1. Search Result

Search Result

Results for "Ang (1-5) Inhibitors" in MCE Product Catalog:

606

Inhibitors & Agonists

3

Screening Libraries

3

Biochemical Assay Reagents

45

Peptides

1

MCE Kits

62

Natural
Products

8

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-P1488
    Bradykinin (1-5)

    Bradykinin Receptor Cardiovascular Disease Endocrinology
    Bradykinin (1-5) is a major stable metabolite of Bradykinin, formed by the proteolytic action of angiotensin-converting enzyme (ACE).
  • HY-P1126
    Dolastatin 15

    DLS 15

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin.
  • HY-110284
    BAM 15

    Others Others
    BAM 15 is a novel mitochondrial protonophore uncoupler.
  • HY-12797
    GF 15

    Others Cancer
    GF 15 is a potent inhibitor of centrosomal clustering in tumor cells.
  • HY-100828
    BGP-15

    PARP Cardiovascular Disease Cancer
    BGP-15 is a PARP inhibitor, with an IC50 and a Ki of 120 and 57 μM, respectively.
  • HY-124899
    Hh-Ag1.5

    SAg1.5

    Hedgehog Metabolic Disease
    Hh-Ag1.5 (SAg1.5) is a potent Hedgehog (Hh) agonist with an EC50 of 1 nM. Hh-Ag1.5 mediated reprogramming breaks the quiescence of noninjured liver stem cells for rescuing liver failure.
  • HY-113336B
    (±)15-HETE

    PROTAC Linker Cancer
    (±)15-HETE is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-101120
    666-15

    Epigenetic Reader Domain Cancer
    666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.
  • HY-125465
    SLLN-15

    Autophagy Cancer
    SLLN-15 is an oral active, selective and potent enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC).
  • HY-104031
    tCFA15

    Notch Neurological Disease
    tCFA15 is a trimethyl cyclohexenonic long chain fatty alcohol containing 15 carbon atoms on the side chain, promotes the differentiation of neurons, and may regulates Notch signaling.
  • HY-135679
    DHODH-IN-15

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-15 (Compound 7b) is a hydroxyfurazan analog of A771726. DHODH-IN-15 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 11 μM for rat liver DHODH. DHODH-IN-15 can be used for rheumatoid arthritis.
  • HY-N6681
    15-Acetoxyscirpenol

    Caspase Bacterial Apoptosis Antibiotic Infection
    15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3.
  • HY-W015422
    1,5-Isoquinolinediol

    PARP Metabolic Disease
    1,5-Isoquinolinediol is a potent PARP inhibitor, with an IC50 of 0.18-0.37 µM. 1,5-Isoquinolinediol attenuates diabetes-induced NADPH oxidase-derived oxidative stress in retina.
  • HY-113075
    1,5-Anhydrosorbitol

    Endogenous Metabolite Metabolic Disease
    1,5-Anhydrosorbitol is a short-term marker for glycemic control.
  • HY-102049
    IL-15-IN-1

    Interleukin Related Inflammation/Immunology
    IL-15-IN-1 is a potent and selective Interleukin 15 (IL-15) inhibitor, inhibiting the proliferation of IL-15-dependent cells with an IC50 of 0.8 μM.
  • HY-128428
    Carboprost

    15(S)-15-Methyl Prostaglandin F2α; 15-Methyl-PGF2α

    Others Endocrinology
    Carboprost (15(S)-15-Methyl Prostaglandin F2α) is a metabolically stable synthetic analog of prostaglandin F2α. Carboprost stimulates uterine contractions and induces abortion. Carboprost is used for postpartum hemorrhage due to uterine atony and for the termination of pregnancy in the second trimester.
  • HY-103476
    Ro15-4513

    GABA Receptor Neurological Disease
    Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect.
  • HY-N6683
    15-Acetyl-deoxynivalenol

    Drug Metabolite Cancer
    15-Acetyl-deoxynivalenol is a highly toxic trichothecene found in cereals, and a metabolite of deoxynivalenol, exhibits toxicity to HepG2 cells.
  • HY-103449
    G15

