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Targets Recommended: Na+/Ca2+ Exchanger
Results for "

CALY Inhibitors

" in MCE Product Catalog:

150

Inhibitors & Agonists

1

Screening Libraries

2

Biochemical Assay Reagents

18

Peptides

33

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-103350
    CA-074

    Cathepsin Cancer Neurological Disease
    CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
  • HY-112698
    CA-5f

    Autophagy Apoptosis Cancer
    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
  • HY-U00354
    CP-060

    Calcium Channel Cardiovascular Disease
    CP-​060 is a potent Ca 2+ antagonist, inhibits Ca 2+ overload and possesses antioxidant and cardioprotective activities.
  • HY-B1424
    Benzthiazide

    Carbonic Anhydrase Cardiovascular Disease Cancer
    Benzthiazide is a long-acting diuretic and a hypertension agent. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively. Benzthiazide also suppresses proliferation of cancer cells.
  • HY-100350
    CA-074 methyl ester

    CA-074Me

    Cathepsin Neurological Disease Cancer
    CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.
  • HY-15754
    CGP37157

    Na+/Ca2+ Exchanger Cancer Neurological Disease
    CGP37157 is a potent, selective inhibitor of Na +/Ca 2+ exchanger, inhibiting the Na +-induced Ca 2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM.
  • HY-15515
    SEA0400

    Na+/Ca2+ Exchanger Cardiovascular Disease
    SEA0400 is a novel and selective inhibitor of the Na +-Ca 2+ exchanger (NCX), inhibiting Na +-dependent Ca 2+ uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM.
  • HY-13513
    U-104

    SLC-0111

    Carbonic Anhydrase Cancer
    U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model.
  • HY-101093
    CA-170

    PD-1/PD-L1 Inflammation/Immunology
    CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of T cells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes.
  • HY-110243
    CAIX Inhibitor S4

    Carbonic Anhydrase Cancer
    CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth.
  • HY-13764
    Tetrandrine

    NSC-77037; d-Tetrandrine

    Calcium Channel Potassium Channel Cancer Inflammation/Immunology
    Tetrandrine (NSC-77037; d-Tetrandrine) is a bis-benzyl-isoquinoline alkaloid, which inhibits voltage-gated Ca 2+ current (ICa) and Ca 2+-activated K + current.
  • HY-14657
    Dantrolene sodium

    F 440

    Calcium Channel Metabolic Disease
    Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm.
  • HY-107658
    SN 6

    Na+/Ca2+ Exchanger Cardiovascular Disease
    SN 6 is a selective Na +/Ca 2+ exchanger (NCX) inhibitor, and inhibits 45Ca 2+ uptake by NCX1, NCX2, and NCX3, with IC50s of 2.9, 16, and 8.6 μM, respectively.
  • HY-14656
    Diltiazem hydrochloride

    CRD-401

    Calcium Channel Cardiovascular Disease
    Diltiazem hydrochloride is a Ca 2+ influx inhibitor (slow channel blocker or calcium antagonist).
  • HY-110105
    NS8593 hydrochloride

    Potassium Channel Neurological Disease
    NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
  • HY-B0109
    Dorzolamide

    L671152; MK507

    Carbonic Anhydrase Cancer
    Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
  • HY-B0109A
    Dorzolamide hydrochloride

    L671152 hydrochloride; MK507 hydrochloride

    Carbonic Anhydrase Others
    Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
  • HY-75839
    Dronedarone Hydrochloride

    Potassium Channel Autophagy Cardiovascular Disease
    Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na +, K + and Ca 2+ currents.
  • HY-100831
    YM-58483

    BTP2

    CRAC Channel Inflammation/Immunology
    YM-58483 (BTP2) is the first selective and potent inhibitor of CRAC channels and subsequent Ca 2+ signals. YM-584832 is a blocker of store-operated Ca 2+ entry (SOCE).
  • HY-P0189
    ω-Conotoxin GVIA

    Calcium Channel Neurological Disease
    ω-Conotoxin GVIA is an inhibitor of the N-type Ca 2+ channel.
  • HY-B0782S
    Acetazolamide D3

