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Results for "

Ca2

" in MCE Product Catalog:

248

Inhibitors & Agonists

1

Screening Libraries

5

Dye Reagents

4

Biochemical Assay Reagents

38

Peptides

48

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • 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-136460
    Calcium ionophore I

    ETH 1001

    Calcium Channel Others
    Calcium ionophore I (ETH 1001) is a selective Ca 2+ ionophore for biological membranes. Calcium ionophore I can be used in Ca2+-selective microelectrodes that can be used for quantitative intracellular measurements of resting Ca2+-activities and of slowly changing Ca2+-levels.
  • 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-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-B0493
    Niflumic acid

    Chloride Channel Inflammation/Immunology
    Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.
  • HY-17403
    Manidipine dihydrochloride

    CV-4093

    Calcium Channel Cardiovascular Disease
    Manidipine dihydrochloride (CV-4093) is a dihydropyridine compound and a calcium channel blocker for Ca2+ current with IC50 of 2.6 nM.
  • HY-10588
    Bay K 8644

    Calcium Channel Neurological Disease
    Bay K 8644, a dihydropyridine compound, is a specific L-type Ca 2+ channel agonist. Bay K 8644 increases Ca2+ influx through sarcolemmal Ca 2+ channels by increasing the open time of the channel.
  • HY-P1479
    Calmodulin-Dependent Protein Kinase II (290-309)

    CaMK Autophagy Neurological Disease
    Calmodulin-Dependent Protein Kinase II (290-309) is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II.
  • HY-P1479A
    Calmodulin-Dependent Protein Kinase II(290-309) acetate

    CaMK Autophagy Neurological Disease
    Calmodulin-Dependent Protein Kinase II (290-309) acetate is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II.
  • HY-16639
    ML314

    Neurotensin Receptor Neurological Disease Endocrinology
    ML314 is a potent molecule agonist of NTR1 (EC50 = 1.9 μM); showed good selectivity against NTR2 and GPR35, but did not stimulate Ca2+ mobilization.
  • 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-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-103319
    Calmidazolium chloride

    R 24571

    CaMK Autophagy Cancer Neurological Disease
    Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to CaMK with a Kd of 3 nM.
  • 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-108592
    UCL 2077

    Others Neurological Disease
    UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization. UCL 2077 is also a subtype-selective blocker of the epilepsy associated KCNQ channels.
  • HY-12962
    NMDA-IN-1

    iGluR Neurological Disease
    NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
  • 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-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-P1075
    CALP3

    Calcium Channel Cancer Neurological Disease
    CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
  • HY-100298
    Caldaret

    MCC-135

    Na+/Ca2+ Exchanger Cardiovascular Disease
    Caldaret is an intracellular Ca 2+ handling modulator that acts through reverse mode Na +/Ca 2+ exchanger inhibition.
  • 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-P1075A
    CALP3 TFA

    Calcium Channel Cancer Neurological Disease
    CALP3 TFA, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
  • HY-101685
    Iganidipine

    Calcium Channel Cardiovascular Disease
    Iganidipine is a Ca 2+ antagonist.
  • HY-D1024
    Coelenterazine h

    2-Deoxycoelenterazine; CLZN-h

    Others Neurological Disease
    Coelenterazine h is a derivative of Coelenterazine. Coelenterazine 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.
  • HY-100718
    SCH00013

    Others Cardiovascular Disease
    SCH00013 is a cardiotonic agent that primarily acts via an increase in myofibrillar Ca++ sensitivity, have a significant Ca(2+)sensitizing effect at pH 7.2 to 7.4.
  • HY-101455
    CDN1163

    Calcium Channel Metabolic Disease
    CDN1163 is an allosteric sarco/endoplasmic reticulum Ca 2+-ATPase (SERCA) activator that improves Ca 2+ homeostasis. CDN1163 attenuates diabetes and metabolic disorders.
  • 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-B0596
    Taltirelin

    TA-0910

    Thyroid Hormone Receptor Neurological Disease Endocrinology
    Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
  • HY-17404
    Cilnidipine

    FRC-8653

    Calcium Channel Cardiovascular Disease
    Cilnidipine is a long-acting, second-generation dihydropyridine Ca 2+-channel blocker on L and N-type Ca 2+ channel. Antihypertensive 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-101428
    NS-638

