
  • HY-P0225
    Autocamtide 2 98.94%
    Autocamtide 2 is a highly selective peptide substrate of calcium/calmodulin-dependent protein kinase II (CaMKII). It can be used in the CaMKII activity assay.
  • HY-171932
    CaMKIIδ-IN-1 Inhibitor 98.41%
    CaMKIIδ-IN-1 (Compound 15e) is a pyrimidine-based inhibitor of CaMKIIδ with an IC50 of 12 nM.
  • HY-146268
    CaMKIIα-IN-1 Inhibitor 98.53%
    CaMKIIα-IN-1 (Compound 4d) is an orally active Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability.
製品番号 製品名 / Synonyms Application Reactivity