    Carbonic Anhydrase Cardiovascular Disease
    Acetazolamide D3 is deuterium labeled Acetazolamide, which is a potent carbonic anhydrase (CA) inhibitor.
  • HY-107319
    Almitrine mesylate

    Almitrine bismesylate; Almitrine bismethanesulfonate; Almitrine dimesylate

    Potassium Channel Neurological Disease Cardiovascular Disease
    Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca 2+-dependent K + channel.
  • HY-124594
    CA inhibitor 1

    GS-6207 analog

    HIV Infection
    CA inhibitor 1 (GS-6207 analog) is a potent HIV capsid inhibitor for HIV inhibition.
  • HY-41076
    Ca2+ channel agonist 1

    Calcium Channel CDK Neurological Disease
    Ca 2+ channel agonist 1 is an agonist of N-type Ca 2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
  • HY-P0189A
    ω-Conotoxin GVIA TFA

    Calcium Channel Neurological Disease
    ω-Conotoxin GVIA TFA is an inhibitor of the N-type Ca 2+ channel.
  • HY-16952A
    Bepridil hydrochloride hydrate

    (±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate

    Calcium Channel Cardiovascular Disease
    Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.
  • HY-N0601
    Ginsenoside Rf

    Panaxoside Rf

    Calcium Channel Endogenous Metabolite Cancer Neurological Disease
    Ginsenoside Rf is a trace component of ginseng root. Ginsenoside Rf inhibits N-type Ca 2+ channel.
  • HY-12498
    GV-58

    Calcium Channel Neurological Disease
    GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
  • HY-12596
    JNJ-26489112

    Calcium Channel Sodium Channel Potassium Channel Neurological Disease
    JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na + channels and N-type Ca 2+ channels, and is effective as a K + channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC50=35 μM) and CA-I (18 μM).
  • HY-B0782
    Acetazolamide

    Carbonic Anhydrase Autophagy Cardiovascular Disease Cancer
    Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX. Diuretic effects.
  • HY-B1546
    Benzamil

    Benzylamiloride

    Sodium Channel Na+/Ca2+ Exchanger Neurological Disease
    Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
  • HY-B1546A
    Benzamil hydrochloride

    Benzylamiloride hydrochloride

    Na+/Ca2+ Exchanger Sodium Channel Neurological Disease
    Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
  • HY-P1076
    CALP2

    Calcium Channel Phosphodiesterase (PDE) Inflammation/Immunology
    CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.
  • HY-B0109S
    Dorzolamide-d5

    Carbonic Anhydrase Cancer
    Dorzolamide-d5 (L671152-d5) is the deuterium labeled Dorzolamide. Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
  • HY-50694
    Senicapoc

    ICA-17043

    Potassium Channel Others
    Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca 2+-activated K + channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca 2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
  • HY-N1370
    Tanshinone IIA sulfonate sodium

    Sodium Tanshinone IIA sulfonate; Tanshinone IIA sodium sulfonate

    CRAC Channel Cardiovascular Disease Cancer
    Tanshinone IIA sulfonate (sodium) is a derivative of tanshinone IIA, which acts as an inhibitor of store-operated Ca 2+ entry (SOCE), and is used to treat cardiovascular disorders.
  • HY-19062
    SM-6586

    Calcium Channel Na+/Ca2+ Exchanger Cardiovascular Disease
    SM-6586 is a calcium channel antagonist and inhibitor of Na +/H + and Na +/Ca 2+ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.
  • HY-136182
    YM-244769 dihydrochloride

    Na+/Ca2+ Exchanger Neurological Disease
    YM-244769 dihydrochloride is a potent Na +/Ca 2+ exchange (NCX) inhibitor that preferentially inhibits NCX3 (IC50=18 nM). Neuronal and renal protection.
  • HY-P1076A
    CALP2 TFA

    Calcium Channel Phosphodiesterase (PDE) Inflammation/Immunology
    CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages.
  • HY-N1369
    Menthol

    Others Neurological Disease
    Menthol is a natural analgesic compound. Menthol could cause a feeling of coolness due to stimulation of ‘cold’ receptors by inhibiting Ca ++ currents of neuronal membranes.
  • HY-N7594
    Senecionine acetate

