ca 2

Compound 4H is a potent carbonic anhydrase inhibitor with an IC50 value of 0.033 μM [1].

CAIX-IN-2 (Compound 9o) is an inhibitor of carbonic anhydrase (CA), targeting CAIX, CA XII, and CAII with IC50 values of 5.6, 7.4, and 430 nM, respectively. This compound effectively inhibits the proliferation of cancer cells such as HCT-116, SW480, MDA-MB 231, and MCF-7, with IC50 values ranging from 14.63 to 29.33 µM. CAIX-IN-2 also integrates into DNA, causing cell cycle arrest at the G1 S phase and inducing apoptosis in MDA-MB-231 cells. Furthermore, it disrupts mitochondrial membrane potential (MMP), elevates intracellular ROS levels, leading to mitochondrial damage, and inhibits the migration of MDA-MB-231 cells. In mouse models, CAIX-IN-2 has demonstrated antitumor activity.

CAIX VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. It exhibits anticancer activity by inhibiting the growth of MCF-7 breast cancer cells (IC50 of 22.33 μM) and mouse fibroblast cell line 3T3, where cell viability is reduced to below 40% at a concentration of 100 μM. This compound is applicable for research in the field of cancer treatment.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Coelenterazine H is a synthetic derivative of coelenterazine (a light-emitting biomolecule).Coelenterazine h (CLZN-h) is more sensitive to Ca 2+ than is the native complex, thus providing a valuable tool for measuring small changes in Ca 2+ concentrations.

Gallopamil (Methoxyverapamil) inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil is a potent antiarrhythmic and vasodilator agent. Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist.

Gallopamil hydrochloride (Methoxyverapamil hydrochloride) is an antagonist of phenylalkylamine calcium. Gallopamil hydrochloride can be used in antiarrhythmic and vasodilator studies.

Oxatomide (Oxatomida) is a potent and orally active dual H1 histamine receptor and P2X7 receptor antagonist with antihistamine and antiallergic activity.Oxatomide can be used to block ATP-induced currents in the human P2X7 receptor with an IC50 value of 0.95 μM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.

JTV-519 is a Ca2+-dependent blocker and prevents abnormal Ca(2+) leak from the sarcoplasmic reticulum in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors.

Bisaramil hydrochloride (Bisaramil) is a novel diazabicyclononane antiarrhythmic compound that inhibits the generation of free radicals.Bisaramil hydrochloride blocks sodium currents and inhibits the slow Ca(2+) action potential induced by isoproterenol in K(+)-depolarized muscle.

KT-362 fumarate is a novel compound that acts as an antagonist of calcium channels, potassium channels and sodium channels.KT-362 fumarate causes vasodilation by affecting intracellular calcium mobilization in atrial muscle cells.KT-362 fumarate has a relaxing effect on femoral and basilar artery strips in rabbits.

Opc 8490 is a cardiotonic agent and a positive inotropic vasodilator that increases Ca current (ICa) in a dose-dependent and reversible manner and prolongs atrial action potential in a concentration-dependent manner.

Vesnarinone HCl (OPC-8212 HCl) is an orally active phosphodiesterase 3 (PDE3) inhibitor.Vesnarinone HCl modulates calcium and potassium ions, increasing calcium flux and decreasing potassium flux.Vesnarinone HCl is a new positive inotropic compound that enhances myocardial contractility and can be be used in heart failure studies.

AY 77 (Unk-Cha-Chg-NH2) is a potent and selective PAR2 agonist. AY 77 showed selectivity for Ca2+ and ERK1 2 signaling (ec50 value of Ca2+ release was 40 nM and ec50 value of ERK1 2 phosphorylation was 2 μM). AY 77 can promote migration of human breast cancer cells in vitro.

Terodiline is a seconal amine with anticholinergic and calcium antagonistic properties that blocks the hERG current (IC50: 375 nM).Terodiline is cardiotoxic and has been used in the study of disorders caused by urethral muscle instability.

Crobenetine (BIII 890 CL) Free Base is a selective NaV channel blocker that eliminates VTD-induced [Ca2+] elevation.

Caldaret HCl is an intracellular Ca2+ modulator that regulates calcium homeostasis at the sarcoplasmic reticulum and cell membrane, and can be used to study acute myocardial infarction and heart failure.

NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor with an IC50 of 574 nM. It acts independently of Ca 2+ and inhibits Nigericin-induced inflammasome activation in THP-1 cells, as well as Imiquimod-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) [1].

Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.

L-Phenylalanine (3-Phenyl-L-alanine) is an essential amino acid and the precursor of the amino acid tyrosine, acts as an antagonist at α2δ calcium channels.

2-Aminoethyl diphenylborinate (2-APB) is a chemical compound that inhibits IP3 receptors and TRP channels, though it activates TRPV1, TRPV2, and TRPV3 at higher concentrations.

Dibutyl phthalate (1,2-Benzenedicarboxylic acid) is a plasticizer, commonly used in industrial manufacturing, that causes cardiac damage by disrupting Ca(2+) transfer from the endoplasmic reticulum to the mitochondria and triggering subsequent cellular death.Dibutyl phthalate induces oxidative damage in the brain of zebrafish.

D-Menthol ((+)-MENTHOL) is a common compound in pharmaceutical and commercial products and a popular additive to cigarettes, it attenuates α±7 mediated Ca 2+ transients in the cell body and neurite, suggests that menthol inhibits α±7-nACh receptors in a noncompetitive manner.

Taurochenodeoxycholic acid sodium (Sodium taurochenodeoxycholate) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid sodium induces apoptosis and shows obvious anti-inflammatory and immune regulation properties. It can increase glucose-induced insulin secretion and stimulate the electrical activity of α2-cells and enhance cytosolic Ca(2+) concentration ([Ca(2+)](c)).