1. Search Result
Search Result
Targets Recommended: CRAC Channel
Results for "

release

" in MCE Product Catalog:

271

Inhibitors & Agonists

3

Screening Libraries

3

Dye Reagents

1

Biochemical Assay Reagents

68

Peptides

59

Natural
Products

5

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-N3114
    Panaxydiol

    Histamine Receptor Inflammation/Immunology
    Panaxydiol exhibits histamine-release inhibition activity.
  • 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-103376
    NBI-27914 hydrochloride

    CRFR Neurological Disease
    NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with a Ki value of 1.7 nM.
  • HY-12206
    Thioperamide

    MR-12842

    Histamine Receptor Neurological Disease
    Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
  • HY-P1213
    JKC363

    Melanocortin Receptor Neurological Disease
    JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect.
  • HY-P1271
    Catestatin

    nAChR Cardiovascular Disease
    Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
  • HY-P1213A
    JKC363 TFA

    Melanocortin Receptor Neurological Disease
    JKC363 TFA, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC363 TFA blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect.
  • HY-P1271A
    Catestatin TFA

    nAChR Cardiovascular Disease
    Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
  • HY-N9337
    Amaroswerin

    NO Synthase Cancer Metabolic Disease Inflammation/Immunology
    Amaroswerin is a bioactive secoiridoid glucoside from Swertia mussotii. Amaroswerin has anti-inflammatory, antidiabetic, antiviral, anticholinergic and immunomodulatory activities. Amaroswerin inhibits NO release with an IC50 value of 5.42 μg/mL in RAW264.7 cells.
  • 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-W033577
    Tricarbonyldichlororuthenium(II) dimer

    CORM-2

    Others Inflammation/Immunology
    Tricarbonyldichlororuthenium(II) dimer is a pharmacological donor of CO releasing. CO releases from Tricarbonyldichlororuthenium(II) dimer prevents gastric mucosal oxidative damage induced by ischemia/reperfusion (I/R) improving gastric blood flow (GBF), decreasing DNA oxidation and inflammatory response on systemic level.
  • HY-135283
    ABT-546

    A-216546

    Endothelin Receptor Endocrinology Cardiovascular Disease
    ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively.
  • HY-100430
    CCF642

    Others Cancer
    CCF642 is a potent protein disulfide isomerases (PDI) inhibitor with an IC50 of 2.9 μM. CCF642 causes acute endoplasmic reticulum (ER) stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release. CCF642 has broad anti-multiple myeloma activity.
  • HY-114458
    Monooctyl succinate

    Others Others
    Monooctyl succinate is a monoester, which can be used as a surfactants and a potential fragrance releaser.
  • 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-P0089
    Human growth hormone-releasing factor

    Growth Hormone Releasing Factor human

    GHSR Endocrinology
    Human growth hormone-releasing factor (Growth Hormone Releasing Factor human) is a hypothalamic polypeptide and stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary.
  • 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-N4323
    14-Deoxyandrographolide

    Apoptosis Metabolic Disease
    14-Deoxyandrographolide, a bioactive compound of Andrographis paniculata, has hepatoprotective efficacy. 14-Deoxyandrographolide desensitizes hepatocytes to TNF-α-mediated apoptosis through the release of TNFRSF1A release.
  • HY-P0089A
    Human growth hormone-releasing factor TFA

    Growth Hormone Releasing Factor human TFA

    GHSR Endocrinology
    Human growth hormone-releasing factor TFA (Growth Hormone Releasing Factor human TFA) is a hypothalamic polypeptide and stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary.
  • HY-110129
    Eplivanserin hemifumarate

    SR-46349 hemifumarate; SR 46349B

    5-HT Receptor Neurological Disease
    Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
  • HY-10792
    Eplivanserin

    SR-46349

    5-HT Receptor Neurological Disease
    Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
  • HY-P2281
    Atrial natriuretic factor (1-28) (human, porcine)

    Atrial natriuretic peptide (1-28)

    Endogenous Metabolite Metabolic Disease Cardiovascular Disease
    Atrial natriuretic factor (1-28) (human, porcine) is a potent suppressor of pro-opiomelanocortin (POMC) mRNA but a weak inhibitor of βEP-LI release.
  • HY-P2004
    FFAGLDD

    MMP Cancer
    FFAGLDD is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.
  • HY-P2004A
    FFAGLDD TFA

    MMP Cancer
    FFAGLDD TFA is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.
  • HY-13571A
    Beclometasone dipropionate

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    Betamethasone dipropionate, the prodrug of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release.
  • HY-12961A
    Bretylium tosylate

    Others Neurological Disease
    Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
  • HY-W009350
    Diazolidinyl urea

    Bacterial Infection
    Diazolidinyl urea, a broad spectrum preservative, is a formaldehyde-releasing compound that releases formaldehyde through its decomposition. Diazolidinyl urea is effective against most contaminating microorganisms, especially Pseudomonas.
  • 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-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-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-N4117
    Hamamelitannin

    Bacterial Infection
    Hamamelitannin, a polyphenol extracted from the bark of Hamamelis virginiana, is a quorum-sensing (QS) inhibitor. Hamamelitannin increases antibiotic susceptibility of staphylococcus aureus biofilms by affecting peptidoglycan biosynthesis and eDNA release.
  • HY-101237
    DHBP dibromide

    Diheptylviologen dibromide

    Calcium Channel Neurological Disease Cardiovascular Disease
    DHBP dibromide is an inhibitor for calcium release and a muscle relaxant.
  • HY-128720
    Diethyl oxalpropionate

    Endogenous Metabolite Metabolic Disease
    Diethyl oxalpropionate is an intermediate for poly((R,S)-3,3-dimethylmalic acid) (PDMMLA) derivative synthesis. PDMMLA derivative can be used in synthesis of nanoparticles and study of warfarin encapsulation and controlled release.
  • HY-12521
    GSK-5498A

    CRAC Channel Inflammation/Immunology
    GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
  • HY-50760
    L-692585

    GHSR Endocrinology
    L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release.
  • HY-119332
    3-Keto petromyzonol

    Others Endocrinology
    3-Keto petromyzonol, a main component of Sea lamprey male sex pheromones, modulates both synthesis and release of gonadotropin releasing hormone (GnRH), and subsequently, hypothalamic-pituitary-gonadal (HPG) output in immature sea lamprey.
  • HY-B1404
    Nylidrin hydrochloride

    Buphenine hydrochloride

    Others Inflammation/Immunology
    Nylidrin hydrochloride was an effective inhibitor of IgE-mediated release of histamine from passively sensitized rat peritoneal mast cells and human basophils, and of IgG1-mediated release of histamine from passively sensitized guinea pig lung slices.
  • HY-16168A
    Degarelix

    GnRH Receptor Cancer Endocrinology
    Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
  • HY-B1197
    Amcinonide

    CL-34699

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    Amcinonide inhibit NO release from activated microglia with IC50 3.38 nM.
  • HY-B1158
    Imidazolidinyl urea