    O-Acetylsenecionine

    Mitochondrial Metabolism Others
    Senecionine acetate (O-Acetylsenecionine) is a pyrrolizidine alkaloid. Senecionine acetate inhibits the sequestration of Ca 2+ in extramitochondrial and mitochondrial compartments possibly by inactivating free sulfhydryl groups.
  • HY-N8493
    Mycalolide B

    Others Others
    Mycalolide-B is a specific inhibitor of actomyosin ATPase isolated from marine sponge. Mycalolide-B inhibits ATP-induced contraction and Mg 2+-ATPase activity in the absence of Ca 2+.
  • HY-N4237
    Saikogenin D

    Prostaglandin Receptor Potassium Channel Inflammation/Immunology
    Saikogenin D is isolated from Bupleurum chinense, has anti-inflammatory effects. Saikogenin D activates epoxygenases that converts arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and the metabolites secondarily inhibit prostaglandin E2 (PGE2) production. Saikogenin D results in an elevation of [Ca 2+]i due to Ca 2+ release from intracellular stores.
  • HY-120261
    GB-88

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca 2+ release with an IC50 of 2 µM.
  • HY-115595
    DS16570511

    Calcium Channel Neurological Disease
    DS16570511 is cell-permeable inhibitor of the mitochondrial calcium uniporter, which blocks the MCU- or MICU1-dependent increase of Ca 2+ influx.
  • HY-N0252
    Catharanthine

    (+)-3,4-Didehydrocoronaridine

    Calcium Channel Cancer Cardiovascular Disease
    Catharanthine is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca 2+ channel, with anti-cancer and blood pressure-lowering activity.
  • HY-108465
    Pyr3

    TRP Channel Others
    Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca 2+ influx.
  • HY-136189
    UK-59811 hydrochloride

    Calcium Channel Neurological Disease
    UK-59811 hydrochloride, a Br-dihydropyridine derivative, is a potent bacterial homotetrameric model voltage-gated Ca 2+ (CaV) channel CaVAb inhibitor with an IC50 of 194 nM.
  • HY-N0252A
    Catharanthine Tartrate

    (+)-3,4-Didehydrocoronaridine Tartrate

    Calcium Channel Cancer Cardiovascular Disease
    Catharanthine Tartrate is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca 2+ channel, with anti-cancer and blood pressure-lowering activity.
  • HY-120691A
    GSK205

    TRP Channel Metabolic Disease Inflammation/Immunology
    GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19  μM for inhibiting TRPV4-mediated Ca 2+ influx.
  • HY-128370
    Calcium trinatrium diethylenetriaminepentaacetic acid hydrate

    Ca-DTPA trisodium salt hydrate

    CMV Infection
    Calcium trinatrium diethylenetriaminepentaacetic acid hydrate (Ca-DTPA trisodium salt hydrate) is a metal chelator and a useful antidote (such as acute cadmium intoxication). Diethylenetriaminepentaacetic acid calcium trisodium salt hydrate is a nontoxic inhibitor of CMV replication.
  • HY-124416
    ML604086

    CCR Inflammation/Immunology Endocrinology
    ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrations.
  • HY-N4267
    Yangambin

    Calcium Channel Infection Cardiovascular Disease
    Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+ influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM.
  • HY-I0096
    Indole-2-carboxylic acid

    Endogenous Metabolite iGluR Neurological Disease
    Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current.
  • HY-103306
    Ryanodine

    Others Neurological Disease
    Ryanodine is a cell permeant ryanodine receptor modulator. Ryanodine can either stimulate or inhibit Ryanodine-mediated Ca 2+ release depending on its concentrations. Poisonous diterpenoid found in Ryania speciosa.
  • HY-P1079
    ω-Agatoxin TK

    Calcium Channel Neurological Disease
    ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca 2+ channel blocker. ω-Agatoxin TK inhibits the high K + depolarisation-induced rise in internal Ca 2+ in cerebral isolated nerve endings with an IC50 of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-type calcium channels.
  • HY-100402
    CFMTI

    mGluR Cancer
    CFMTI inhibits L-glutamate-induced intracellular Ca 2+ mobilization in CHO cells expressing human and rat mGluR1a, with IC50s of 2.6 and 2.3 nM, respectively.
  • HY-N6771
    Cyclopiazonic acid