    Calcium Channel Neurological Disease
    NS-638 is a small nonpeptide molecule with Ca 2+-channel blocking properties. K +-stimulated intracellular Ca 2+-elevation is blocked with an IC50 value of 3.4 μM.
  • HY-136283
    DMNPE-4 AM-caged-calcium

    Others Neurological Disease
    DMNPE-4 AM-caged-calcium, photolabile analogues of EGTA, is an extremely effective Ca 2+ selective cage, with a Kd for Ca 2+ of 48 nM and 19 nM at pH 7.2 and pH 7.4, respectively. DMNPE-4 AM-caged-calcium has a lower affinity for Ca 2+ (Kd=~2 nM) after photolysis.
  • HY-B0596A
    Taltirelin acetate

    TA-0910 acetate

    Thyroid Hormone Receptor Neurological Disease Endocrinology
    Taltirelin acetate (TA-0910 acetate) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
  • 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-113970A
    Nebracetam hydrochloride

    WEB 1881 FU hydrochloride

    mAChR Neurological Disease
    Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca 2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca 2+]i.
  • HY-19608
    GSK1016790A

    TRP Channel Calcium Channel Metabolic Disease Cardiovascular Disease
    GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca 2+ influx and elevate intracellular Ca 2+ in HEK cells.
  • 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-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-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-10171
    NPS-2143 hydrochloride

    SB-262470A hydrochloride

    CaSR Metabolic Disease
    NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
  • HY-10007
    NPS-2143

    SB-262470A

    CaSR Metabolic Disease
    NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
  • HY-W018035
    DL-Glyceric Acid

    Glyceric Acid (20% in Water,Ca.2 mol/L)

    Endogenous Metabolite Metabolic Disease
    DL-Glyceric Acid is a compound that is secreted excessively in the urine by patients suffering from D-glyceric aciduria.
  • HY-15293B
    JTV-519 hemifumarate

    K201 hemifumarate

    Calcium Channel Cardiovascular Disease
    JTV-519 hemifumarate (K201 hemifumarate) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
  • HY-75161
    (-)-Menthol

    TRP Channel Endogenous Metabolite Cancer
    (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca 2+-permeable nonselective cation channel, to increase [Ca 2+]i. Antitumor activity.
  • HY-113308A
    Taurolithocholic acid sodium salt

    Calcium Channel Metabolic Disease
    Taurolithocholic acid sodium salt, a potent cholestatic agent, is a potent Ca 2+ agonist.
  • 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-15293A
    JTV-519 free base

    K201 free base

    Calcium Channel Cardiovascular Disease
    JTV-519 free base (K201 free base) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
  • 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-U00026
    Semotiadil recemate fumarate

    Calcium Channel Cardiovascular Disease
    Semotiadil recemate fumarate is the recemate of Semotiadil fumarate. Semotiadil fumarate is a novel vasoselective Ca 2+ channel antagonist.
  • HY-133168
    Englerin A

    TRP Channel Cancer
    Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload.
  • HY-P0189
    ω-Conotoxin GVIA

    Calcium Channel Neurological Disease
    ω-Conotoxin GVIA is an inhibitor of the N-type Ca 2+ channel.
  • 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-U00212
    Aranidipine

    MPC1304

    Calcium Channel Cardiovascular Disease
    Aranidipine (MPC1304) is a Ca 2+ channel antagonist with potent and long-lasting antihypertensive effects.
  • HY-103660
    18:0 LYSO-PE

    Stearoyl lysophosphatidylethanolamine

    Others Neurological Disease
    18:0 LYSO-PE is an agent that can induce [Ca 2+]i increase.
  • HY-116330A
    Hyperforin dicyclohexylammonium salt

    Hyperforin DCHA

    TRP Channel Calcium Channel Neurological Disease
    Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
  • HY-19721
    ABT-639

    Calcium Channel Neurological Disease
    ABT-639 is a novel, peripherally acting, selective T-type Ca 2+ channel blocker.
  • 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-101616
    ABT-639 hydrochloride

    Calcium Channel Neurological Disease
    ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca 2+ channel blocker.
  • HY-101669
    TDN345