    Bacterial Infection
    Imidazolidinyl urea is an antimicrobial preservative used in cosmetics, acts as a formaldehyde releaser.
  • 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-B0564
    Sodium nitroprusside

    Ro 21-2498

    Others Cancer Cardiovascular Disease
    Sodium nitroprusside (Ro 21-2498) is a potent vasodilator working through releasing NO spontaneously in blood.
  • HY-P0086A
    Corticotropin-releasing factor (human) (acetate)

    Human CRF acetate; Human corticotropin-releasing factor acetate

    CRFR Neurological Disease
    Corticotropin-releasing factor human acetate (Human CRF acetate) stimulates the synthesis and secretion of adrenocorticotropin in the anterior pituitary.
  • HY-100305
    Substituted piperidines-1

    Others Endocrinology
    Substituted piperidines-1 is a compound that can promote the release of growth hormone in humans and animals.
  • HY-P0086
    Corticotropin-releasing factor (human)

    Human CRF; Human corticotropin-releasing factor

    CRFR Neurological Disease
    Corticotropin-releasing factor human (Human CRF) stimulates the synthesis and secretion of adrenocorticotropin in the anterior pituitary.
  • HY-14130
    CP 376395

    CRFR Neurological Disease Endocrinology
    CP 376395 is a potent and selective Corticotropin releasing factor 1 (CRF1) receptor antagonist.
  • HY-U00289
    opigolix

    GnRH Receptor Inflammation/Immunology Endocrinology
    Opigolix is a Gonadotropin-releasing hormone (GnRH) receptor antagonist, used for the research of endometriosis and rheumatoid arthritis.
  • HY-14367
    Emicerfont

    GW876008

    CRFR Neurological Disease Endocrinology
    Emicerfont is a corticotropin-releasing factor type 1 (CRF1) receptor antagonist with an IC50 of 66 nM.
  • HY-N0214
    Peimisine

    Ebeiensine

    mAChR Inflammation/Immunology
    Peimisine (Ebeiensine) non-competitively antagonizes tracheal smooth muscle muscarinic M receptor and inhibits smooth muscle contraction caused by Ach. Peimisine excits β-receptor, restrains the release of internal calcium, and promotes to releaseing NO in order to relax tracheal smooth muscle and relieve asthma.
  • HY-B1269
    Testosterone propionate

    Androgen Receptor Others
    Testosterone propionate is a slower releasing anabolic steroid used mainly in the treatment of low testosterone levels in men.
  • HY-P0195
    Bombesin

    Bombesin Receptor Metabolic Disease Neurological Disease
    Bombesin, a tetradecapeptide, plays an important role in the release of gastrin and the activation of G-protein receptors.
  • HY-P1558
    ACTH (11-24)

    Adrenocorticotropic Hormone (11-24)

    Melanocortin Receptor Inflammation/Immunology
    ACTH (11-24) is a fragment of adrenocorticotrophin, acts as an antagonist of adrenocorticotropic hormone (ACTH) receptor, and induces cortisol release.
  • HY-B0967
    Phthalylsulfacetamide

    Bacterial Infection
    Phthalylsulfacetamide is a sulfa drug, after oral administration, slowly decompose in the intestine,and release sulfacetamide ,generating antibacterial effect.
  • HY-101744
    Ipsalazide

    Autophagy Inflammation/Immunology
    Ipsalazide is a novel sulfasalazine analog designed to release 5-aminosalicylic acid and a nontoxic carrier molecule in the gastrointestinal tract.
  • HY-133025
    FK962

    Others Neurological Disease
    FK962 is an enhancer of somatostatin release, exerts cognitive-enhancing actions. Anti-dementia properties.
  • HY-106087
    IX 207-887

    Interleukin Related Inflammation/Immunology
    IX 207-887 is a novel antiarthritic agent which inhibits the release of interleukin-1 (IL-1).
  • HY-100143
    Pentiapine

    CGS 10746

    Dopamine Receptor Neurological Disease
    Pentiapine (CGS 10746) is a dopamine release inhibitor without binding to synaptic dopamine receptor sites.
  • HY-13534
    Abarelix

    R3827; PPI 149

    GnRH Receptor Cancer Endocrinology
    Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
  • HY-12131
    DMP 696

    Others Endocrinology Neurological Disease
    DMP 696 is a selective corticotropin-releasing hormone receptor 1 (CRHR1) antagonist, used for the treatment of anxiety and depression.
  • HY-101577
    NCX899

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    NCX899 is a NO-releasing derivative of enalapril, and shows inhibitory activity against angiotensin-converting enzyme (ACE) activity.
  • 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-U00364
    CI-949

    Histamine Receptor Prostaglandin Receptor Leukotriene Receptor Inflammation/Immunology Endocrinology
    CI-949 is an allergic mediator release inhibitor, which inhibits histamine, leukotriene C4/D4 (LTC4/LTD4), and thromboxane B2 (TXB2) release with IC50s of 11.4 μM, 0.5 μM and 0.1 μM, respectively.
  • HY-N7058
    cis-​Jasmone

    Others Others
    Cis-Jasmone is a plant-derived natural product. Cis-Jasmone is constitutively released by many flowers and sometimes by leaves as an attractant for pollinators or as a chemical cue for host location by insect flower herbivores. Cis-Jasmone treatment of crop plants not only induces direct defense against herbivores, but also induces indirect defense by releasing VOCs that attract natural enemies.
  • HY-P2320
    IDR-1

    Bacterial Infection Inflammation/Immunology
    IDR-1 is an antimicrobial peptide that is active against Gram-positive and Gram-negative bacteria. IDR-1 counters infection by selective modulation of innate immunity without obvious toxicities. IDR-1 has anti-inflammatory and anti-infective properties, enhances the levels of monocyte chemokines, and attenuates pro-inflammatory cytokine release.
  • HY-113331
    Thromboxane B2

    Others Inflammation/Immunology
    Thromboxane B2 is a prostaglandin derivative that is released during anaphylaxis. Thromboxane B2 induces arterial contraction and platelet aggregation.
  • HY-12339
    NVS-CRF38

    CRFR Endocrinology
    NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
  • HY-U00187
    NCX1022

    Others Inflammation/Immunology
    NCX1022 is an NO-releasing derivative of Hydrocortisone, which is the most widely used anti-inflammatory drug for the treatment of skin inflammation.
  • HY-B0194A
    Tizanidine hydrochloride

    Adrenergic Receptor Cancer Neurological Disease Endocrinology
    Tizanidine hydrochloride is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
  • HY-109804
    CORM-401

    Others Inflammation/Immunology
    CORM-401 is an oxidant-sensitive CO-releasing molecule, can be used in the research of inflammatory and oxidative stress-mediated pathologies.
  • HY-B0194
    Tizanidine

    Adrenergic Receptor Neurological Disease Endocrinology Cancer
    Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
  • HY-U00027
    Quinotolast sodium

    FR71021

    Histamine Receptor Leukotriene Receptor Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.
  • HY-133534
    PA-Nic TFA