    Calcium Channel Others
    Cyclopiazonic acid (CPA), a neurotoxic secondary metabolite (SM) made by A. flavus, is a nanomolar inhibitor of endoplasmic reticulum calcium ATPase (Ca 2+ATPase; SERCA) and a potent inducer of cell death in plants.
  • HY-12504
    Pyr6

    N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide

    TRP Channel Others
    Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).
  • HY-N6688
    Verruculogen

    Potassium Channel Bacterial Antibiotic Infection
    Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca 2+-activated K + channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle.
  • HY-120597
    SAK3

    Calcium Channel Neurological Disease
    SAK3 is a potent T-type voltage-gated Ca 2+ channels (T-VGCCs) enhancer. SAK3 enhances Cav3.1 and Cav3.3 T-type Ca 2+ channel currents. Acute SAK3 administration improves memory deficits in olfactory-bulbectomized mice. SAK3 inhibits amyloid β plaque formation in APP-KI mice by activating the proteasome activity.
  • HY-10341A
    Fasudil

    HA-1077; AT877

    ROCK Calcium Channel Autophagy PKA PKC Cancer
    Fasudil (HA-1077; AT877), is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca2+channel antagonist and vasodilator.
  • HY-P3278
    Caloxin 2A1

    Proton Pump Metabolic Disease
    Caloxin 2A1 is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 does not affect basal Mg 2+-ATPase or Na +-K +-ATPase.
  • HY-101015A
    OBAA

    Phospholipase Apoptosis Inflammation/Immunology
    OBAA is a potent phospholipase A2 (PLA2) inhibitor with an IC50 of 70 nM. OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei with an IC50 of 0.4 μM.
  • HY-P0271
    Syntide 2

    CaMK Calcium Channel Autophagy Neurological Disease
    Syntide 2, a Ca 2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected.
  • HY-111208
    CCT129957

    Phospholipase Cancer
    CCT129957 is an indole derivative and a potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of ~3 μM and a GC50 of 15 μM. CCT129957 inhibits Ca 2+ release in squamous carcinoma cells at ~15 μM.
  • HY-100886
    BAY1082439

    PI3K Apoptosis Cancer
    BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
  • HY-103316A
    Ned 19

    Calcium Channel Cancer
    Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca 2+ signaling, with an IC50 of 65 nM. Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice.
  • HY-108464A
    Phenamil methanesulfonate

    Sodium Channel TRP Channel Metabolic Disease Inflammation/Immunology
    Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
  • HY-128678
    ORM-10103

    Na+/Ca2+ Exchanger Cardiovascular Disease
    ORM-10103 is a specific inhibitor of the Na+/Ca2+ exchanger (NCX), which decreases the NCX current with estimated IC50s of 55 and 67 nM at -80 and at 20 mV, respectively.
  • HY-N0252B
    Catharanthine Sulfate

    (+)-3,4-Didehydrocoronaridine Sulfate

    Calcium Channel Cancer Cardiovascular Disease
    Catharanthine Sulfate ((+)-3,4-Didehydrocoronaridine Sulfate) is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca 2+ channel, with anti-cancer and blood pressure-lowering activities.
  • HY-P0271A
    Syntide 2 TFA

    CaMK Calcium Channel Neurological Disease
    Syntide 2 (TFA), a Ca 2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected.
  • HY-100779
    Rimacalib

    SMP 114

    CaMK Autophagy Metabolic Disease
    Rimacalib (SMP 114) is a Ca 2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.
  • HY-P3278A
    Caloxin 2A1 TFA

    Proton Pump Metabolic Disease
    Caloxin 2A1 TFA is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg 2+-ATPase or Na +-K +-ATPase.
  • HY-P1247
    Calcineurin autoinhibitory peptide

    Phosphatase Neurological Disease
    Calcineurin autoinhibitory peptide is a selective inhibitor of Ca 2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. Calcineurin autoinhibitory peptide could protect neurons from excitatory neuronal death.
  • HY-19408
    Pyr10

    TRP Channel Others
    Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels.
  • HY-P1080
    ω-Agatoxin IVA