    Estrogen Receptor/ERR Cancer
    G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
  • HY-15948
    Kif15-IN-1

    Kinesin Cancer Inflammation/Immunology Cardiovascular Disease
    Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member 15 (Kif15), and is used for the research of cellular proliferative diseases.
  • HY-100441
    Treprostinil

    LRX-15

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Treprostinil (LRX-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
  • HY-15949
    Kif15-IN-2

    Kinesin Inflammation/Immunology Cardiovascular Disease Cancer
    Kif15-IN-2 is an inhibitor of the mitotic kinesin Kif15, and is used for the research of cellular proliferative diseases.
  • HY-100437
    HA15

    HSP Autophagy Apoptosis Cancer
    HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.
  • HY-W016750
    Pentane-1,5-diamine dihydrochloride

    Endogenous Metabolite Metabolic Disease
    Pentane-1,5-diamine dihydrochloride is an endogenous metabolite.
  • HY-B2087S
    Glycerol phenylbutyrate-D15

    HPN-100-D15

    Sigma Receptor Cardiovascular Disease
    Glycerol phenylbutyrate-D15 is a deuterium labeled Glycerol phenylbutyrate. Glycerol phenylbutyrate is a sigma-2 (σ2) receptor ligand, with a pKi of 8.02. Glycerol phenylbutyrate (GPB) is a new generation ammonia scavenger drug.
  • HY-101807
    Ro-15-2041

    Phosphodiesterase (PDE) Cardiovascular Disease
    Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties.
  • HY-P1521
    β-Amyloid 15-21

    Beta-Amyloid (15-21)

    Amyloid-β Neurological Disease
    β-amyloid (15-21) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.
  • HY-141023
    Bis-PEG15-acid

    PROTAC Linker Cancer
    Bis-PEG15-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-17567C
    Heparin sodium salt (MW 15kDa)

    Sodium heparin (MW 15kDa); Sodium heparinate (MW 15kDa)

    Thrombin Factor Xa Autophagy Cardiovascular Disease
    Heparin sodium salt (MW 15kDa) (Sodium heparin (MW 15kDa)) is a polymer of Heparin with the molecular weight of 15kDa. Heparin sodium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin factor IIa and factor Xa.
  • HY-120724
    HO-PEG15-OH

    PROTAC Linker Cancer
    HO-PEG15-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-133397
    Azido-PEG15-azide

    PROTAC Linker Cancer
    Azido-PEG15-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141221
    m-PEG15-alcohol

    PROTAC Linker Cancer
    m-PEG15-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-108568
    15-Deoxy-Δ-12,14-prostaglandin J2

    15d-PGJ2; 15-Deoxy-Δ12,14-PGJ2

    PPAR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM.
  • HY-125873
    KRAS G12C inhibitor 15

    Ras Cancer
    KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 22, has an IC50 of 5 nM.
  • HY-128879
    VP3.15

    Phosphodiesterase (PDE) GSK-3 Neurological Disease
    VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
  • HY-P1046
    β-Amyloid 1-15

    Amyloid β-Protein (1-15)

    Amyloid-β Neurological Disease
    β-Amyloid (1-15) is a fragment of β-Amyloid peptide. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
  • HY-N7384
    Vitamin B15

    PAngamic Acid

    Others Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Vitamin B15 (Pangamic Acid) is a natural, ubiquitously in plant seeds substance and can used be as an agent stimulating cellular respiration. Vitamin B15 contains D-gluconodimethyl amino acetic acid. Vitamin B15 is also a immune-correcting agent. Vitamin B15 can be used for wide range of diseases.
  • HY-130829
    m-PEG15-NHS ester

    PROTAC Linker Cancer
    m-PEG15-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140238
    Cbz-N-PEG15-amine

    PROTAC Linker Cancer
    Cbz-N-PEG15-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-133356
    Boc-NH-PEG15-azide