    Calcium Channel Neurological Disease
    TDN345 is a Ca 2+ antagonist, used for the treatment of vascular and senile dementia including Alzheimer's disease.
  • HY-136909
    SR33805

    Calcium Channel Cardiovascular Disease
    SR33805 is a potent Ca 2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca 2+ channels. SR33805 can be used for the research of acute or chronic failing hearts.
  • 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-101693A
    Senazodan hydrochloride

    MCI 154 hydrochloride

    Phosphodiesterase (PDE) Cardiovascular Disease
    Senazodan (MCI 154) (hydrochloride), as a Ca 2+ sensitiser, shows inhibition effect on PDE III.
  • HY-135897
    Urolithin C

    Calcium Channel Reactive Oxygen Species Apoptosis Endogenous Metabolite Metabolic Disease
    Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca 2+ channel opener and enhances Ca 2+ influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation.
  • 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-101693
    Senazodan

    MCI 154

    Phosphodiesterase (PDE) Cardiovascular Disease
    Senazodan (MCI 154) is a Ca 2+ sensitiser, and also shows inhibition effect on PDE III.
  • HY-19025
    CV-159

    Calcium Channel Inflammation/Immunology
    CV-159 is a unique dihydropyridine Ca 2+ antagonist with an anti-calmodulin (CaM) action, and has antiinflammatory activities.
  • HY-133596
    12,14-Dichlorodehydroabietic acid

    Potassium Channel GABA Receptor Neurological Disease
    12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release.
  • 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-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-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-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-12323
    ISX-9

    Isoxazole 9

    Calcium Channel Neurological Disease
    ISX-9 (Isoxazole 9) is a potent inducer of adult neural stem cell differentiation. ISX-9 activates Ca 2+ influx through both voltage-gated Ca 2+ channels and NMDA receptors and increases neuroD expression. ISX-9 also induces cardiomyogenic differentiation of Notch-activated epicardium-derived cells (NECs).
  • 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-108593
    BMS-191011

    BMS-A

    Potassium Channel Neurological Disease
    BMS-191011 (BMS-A) is an opener of the large-conductance, Ca 2+-activated potassium (maxi-K) channel, effective in stroke models.
  • HY-10388
    TTA-Q6

    Calcium Channel Neurological Disease
    TTA-Q6 is a selective T-type Ca 2+ channel antagonist, which can be used in the research of neurological disease.
  • 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-113308AS1
    Taurolithocholic Acid-d5 sodium salt

    Calcium Channel Metabolic Disease
    Taurolithocholic Acid-d5 sodium salt is the deuterium labeled Taurolithocholic acid sodium salt. Taurolithocholic acid sodium salt, a potent cholestatic agent, is a potent Ca 2+ agonist.
  • 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-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-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-131948
    3-Chlorodiphenylamine

    Potassium Channel Cardiovascular Disease
    3-Chlorodiphenylamine is a high affinity Ca 2+ sensitizer of cardiac muscle. 3-Chlorodiphenylamine is based on diphenylamine and binds to the isolated N-domain of cardiac troponin C (cTnC) (Kd=6 µM). 3-Chlorodiphenylamine is an excellent starting scaffold for the development of more potent Ca 2+-sensitizing compounds due to its small size, and can be used for systolic heart failure research.
  • HY-136395
    Cartap

    Others Others
    Cartap, an organonitrogen insecticide, can cause a marked irreversible Ca 2+-dependent contracture in both isolated mouse and rabbit phrenic nerve-diaphragms.
  • HY-15416
    NS309

    Potassium Channel Neurological Disease Cardiovascular Disease
    NS309 is a potent and selective activator of the Ca 2+-activated SK/IK potassium channels, but displays no activity at BK channels.
  • HY-W010451
    1,2,4-Trihydroxybenzene

    Calcium Channel Cardiovascular Disease
    1,2,4-Trihydroxybenzene (Hydroxyhydroquinone), a by-product of coffee bean roasting, increases intracellular Ca 2+ concentration in rat thymic lymphocytes.
  • HY-N7063
    Nerol

    Reactive Oxygen Species Fungal Mitochondrial Metabolism Apoptosis Endogenous Metabolite Infection
    Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca 2+ and ROS. Antifungal activity.
  • HY-131012
    GoSlo-SR-5-69