    Calcium Channel Neurological Disease
    ω-Agatoxin IVA is a potent, selective P/Q type Ca 2+ channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ channels, respectively. ω-Agatoxin IVA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels.
  • HY-P1247A
    Calcineurin autoinhibitory peptide TFA

    Phosphatase Neurological Disease
    Calcineurin autoinhibitory peptide TFA is a selective inhibitor of Ca 2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. Calcineurin autoinhibitory peptide TFA could protect neurons from excitatory neuronal death.
  • HY-13433
    Thapsigargin

    Calcium Channel SARS-CoV Apoptosis Cancer Infection
    Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca 2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types.
  • HY-118467
    Benzolamide

    CL11366

    Carbonic Anhydrase Neurological Disease
    Benzolamide (CL11366) is a potent carbonic anhydrase (CA) inhibitor, with Kis of 15 nM, 9 nM, 94 nM and 78 nM for hCA I, hCA II, EcoCAγ and VchCAγ, respectively. Benzolamide also inhibits CAS3, with a Ki of 54 nM. Benzolamide can be used for the research of glaucoma and seizures.
  • HY-W009724
    2-Aminoethyl diphenylborinate

    2-APB

    Calcium Channel TRP Channel Others
    2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca 2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
  • HY-122898
    Ru360

    Calcium Channel Mitochondrial Metabolism Cardiovascular Disease
    Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca 2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects.
  • HY-107411
    Bromoenol lactone

    (6E)-Bromoenol lactone

    Phospholipase Inflammation/Immunology
    Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca 2+ influx.
  • HY-N2344
    Procyanidin A1

    Proanthocyanidin A1

    PKC Inflammation/Immunology
    Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.
  • HY-118630
    Vacuolin-1

    PIKfyve Autophagy Cancer
    Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca 2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation.
  • HY-P1250
    RFRP-3(human)

    Neuropeptide VF(124-131)(human)

    Neuropeptide Y Receptor Neurological Disease
    RFRP-3 (Neuropeptide VF(124-131))(human), a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca 2+ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 nM.
  • HY-P0190
    Iberiotoxin

    Potassium Channel Cardiovascular Disease
    Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.
  • HY-W013857
    Lavendustin C

    CaMK EGFR Src Cancer
    Lavendustin C is a potent Ca 2+ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC50 of 0.2 µM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC50=0.012 µM) and pp60 c-src(+) kinase (IC50=0.5 µM) .
  • HY-16690
    BTS

    N-Benzyl-p-toluenesulfonamide; N-Tosylbenzylamine

    Myosin Others
    BTS (N-Benzyl-p-toluenesulfonamide) is a potent and selective inhibitor of skeletal muscle myosin II subfragment 1 (S1) ATPase activity, with an IC50s of ~5 µM for actin- and Ca 2+-stimulated myosin S1 ATPase. BTS specifically inhibits the contraction of fast skeletal muscle fibers.
  • HY-P1250A
    RFRP-3(human) TFA

    Neuropeptide VF(124-131)(human) TFA

    Neuropeptide Y Receptor Neurological Disease
    RFRP-3 (Neuropeptide VF(124-131))(human) TFA, a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca 2+ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 nM.
  • HY-12949
    ML204

    TRP Channel Neurological Disease
    ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
  • HY-15415
    KB-R7943 mesylate

    Na+/Ca2+ Exchanger Autophagy Cancer
    KB-R7943 mesylate is a widely used inhibitor of the reverse Na +/Ca 2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.
  • HY-B0124A
    Zonisamide sodium

    AD 810 sodium; CI 912 sodium

    Carbonic Anhydrase Calcium Channel Sodium Channel Neurological Disease
    Zonisamide sodium (AD 810 sodium) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide sodium has antiepileptic activity. Zonisamide sodium can be used for the rsearch for epilepsy, seizures and Parkinson's disease.
  • HY-12949A
    ML204 hydrochloride

    TRP Channel Neurological Disease
    ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
  • HY-B1837A
    β-Cyfluthrin

    beta-Cyfluthrin

    Calcium Channel Neurological Disease
    β-Cyfluthrin (beta-Cyfluthrin) is a type II synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibiting Ca 2+ ATPase involved in calcium transport.
  • HY-B0124
    Zonisamide

