camkⅴ

Dibucaine (Cinchocaine), a local anesthetic of the amide type, is now usually used for surface anesthesia.

Trifluoperazine dihydrochloride (SKF5019) is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic.

Melatonin (Melatonine) is a natural hormone secreted by the pineal gland that activates melatonin receptors. Melatonin is a hormone that regulates the biological clock and also has antioxidant and anti-inflammatory activities.

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

A-484954 (A 484954) is a highly specific eukaryotic elongation factor-2 (eEF2, IC50: 280 nM) inhibitor.

Autocamtide-2-related inhibitory peptide, myristoylated acetate is a CaM kinase II inhibitor; enhanced cell permeable derivative of Autocamtide-2-related inhibitory peptide.

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

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

K-252a is a protein kinase inhibitor targeting serine-threonine, tyrosine, and CAM kinases. In vitro, it blocks NGF-induced TrkA signalling and neural differentiation, exhibiting antitumour, antibacterial, anti-inflammatory, and neuroprotective activities.

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

PTCA is a potent ligand for Ca2+ calmodulin-dependent protein kinase II α (CaMKIIα), with a pKi value of 7.2.

RA306 is an orally active CAMK2 inhibitor that effectively disrupts the PEAK1/CAMK2 signaling pathway. It demonstrates anti-tumor activity by inhibiting proliferation, migration, and invasion of breast cancer cells. Additionally, RA306 shows potential in cardiac disease research, as it improves dilated cardiomyopathy in mice.

Fluoxetine-Conjugated Platinum(IV) prodrug-1 is an eEF2K inhibitor that can hinder the proliferation of cancer cells, induce DNA damage, and cause cell cycle arrest at the S phase, leading to apoptosis (Apoptosis). It also promotes the accumulation of reactive oxygen species (ROS) and disrupts mitochondrial function. This prodrug inhibits the migration and invasion of TNBC cells by suppressing MMP-2 activity and induces autophagy in TNBC cells through AMPK activation. In the 4T1-Luc mouse model, it exhibits antitumor activity and triggers immune suppression. Fluoxetine-Conjugated Platinum(IV) prodrug-1 is relevant for research in triple-negative breast cancer (TNBC).

W-9 hydrochloride is a calmodulin antagonist.

KN-93 (Phosphate) can competitively block the binding of calmodulin to the corresponding kinase. It is a calcium/calmodulin-dependent kinase II (CaMKII) inhibitor with a Ki of 370 nM. It can also inhibit the proliferation of human hepatic stellate cells.

STO-609 is a specific and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK) for recombinant CaM-KKα/KKβ (Ki: 80/15 ng/mL).

STO-609 acetate is selective, cell-permeable inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki: 80/15 ng/ml, for CaM-KKα/KKβ); competes for the ATP-binding site. It displays > 80-fold selectivity over CaMK1/2/4, PKC, MLCK, PKA and p42 MAPK.

Praeruptorin A ((+)-Praeruptorin A) has the potential to inhibit migration/fusion of preosteoclasts in vitro and bone erosion in vivo by targeting calmodulin and inhibiting the Ca(2+)/calmodulin-CaMKIV-CREB-NFATc1 and/or Ca(2+)/calmodulin-calcineurin-NFATc1 signaling axis.

Berbamine is a natural product extracted from Phellodendron amurense. It acts as a calcium channel blocker and possesses anti-tumor, immunomodulatory, and cardiovascular effects.

CaMKIIα-PHOTAC is a photochemically targeted chimera (PHOTAC) that specifically targets Ca2+ calmodulin-dependent protein kinase II α (CaMKIIα), facilitating its ubiquitination and subsequent proteasome-mediated degradation when exposed to specific light wavelengths. Under illumination, CaMKIIα-PHOTAC diminishes synaptic functions and weakens evoked field excitatory postsynaptic potentials in the mouse hippocampus, impacting physiological responses and sustaining long-term potentiation and memory functions within dendritic domains [1].

Myristoylated AC3-I is a biologically active peptide and a myristoylated variant of the Autocamtide-3-Derived Inhibitory Peptide (AC3-I). It acts as a highly specific inhibitor of Calmodulin-Dependent Protein Kinase II (CaMKII) with enhanced resistance to proteolysis. This compound is a derivative of Autocamtide-3, where the Thr-9 phosphorylation site is replaced by Ala.

Myristoylated Calmodulin Kinase IINtide (Myr-CaMKIINtide) serves as a selective and noncompetitive inhibitor of CaMKII [1].

Trifluoperazine (trifluoroperazine) is a Dopamine D2 receptor inhibitor(IC50 : 1.2 nM), and Treatment of schizophrenia.

KN-92 hydrochloride is an inactive derivative of the selective Ca2+/calmodulin-dependent kinase II (CaMKII) inhibitor KN-93, which competitively blocks CaM binding to the kinase with a Ki of 370 nM.