    Potassium Channel Others
    GoSlo-SR-5-69 is a potent activator of large conductance Ca 2+-activated K + (BK) channels, with an EC50 of 251 nM.
  • HY-10388A
    TTA-Q6(isomer)

    Others Others
    TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca 2+ channel antagonist.
  • HY-138620
    MCU-i4

    Mitochondrial Metabolism Metabolic Disease
    MCU-i4 blocks the IP3-dependent mitochondrial Ca 2+-uptake, maintaining the gatekeeping role of their target.
  • HY-131041
    Ned-K

    Calcium Channel Cardiovascular Disease
    Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist. Ned-K is effective at dampening simulated ischaemia and reperfusion (sIR)-induced Ca 2+ oscillations in cardiomyocytes.
  • 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-114400A
    TRPV4 agonist-1

    Inflammation/Immunology
    TRPV4 agonist-1 is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC50 of 60 nM in the hTRPV4 Ca 2+ assay.
  • HY-N2060
    Evocarpine

    Apoptosis Bacterial Cancer Infection Inflammation/Immunology
    Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca 2+ influx through voltage-dependent calcium channels. Antimycobacterial activity.
  • 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-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-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-120588
    CCR1 antagonist 8

    CCR Inflammation/Immunology Endocrinology
    CCR1 antagonist 8 (compound 19n), a third azaindazole series compound, is a CCR1 antagonist, with an IC50 of 1.8 nM in Ca 2+ flux assay.
  • HY-133614
    Dihydroisopimaric acid

    Potassium Channel Others
    Dihydroisopimaric acid activates large conductance Ca 2+ activated K + (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp.
  • HY-114400
    TRPV4 agonist-1 free base

    TRP Channel Inflammation/Immunology
    TRPV4 agonist-1 free base is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC50 of 60 nM in the hTRPV4 Ca 2+ assay.
  • 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-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-121604
    (Rac)-MEM 1003

    Calcium Channel Others
    (Rac)-MEM 1003 is the racemate of MEM 1003. MEM 1003, a dihydropyridine compound, is a potent L-type Ca 2+ channel antagonist and has the potential for Alzheimer’s disease research.
  • HY-15124
    (S)-(-)-Bay-K-8644

    Calcium Channel Cardiovascular Disease
    (S)-(-)-Bay-K-8644 is an agonist of L-type Ca 2+ channel. (S)-(-)-Bay-K-8644 activates Ba 2+ currents (IBa) (EC50=32 nM).
  • HY-131942
    sFTX-3.3

    Calcium Channel Neurological Disease
    sFTX-3.3 is a Ca 2+ channel antagonist with IC50s of approximately 0.24 mM and 0.70 mM against P-type and N-type channels.
  • HY-B0632
    Diltiazem

    Calcium Channel Cardiovascular Disease
    Diltiazem is an orally active L-type Ca 2+ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.
  • HY-P0188
    ω-Conotoxin MVIIC

    Calcium Channel Neurological Disease
    ω-Conotoxin MVIIC is a N- and P/Q-type Ca 2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.
  • 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-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-100783A
    (-)-Bicuculline methochloride

    l-Bicuculline methochloride

    GABA Receptor Neurological Disease
    (-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
  • HY-10167A
    Tecalcet Hydrochloride

    R-568 hydrochloride

    CaSR Others
    Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+.
  • HY-101017
    Palmitoylcarnitine chloride

    Endogenous Metabolite Cancer Inflammation/Immunology
    Palmitoylcarnitine chloride is a fatty acid-derived mitochondrial substrate, and selectively decreases cell survival in colorectal and prostate cancer cells by affecting on pro-inflammatory pathways, Ca 2+ influx, and DHT-like effects.
  • HY-P0188A
    ω-Conotoxin MVIIC TFA

    Calcium Channel Neurological Disease
    ω-Conotoxin MVIIC TFA is a N- and P/Q-type Ca 2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.
  • HY-15705
    GPR35 agonist 2

