Calmodulin Inhibitor

SGC-CAMKK2-1, a chemical probe, is the selective, inhibitor for calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) with an IC₅₀ of 30 nM. SGC-CAMKK2-1 inhibits AMPK phosphorylation in cell C4-2 with an IC₅₀ of 1.6 μM.

Aprindine hydrochloride is an Ib-class anti-arrhythmic agent. Aprindine hydrochloride mainly exerts its effect by blocking sodium channels (I_Na), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine hydrochloride significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine hydrochloride can also regulate intracellular calcium ion concentration by inhibiting Na⁺/Ca²⁺ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine hydrochloride can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias.

IGS-1.76 efficiently inhibits the human NCS-1/Ric8a complex. IGS-1.76 shows a significantly increased affinity for hNCS-1 and is able to modulate the hNCS-1/Ric8a interaction efficiently.

Aprindine is an Ib-class anti-arrhythmic agent. Aprindine mainly exerts its effect by blocking sodium channels (I_Na), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine can also regulate intracellular calcium ion concentration by inhibiting Na⁺/Ca²⁺ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias.

Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (K_d=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).

Probimane (AT-2153) is a potent anticancer agent. Probimane is effective against mouse tumors S37, S180, Lewis lung carcinoma, L1210 and human pulmonary adenocarcinoma heterotransplanted into nude mice.

Albanin A, a flavonoid, suppresses glutamate release by decreasing Ca²⁺/calmodulin/adenylate Cyclase 1 (AC1) activation in synaptosomes and exerts neuroprotective effect in vivo. Albanin A has anti-inflflammatory activity.

Metofenazate is a selective calmodulin inhibitor.

Neurogranin (48-76), mouse is a peptide corresponding to residues 48-76 of Neurogranin. Neurogranin, a calmodulin-binding protein, is exclusively expressed in the post-synapse, and mediates NMDAR driven synaptic plasticity by regulating the calcium-calmodulin (Ca²⁺-CaM) pathway.

Zaldaride (CGS-9343B free base) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC₅₀ of 3.3 nM. Zaldaride prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na⁺, Ca²⁺ and K⁺ currents in PC12 cells and inhibits nAChR.

KS 501 is a potent and selective calmodulin inhibitor. KS 501 inhibits the activation of calmodulin kinase I and II, but has less effect against cyclic adenosine 3’,5’-monophosphate (cyclic AMP)-sensitive kinase. KS 501 inhibits the enzyme through interfering with calmodulin activation rather than through a direct effect on the enzyme. KS 501 can be used for the study of leukemia.

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 K_d of 19.40 nM.

DY-9760e is a calmodulin (CaM) inhibitor. DY-9760e selectively inhibits the activity of various calmodulin-dependent enzymes by antagonizing the Ca²⁺/CaM complex, exhibiting the strongest inhibitory activity against nNOS, CaM kinase II, and calcineurin (K_i: 0.9, 1.4, and 2.0 μM, respectively). DY-9760e inhibits excessive nitric oxide production and protein tyrosine nitration, as well as the activation of calpain and caspase-3. DY-9760e reduces infarct size, improves cardiac function, and inhibits oxidative stress and cell death. DY-9760e can be used in research on the treatment of myocardial infarction, cerebral ischemia, and other diseases.

Beauverolide Ja, a cyclotetradepsipeptide, is a potent calmodulin (CaM) inhibitor with a K_d of 0.078 μM and a K_i of 0.39 μM for Ca²⁺-CaM. Beauverolide Ja is a secondary metabolite of Isaria fumosorosea.

(S)-O-Methylencecalinol (compound 10) is a calmodulin-targeting molecule isolated from the aerial parts of Ageratina grandifolia.

Encecalinol, extracted from aerial parts of Ageratina grandifolia, is a potent inhibitor of calmodulin inhibitor.

Calmodulin-Dependent Protein Kinase II (281-309) is a peptide of calcium/calmodulin-dependent protein kinase II (CaM-kinase II).

Aprindine hydrochloride (Standard) is the analytical reference standard of Aprindine hydrochloride (HY-A0236A). This product is used for research and analytical applications. Aprindine hydrochloride is an Ib-class anti-arrhythmic agent. Aprindine hydrochloride mainly exerts its effect by blocking sodium channels (I_Na), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine hydrochloride significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine hydrochloride can also regulate intracellular calcium ion concentration by inhibiting Na⁺/Ca²⁺ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine hydrochloride can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias.

Psoralenoside is a benzofuran glycoside from Psoralea corylifolia. Psoralenoside exhibits high binding affinities against histaminergic H1, calmodulin, and voltage-gated L-type calcium channels (E-value≥-6.5 Kcal/mol). Psoralenoside shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.

Bromoriluzole is a derivative of Riluzole (HY-B0211). Bromoriluzole inhibits Ca²⁺ -dependent Calmodulin-SK4 channel interaction. Bromoriluzole is used for the research of neurodegenerative diseases.