    PROTAC Linker Cancer
    Boc-NH-PEG15-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-P1301
    [Arg14,Lys15]Nociceptin

    Opioid Receptor Neurological Disease
    [Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.
  • HY-109017
    Vamorolone

    VBP15

    Glucocorticoid Receptor Mineralocorticoid Receptor NF-κB Inflammation/Immunology
    Vamorolone (VBP15) is a first-in-class, orally active dissociative steroidal anti-inflammatory drug and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone shows potent NF-κB inhibition and substantially reduces hormonal effects.
  • HY-N4326
    14,15 β-Dihydroxyklaineanone

    Others Cancer
    14,15 D-dihydroxyklaineanone, a quassinoid isolated from the root of Eurycoma longifolia, possesses anti-cancer activity.
  • HY-128879A
    VP3.15 dihydrobromide

    Phosphodiesterase (PDE) GSK-3 Neurological Disease
    VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
  • HY-140783
    Azido-PEG15-t-butyl ester

    PROTAC Linker Cancer
    Azido-PEG15-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-P1301A
    [Arg14,Lys15]Nociceptin TFA

    Opioid Receptor
    [Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.
  • HY-140235
    Boc-NH-PEG15-NH2

    PROTAC Linker Cancer
    Boc-NH-PEG15-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-133329
    Amino-PEG15-amine

    H2N-PEG15-CH2CH2NH2

    PROTAC Linker Cancer
    Amino-PEG15-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-13989
    b-AP15

    NSC 687852

    Deubiquitinase Apoptosis Cancer
    b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
  • HY-10969A
    Obatoclax

    GX15-070

    Bcl-2 Family Autophagy Parasite Cancer Infection
    Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.
  • HY-135330
    Lamivudine 13C,15N2

    HIV Reverse Transcriptase Infection
    Lamivudine 13C,15N2 is a labelled impurity of Lamivudine (BCH-189). Lamivudine is a nucleoside reverse transcriptase inhibitors (NRTIs), and can inhibit HIV reverse transcriptase 1/2 and the reverse transcriptase of hepatitis B virus.
  • HY-125906
    VHL Ligand-Linker Conjugates 15

    E3 Ligase Ligand-Linker Conjugates 56

    E3 Ligase Ligand-Linker Conjugate Cancer
    VHL Ligand-Linker Conjugates 15 incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 15 can be used to design PROTACs.
  • HY-N0164
    Matrine

    Matridin-15-one; Vegard; α-Matrine

    Opioid Receptor Autophagy Mitophagy Cancer
    Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor and u-receptor agonist.
  • HY-I0301
    D-(+)-Glucono-1,5-lactone

    Gluconic acid lactone

    Endogenous Metabolite Reactive Oxygen Species Others
    D-(+)-Glucono-1,5-lactone is a polyhydroxy (PHA) that is capable of metal chelating, moisturizing and antioxidant activity.
  • HY-42776
    NH2-PEG3-C2-NH-Boc

    PROTAC Linker 15

    PROTAC Linker Cancer
    NH2-PEG3-C2-NH-Boc (PROTAC Linker 15) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-P1340
    [Ala11,D-Leu15]-Orexin B(human)

    Orexin Receptor (OX Receptor) Neurological Disease
    [Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM).
  • HY-128813
    cIAP1 Ligand-Linker Conjugates 15

    E3 ligase Ligand-Linker Conjugates 34

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 15 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 can be used to design SNIPERs.
  • HY-133706S
    2-Nitrobenzaldehyde semicarbazone 13C,15N2

    Others Others
    2-Nitrobenzaldehyde semicarbazone 13C,15N2 is used for analysis of semicarbazide in the LC-MS/MS method.
  • HY-15323
    PRT062607 Hydrochloride

    P505-15 Hydrochloride

    Syk Cancer
    PRT062607 Hydrochloride (P505-15 Hydrochloride) is a highly specific and potent inhibitor of purified Syk (IC50 1-2 nM).
  • HY-12444
    Y15

