CaMK II Inhibitor

KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a K_i of 370 nM.

KN-93 phosphate is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.

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.

KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a K_i 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.

Oxoglaucine (O-Methylatheroline) is a natural product with multiple activities including autophagy activation, anti-inflammation, antibacterial activity, and immunoregulation. Oxoglaucine inhibits the TRPV5/calmodulin/CAMK-II pathway, suppresses TGFβ-induced Smad2 phosphorylation by upregulating Smad7, blocks Ca²⁺ influx, activates autophagy, alleviates apoptosis and inflammation, inhibits ROS production and the expression of fibrosis markers in hepatocytes, and regulates immune cell populations and responses. Oxoglaucine protects against infections caused by Candida albicans and Klebsiella pneumoniae, and exerts effects on adjuvant-induced arthritis. Oxoglaucine can be used in studies related to arthritis, liver fibrosis, bacterial infections, and fungal infections.

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.

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.

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.

KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a K_i of 370 nM.

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.

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.

Autocamtide-2-related inhibitory peptide (TFA) is a highly specific and potent inhibitor of CaMKII with an IC₅₀ of 40 nM.

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.

(-)-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.

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.

CaMKIIδ-IN-1 (Compound 15e) is a pyrimidine-based inhibitor of CaMKIIδ with an IC₅₀ of 12 nM.

CaMKIIα-IN-1 (Compound 4d) is an orally active Ca²⁺/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a K_D of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability.

Cucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable EGFR inhibitor with an IC₅₀ of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the EGFR-MAPK signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer.

Lavendustin C is a potent Ca²⁺ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC₅₀ of 0.2 μM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC₅₀=0.012 μM) and pp60^c-src(+) kinase (IC₅₀=0.5 μM) .

Rimacalib (SMP 114) is a Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC₅₀s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.