    Others Others
    PA-Nic TFA is a photoactivatable nicotine, whcih can be photolyzed with ~405 nm laser flashes to efficiently release nicotine.
  • HY-N6928
    Mogroside III-E

    Others Cancer Metabolic Disease
    Mogroside III-E is a cucurbitane-type compound isolated from Siraitia grosvenorii, inhibits NO release, with anti-fibrotic activity.
  • HY-N0300
    Tetrahydropalmatine

    DL-Tetrahydropalmatine

    Dopamine Receptor Apoptosis Neurological Disease
    Tetrahydropalmatine possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
  • HY-N0472
    Geraniin

    TNF Receptor Cancer Metabolic Disease Inflammation/Immunology
    Geraniin is a TNF-α releasing inhibitor with numerous activities including anticancer, anti-inflammatory, and anti-hyperglycemic activities, with an IC50 of 43 μM.
  • HY-10978
    Crisaborole

    AN-2728; PF-06930164

    Phosphodiesterase (PDE) Inflammation/Immunology
    Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
  • HY-P0009B
    Cetrorelix diacetate

    SB-75 diacetate

    GnRH Receptor Endocrinology Neurological Disease
    Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
  • HY-P0009A
    Cetrorelix Acetate

    SB-75 acetate

    GnRH Receptor Neurological Disease Endocrinology
    Cetrorelix Acetate (SB-75 acetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
  • HY-13534A
    Abarelix Acetate

    PPI 149 Acetate; R 3827 Acetate

    GnRH Receptor Cancer Endocrinology
    Abarelix Acetate (PPI 149 Acetate; R 3827 Acetate) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer research.
  • HY-101757
    NO-prednisolone

    NCX-1015

    Interleukin Related Inflammation/Immunology
    NO-prednisolone is a nitric oxide (NO)-releasing derivative of Prednisolone. NO-prednisolone potently stimulates IL-10 production in vivo.
  • HY-19354
    Aglafoline

    Aglafolin; Rocaglamide U; (-)-Methyl rocaglate

    Others Cardiovascular Disease
    Aglafoline inhibits in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor).
  • HY-123454
    SKF1

    FKBP Reactive Oxygen Species Infection
    SKF1 is a FK506 suppressor, causes a mitochondrially induced death in low salt, concomitant with the release of reactive oxygen species (ROS).
  • HY-100209
    Sufugolix

    TAK-013

    Others Endocrinology
    Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
  • HY-12127
    Pexacerfont

    BMS-562086

    CRFR Neurological Disease Endocrinology
    Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1±0.6 nM for human CRF1 receptor.
  • HY-14789
    (R)-Elagolix

    NBI-56418

    GnRH Receptor Cancer Endocrinology
    Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
  • HY-N0300A
    Tetrahydropalmatine hydrochloride

    DL-Tetrahydropalmatine hydrochloride

    Dopamine Receptor Neurological Disease
    Tetrahydropalmatine (DL-Tetrahydropalmatine) hydrochloride possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
  • HY-U00168
    KP136

    AL136

    Histamine Receptor Inflammation/Immunology Endocrinology
    KP136 (AL136) is an orally effective antiallergic agent. The IC50 is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation.
  • HY-117178
    TA 0910 acid-type

    Others Metabolic Disease
    TA 0910 acid-type is a metabolite of TA 0910. TA-0910 is a metabolically stable analogue of thyrotropin releasing hormone (TRH).
  • HY-108590
    DMP-543

    XR-543

    Potassium Channel Neurological Disease
    DMP-543 (XR-543) is a KV7 channel blocker, also acts as a potent neurotransmitter release enhancer.
  • HY-11010
    AS601245

    JNK Cancer Inflammation/Immunology Neurological Disease
    AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties.
  • HY-N0127
    Yohimbine Hydrochloride

    Adrenergic Receptor Endocrinology
    Yohimbine Hydrochloride is an alpha 2-adrenoreceptor antagonist, blocking the pre- and postsynaptic alpha-2 adrenoreceptors and causing an increased release of noradrenaline and dopamine.
  • HY-N2339
    Cholesteryl behenate

    Cholesteryl docosanoate; Cholesterol behenate

    Endogenous Metabolite Metabolic Disease
    Cholesteryl behenate is a cholesterol ester associated with the neutral core of low density lipoprotein Receptor-LDL complexes are taken up by lysosomes and hydrolyzed to release cholesterol from the esters.
  • HY-12325
    GSK2194069

    Others Cancer
    GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM in an assay detecting released CoA.
  • HY-P0051
    Lecirelin

    GnRH Receptor Cancer Endocrinology
    Lecirelin, a synthetic gonadotropin-releasing hormone (GnRH) analogue, acts as a GnRH agonist. Lecirelin is widely used for the research of bovine ovarian follicular cysts.
  • HY-N7798
    Pennogenin

    Others Inflammation/Immunology
    Pennogenin is a bioactive component which can be isolated from T. govanianum rhizomes. Pennogenin exhibits significant in vitro inhibitory effect on release of ROS.
  • HY-B1582A
    Canrenoate potassium

    Aldadiene potassium; SC-14266

    Mineralocorticoid Receptor Cardiovascular Disease
    Canrenoate (Aldadiene) potassium, a prodrug that releases canrenone, is a potent, competitive mineralocorticoid receptor (aldosterone receptor) antagonist. Potassium canrenoate, as a diuretic, is used for the research of hypertension.
  • HY-15277
    AM966

    LPL Receptor Inflammation/Immunology
    AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM).
  • HY-19084
    Ro-24-0238

    Others Inflammation/Immunology
    Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF.
  • HY-107380A
    PGlu-3-methyl-His-Pro-NH2 TFA

    A-42872 TFA

    Others Endocrinology
    PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole.
  • HY-19363
    GW4869

    Phospholipase Inflammation/Immunology Cardiovascular Disease
    GW4869 is a noncompetitive neutral sphingomyelinase (N-SMase) inhibitor with an IC50 of 1 μM. GW4869 is an inhibitor of exosome biogenesis/release.
  • HY-U00170
    Bunaprolast

    U66858

    Leukotriene Receptor Prostaglandin Receptor Lipoxygenase Inflammation/Immunology Endocrinology
    Bunaprolast (U66858) is a potent inhibitor of LTB4 production in human whole blood. Bunaprolast (U66858) also exhibits significant inhibition of lipoxygenase and TXB2 release.
  • 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-14875
    Verucerfont

    GSK561679

    CRFR Neurological Disease Endocrinology
    Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively.
  • HY-14739
    Choline Fenofibrate

    ABT-335

    PPAR COX Cardiovascular Disease
    Choline Fenofibrate (ABT-335), a choline salt of Fenofibric acid (HY-B0760), releases free Fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect.
  • HY-133080
    BAY-784

    GnRH Receptor Cancer
    BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively.
  • HY-B1069
    Molsidomine

    SIN-10; Morsydomine

    Others Cardiovascular Disease
    Molsidomine is an orally active, long acting vasodilating drug, metabolized in the liver to the active metabolite linsidomine, which is an unstable compound that releases nitric oxide (NO) upon decay as the actual vasodilating compound.
  • HY-107632
    GYY4137

