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Antimalarial
Quinine is a primary alkaloid of various species of Cinchona, optical isomer of Quinidine and an anti-malarial, skeletal, muscle relaxant.- Claudia Alvarez Baron, .et al. , Sci Rep, 2025, Aug 16;15(1):29995 PMID: 40819150
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sodium-potassium pump inhibitor
Digoxin is a sodium-potassium pump inhibitor.- Ella Martin, .et al. , ACS Pharmacol Transl Sci, 2025, May 12;8(9):2996-3006 PMID: 40969890
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Ion channel blocker
Vernakalant Hcl is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.- Joe Z.Zhang, .et al. , Cell Stem Cell, 2019, 24, 1-10 PMID: 30880024
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Kir7.1 potassium channels blocker
ML418 is a selective, sub-micromolar pore blocker of Kir7.1 potassium channels. The inward rectifier potassium (Kir) channel Kir7.1 (KCNJ13) is a key regulator of melanocortin signaling in the brain, electrolyte homeostasis in the eye, and uterine muscle contractility during pregnancy.- Keisuke Obara, .et al. , Journal of Pharmacological Sciences, 2026, 160: 41-50
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Kv1.3 blocker
PAP-1 is a selective inhibitor of Kv1.3, voltage-gated potassium channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity.- Samuel Drinkall, .et al. , Glia, 2022, Jul;70(7):1301-1316 PMID: 35353387
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Potassium Channel Blocker
TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM). Exhibits 200-1500-fold selectivity over KV, BKCa, KCa2, Na+, CRAC and Cl- channels. Suppresses the reactivation of lymphocytes by mitogenic stimuli.- Samuel Drinkall, .et al. , Glia, 2022, Jul;70(7):1301-1316 PMID: 35353387
- Cheong Hoon Seo, .et al. , Transl Res, 2021, Apr 24 PMID: 33905948
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HIF-1α inhibitor
Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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Kir6.2/SUR inhibitor
Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus. - Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.
- Minoxidil (U-10858) is a selective ATP dependent K+ (Kir6) channel activator.
- Nateglinide(Starlix) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
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Potassium Channel inhibitor
Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell. -
iron mobilizer
Guanosine 5'-diphosphate disodium salt is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway. -
non-narcotic antitussive
Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect. -
OPRM1/OPRD1 agonist
ML335 (CYM 51010, CID-23723457) is an agonist for OPRM1(μ-opioid receptor)-OPRD1(δ-opioid receptor) heterodimerization with EC50 of 403 nM demonstrating selectivity over the individual OPRM1 and OPRD1 receptors and the serotonin HT5A receptor with EC50 of 14.9 μM, 1.1 μM, and >40 μM, respectively. - Eleclazine, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for treatment of coronary vasodilators, antiarrhythmics and vasodilators.
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KCNQ2/Q3 potassium channel activator
ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM. -
KCC2 inhibitor
VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells). -
HERG activator
RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes. -
mitoKATP channels
BMS-191095 is an activators of mitochondrial ATP-sensitive potassium (mitoKATP) channels. -
KATP activator
Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K+ channel (KATP) activator. -
Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.