    FAK Inhibitor 14

    FAK Cancer
    Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
  • HY-P1340A
    [Ala11,D-Leu15]-Orexin B(human) TFA

    Orexin Receptor (OX Receptor) Neurological Disease
    [Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM).
  • HY-128813A
    cIAP1 Ligand-Linker Conjugates 15 hydrochloride

    E3 ligase Ligand-Linker Conjugates 34 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 15 hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 hydrochloride can be used to design SNIPERs.
  • HY-133361
    Fmoc-NH-PEG15-CH2CH2COOH

    PROTAC Linker Cancer
    Fmoc-NH-PEG15-CH2CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-10969
    Obatoclax Mesylate

    GX15-070 Mesylate

    Bcl-2 Family Autophagy Parasite Cancer Infection
    Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.
  • HY-N0788
    Indaconitine

    15-Deoxyaconitine

    Others Neurological Disease
    Indaconitine is a natural product.
  • HY-N0562
    5,15-Diacetyl-3-benzoyllathyrol

    Euphorbia factor L3

    Others Cancer
    5,15-Diacetyl-3-benzoyllathyrol is one of the lathyrane diterpenoids, that has anti-cancer activity.
  • HY-112735
    Hexadimethrine bromide

    1,5-Dimethyl-1,5-diazaundecamethylene polymethobromide

    Others Cancer
    Hexadimethrine bromide is a cationic polymer discovered to enhance retroviral transduction.
  • HY-P1019A
    [Ala1,​3,​11,​15]​-​Endothelin (53-63) (TFA)

    Endothelin Receptor Cardiovascular Disease Endocrinology
    [Ala1,3,11,15]-Endothelin (53-63) (TFA), a linear peptide analog of endothelin (ET)-1, is a highly selective endothelin B (ETB) receptor.
  • HY-N1974
    Fuziline

    15α-Hydroxyneoline

    Others Cardiovascular Disease
    Fuziline is a alkaloid isolated from the lateral roots of Aconitum carmichaelii.
  • HY-100248
    Sarmazenil

    Ro 15-3505

    GABA Receptor Neurological Disease
    Sarmazenil is a benzodiazepine receptor antagonist.
  • HY-14892
    Gemigliptin

    LC15-0444

    Dipeptidyl Peptidase Metabolic Disease
    Gemigliptin is a highly selective dipeptidyl peptidase 4 (DPP4) inhibitor with a KD of 7.25 nM.
  • HY-B0009
    Flumazenil

    Ro 15-1788

    GABA Receptor Neurological Disease
    Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
  • HY-U00011
    Temarotene

    Ro 15-0778

    Others Inflammation/Immunology
    Temarotene is an orally administered, particular arotinoid.
  • HY-16504
    Treprostinil sodium

    UT-15

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
  • HY-15322
    PRT062607

    P505-15; PRT-2607; BIIB-057

    Syk Inflammation/Immunology
    PRT062607(P505-15; PRT-2607; BIIB-057) is a highly specific and potent inhibitor of Syk with IC50 of 1-2 nM; >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.
  • HY-128846
    Pomalidomide-C2-NH2

    Cereblon Ligand-Linker Conjugates 15

    E3 Ligase Ligand-Linker Conjugate Cancer
    Pomalidomide-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a PEG linker used in PROTAC technology.
  • HY-118844
    Flumazenil acid

    Ro 15-3890

    GABA Receptor Drug Metabolite Neurological Disease
    Flumazenil acid is a metabolite of Flumazenil. Flumazenil is a GABAA receptor antagonist.
  • HY-B0359
    Fenticonazole Nitrate

    REC 15-1476

    Fungal Antibiotic Infection
    Fenticonazole Nitrate is an azole antifungal agent.
  • HY-128846A
    Pomalidomide-C2-NH2 hydrochloride

    Cereblon Ligand-Linker Conjugates 15 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    Pomalidomide-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
  • HY-B1894A
    Cefetamet pivoxil hydrochloride