    Others Cancer Inflammation/Immunology Neurological Disease Cardiovascular Disease
    GYY4137 is a slow releasing H2S donor with vasodilator and antihypertensive activity. GYY4137 also exhibits anti-inflammatory and anticancer activity.
  • HY-B0323
    Sulfisoxazole

    Sulfafurazole

    Bacterial Endothelin Receptor Antibiotic Cancer Infection Endocrinology
    Sulfisoxazole (Sulfafurazole), an endothelin receptor antagonist, is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A.
  • HY-101161
    SG3199

    DNA Alkylator/Crosslinker ADC Cytotoxin Cancer
    SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PDB) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249).
  • HY-P2287
    Cortagine

    CRFR Neurological Disease
    Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.
  • HY-N2429
    Sphondin

    COX Inflammation/Immunology
    Sphondin possesses an inhibitory effect on IL-1β-induced increase in the level of COX-2 protein and PGE2 release in A549 cells.
  • 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-14804A
    Tasisulam sodium

    LY 573636 sodium

    Apoptosis Cancer
    Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization.
  • HY-P1752
    Urocortin II, human

    CRFR Metabolic Disease Endocrinology
    Urocortin II (human) is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. For investigating the role of the CRF (2) receptor in ingestive behavior.
  • HY-N2197
    Hirsuteine

    Others Neurological Disease
    Hirsuteine is an indole alkaloid extracted from Uncaria genus. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes.
  • HY-14608
    L-Glutamic acid

    Endogenous Metabolite iGluR Ferroptosis Apoptosis Neurological Disease
    L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  • HY-14804
    Tasisulam

    LY 573636

    Apoptosis Cancer
    Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization.
  • HY-B0194S
    Tizanidine-d4

    Adrenergic Receptor Neurological Disease Endocrinology Cancer
    Tizanidine-d4 is the deuterium labeled Tizanidine. Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
  • HY-W087952
    (R)-(-)-2-Butanol

    Others Metabolic Disease
    (R)-(-)-2-Butanol is released by the females of the white grub beetle, Dasylepida ishigakiensis, to attract males. (R)-(-)-2-Butanol is an intermediate of pharmaceutical synthesis by coupling.
  • HY-P1752A
    Urocortin II, human TFA

    CRFR Metabolic Disease Endocrinology
    Urocortin II, human (TFA) is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. For investigating the role of the CRF (2) receptor in ingestive behavior.
  • HY-14608A
    L-Glutamic acid monosodium salt

    Monosodium glutamate

    iGluR Apoptosis Ferroptosis Neurological Disease
    L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  • HY-U00462
    D-Mannoheptulose

    Others Metabolic Disease
    D-Mannoheptulose is a major non-structural carbohydrate in avocado. D-mannoheptulose is a specific inhibitor of D-glucose phosphorylation. D-Mannoheptulose can block insulin release and utilization of carbohydrate in rat.
  • HY-13673
    Goserelin

    ICI 118630

    GnRH Receptor Apoptosis Cancer Endocrinology
    Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
  • HY-P1747
    Pneumadin, rat

    PNM

    Others Metabolic Disease
    Pneumadin, rat (PNM) is a decapeptide, which possess a potent stimulating effect on arginine-vasopressin (AVP) release. Pneumadin, rat (PNM) exerts a marked antidiuretic effect in animals with functional AVP system.
  • HY-N2247A
    (+)-Guaiacin

    Others Metabolic Disease
    (+)-Guaiacin is a compound extracted of the bark of Machilus wangchiana Chun. (Lauraceae). (+)-Guaiacin shows potent in vitro activities against the release of β-glucuronidase in rat polymorphonuclear leukocytes (PMNs) induced by platelet-activating factor (PAF) .
  • HY-13673A
    Goserelin acetate

    ICI-118630 acetate

    GnRH Receptor Apoptosis Endocrinology Cancer
    Goserelin acetate (ICI-118630 acetate), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin acetate can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
  • HY-121885
    LMD-009

    CCR Metabolic Disease Endocrinology
    LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC50s from 11 to 87 nM.
  • HY-N1120
    Triptoquinone B

    (+)-Triptoquinone B

    Interleukin Related Inflammation/Immunology
    Triptoquinone B ((+)-Triptoquinone B), a sesquiterpene alkaloid, is an interleukin-1 inhibitor. Triptoquinone B shows potent inhibitory activities against interleukin 1α and β releases for human peripheral mononuclear cells.
  • HY-113920A
    Azumolene

    EU4093 free base

    Calcium Channel Metabolic Disease
    Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.
  • HY-120166
    DiFMUP

    6,8-Difluoro-4-methylumbelliferyl phosphate

    Others Others
    DiFMUP is a fluorogenic substrate, and has been widely used for the continuous detection of phosphatase activities. DiFMUP is hydrolysis by a phosphatase results in the release of Xuorescent DIFMU, which can be easily followed in continuous mode by a Xuorescence reader.
  • HY-N6996
    Methyl Eugenol

    Others Others
    Methyl Eugenol, a phenylpropanoid chemical in leaves, fruits, stems, and/or roots, may be released when that corresponding part of a plant is damaged as a result of feeding by an herbivore. Methyl Eugenol is used for male annihilation of the oriental fruit fly.
  • HY-136066
    Tauro-ω-muricholic acid sodium

    TωMCA sodium

    Others Metabolic Disease
    Tauro-ω-muricholic acid sodium (TωMCA sodium) is a bile acid released by the liver and an analog of tauro-α-muricholic acid. Tauro-ω-muricholic acid sodium is investigated as a potential marker in plasma for early-onset neonatal sepsis (EOS) and cholestasis studies
  • HY-108335
    Sipatrigine

    619C89; BW 619C89

    Sodium Channel Calcium Channel Neurological Disease
    Sipatrigine (619C89), a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has the potential in the study for focal cerebral ischemia and stroke.
  • HY-P0107A
    RC-3095 TFA

    Bombesin Receptor Inflammation/Immunology
    RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist. RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice.
  • HY-108661
    NF546

    P2Y Receptor Inflammation/Immunology
    NF546 is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells.
  • HY-12085
    Apremilast

    CC-10004

    Phosphodiesterase (PDE) Apoptosis TNF Receptor Inflammation/Immunology
    Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
  • HY-17043
    Loratadine

    Loratidine; SCH 29851

    Histamine Receptor Influenza Virus Infection Endocrinology Inflammation/Immunology
    Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
  • HY-136151
    UNC10217938A

    Others Others
    UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides.
  • HY-B0640A
    Epinastine hydrochloride

    WAL801 hydrochloride

    Histamine Receptor Endocrinology Inflammation/Immunology
    Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action.
  • HY-I1070
    D-Isoleucine

    (R)-Isoleucine

    Others Neurological Disease
    D-Isoleucine ((R)-Isoleucine), an isoleucine stereoisomer, is a selective activator of Asc-1 antiporter, which enhances long-term potentiation at the hippocampal CA1-CA3 via release of endogenous D-serine.
  • HY-N2600
    Kuwanon H

