ca2+ influx

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.

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

CGP52411 is an orally active, and ATP-competitive inhibitor of EGFR (IC50: 0.3 μM). CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells and dramatically inhibits and reverses the formation of β-amyloid Aβ42 fibril aggregates. CGP52411 can be used in studies about Alzheimer's diseases.

HC-030031 (TOSLAB 829227) is a potent TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.

Addition of the Rhamnose (6-Deoxy-L-mannose)-rich polysaccharide, RROP-1, to normal human dermal fibroblasts (NHDFs) and human endothelial cells produced a dose-dependent stimulation of the calcium-signaling pathway, inducing fast and transient increases in Ca2 influx and intracellular free Ca2 level.

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived relaxing factor, nitric oxide.

CALP1 acetate is a calmodulin (CaM) agonist (Kd of 88 µM) that binds to the CaM EF-hand/Ca2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) by inhibiting the open of calcium channel. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.

1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.

Chembridge-5861528 (TCS 5861528) is a TRPA1 channel blocker that inhibits AITC- and 4-HNE-induced calcium influx with IC50 values of 14.3 μM and 18.7 μM, respectively.

Pyr10 is a pyrazole derivative and a selective TRP cation 3 inhibitor that distinguishes between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1) Orai1 channels. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells (IC50: 0.72 μM) and has an IC50 of 13.08 μM for store-operated Ca2+ entry in BRL-2H3 cells.

Procyanidin A1 (Proanthocyanidin A1) has antiallergic effects, it inhibits degranulation downstream of protein kinase C activation or Ca2+; influx from an internal store in RBL-2H3 cells.

Atosiban acetate (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban acetate (RW22164) inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, Atosiban acetate (RW22164) suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

NMDA-IN-1 is a potent and NR2B-selective antagonist of NMDA, with an NMDA Ki of 0.85 nM and an NR2B Ca2+ influx IC50 of 9.7 nM.

Pyr6 (N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide) is a selective TRPC3 inhibitor with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).Pyr6 is an inhibitor of Ca2+ entry, which displays higher potency to inhibit Ca2+ entry mediated by CRAC channel than by TRPC3.

HUP30 is a potent vasodilating agent. HUP30 can stimulate soluble guanylyl cyclase, activate K+ channels, and block extracellular Ca2+ influx.

Pyr3 is a selective transient receptor potential canonical channel 3 inhibitor. Pyr3 inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner(IC50 = 700 nM).

DS16570511 is a novel, cell-permeable inhibitor targeting the mitochondrial calcium uniporter. It effectively blocks the increase in Ca2+ influx dependent on MCU or MICU1 [1].

Syringomycin E, an antifungal cyclic lipodepsinonapeptide, inhibits the growth of Saccharomyces cerevisiae by interacting with the plasma membrane. It induces K+ efflux, Ca2+ influx, and alterations in membrane potential, associated with channel formation [1] [2].

Nantenine is an acetylcholinesterase inhibitor, it functions as an effective antagonist against a wide range of MDMA-induced effects in mice. Nantenine has anticonvulsant effect, which seems attributable to its stimulation and the resultant decrease of Ca

MRS4719, a potent P2X4 receptor antagonist, exhibits a half-maximal inhibitory concentration (IC50) of 0.503 μM for the human P2X4 receptor. Demonstrating both neuroprotective and neuro-rehabilitative effects, it can decrease infarct volume and brain atrophy in an ischemic stroke model. Additionally, MRS4719 mitigates ATP-induced calcium influx in primary human monocyte-derived macrophages, making it a valuable tool for researching ischemic stroke.

A-80b is a synthesized pyridazino[4,5-b]indole derivate with potent and long-lasting antihypertensive activity. The decrease in diastolic pressure was greater than the decrease in systolic pressure and cardiac frequency was not modified significantly. A-8

Hirsutine induces apoptosis and is a potent Dengue virus inhibitor exhibiting low cytotoxicity.Hirsutine has anticancer, cardioprotective, anti-hypertensive and anti-arrhythmic activities, it also has vasodilatation activity, the mechanism is related to blockade of Ca2+ influx through L-type Ca2+ channels and inhibition of intracellular Ca2+ release may have no relationship with K+ channels.

TRPV2-selective blocker 1 (compound IV2-1) is a selective inhibitor of the TRPV2 channel, with an IC50 value of 6.3 μM, specifically targeting the TRPV2 channel without affecting TRPV1, TRPV3, or TRPV4 channels, and effectively suppresses TRPV2-mediated calcium influx in macrophages, inhibiting their phagocytic activity [1].

