calmodulin-dependent protein kinase ii

Calmodulin-Dependent Protein Kinase II (290-309) is a potent CaMK antagonist with an IC50 of 52 nM for inhibiting Ca2+/calmodulin-dependent protein kinase II.

Calmodulin-Dependent Protein Kinase II (281-309) is a synthetic peptide phosphorylatable at Thr286 by PKC, inhibiting CaM kinase II with an IC50 of 80 nM.

Calmodulin-Dependent Protein Kinase II (290-309) acetate is a potent CaMK antagonist with an IC50 of 52 nM for the inhibition of Ca2+/calmodulin-dependent protein kinase II [1].

Calmodulin-Dependent Protein Kinase II 290-309 acetate is an effective antagonist of Ca2+/calmodulin-dependent protein kinase II (IC50 = 52 nM).

[Ala286]-Calmodulin-Dependent Protein Kinase II (281-302) is a modified fragment of the calcium ion/calcium-binding protein-dependent kinase II (CaMKII), featuring the active region of CaMKII with an alanine substitution at position 286. This particular modification allows for the potential development of more effective CaMKII inhibitors.

Autocamtide 2 TFA is a highly selective peptide substrate of calcium/calmodulin-dependent protein kinase II (CaMKII). Autocamtide 2 TFA can be used in the CaMKII activity assay.

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.

Rimacalib is an inhibitor of Ca2+/calmodulin-dependent protein kinase II (IC50s: ~1 μM for CaMKIIα and ~30 μM for CaMKIIγ).

Purine riboside-5'-O-triphosphate sodium is an active metabolite of Nebularine and acts as an inhibitor of DNA primase ATP and GTP polymerization activities, with IC50 values of 35 µM and 28 µM, respectively. It also inhibits calmodulin-dependent protein kinase II (CaMKII), with a Ki value of 590 µM.

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

MCB-22-174 is a potent agonist of Piezo1 with an EC50 value of 6.28 µM. It activates Ca2+-related extracellular signal-regulated kinase and calcium-calmodulin (CaM)-dependent protein kinase II (CaMKII) pathways, and it promotes mesenchymal stem cell osteogenic differentiation, indicating its potential application in the study of disuse osteoporosis (OP).

KN-62 is a potent and specific Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM.

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).

12(S)-HpETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of platelet or leukocyte 12-lipoxygenase (12-LO) on arachidonic acid. It activates human blood leukocyte 5-LOE. 12(S)-HpETE is the mediator of many biological functions, including induction of c-fos and c-jun, activation of AP-1, and endothelium-dependent vasoconstriction. It mediates the inhibitory synaptic response to FMRF-amide in Aplysia sensory neurons and inhibits Ca2+/calmodulin-dependent protein kinase II from rat brain cortex.

Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i

Gomisin J is a natural product and have vasodilatory activity. Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells.

CaMKIIα-IN-1 (Compound 4d) is an orally active inhibitor of Ca 2+ /calmodulin-dependent protein kinase II α (CaMKIIα) with a Kd of 219 nM for CaMKIIα WT hub, and it demonstrates good metabolic stability [1].

NYX-2925, an orally active NMDAR (N-methyl-D-aspartate receptor) modulator, enhances activated Src levels and Src phosphorylation at GluN2A and GluN2B sites in the mPFC (medial prefrontal cortex), without affecting CAMKII (Ca2+/calmodulin-dependent protein kinase II) or exhibiting addictive or sedative/ataxic side effects. It is utilized in the study of various CNS (central nervous system) disorders mediated by NMDA receptors.

Syntide 2 (TFA), a substrate peptide for Ca2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII), selectively inhibits the gibberellin (GA) response without affecting constitutive and abscisic acid-regulated events [1].

Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, serves as a highly selective substrate for protein kinase C (PKC) with a K_m of 7 μM. It is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca^2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, making it an ideal candidate for protein kinase C assays in crude tissue extracts, ensuring minimal background interference [1] [2].

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.

Ziptide, a peptide substrate, is recognized by several serine/threonine protein kinases, such as MAPK activated protein kinase 2 (MAPKAPK2), MAPKAPK3, MAPKAPK5, checkpoint kinase 1 (Chk1), AMP-activated protein kinase (AMPK), and calcium/calmodulin-dependent protein kinase II (CamKII). It serves as a tool in evaluating CamKII activity for the development of inhibitors.

Autocamtide-2 is a highly selective peptide substrate for calcium/calmodulin-dependent protein kinase II (CaMKII), which belongs to the CAMK Ser/Thr protein kinase family.