    Bombesin Receptor Cancer
    Kuwanon H is a flavonoid isolated from Morus bombycis, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells.
  • HY-W088037
    Tridecane

    Others Others
    Tridecane is a short chain aliphatic hydrocarbon containing 13 carbon atoms. Tridecane is an volatile oil component isolated from essential oil of Piper aduncum L. Tridecane is a stress compound released by the brown marmorated stink bugs stress compound.
  • HY-B0640
    Epinastine

    WAL801

    Histamine Receptor Inflammation/Immunology Endocrinology
    Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action.
  • HY-P1096
    A71623

    Cholecystokinin Receptor Metabolic Disease
    A71623 is a potent selective full agonist of CCKA receptor, with an IC50 of 3.7 nM in radioligand binding assays. A71623 can stimulate pancreatic amylase release and phosphoinositide breakdown in pancreas. A71623 suppresses food intake in vivo.
  • HY-B1350A
    Fusidic acid sodium salt

    Sodium fusidate; SQ-16360

    Bacterial Antibiotic Infection
    Fusidic acid sodium salt (Sodium fusidate), a bacteriostatic antibiotic produced from the Fusidium coccineum fungus, belongs to the class of steroids. Fusidic acid sodium salt has no corticosteroid effects. Fusidic acid sodium salt inhibits the growth of bacteria by preventing the release of translation elongation factor G (EF-G) from the ribosome.
  • HY-N2374
    Eupatorin

    Others Cancer
    Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage.
  • HY-B0402A
    Amantadine hydrochloride

    1-Adamantanamine hydrochloride; 1-Adamantylamine hydrochloride; 1-Aminoadamantane hydrochloride

    Influenza Virus Infection
    Amantadine (1-Adamantanamine) hydrochloride is an antiviral agent with activity against influenza A viruses. Amantadine hydrochloride blocks the proton flow through the M2 ion channel and thus prevents the release of viral RNA into the cytoplasm of the infected cells. Amantadine hydrochloride is an antiparkinsonian agent.
  • HY-B1350
    Fusidic acid

    Fusidate; SQ-16603

    Bacterial Antibiotic Infection
    Fusidic acid (Fusidate) a bacteriostatic antibiotic produced from the Fusidium coccineum fungus, belongs to the class of steroids. Fusidic acid has no corticosteroid effects. Fusidic acid inhibits the growth of bacteria by preventing the release of translation elongation factor G (EF-G) from the ribosome.
  • HY-12206A
    Thioperamide maleate

    MR-12842 maleate

    Histamine Receptor Neurological Disease
    Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide maleate inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
  • HY-A0150
    Alclometasone

    7a-​Chloro-​16a-​methyl prednisolone

    Glucocorticoid Receptor Inflammation/Immunology
    Alclometasone (7a-Chloro-16a-methyl prednisolone) is a glucocorticoid and inhibits the release of pro-inflammatory mediators from leukocytes. Alclometasone can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis, eczema, psoriasis and allergic dermatitis.
  • HY-P1298
    Sauvagine

    CRFR Endocrinology Neurological Disease Cardiovascular Disease
    Sauvagine, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine is effective at releasing ACTH from rat pituitary cells. Sauvagine possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
  • HY-N9536
    Cinnamtannin A2

    Others Metabolic Disease
    Cinnamtannin A2, a tetrameric procyanidin, can increases GLP-1 and insulin secretion in mice. Cinnamtannin A2 could upregulate the expression of corticotrophin releasing hormone. Cinnamtannin A2 exhibits antioxidant, anti-diabetic and nephroprotective effect.
  • HY-16261
    Aldoxorubicin

    INNO-206; DOXO-EMCH

    Topoisomerase ADC Cytotoxin Cancer
    Aldoxorubicin (INNO-206) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
  • HY-P0276
    GIP, human

    Gastric Inhibitory Peptide (GIP), human

    Insulin Receptor Metabolic Disease
    GIP, human, a peptide hormone consisting of 42 amino acids, is a stimulator of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. GIP, human acts as an incretin hormone released from intestinal K cells in response to nutrient ingestion.
  • HY-108295
    Pivagabine

    CXB-722

    GABA Receptor Neurological Disease
    Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain.
  • HY-100581
    CORM-3

    NF-κB NOD-like Receptor (NLR) Inflammation/Immunology
    CORM-3, a carbon monoxide-releasing molecule, attenuates NF-κB p65 nuclear translocation, reduces ROS generation and enhances intracellular glutathione and superoxide dismutase levels. CORM-3 reduces NLRP3 inflammasome activation.
  • HY-101942
    Zegocractin

    CM-4620

    CRAC Channel Neurological Disease
    Zegocractin (CM-4620) is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.
  • HY-17507
    Pantoprazole

    BY1023; SKF96022

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-17507B
    Pantoprazole sodium hydrate

    BY1023 sodium hydrate; SKF96022 sodium hydrate

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole sodium hydrate (BY10232 sodium hydrate) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium hydrate, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium hydrate improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium hydrate significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-17507A
    Pantoprazole sodium

    BY1023 sodium; SKF96022 sodium

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole sodium (BY10232 sodium) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-P0276A
    GIP, human TFA

    Gastric Inhibitory Peptide (GIP), human TFA

    Insulin Receptor Metabolic Disease
    GIP, human TFA, a peptide hormone consisting of 42 amino acids, is a stimulator of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. GIP, human TFA acts as an incretin hormone released from intestinal K cells in response to nutrient ingestion.
  • HY-P1298A
    Sauvagine TFA

    CRFR Endocrinology Neurological Disease Cardiovascular Disease
    Sauvagine TFA, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine TFA is effective at releasing ACTH from rat pituitary cells. Sauvagine TFA possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
  • HY-B2155
    Acotiamide monohydrochloride trihydrate

    AChE Metabolic Disease
    Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic receptor antagonism and acetylcholinesterase (AChE) inhibition, thereby enhancing gastric emptying and gastric accommodation.
  • HY-117432
    JC-171

    NOD-like Receptor (NLR) Inflammation/Immunology
    JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages.
  • HY-B0495
    Lamotrigine

    LTG; BW430C

    Sodium Channel Autophagy Neurological Disease
    Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na + channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al.
  • HY-100375
    Diroximel fumarate

    ALKS 8700; BIIB098

    Others Others
    Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) prodrug in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS).
  • HY-141510
    myo-Inositol trispyrophosphate hexasodium

    ITPP hexasodium

    Others Cancer
    myo-Inositol trispyrophosphate (ITPP) hexasodium, a modifier of haemoglobin, is an allosteric effector that reduces the oxygen‐binding affinity of haemoglobin and facilitates the release of oxygen by red blood cells. myo-Inositol trispyrophosphate can reverse hypoxia, control tumor growth and improve chemotherapy response.
  • HY-W011404
    Tributyrin