Celangulin, an insecticidal component derived from Celastrus angulatus, functions by activating calcium channels on the plasma membrane, which leads to an increase in intracellular Ca2+ due to influx from the external environment. Additionally, Celangulin stimulates calcium channels in the endoplasmic reticulum (ER) [1].

Cerebroside A, a single molecule cerebroside extracted and isolated from an edible mushroom, provides potent neuroprotection after cerebral ischemia by reducing glutamate release and Ca²⁺ influx of NMDA receptors [1].

ω-Agatoxin IVA TFA is a potent selective inhibitor of P Q type Ca2+ (Cav2.1) channels, with IC50 values of 2 nM for P-type and 90 nM for Q-type channels. It effectively inhibits glutamate exocytosis and calcium influx induced by high potassium, with IC50 values ranging from 30 to 225 nM. Additionally, it blocks high potassium-induced serotonin and norepinephrine release, without impacting L-type or N-type calcium channels [1][2].

1-Stearoyl-2-arachidonoyl-sn-glycerol (DAG) is a diacylglycerol (DAG) substrate that can be hydrolyzed to 2-arachidonic acid glycerol. 1-Stearoyl-2-arachidonoyl-sn-glycerol activates PKC, induces Ca2+ influx, and can induce tracheal smooth muscle contraction.

Cell-permeable calmodulin (CaM) agonist that binds to the EF-hand/Ca2+-binding site; produces CaM-dependent activation of phosphodiesterase. Also binds to cytoplasmic sites on other Ca2+ channels, including NMDA and HIV-1 gp120-activated channels, inhibit

Evocarpine shows antimycobacterial, and vasorelaxant effects, it can inhibit Ca2+ influx through voltage-dependent calcium channels.

OBAA is a potent inhibitor of phospholipase A2 (PLA2) with an IC 50 of 70 nM. OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei with an IC 50 of 0.4 μM [1] [2] [3].

1,6-O,O-Diacetylbritannilactone(OODBL) has anti-inflammatory activity, it has a potential therapeutic efficacy on inflammatory diseases especially allergic airway disease as a lead compound. OODBL has anti-asthmatic activity, it reduces leukotriene C4 pro

Bay K 8644 (SQ 28,873) is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.

Asocainol hydrochloride ia an antiarrhythmic drug which inhibits slow Ca2+ influx. This is accompanied by alterations in normal Na+-carried action potentials. Therefore, Asocainol not only inhibits Ca2+ inflow but also interferes with the fast inward Na+ current.

Atosiban (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

FS-2 is a potent, specific inhibitor of L-type CaV channels, effectively impeding high K+ or glucose-induced L-type Ca2+ influx in RIN beta cells [1].

KS-133 TFA is a selective and potent antagonist of the vasoactive intestinal peptide receptor 2 (VIPR2), exhibiting IC50 values of 24.8 nM in Ca2+ influx assays and 500 nM in cAMP assays. It plays a significant role in research on schizophrenia.

CALP1 TFA, a calmodulin (CaM) agonist with a dissociation constant (Kd) of 88 µM, selectively binds to the CaM EF-hand/Ca2+-binding site, inhibiting calcium channel opening. This action blocks calcium influx and apoptosis with an IC50 of 44.78 µM, modulates glutamate receptor channel activity, and impedes a store-operated nonselective cation channel. Additionally, CALP1 TFA enhances CaM-dependent phosphodiesterase activity, denoting its multifaceted role in modulating cellular calcium dynamics [1] [2] [3] [4].

ITH-12575 is an inhibitor of Mitochondrial Na+/Ca2+ exchange (mNCX). ITH12575 reduces Ca(2+) influx through CALHM1 at low micromolar concentrations.

Yangambin is a selective antagonist of the cardiovascular effects of platelet activating factor (PAF); it has hypotensive effect, which is probably due to a peripheral vasodilatation that involves, at least, the inhibition the Ca2+ influx through voltage-gated Ca2+ channels. Yangambin also has central nervous system activity.

(±)-1,2-Diolein [1,2-Dioleoyl-rac-glycerol] is a PKC activator that can increase Ca²⁺ influx in myotubes.

Cyclic ADP-ribose (cADP-ribose) is an endogenous metabolite of NAD+ that mobilizes the release of stored Ca2+ in the endoplasmic reticulum via ryanodine receptors in various cell types.[1],[2],[3],[4],[5] This second messenger is generated via the cADP-ribose synthases CD38 and CD157.[6],[5],[7] cADP-Ribose may also trigger the cell surface Ca2+ influx channel TRPM2 in a temperature-dependent manner.[8] In vitro, cADP-ribose modulates Ca2+ signaling in rat and mouse cardiomyocytes treated with isoproterenol , and treatment with this metabolite at 100 μM under heat stress conditions induces the release of oxytocin from the mouse hypothalamus.[9],[4]