    AD 810; CI 912

    Carbonic Anhydrase Calcium Channel Sodium Channel Neurological Disease
    Zonisamide (AD 810) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide has antiepileptic activity. Zonisamide can be used for the rsearch for epilepsy, seizures and Parkinson's disease.
  • HY-103442
    CGP52411

    DAPH

    EGFR Amyloid-β Cancer Neurological Disease
    CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
  • HY-103320A
    Calhex 231 hydrochloride

    CaSR Metabolic Disease
    Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca 2+-induced accumulation of [ 3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment.
  • HY-100202
    TPEN

    TPEDA

    Reactive Oxygen Species Apoptosis Autophagy Cancer
    TPEN (TPEDA) is a specific cell-permeable heavy metal chelator. TPEN has a higher affinity for Zn 2+, but a lower affinity for Mg 2+ and Ca 2+. TPEN induces DNA damage and increases intracellular ROS production. TPEN also inhibits cell proliferation and induces apoptosis.
  • HY-12728
    Tautomycin

    Phosphatase Inflammation/Immunology
    Tautomycin, an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus, is a potent and specific inhibitor of protein phosphatases 1 and 2A and induces contraction of smooth muscle under Ca 2+-free conditions, with Kiapp values of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively.
  • HY-19805
    STO-609

    CaMK AMPK Autophagy Metabolic Disease
    STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
  • HY-N6778
    Paxilline

    Potassium Channel Calcium Channel Neurological Disease
    Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca 2+ ATPase (SERCA) with IC50s between 5 μM and 50 μM for differing isoforms. Paxilline possesses significant anticonvulsant activity.
  • HY-B1471
    Fluorometholone acetate

    Carbonic Anhydrase Inflammation/Immunology
    Fluorometholone acetate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester. Fluorometholone acetate potently inhibits carbonic anhydrase (CA) with IC50s of 2.18 μM and 17.5 μM for hCA-I and hCA-II, respectively. Fluorometholone acetate has anti-inflammatory effect and has the potential for external ocular inflammation research.
  • HY-100912
    W-7 hydrochloride

    CaMK Phosphodiesterase (PDE) Myosin Apoptosis Cancer
    W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca 2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively. W-7 hydrochloride induces apoptosis and has antitumor activity.
  • HY-100545
    BAPTA-AM

    Potassium Channel Cardiovascular Disease
    BAPTA-AM is a well-known membrane permeable Ca 2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.
  • HY-B1221
    Flufenamic acid

    COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
  • HY-N6701
    Dihydrocytochalasin B

    Arp2/3 Complex Cancer
    Dihydrocytochalasin B (H2CB) is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport. Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis. Dihydrocytochalasin B (H2CB) inhibits active calcium transport and causes a Ca 2+increase in the mucosal scrapings.
  • HY-101379A
    8-Bromo-cGMP sodium

    Calcium Channel Neurological Disease Cardiovascular Disease
    8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator. 8-Bromo-cGMP sodium significantly inhibits Ca 2+ macroscopic currents and impairs insulin release stimulated with high K +. 8-Bromo-cGMP sodium has antinociceptive effects and results in vasodilator responses.
  • HY-N6687
    Calcimycin

    A-23187; Antibiotic A-23187

    Bacterial Fungal Apoptosis Autophagy Antibiotic Cancer Infection
    Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin induces apoptosis.
  • HY-16697
    CID 16020046

    GPR55 Cancer
    CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.
  • HY-13898
    Taselisib

    GDC-0032; RG-7604

    PI3K Cancer
    Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
  • HY-16689
    VU 0240551

    Potassium Channel Others
    VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca 2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission.
  • HY-135746
    OR-1896

    Potassium Channel Phosphodiesterase (PDE) Drug Metabolite Apoptosis Cardiovascular Disease
    OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K + channels and has Ca 2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.
  • HY-12496
    NS-1619

    Potassium Channel Apoptosis Cancer Cardiovascular Disease
    NS-1619 is an opener of large conductance Ca 2+-activated K + (BK) channel. NS-1619 is a highly effective relaxant with an EC50 of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells.
  • HY-114252
    Strophanthidin

