camkiiα

CaMKII-IN-1, a potent and highly selective inhibitor of CaMKII (IC50 = 63 nM), exhibits over 100-fold higher selectivity for CaMKII compared to CaMKIV, MLCK, p38a, Akt1, and PKC.

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

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].

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].

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

Y-33075 (Y-39983 free base) is a ROCK inhibitor that lowers intraocular pressure (IOP), increases blood flow to the optic nerve head (ONH), and increases the number of RGCs (retinal ganglion cells) in the body with regenerating axons.

Y-33075 dihydrochloride is a selective inhibitor of ROCK with an IC50 of 3.6 nM.

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.

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

NH125 is a selective eEF-2 kinase inhibitor with IC50 of 60 nM, >125-fold selectivity over PKC, PKA, and CaMKII, and also a potent histidine kinase inhibitor.

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.

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

Syntide-2 acetate is a synthetic peptide recognized as a substrate by Ca2+/calmodulin-dependent protein kinase II (CaMKII; Km = 12 μM).

CaMKIIδ-IN-1 (compound 15e) is a pyrimidine-based inhibitor of CaMKIIδ, with an IC50 value of 0.012 μM.

CaMKII inhibitory peptide KIIN serves as a potent inhibitor of CaMKII [1] [2].

H-1152 dihydrochloride (H-1152 2HCl) is a specific inhibitor of Rho-associated protein kinase (ROCK) with an IC50 of 12 nM and a Ki of 1.6 nM. H-1152 dihydrochloride inhibits PKA, PKC, PKG, Aurora A and CaMKII with IC50 values of 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.

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.

KN-93 hydrochloride is a cell-permeable, reversible, and competitive inhibitor of calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM. KN-93 hydrochloride induces G1 cell cycle arrest in 95% of treated cells after two days, with the arrest being reversible; one day after KN-93 withdrawal, a peak of cells progresses into S and G2-M phases, providing a robust tool for cell cycle regulation studies and mechanistic investigation of CaMKII-dependent signaling.

KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase.

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).

1-Naphthyl PP1 (1-NA-PP 1) is a selective Src inhibitor, targeting v-Src and c-Fyn, c-Abl, CDK2, and CAMK II with IC50 values of 1.0, 0.6, 0.6, 18, and 22 μM, respectively.

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

lavendustin C (NSC 666251) is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase.

KN-92 phosphate (KN92-H3PO4) is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).