    Ro 15-8075

    Bacterial Antibiotic Infection
    Cefetamet pivoxil hydrochloride is an oral third generation cephalosporin antibiotic.
  • HY-B1303
    Mebhydrolin napadisylate

    Mebhydroline 1,5-naphthalenedisulfonate salt

    Histamine Receptor Inflammation/Immunology Endocrinology
    Mebhydrolin napadisylate is a specific histamine H1 receptor antagonist.
  • HY-12403
    Angiotensin (1-7)

    Ang-(1-7)

    Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Inflammation/Immunology Cardiovascular Disease Endocrinology
    Angiotensin 1-7 (Ang-(1-7)) is a major active component of the renin-angiotensin system (RAS), produced from cleavage of Ang II by angiotensin-converting-enzyme type 2 (ACE2). 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-N2526
    Nervonic acid

    Selacholeic acid; cis-15-Tetracosenoic acid

    Endogenous Metabolite Neurological Disease
    Nervonic acid is a monounsaturated fatty acid important in the biosynthesis of myelin.
  • HY-128836
    (4R,5S)-Nutlin carboxylic acid

    MDM2 ligand 2; E3 ligase Ligand 15

    Ligand for E3 Ligase Cancer
    (4R,5S)-Nutlin carboxylic acid (MDM2 ligand 2) is the Nutlin 3-based MDM2 ligand. (4R,5S)-Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTACs.
  • HY-103612
    Thalidomide-O-amido-C3-COOH

    Cereblon Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 15

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-O-amido-C3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
  • HY-N0077
    Ginkgolic Acid

    Ginkgolic acid (15:1); Ginkgolic acid I; Romanicardic acid

    E1/E2/E3 Enzyme Cancer
    Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
  • HY-Y1139
    Pimelic acid

    Heptanedioic acid; 1,5-Pentanedicarboxylic acid; 1,7-Heptanedioic acid

    Endogenous Metabolite Metabolic Disease
    Pimelic acid is the organic compound and its derivatives are involved in the biosynthesis of the amino acid called lysine.
  • HY-W016622
    Watermelon ketone

    7-Methyl-2H-1,5-benzodioxepin-3(4H)-one

    Others Others
    Watermelon ketone is fragrance chemical compound with special odorant which has been widely used in the fragrance industry, extracted from patent CN 103058984 A.
  • HY-N1412
    1,3-Dicaffeoylquinic acid

    1,3-O-Dicaffeoylquinic acid; 1,5-Dicaffeoylquinic acid

    PI3K Akt Reactive Oxygen Species Neurological Disease
    1,3-Dicaffeoylquinic acid is a caffeoylquinic acid derivative that exhibits antioxidant activity and radical scavenging activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-P0216
    A 779

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.
  • HY-W000434
    Fmoc-NH-PEG4-CH2CH2COOH

    Fmoc-15-amino-4,7,10,13-tetraoxapentadecanoic acid

    ADC Linker Cancer
    Fmoc-NH-PEG4-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-15778A
    AVE 0991 sodium salt

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [ 125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50 of 21 nM.
  • HY-103157
    PD146176

    NSC168807

    Autophagy Ferroptosis Cardiovascular Disease
    PD146176 (NSC168807) is a 15-Lipoxygenase (15-LO) inhibitor, which inhibits rabbit reticulocyte 15-LO with a Ki of 197 nM. PD146176 (NSC168807) has a dramatic effect in reducing atherogenesis.
  • HY-14183
    Vernakalant Hydrochloride

    RSD1235 hydrochloride

    Potassium Channel Cardiovascular Disease
    Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
  • HY-P1536
    Thrombin Receptor Activator for Peptide 5 TRAP-5

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Thrombin Receptor Activator for Peptide 5 (TRAP-5) is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD).
  • HY-W004283
    Pentadecanoic acid

    Endogenous Metabolite Others
    Pentadecylic acid is a saturated fatty acid with a 15-carbon backbone.
  • HY-12176
    Aliskiren