    Others Metabolic Disease Inflammation/Immunology
    GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC50s of 26 and 3.2 nM in the β-arrestin and Ca 2+ release assay, respectively.
  • HY-100783
    (-)-Bicuculline methobromide

    l-Bicuculline methobromide

    GABA Receptor Neurological Disease
    (-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
  • 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-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-B0493S
    Niflumic Acid-d5

    Chloride Channel Inflammation/Immunology
    Niflumic Acid-d5 is the deuterium labeled Niflumic acid. Niflumic acid, a Ca 2+-activated Cl - channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.
  • 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-116429
    Maresin 1

    Reactive Oxygen Species Inflammation/Immunology
    Maresin 1, produced by human Mφs from endogenous docosahexaenoic acid (DHA) and a specialized proresolving mediator, stimulates intracellular [Ca 2+] and secretion. Maresin 1 possesses anti-inflammatory activity.
  • 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-P0256
    Apamin

    Apamine

    Potassium Channel Inflammation/Immunology Neurological Disease
    Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca 2+-activated K + (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.
  • HY-137175
    TMBIM6 antagonist-1

    mTOR Cancer
    TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca 2+.
  • 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-135891
    AZD2423

    CCR Neurological Disease
    AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux [1].
  • 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-121186
    Bevantolol hydrochloride

    Adrenergic Receptor Calcium Channel Metabolic Disease Neurological Disease
    Bevantolol hydrochloride is a selective β1 and α1-adrenergic receptor antagonist with pKi values of 7.83, 6.9 in rat cerebral cortex, respectively. Bevantolol hydrochloride is a potent Ca 2+ antagonist.
  • HY-B0358A
    Flunarizine dihydrochloride

    Calcium Channel Sodium Channel Dopamine Receptor Neurological Disease
    Flunarizine dihydrochloride is a potent dual Na +/Ca 2+ channel (T-type) blocker. Flunarizine dihydrochloride is a D2 dopamine receptor antagonist. Flunarizine dihydrochloride, a diphenylpiperazine derivative, has the potential for peripheral vessels dilator and migraine prophylaxis.
  • 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-15553A
    Mibefradil dihydrochloride

    Ro 40-5967 dihydrochloride

    Calcium Channel Cardiovascular Disease
    Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) is a calcium channel blocker with moderate selectivity for T-type Ca 2+ channels (IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively).
  • 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-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-N5123
    α-L-Rhamnose

    Others Others
    α-L-Rhamnose is a terminal residue of steviol glycosides Dulcoside A and Dulcoside B. α-L-Rhamnose recognizing lectin site of human dermal fibroblasts functions as a signal transducer: modulation of Ca 2+ fluxes and gene expression.
  • HY-P0256A
    Apamin TFA

    Apamine TFA

    Potassium Channel Inflammation/Immunology Neurological Disease
    Apamin TFA (Apamine TFA) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca 2+-activated K + (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.
  • HY-15553
    Mibefradil

    Ro 40-5967

    Calcium Channel Cardiovascular Disease
    Mibefradil (Ro 40-5967) is a calcium channel blocker with moderate selectivity for T-type Ca 2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.
  • HY-110153
    NS19504

    Potassium Channel Neurological Disease
    NS19504 is a Ca 2+-activated K + channel (BK channel, KCa1.1 channel) activator (EC50=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.
  • 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-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-N0607
    Ginsenoside Ro

    Polysciasaponin P3; Chikusetsusaponin 5; Chikusetsusaponin V

    Calcium Channel Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Ginsenoside Ro (Polysciasaponin P3; Chikusetsusaponin 5; Chikusetsusaponin V) exhibits a Ca 2+-antagonistic antiplatelet effect with an IC50 of 155  μM. Ginsenoside Ro reduces the production of TXA2 more than it reduces the activities of COX-1 and TXAS.
  • HY-131614
    TPC2-A1-N

    Calcium Channel Others
    TPC2-A1-N is a powerful and Ca 2+-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca 2+ responses from TPC2 (EC50=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells.
  • 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-N0219
    Bicuculline

    (+)-Bicuculline; d-Bicuculline

    GABA Receptor Neurological Disease
    Bicuculline ((+)-Bicuculline; d-Bicuculline), as a convulsant alkaloid, is a competitive neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+-activated potassium (SK) channels and subsequently blocks the slow afterhyperpolarization (slow AHP) [1].
  • HY-15084B
    Dizocilpine

