calmodulin-dependent kinases

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

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

Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist with a Kd of 3 nM, which inhibits CaM-dependent phosphodiesterase (IC50 = 0.15 μM) and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase (IC50 = 0.35 μM). It also induces apoptosis in certain cancer cell lines.

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.

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

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

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).

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

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.

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

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

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It inhibits PKC and casein kinase I with Ki values of 47 μM and 80 μM, respectively[1], and also inhibits PKA (Ki=4.3 μM), casein kinase II (Ki=5.1 μM), and myosin light chain kinase (MLCK) (Ki=7.4 μM).

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.

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).

NPC-15437 dihydrochloride is a synthetic prototype belonging to a novel structural class of protein kinase C (PKC) inhibitors. NPC 15437 potently inhibits PKC enzymatic activity and phorbol ester binding with IC50 values around 19 μM and 23 μM, respectively, without affecting cAMP-dependent or Ca2+/calmodulin-dependent kinases at concentrations up to 300 μM, thereby demonstrating selectivity for PKC and serving as an important tool compound for dissecting PKC-mediated cellular signaling mechanisms.

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].

Calmodulin-Dependent Protein Kinase Substrate Analog, a synthetic peptide substrate, is activated by Ca2+ and calmodulin (CaM). It serves as a substrate for protein kinases, leveraging a dependency on Ca2+ and CaM for its function [1].

Calmodulin Dependent Protein Kinase Substrate is a synthetic peptide that interacts specifically with calmodulin-dependent protein kinases (CaMK) and requires calcium ions (Ca 2+) and calmodulin (CaM) for activation. It is utilized in studies involving protein kinase activity [1].

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.

Ziptide serves as a substrate for various kinases, including MAPK protein kinase 2 (MAPKAPK2, Km= 5 μM), MAPKAPK3 (Km= 30 μM), PARK (Km= 40 μM), checkpoint kinase 1 (Chk1, Km= 5 μM), AMP-activated protein kinase (AMPK, Km= 75 μM), and calcium/calmodulin-dependent protein kinase II (CamKII, Km= 300 μM).