calmodulin-dependent kinases

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

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

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

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

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).

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

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

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).

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).

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].

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

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.

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.

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].

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.

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].