    Glyceryl tributyrate

    Apoptosis Metabolic Disease
    Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects.
  • HY-121955
    FW1256

    NF-κB Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    FW1256 is a phenyl analogue and a slow-releasing hydrogen sulfide (H2S) donor. FW1256 inhibits NF-κB activity and induces cell apoptosis. FW1256 exerts potent anti-inflammatory effects and has the potential for cancer and cardiovascular disease treatment.
  • 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-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-10936
    S 18986

    iGluR Neurological Disease
    S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
  • HY-136561
    GRK5-IN-2

    Others Metabolic Disease
    GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research.
  • HY-N8277
    Kdo2-Lipid A ammonium

    Toll-like Receptor (TLR) TNF Receptor Others
    Kdo2-Lipid A ammonium is a chemically defined lipopolysaccharide (LPS) with endotoxin activity equal to LPS. Kdo2-Lipid A ammonium is highly selective for TLR4. Kdo2-Lipid A ammonium stimulates the release of both TNF and PGE2.
  • HY-B1497
    Silver sulfadiazine

    AgSD

    Bacterial DNA/RNA Synthesis Antibiotic Infection
    Silver sulfadiazine (AgSD), a sulfonamide antibiotic, effects a dual inhibitory action on bacterial growth by its sulfa moiety (SD-SDZ) that prevents bacterial folate absorption and subsequent DNA synthesis. The silver that is released from Silver sulfadiazine binds and disrupts the DNA structure, precluding bacterial DNA replication.
  • HY-N0349
    Methyl Paraben

    Methyl 4-hydroxybenzoate

    Bacterial Endogenous Metabolite Infection
    Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, drugs and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity.
  • HY-139306
    BAMEA-O16B

    Others Inflammation/Immunology
    BAMEAO16B is a lipid nanoparticle. BAMEAO16B integrated with disulfide bonds, can efficiently deliver Cas9 mRNA and sgRNA into cells while releasing RNA in response to the reductive intracellular environment for genome editing. BAMEAO16B can be used for the research of gene editing.
  • HY-12085S
    Apremilast D5

    CC-10004 D5

    Phosphodiesterase (PDE) TNF Receptor Apoptosis Inflammation/Immunology
    Apremilast D5 (CC-10004 D5) is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
  • HY-N2350
    Cynaropicrin

    MMP NF-κB TNF Receptor Cancer
    Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
  • HY-N0646
    Silydianin

    Phosphatase Cancer
    Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38 μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products.
  • HY-18332C
    DOV-216,303 Free Base

    Serotonin Transporter Dopamine Transporter Neurological Disease
    DOV-216,303 (Free Base) is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats.
  • HY-W020468
    Linopirdine

    DuP 996

    Potassium Channel TRP Channel Neurological Disease
    Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.
  • HY-130592
    Compound 48/80 trihydrochloride

    C48/80 trihydrochloride

    Phospholipase Neurological Disease
    Compound 48/80 trihydrochloride (C48/80 trihydrochloride) is a mixture of condensation products of N-methyl-p-methoxyphenethylamine with formaldehyde. Compound 48/80 trihydrochloride is also a histamine releaser and a mast cell degranulator. Compound 48/80 inhibits phosphatidylinositol-specific phospholipase C activity from human platelets .
  • HY-P1422
    Spadin

    Potassium Channel Neurological Disease
    Spadin, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin binds specifically to TREK-1 with an affinity of 10 nM. Spadin is an efficient antidepressant in mice.
  • HY-119322
    Tifenazoxide

    NN414

    Potassium Channel Metabolic Disease
    Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective K ATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis.
  • HY-B1811
    Vasopressin

    Endogenous Metabolite Neurological Disease
    Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors.
  • HY-W008610
    GBR 12783

    Dopamine Receptor Neurological Disease
    GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats.
  • HY-103661
    BI-6C9

    Mitochondrial Metabolism Apoptosis Neurological Disease
    BI-6C9 is a highly specific BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from mitochondrial apoptosis inducing factor (AIF) release and caspase-independent cell death in neurons.
  • HY-112390A
    Syk Inhibitor II

    Syk 5-HT Receptor Inflammation/Immunology
    Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
  • HY-N7395
    Cyclic ADP-​ribose

    cADPR

    Calcium Channel TRP Channel Endogenous Metabolite Infection Endocrinology Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.
  • HY-N0157
    Orotic acid

    6-Carboxyuracil; Vitamin B13

    Nucleoside Antimetabolite/Analog Endogenous Metabolite Metabolic Disease
    Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats.
  • HY-101402
    Cyclo(his-pro)

    Cyclo(histidyl-proline); Histidylproline diketopiperazine

    NF-κB Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
  • HY-N6776
    Penitrem A

    Potassium Channel Cancer Neurological Disease
    Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.
  • HY-P1423A
    BA 1 TFA

    Bombesin Receptor Cancer Metabolic Disease
    BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM.
  • HY-N0157A
    Orotic acid zinc

    Nucleoside Antimetabolite/Analog Endogenous Metabolite Metabolic Disease
    Orotic acid (zinc), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid (zinc) is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid (zinc) can induce hepatic steatosis and hepatomegaly in rats.
  • HY-P1423
    BA 1

    Bombesin Receptor Cancer Metabolic Disease
    BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM.
  • HY-100968
    GBR 12783 dihydrochloride

    Dopamine Receptor Neurological Disease
    GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats.
  • HY-B1446
    Esomeprazole magnesium

    (S)-Omeprazole magnesium; (-)-Omeprazole magnesium

    Proton Pump Endocrinology
    Esomeprazole magnesium ((S)-Omeprazole magnesium) is a potent and orally active H +, K +-ATPase inhibitor. Esomeprazole magnesium has the potential for upper intestinal disorders and gastroesophageal reflux disease research. Esomeprazole magnesium acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H +-ATPases.
  • HY-19717
    DCVC

    S-[(1E)-1,2-dichloroethenyl]--L-cysteine

    TNF Receptor Inflammation/Immunology
    DCVC (S-[(1E)-1,2-dichloroethenyl]--L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures.
  • HY-101775A
    9-Hydroxyellipticine hydrochloride

    Topoisomerase Cancer Cardiovascular Disease
    9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC50 values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively.
  • HY-119307
    Apratastat

    MMP TNF Receptor Cancer
    Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively.
  • HY-138170
    ALC-0315

    Others SARS-CoV Infection
    ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine.
  • HY-D0162
    Malachite green oxalate

    IKK NF-κB Apoptosis Cancer
    Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo.
  • HY-N0392
    Polygalasaponin F

    Toll-like Receptor (TLR) PI3K Akt NF-κB Inflammation/Immunology
    Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway .
  • HY-109127
    Berotralstat

    Others Others
    Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.
  • HY-19026
    Siguazodan

    SKF 94836

    Phosphodiesterase (PDE) Cardiovascular Disease
    Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM.
  • HY-P1422A
    Spadin TFA