    MK-801

    iGluR Neurological Disease
    Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux.
  • 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-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-107855
    DL-Mevalonolactone

    (±)-Mevalonolactone; Mevalolactone

    Endogenous Metabolite Metabolic Disease
    DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca 2+ in the brain, besides inducing mitochondrial swelling.
  • 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-120528A
    GB-110 hydrochloride

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-P1366
    des-​Gln14-​Ghrelin

    GHSR Metabolic Disease
    des-Gln14-Ghrelin is a second endogenous ligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca 2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM.
  • 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-120528
    GB-110

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM.
  • 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-136190
    TRPC6-PAM-C20

    TRP Channel
    TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca 2+ concentrations ([Ca 2+]i) in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals.
  • HY-P1366A
    des-​Gln14-​Ghrelin TFA

    GHSR Metabolic Disease
    des-Gln14-Ghrelin TFA is a second endogenous ligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca 2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM.
  • 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-124873
    SERCA2a activator 1

    Calcium Channel Cardiovascular Disease
    SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.
  • 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-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-100973A
    Adenosine 5′-diphosphoribose sodium

    ADP ribose sodium

    TRP Channel Autophagy Endocrinology Metabolic Disease
    Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD +) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca 2+-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy.
  • 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-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-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-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) [1].
  • HY-129851
    NTP42

    Prostaglandin Receptor Cardiovascular Disease
    NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca 2+] mobilization following stimulation of cells with the alternative TP agonist U46609. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH).
  • HY-N4104
    Agaric acid

    Agaricinic Acid

    Mitochondrial Metabolism Metabolic Disease
    Agaric acid (Agaricinic Acid) is obtained from various plants of the fungous tribe, i.e. Polyporus officinalis and Polyporus igniarius. Agaric acid induces mitochondrial permeability transition through its interaction with the adenine nucleotide translocase. Agaric acid promotes efflux of accumulated Ca 2+, collapse of transmembrane potential, and mitochondrial swelling. Agaric acid is used to regulate lipid metabolism.
  • HY-P1437A
    Neuropeptide S(Mouse) TFA

    Neuropeptide Y Receptor
    Neuropeptide S(Mouse) TFA is a potent endogenous neuropeptide S receptor (NPSR) agonist (EC50=3 nM). Neuropeptide S(Mouse) TFA induces mobilization of intracellular Ca 2+. Neuropeptide S(Mouse) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Mouse) TFA also reduces anxiety-like behavior in mice.
  • HY-A0236A
    Aprindine hydrochloride

    Potassium Channel Cardiovascular Disease
    Aprindine hydrochloride is a class I-b anti-arrhythmic agent and a hERG channel blocker with an IC50 of 0.23 μM. Aprindine hydrochloride has inhibitory effects on Na +/Ca 2+ exchanger currents, which is partly responsible for their antiarrhythmic and cardioprotective effects. Aprindine hydrochloride is widely used for trial and ventricular tachyarrhythmias treatment research.
  • HY-13103
    NS 11021

    Potassium Channel Others
    NS 11021 is a potent and specific Ca 2+-activated big-conductance K + Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials.
  • 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-B1193
    Terfenadine

    (±)-Terfenadine; MDL-991

    Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis Cancer Inflammation/Immunology Endocrinology
    Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca 2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
  • 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-A0082
    Diphenidol hydrochloride

    Difenidol hydrochloride

    mAChR Sodium Channel Neurological Disease
    Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride is a potential drug of choice for experimental spinal anesthesia.
  • HY-16489A
    Terodiline hydrochloride

    mAChR Calcium Channel Neurological Disease
    Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence.
  • 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-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-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-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-P1792
    Angiotensin II (1-4), human

    Angiotensin Receptor Metabolic Disease Endocrinology
    Angiotensin II (1-4), human is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
  • 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-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-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-105189
    Meclinertant

    SR 48692

    Neurotensin Receptor Neurological Disease
    Meclinertant (SR 48692) is a potent, selective, nonpeptide and orally active neurotensin receptor 1 (NTS1) antagonist. In human colon carcinoma (HT-29) cells, Meclinertant competitively antagonizes neurotensin-induced intracellular Ca 2+ mobilization with a pA2 values of 8.13. Meclinertant has anxiolytic, anti-addictive and memory-impairing effects.
  • 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-P1397A
    RVD-Hpα TFA