    Na+/K+ ATPase Cardiovascular Disease
    Strophanthidin is a naturally available cardiac glycoside. Strophanthidin 0.1 and 1 nmol/L increases and 1~100 µmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal. Strophanthidin increases both diastolic and systolic intracellular Ca 2+ concentration.
  • HY-N6732
    K-252a

    SF2370; Antibiotic K 252a; Antibiotic SF 2370

    PKC PKA CaMK Trk Receptor Autophagy Antibiotic Infection Inflammation/Immunology
    K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
  • HY-105118A
    Zaldaride maleate

    CGS-9343B; KW 5617

    nAChR Metabolic Disease Inflammation/Immunology Neurological Disease
    Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR.
  • HY-100560
    Abscisic acid

    (S)​-​(+)​-​Abscisic acid; ABA

    Endogenous Metabolite Proton Pump Metabolic Disease
    Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome.
  • HY-N6687B
    Calcimycin hemimagnesium

    A-23187 hemimagnesium; Antibiotic A-23187 hemimagnesium

    Bacterial Fungal Apoptosis Autophagy Cancer Infection
    Calcimycin (A-23187) hemimagnesium is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemimagnesium induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemimagnesium inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemimagnesium also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemimagnesium induces apoptosis.
  • HY-16992A
    W-54011

    Complement System Reactive Oxygen Species Inflammation/Immunology
    W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively.
  • HY-B0193A
    Prazosin hydrochloride

    Adrenergic Receptor Autophagy Cardiovascular Disease Endocrinology Cancer
    Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.
  • HY-N6687A
    Calcimycin hemicalcium salt

    A-23187 hemicalcium salt; Antibiotic A-23187 hemicalcium salt

    Bacterial Fungal Apoptosis Autophagy Antibiotic Cancer Infection
    Calcimycin hemicalcium salt (A-23187 hemicalcium salt) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemicalcium salt induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemicalcium salt inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemicalcium salt also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemicalcium salt induces apoptosis.
  • HY-123205
    Oxatomide

    Histamine Receptor P2X Receptor 5-HT Receptor Inflammation/Immunology
    Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca 2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.
  • HY-100414
    Soraprazan

    BYK61359

    Proton Pump Metabolic Disease
    Soraprazan (BYK61359) is a selective, reversible K-competitive inhibitor of the H,K-ATPase (Ki=6.4 nM), with an IC50 of 0.19 μM in gastric glands. Soraprazan binds to the H,K-ATPase with a Kd of 28.27 nM. Soraprazan shows immediate inhibition of acid secretion and is more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases.
  • HY-108232
    MK-2206

    Akt Autophagy Apoptosis Cancer
    MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. Anticancer activities.
  • HY-126010
    Dooku1

    Others Cardiovascular Disease
    Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca 2+-entry with IC50 values of 1.3 μM (in HEK 293 cells) and 1.5 μM (in HUVECs). Dooku1 inhibits Yoda1-induced relaxation of aorta.
  • HY-N2359
    Chelerythrine

    PKC Bcl-2 Family Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology
    Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.
  • HY-125836
    CCR4 antagonist 2

    CCR Cancer Endocrinology
    CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.
  • HY-129440
    N-(p-Coumaroyl) Serotonin

    PDGFR Metabolic Disease Inflammation/Immunology
    N-(p-Coumaroyl) Serotonin is a polyphenol isolated from the seeds of safflower and has antioxidative, anti-atherogenic and anti-inflammatory properties. N-(p-Coumaroyl) Serotonin inhibits PDGF-induced on phosphorylation of PDGF receptor and Ca 2+ release from sarcoplasmic reticulum. N-(p-Coumaroyl) Serotonin ameliorates atherosclerosis and distensibility of the aortic wall in vivo and is usually used for the atherosclerosis research.
  • HY-B0124S
    Zonisamide-d4