    Potassium Channel Neurological Disease
    Spadin TFA, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin TFA binds specifically to TREK-1 with an affinity of 10 nM. Spadin TFA is an efficient antidepressant in mice.
  • HY-P1858
    Urocortin III, mouse

    CRFR Neurological Disease Cardiovascular Disease Endocrinology
    Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2. Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics.
  • 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-101402A
    Cyclo(his-pro) TFA

    Cyclo(histidyl-proline) TFA; Histidylproline diketopiperazine TFA

    NF-κB Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
  • 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-P1858A
    Urocortin III, mouse TFA

    CRFR Neurological Disease Cardiovascular Disease Endocrinology
    Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2. Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics.
  • HY-N7395A
    Cyclic ADP-​ribose ammonium

    cADPR ammonium

    Calcium Channel TRP Channel Endogenous Metabolite Infection Endocrinology Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.
  • HY-N8160
    Dehydrocurdione

    Keap1-Nrf2 Reactive Oxygen Species Inflammation/Immunology
    Dehydrocurdione, a zedoary-derived sesquiterpene, induces heme oxygenase (HO)-1, an antioxidative enzyme, in RAW 264.7 macrophages. Dehydrocurdione interacts with Keap1, resulting in Nrf2 translocation followed by activation of the HO-1 E2 enhancer. Dehydrocurdione suppresses lipopolysaccharide-induced NO release, a marker of inflammation. Anti-inflammatory activity.
  • HY-Y0469
    1-Aminohydantoin hydrochloride

    Others Others
    1-Aminohydantoin hydrochloride is a major metabolite of nitrofurantoin in animal tissues and can be used as a standard for the determination of residues of veterinary agents in meat, milk et.al. 1-Aminohydantoin hydrochloride covalently binds to tissue proteins and is released from the tissues under slightly acidic conditions and derivatized with 2-nitrobenzaldehyde to form nitrophenyl derivatives of AHD before detection.
  • HY-P2090
    Angiopeptin

    Somatostatin Receptor Cardiovascular Disease
    Angiopeptin, a cyclic octapeptide analogue of somatostatin, markedly inhibits myointimal proliferation in response to endothelial cell injury. Angiopeptin is a potent and full agonists to inhibit adenylate cyclase or stimulate extracellular acidification through the sst2 or sst5 receptor. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 production.
  • HY-17022
    Esomeprazole magnesium trihydrate

    (S)-Omeprazole magnesium trihydrate; (-)-Omeprazole magnesium trihydrate

    Proton Pump Endocrinology
    Esomeprazole magnesium trihydrate ((S)-Omeprazole magnesium trihydrate) is a potent and orally active H +, K +-ATPase inhibitor. Esomeprazole magnesium trihydrate has the potential for upper intestinal disorders and gastroesophageal reflux disease research. Esomeprazole magnesium trihydrate acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H +-ATPases.
  • HY-N7056
    4'-Hydroxychalcone

    Proteasome Cancer Inflammation/Immunology
    4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.
  • HY-12203
    PFK-158

    Autophagy Apoptosis Cancer
    PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria.
  • HY-130354
    Dibutyryl-cGMP sodium

    Bt2cGMP sodium

    Potassium Channel Cardiovascular Disease
    Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels.
  • 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-17023
    Esomeprazole sodium

    (S)-Omeprazole sodium; (-)-Omeprazole sodium

    Proton Pump Endocrinology
    Esomeprazole sodium ((S)-Omeprazole sodium) is a potent and orally active proton pump inhibitor. Esomeprazole reduces acid secretion through inhibition of the H +, K +-ATPase in gastric parietal cells. Esomeprazole acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H +-ATPases. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research.
  • HY-128859
    EMT inhibitor-2

    Cytochrome P450 Metabolic Disease
    EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
  • HY-110135A
    NBI-31772 hydrate

    IGF-1R Neurological Disease
    NBI-31772 hydrate is a potent inhibitor of interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). NBI-31772 hydrate is also a nonpeptide ligand that releases bioactive IGF-I from the IGF-I/IGFBP-3 complex (Kis=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects.
  • HY-107794
    Clodronate disodium tetrahydrate

    Disodium clodronate tetrahydrate

    Others Inflammation/Immunology Neurological Disease
    Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain.
  • HY-13954
    A 839977

    P2X Receptor Neurological Disease Inflammation/Immunology
    A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
  • 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-N0074
    Byakangelicol

    COX Inflammation/Immunology
    Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory drug on airway inflammation.
  • HY-P1428
    RFRP-1(human)

    Neuropeptide Y Receptor Endocrinology
    RFRP-1(human) is a gonadotropin-inhibitory hormone (GnIH) homolog. RFRP-1(human) targets human gonadotropin-releasing hormone (GnRH) neurons and gonadotropes and potently inhibits gonadotropin. RFRP-1(human) is a potent Neuropeptide FF (NPFF) receptor agonist with EC50s of 0.0011 nM and 29 nM for NPFF2 and NPFF1, respectively.
  • 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-135674
    SR-318

    p38 MAPK TNF Receptor Cancer Inflammation/Immunology
    SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.
  • HY-P2543
    Neuropeptide Y (3-36) (human, rat)

    Neuropeptide Y Receptor Metabolic Disease
    Neuropeptide Y (3-36) (human, rat), a neuropeptide Y (NPY) metabolite formed from dipeptidyl peptidase-4 (DPP4), is a selective Y2 receptor agonist. Neuropeptide Y (3-36) (human, rat) is a NPY metabolite formed from dipeptidyl peptidase-4 (DPP4). Neuropeptide Y (3-36) (human, rat) decreases release of norepinephrine via the Y2 receptor.
  • HY-101092
    QS-21

    Stimulon

    NOD-like Receptor (NLR) Inflammation/Immunology
    QS-21, an immunostimulatory saponin, could be used as a potent vaccine adjuvant. QS-21 stimulates Th2 humoral and Th1 cell-mediated immune responses through action on antigen presenting cells (APCs) and T cells. QS-21 can activate the NLRP3 inflammasome with subsequent release of caspase-1 dependent cytokines, IL-1β and IL-18.
  • HY-100740C
    (1α,1'S,4β)-Lanabecestat

    (1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814

    Beta-secretase Neurological Disease
    (1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) is a Beta site APP Cleaving Enzymel (BACE1) inhibitor extracted from patent WO2012087237A1, compound 20a, has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively.
  • 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-100403
    Ro 67-7476

    mGluR Cancer
    Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM. Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM).
  • HY-101283
    HCH6-1

    Others Inflammation/Immunology
    HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases.
  • HY-126252
    A-9758

    ROR Interleukin Related Inflammation/Immunology
    A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation.
  • HY-127019
    Nigericin

    Sodium Channel NOD-like Receptor (NLR) Bacterial Apoptosis Antibiotic Cancer Infection
    Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K +/H + ionophore, promoting K +/H + exchange across mitochondrial membranes.Nigericin can be a NLRP3 activator that induces the release of IL-1β as a NALP3-dependent manner. Nigericin triggers eryptosis, an effect paralleled by ROS formation, and in part due to induction of oxidative stress. Nigericin triggers apoptosis.
  • HY-116141
    7-Hydroxycoumarinyl arachidonate