    Cannabinoid Receptor
    RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
  • HY-P1792A
    Angiotensin II (1-4), human TFA

    Angiotensin Receptor Endocrinology Metabolic Disease
    Angiotensin II (1-4), human (TFA) is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
  • 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-103370
    Talniflumate

    BA 7602-06

    Chloride Channel Inflammation/Immunology
    Talniflumate (BA 7602-06) is the prodrug of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase. Talniflumate is an orally active Ca 2+-activated Cl - channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome.
  • HY-P1769
    Angiotensin II (5-8), human

    Angiotensin Receptor Metabolic Disease Endocrinology
    Angiotensin II (5-8), human is an endogenous C-terminal fragment of the peptide vasoconstrictor angiotensin II. Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
  • 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-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-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-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-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-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-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-B1193S
    Terfenadine-d3

    Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis Cancer Inflammation/Immunology Endocrinology
    Terfenadine-d3 ((±)-Terfenadine-d3) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca 2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
  • HY-14350
    AC-55541

    Protease-Activated Receptor (PAR) Others
    AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. AC-55541 has pEC50 values of 5.9 and 6.6 in PI hydrolysis assays and Ca 2+ mobilization assays and exhibits pronociceptive activity in vivo.
  • 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-115681
    (2R/S)-6-PNG

    6-Prenylnaringenin

    Calcium Channel Neurological Disease
    (2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca 2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice.
  • 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-15671
    GKA50

    Glucokinase Metabolic Disease
    GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats.
  • HY-131001
    DPNB-ABT594

    nAChR Neurological Disease
    DPNB-ABT594 is a nitrobenzyl-caged ABT594 (HY-14316A) and activates nAChRs containing the α4β2 subunits with good selectivity than the α7 subunit. DPNB-ABT594 can be used to map the distribution of nAChRs on neurons of the medial habenula (MHb) and helps to gain a deeper understanding of the nAChR‐mediated Ca 2+ signalling in the MHb.
  • HY-P1077
    CALP1

    Calcium Channel mGluR Phosphodiesterase (PDE) Apoptosis Inflammation/Immunology
    CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.
  • 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-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-107678
    SEN12333

    WAY-317538

    nAChR Neurological Disease
    SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca 2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research.
  • HY-P1077A
    CALP1 TFA

    Calcium Channel mGluR Phosphodiesterase (PDE) Apoptosis Inflammation/Immunology
    CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.
  • 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-N0081
    (±)-Praeruptorin A

    Calcium Channel Infection
    (±)-Praeruptorin A is the di-esterified product of cis-khellactone (CKL) and the major active ingredient in Peucedani Radix which consists of the dried roots of Peucedanum praeruptorumDunn (Apiaceae). (±)-Praeruptorin A has been widely employed as one of the famous traditional Chinese medicines (TCMs) for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper respiratory infections for centuries in China. (±)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker.
  • HY-B1671
    (+)-Kavain

    GABA Receptor Sodium Channel Calcium Channel Metabolic Disease Neurological Disease
    (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.
  • HY-15671A
    GKA50 quarterhydrate

    Glucokinase Metabolic Disease
    GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats.
  • 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-N0385
    Gomisin J

    AMPK Calcium Channel Metabolic Disease Cardiovascular Disease
    Gomisin J is a small molecular weight lignan found in Schisandra chinensis and has been demonstrated to have vasodilatory activity. Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca 2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells. gomisin J has potential benefits in treating nonalcoholic fatty liver disease.
  • 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-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-108496
    Sphingosine-1-phosphate

    S1P

    Endogenous Metabolite LPL Receptor Endocrinology
    Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca 2+ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids.
  • 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-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-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-133011
    nAChR agonist 1

    nAChR Neurological Disease
    nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
  • 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-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-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-P1345
    TLQP-21

    Complement System Endocrinology Neurological Disease
    TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.
  • 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-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-P1345A
    TLQP-21 TFA

    Complement System Endocrinology Neurological Disease
    TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.
  • 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.
  • 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-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.