KN-62 is a sective, cell-permeable inhibitor of CaM kinase II (IC50 = 0.9 μM).

STO-609 is a selective, cell-permeable inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki values are 80 and 15 ng/ml for inhibition of CaM-KKα and CaM-KKβ respectively); competes for the ATP-binding site.

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

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.

Autocamtide-2-related inhibitory peptide, myristoylated TFA 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.

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

Calmodulin antagonist-1 (W-7) is a calmodulin (CaM) antagonist. Calmodulin antagonist-1 inhibits calmodulin-activated Ca2+-phosphodiesterase (PDE) (IC50=28 μM). Calmodulin antagonist-1 also inhibits trypsin-treated Ca2+-PDE (IC50=375 μM) in a competitive fashion with respect to cyclic GMP and the Ki value is 300 μM.

Acremoxanthone C is a potent calmodulin (CaM) inhibitor found in Purpureocillium lilacinum. Acremoxanthone C binds to the human calmodulin (hCaM) biosensor hCaM M124C-mBBr, with Kd of 18.25 nM.

Acremonidin A is a potent calmodulin (CaM) inhibitor found in Purpureocillium lilacinum. Acremonidin A binds to the human calmodulin (hCaM) biosensor hCaM M124C-mBBr, with Kd of 19.40 nM.

AS105 (AS-105) is a highly potent, ATP-competitive CaMKII inhibitor, inhibits CaMKIIδ with IC50 of 8 nM, Ki of 3 nM. AS105 is also effective against autophosphorylated CaMKII (in contrast to the commonly used allosteric CaMKII-inhibitor KN-93). In isolated atrial cardiomyocytes from human donors and ventricular myocytes from CaMKIIδC-overexpressing mice with heart failure, AS105 effectively reduced diastolic SR Ca2+ leak by 38% to 65% as measured by Ca2+-sparks or tetracaine-sensitive shift in [Ca2+]i. AS105 effectively reduced SR Ca2+-leak, thus improving SR Ca2+-accumulation and reducing cellular arrhythmogenic correlates, without negatively influencing excitation-contraction coupling.

CaMK1D-IN-18 is a potent, selective CaMK1D inhibitor with IC50 of 31 nM, >150-fold greater activity against CaMK1D than all non-CaMK1 kinases.CaMK1D-IN-18 improves insulin sensitivity and glucose control in the diet-induced obesity mouse model after both acute and chronic administration.

CS640 (CS-640) is a potent, selective CaMK1D inhibitor with nanomolar range at both the enzymatic and cellular levels.CS640 prevent Aβ induced tau hyperphosphorylation in culture, but were not able to protect cells from Aβ induced toxicity.CS640 was able to ablate Aβ induced increased tau phosphorylation at Thr181 in mouse primary neurons.

GS-680 (GS680) is a novel selective and ATP-competitive CaMKII inhibitor with biochemical IC50 of 2.3 and 15.9 nM against CaMKIIδ and CaMKIIα, respectively.GS-680 inhibited phospholamban phosphorylation in NRVM with an EC50 of 98.9 nM.GS-680 inhibits premature atrial contractions.GS-680 significantly reduced CaMKII autophosphorylation.GS-680 inhibits pro-arrhythmic activity in human atrium and improves contractility in failing human ventricle.

RA306 (RA-306) is a selective, potent, orally active, ATP-competitive CaMKII inhibitor, inhibits CaMKII delta (IC50=15 nM), gamma (IC50=25 nM), and alpha (IC50=61 nM) isoforms.RA306 displays a good selectivity profile vs. kinases and non-kinase targets, as compared with KN-93.RA306 also displays a good cellular activity in cardiomyocytes from human, rat, and mice, with IC50s in the 200 nM range.Isoproterenol-induced phosphorylation of Thr17-PLN, normalized to total PLN, was fully inhibited by RA306 in a dose-dependent manner, with IC50s of 140 nM in rat, 205 nM in mouse, and 220 nM in human cardiomyocytes.

RA608 (RA-608) is a potent, selective, ATP-competitive, orally available CaMKII inhibitor, inhibits human CaMKIIδ, CaMKIIγ, CaMKIIα, and CaMKIIβ with IC50 of 22, 51, 121, and 1135 nM, respectively.RA608 displays a good selectivity profile against a broad panel of 304 human recombinant kinases.RA608 significantly reduces SR Ca leak in human atrial cardiomyocytes, reduces diastolic tension of human atrial trabeculae, does not affect action potential characteristics; attenuates heart failure in the murine HF model induced by TAC.

TIM-063 (TIM063) is a potent, selective, ATP-competitive CaMKK inhibitor with Ki of 0.35/0.2 uM for CaMKKα and CaMKKβ, respectively.TIM-063 directly targets the catalytic domain of CaMKK, similar to STO-609.TIM-063 suppressed the ionomycin-induced phosphorylation of exogenously expressed CaMKI, CaMKIV, and endogenous AMPKα in HeLa cells with an IC50 of 0.3 uM.TIM-063 suppressed CaMKK isoform-mediated CaMKIV phosphorylation in transfected COS-7 cells.TIM-063 displayed cell permeability and the ability to inhibit CaMKK activity in cells. TIM-063 is a useful chemical probe for the precise analysis of CaMKK-mediated signaling pathways.

Ph-HTBA is a high-affinity, brain-penetrating modulator for CaMKIIα. Ph-HTBA has binding affinity for CaMKIIα with a Kd value of 757 nM. Ph-HTBA can be used for the research of ischemia and neurodegenerative disorders.

CC-8977 is a hgihly potent, selective inhibitor of calcium/calmodulin-dependent kinase kinase II (CaMKK2) with binding IC50 of 7 nM.

SMP-114 (Rimacalib) is a potent, specific and orally available CaMKII inhibitor with potential for treatment of rheumatoid arthritis.