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potassium currents blocker
Gliclazide is used as an antidiabetic. It is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
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Potassium Channel inhibitor
Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion. -
Serotonergic Receptor Antagonist
Hymenidin is a natural antagonist of serotonergic receptors, exhibiting significant inhibitory effects on voltage-gated potassium channels. This compound demonstrates the ability to induce apoptosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutics targeting serotonergic signaling pathways. Its dual action on ion channels and receptor antagonism positions Hymenidin as a noteworthy reagent for exploring complex cellular mechanisms in neurobiology and oncology. -
K+ Channels Activator
1-EBIO is an activator of Ca2+-sensitive K+ channels, playing a crucial role in the modulation of membrane potential and cellular excitability. This compound is utilized in research to investigate the physiological functions and pathophysiological roles of K+ channels, contributing to a deeper understanding of cellular signaling processes and potential therapeutic targets in various diseases. -
Anti-microbial Agent/Kir3.2 Blocker
3,6-Diaminoacridine hemisulfate is an acridine compound that functions primarily as a broad-spectrum antimicrobial agent and a Kir3.2 potassium channel blocker. Its mechanism involves insertion into bacterial DNA, thereby disrupting replication and transcription, which ultimately leads to bacterial lysis. Additionally, this compound is utilized in research to investigate the neurological phenotype associated with Down syndrome. Due to its ability to penetrate the stratum corneum and accumulate in the cell nucleus, prolonged exposure warrants caution due to potential oncogenic effects. -
Stable Isotope
Terfenadine-d3 is the deuterated form of Terfenadine, which primarily targets the hERG potassium channel as a potent open-channel blocker with an IC50 of 204 nM. As an H1 histamine receptor antagonist, Terfenadine-d3 demonstrates significant biological activity by inducing apoptosis in melanoma cells through the modulation of calcium homeostasis. Its mechanism includes the generation of reactive oxygen species (ROS) and the subsequent activation of caspases -4, -2, and -9, making it valuable for research in cancer biology and apoptosis pathways. -
HDAC inhibitor
HL23 is a histone deacetylase (HDAC) inhibitor with demonstrated efficacy against hepatocellular carcinoma (HCC). It enhances acetylation at the TXNIP promoter, leading to upregulation of TXNIP expression and modulation of potassium channel activity, ultimately inducing TXNIP-dependent potassium deprivation. HL23 effectively suppresses HCC progression and metastasis, and exhibits a synergistic antitumor effect when combined with Sorafenib, outperforming the combination of Sorafenib and Vorinostat in preclinical models. -
TNFα/IL-2 Inhibitor
Immuno modulator-1 is a potent inhibitor of TNFα and IL-2, displaying IC50 values of 4.7 nM and 26 nM, respectively, in human peripheral blood mononuclear cells (hPBMC). This compound is valuable for investigating immune response modulation and inflammatory pathways. Additionally, Immuno modulator-1 demonstrates a hERG potassium channel blocking effect, exhibiting a 20% inhibitory percentage at a concentration of 3 μM, making it relevant for studies involving cardiac safety profiles. -
Potassium Channel Inhibitor
Endoxifen Z-isomer hydrochloride is a selective potassium channel inhibitor that acts as a potent metabolite of Tamoxifen, exhibiting over 100-fold increased potency compared to its parent compound. This compound effectively inhibits PKCβ1 kinase activity, leading to decreased phosphorylation of AKT at Ser473 and its substrates, which ultimately promotes apoptosis. Endoxifen Z-isomer hydrochloride demonstrates significant anticancer effects, particularly against hormone-resistant metastatic breast cancer, making it a valuable reagent for cancer research applications. -
Stable Isotope
Trimebutine-d5 fumarate is a deuterium-labeled derivative of Trimebutine fumarate, functioning primarily as a multi-target inhibitor and opioid receptor agonist. This compound exhibits key biological activities, including the inhibition of L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa), which regulate calcium influx and potassium efflux. Additionally, Trimebutine-d5 fumarate targets Toll-like receptors, modulating inflammatory signaling pathways, and promotes apoptosis in tumor cells via the AKT/ERK pathway. Its applications are particularly relevant in the study of gastrointestinal disorders, including irritable bowel syndrome (IBS), due to its ability to inhibit excessive smooth muscle contraction. -
Progranulin secretion Activator
Progranulin modulator-1 is a selective activator of progranulin (PGRN) secretion. It significantly increases PGRN levels in BV-2 cells and exhibits low cytotoxicity with an EC50 value of 83 nM for PGRN. Additionally, Progranulin modulator-1 inhibits the hERG potassium channel with an IC50 of 3100 nM, making it a valuable tool for research on neuroinflammation and associated neurodegenerative disorders.