    Carbonic Anhydrase Calcium Channel Sodium Channel Neurological Disease
    Zonisamide-d4 (AD 810-d4) is the deuterium labeled Zonisamide. Zonisamide (AD 810) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide has antiepileptic activity. Zonisamide can be used for the rsearch for epilepsy, seizures and Parkinson's disease.
  • HY-N2500
    Deoxypodophyllotoxin

    Microtubule/Tubulin Apoptosis Autophagy Infection Cardiovascular Disease
    Deoxypodophyllotoxin (DPT), a derivative of podophyllotoxin, is a lignan with potent antimitotic, anti-inflammatory and antiviral properties isolated from rhizomes of Sinopodophullumhexandrum (Berberidaceae). Deoxypodophyllotoxin, targets the microtubule, has a major impact in oncology not only as anti-mitotics but also as potent inhibitors of angiogenesis. Deoxypodophyllotoxin induces cell autophagy and apoptosis. Deoxypodophyllotoxin evokes increase of intracellular Ca 2+ concentrations in DRG neurons.
  • HY-131040
    NLRP3-IN-NBC6

    NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor (IC50= 574 nM) that acts independently of Ca 2+. NLRP3-IN-NBC6 inhibits Nigericin (HY-127019)-induced inflammasome activation in THP-1 cells and Imiquimod (HY-B0180)-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs).
  • HY-100001
    SKF-96365 hydrochloride

    TRP Channel CRAC Channel Potassium Channel Autophagy Apoptosis Cancer Cardiovascular Disease
    SKF-96365 hydrochloride is a potent TRP channel blocker and a store-operated Ca 2+ entry (SOCE) inhibitor. SKF-96365 hydrochloride significantly inhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3 current, and significantly prolongs the QTc interval in isolated guinea pig hearts. SKF-96365 hydrochloride exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells.
  • HY-10341
    Fasudil Hydrochloride

    HA-1077 Hydrochloride; AT-877 Hydrochloride

    ROCK Calcium Channel Autophagy PKA PKC HIV Cancer
    Fasudil Hydrochloride (HA-1077 Hydrochloride; AT877 Hydrochloride), is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator.
  • HY-101906
    DC260126

    GPR40 Apoptosis Metabolic Disease
    DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca 2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively). DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis.
  • HY-N1584
    Halofuginone

    RU-19110

    DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Cancer Infection Inflammation/Immunology Cardiovascular Disease
    Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
  • HY-126750
    GNF362

    Phosphatase Inflammation/Immunology
    GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca 2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4].
  • HY-N0043
    Ginsenoside Rd

    Gypenoside VIII

    NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease Cancer
    Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
  • HY-137458
    Vevorisertib

    ARQ 751

    Akt Cancer
    Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations.
  • HY-103309A
    ML218 hydrochloride

    Calcium Channel Neurological Disease
    ML218 hydrochloride is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 hydrochloride inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 hydrochloride has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 hydrochloride can penetrate the blood-brain barrier.
  • HY-15244
    Alpelisib

    BYL-719

    PI3K Cancer
    Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.
  • HY-103309
    ML218

    Calcium Channel Neurological Disease
    ML218 is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier.
  • HY-N1584A
    Halofuginone hydrobromide

    RU-19110 hydrobromide

    DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Cancer Infection Inflammation/Immunology Cardiovascular Disease
    Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
  • HY-N3945
    Glaucine

    O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396

    Phosphodiesterase (PDE) Calcium Channel Adrenergic Receptor Dopamine Receptor Influenza Virus Infection Inflammation/Immunology
    Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca 2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities.
  • HY-N1940
    β-Anhydroicaritin

    Interleukin Related TNF Receptor MMP Inflammation/Immunology
    β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
  • HY-120072
    PF-3450074

    PF-74

    HIV Infection
    PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
  • HY-15724A
    Vercirnon sodium

    GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium

    CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
  • HY-15724
    Vercirnon

    GSK-1605786; CCX282-B; Traficet-EN

    CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
  • HY-101044
    PPADS tetrasodium

    P2X Receptor Na+/Ca2+ Exchanger Neurological Disease
    PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca²⁺exchanger in guinea pig airway smooth muscle.
  • HY-N0515
    Ophiopogonin D

    PPAR NF-κB Calcium Channel Inflammation/Immunology Cardiovascular Disease
    Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.