    7-HCA; Umbelliferyl Arachidonate; 7-HC-arachidonate

    Phospholipase MAGL Others
    7-Hydroxycoumarinyl arachidonate (7-HCA) is a fluorogenic substrate of cytosolic phospholipase A2 (PLA2). 7-Hydroxycoumarinyl arachidonate is also a fluorogenic substrate for monoacylglycerol lipase (MAGL). MAGL protein catalyzes the hydrolysis of 7-Hydroxycoumarinyl arachidonat to generate Arachidonic acid (AA) and the highly fluorescent 7-hydroxyl coumarin (7-HC; HY-N0573). Release of 7-HC can be measured using a fluorometer.
  • HY-13205
    Belnacasan

    VX-765

    Caspase Inflammation/Immunology
    Belnacasan (VX-765) is an orally bioactive prodrug of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM.
  • HY-19411
    SSR180711 hydrochloride

    nAChR Neurological Disease
    SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus.
  • HY-A0098
    Tunicamycin

    Bacterial Fungal Influenza Virus Antibiotic Cancer Infection Inflammation/Immunology
    Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity.Tunicamycin increases exosome release in cervical cancer cells.
  • HY-N1942
    5-O-Demethylnobiletin

    5-Demethylnobiletin

    Lipoxygenase Leukotriene Receptor Inflammation/Immunology Neurological Disease Cancer
    5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Sideritis tragoriganum, is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM.
  • HY-123857
    JNJ-55308942

    P2X Receptor Inflammation/Immunology Neurological Disease
    JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain.
  • 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-16474
    Relugolix

    TAK-385

    GnRH Receptor Cancer Endocrinology
    Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.
  • HY-19618
    BRD3308

    HDAC HIV Apoptosis Infection Metabolic Disease
    BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency.
  • HY-N2326
    (±)-Anatoxin A fumarate

    nAChR Neurological Disease
    (±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM).
  • HY-A0003B
    Lenalidomide hemihydrate

    CC-5013 hemihydrate

    Ligand for E3 Ligase Molecular Glue Apoptosis Cancer
    Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
  • HY-110220
    CIM0216

    TRP Channel Neurological Disease
    CIM0216, a synthetic TRPM3 ligand, acts as a potent and selective agonist of TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts in a TRPM3-dependent manner to induce pain and evoke neuropeptide release from sensory nerve terminals in vitro. CIM0216 is a powerful tool for studies of the physiological functions of TRPM3, and can be used for neurogenic inflammation research.
  • HY-122720
    SEC inhibitor KL-1

    KL-1

    Others Cancer
    SEC inhibitor KL-1 (KL-1), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-1 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 3.48 μM.
  • HY-123972
    SEC inhibitor KL-2

    KL-2

    Others Cancer
    SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM.
  • HY-123633
    4-Methylumbelliferyl β-D-Glucopyranoside

    Others
    4-Methylumbelliferyl β-D-Glucopyranoside, a β-D-glucoside, is a fluorogenic substrate for β-glucosidase, utilizes to assay β-glucosidase activity. 4-Methylumbelliferyl β-D-Glucopyranoside releases the highly fluorescent 4-methylumbelliferyl (4-MU), which has an emission maximum at 445-454 nm. The excitation maximum for 4-MU is pH-dependent: 330, 370, and 385 nm at pH 4.6, 7.4, and 10.4, respectively.
  • HY-A0003
    Lenalidomide

    CC-5013

    Ligand for E3 Ligase Molecular Glue Apoptosis Cancer Inflammation/Immunology
    Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
  • HY-117163
    FzM1.8

    Wnt β-catenin Cancer
    FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
  • 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-103286
    PD176252

    Bombesin Receptor Cancer
    PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
  • HY-A0003A
    Lenalidomide hydrochloride

    CC-5013 hydrochloride

    Ligand for E3 Ligase Molecular Glue Cancer Inflammation/Immunology
    Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
  • HY-103539
    3,5-Bis(4-nitrophenoxy)benzoic acid

    γ-secretase Metabolic Disease
    3,5-Bis(4-nitrophenoxy)benzoic acid is an inhibitor of γ-secretase. 3,5-Bis(4-nitrophenoxy)benzoic acid causes a decrease in the released levels of Aβ42 and notch-1 Aβ-like peptide 25 (Nβ25). 3,5-Bis(4-nitrophenoxy)benzoic acid, as a marker for fetal hypothyroidism, is a 3,3’-diiodothyronine sulfate (T2S) cross-reactive material in maternal serum.
  • HY-N6682
    Cytochalasin D

    Zygosporin A; NSC 209835

    Arp2/3 Complex Bacterial Antibiotic YAP Infection
    Cytochalasin D (Zygosporin A; NSC 209835) is a potent and cell-permeable inhibitor of actin polymerization derived from fungus, inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D (Zygosporin A; NSC 209835) also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells.Cytochalasin D can reduce exosome release, in turn reducing the amount of survivin present in the tumour environment. Cytochalasin D induces phosphorylation and cytoplasmic retention of YAP.
  • HY-70057
    Safinamide

    FCE 26743; EMD 1195686

    Monoamine Oxidase Neurological Disease
    Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
  • HY-122624
    MMP13-IN-2

    MMP Inflammation/Immunology
    MMP13-IN-2 is a potent, selective and orally active MMP-13 inhibitor. MMP13-IN-2 exhibits excellent potency for MMP-13 (IC50=0.036 nM) and selectivities (greater than 1,500-fold) over MMP-1, 3, 7, 8, 9, 14, and TACE. MMP13-IN-2 has the ability to block the release of collagen from cartilage in vitro. MMP13-IN-2 has the potential for collagenase related disease research.
  • HY-100008
    Peretinoin

    NIK333

    RAR/RXR SphK Autophagy HCV Cancer Infection
    Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM.
  • HY-70057A
    Safinamide mesylate

    FCE 26743 mesylate; EMD 1195686 mesylate

    Monoamine Oxidase Neurological Disease Cardiovascular Disease
    Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 nM). Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al.
  • HY-12403A
    Angiotensin (1-7) (acetate)

    Ang-(1-7) (acetate)

    Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Endocrinology Inflammation/Immunology Cardiovascular Disease
    Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium.
  • 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-12403
    Angiotensin (1-7)

    Ang-(1-7)

    Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease Endocrinology
    Angiotensin 1-7 (Ang-(1-7)) is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
  • HY-70057S
    Safinamide-d4

    Monoamine Oxidase Neurological Disease
    Safinamide-d4 (FCE 26743-d4) is the deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
  • HY-117937
    BC-1215

    Ligand for E3 Ligase Inflammation/Immunology
    BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCF Fbxo3 catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6. BC-1215, interacts with ApaG to profoundly inhibit secretion of a broad spectrum of TH1 panel cytokines from human PBMC.
  • HY-122818
    bpV(phen) trihydrate

    PTEN Phosphatase Parasite Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology
    bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.