    CGP 60536; CGP60536B; SPP 100

    Renin Autophagy Cardiovascular Disease Cancer
    Aliskiren(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.
  • HY-12177
    Aliskiren hemifumarate

    CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate

    Renin Autophagy Cardiovascular Disease Cancer
    Aliskiren hemifumarate(CGP 60536 hemifumarate) is a direct renin inhibitor with IC50 of 1.5 nM.
  • HY-100240
    Lodelaben

    SC-39026; Declaben

    Elastase Metabolic Disease Cardiovascular Disease
    Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.
  • HY-123960
    Raphin1

    Phosphatase Neurological Disease
    Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
  • HY-123960A
    Raphin1 acetate

    Phosphatase Neurological Disease
    Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
  • HY-10532
    SRT 1720

    Sirtuin Autophagy Metabolic Disease
    SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities agaiinst SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.
  • HY-18697
    JD-5037

    Cannabinoid Receptor Metabolic Disease Cancer
    JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.
  • HY-13305
    MK-2048

    HIV HIV Integrase Infection
    MK-2048 is a potent inhibitor of integrase and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.
  • HY-111482
    SM 16

    TGF-β Receptor Cancer Inflammation/Immunology Cardiovascular Disease
    SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
  • HY-100422
    KDM5-IN-1

    Histone Demethylase Cancer
    KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
  • HY-U00446
    PBOX 6

    Apoptosis Microtubule/Tubulin Cancer
    PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound, acts as a microtubule-depolymerizing agent and an apoptotic agent.
  • HY-10268
    Betrixaban

    PRT054021

    Factor Xa Cardiovascular Disease
    Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with IC50 of 1.5 nM.
  • HY-12176AS
    Aliskiren D6 Hydrochloride

    CGP 60536 D6 Hydrochloride; CGP60536B D6 Hydrochloride; SPP 100 D6 Hydrochloride

    Renin Cardiovascular Disease Cancer
    Aliskiren D6 Hydrochloride (CGP 60536 D6 Hydrochloride) is is deuterium labeled Aliskiren, which is a direct renin inhibitor with IC50 of 1.5 nM.
  • HY-W018931
    DDR Inhibitor

    Discoidin Domain Receptor Cancer
    DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
  • HY-111543
    AN11251

    Parasite Infection
    AN11251 is a potent and oral active anti-Wolbachia agent with potential for treatment of onchocerciasis and lymphatic filariasis, with EC50 values of 1.5 nM in LDW1 cell lines and 15 nM in C6/36 cell lines.
  • HY-P1439
    RS 09

    Toll-like Receptor (TLR) Inflammation/Immunology
    RS 09 is a TLR4 agonist. RS 09 promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 acts as an adjuvant in vivo; RS 09 enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
  • HY-16688
    RU 24969

    5-HT Receptor Neurological Disease
    RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors.
  • HY-101035
    LOM612

    Others Cancer
    LOM612 is a potent FOXO relocator, with an EC50 value of 1.5 μM in U2fox RELOC cells.
  • HY-13917
    PND-1186

    VS-4718; SR-2516

    FAK Apoptosis Cancer
    PND-1186 (VS-4718; SR-2516) is a potent and reversible inhibitor of FAK with an IC50 of 1.5 nM in cell assay.
  • HY-16115
    BPH-652

    Others Metabolic Disease
    BPH-652 is a S. aureus dehydrosqualene synthase (CrtM) inhibitor, with a Ki of 1.5 nM and an IC50 of 100-300 nM (S. aureus pigment formation).
  • HY-12056
    BIX02189

    MEK ERK Cancer
    BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
  • HY-10614
    A-966492

    PARP Cancer
    A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
  • HY-101055
    Kinetin riboside

    N6-Furfuryladenosine

    Apoptosis Cancer
    Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM.
  • HY-15617
    JNK-IN-7

    JNK inhibitor

    JNK Cancer
    JNK-IN-7 is a potent JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, respectively.
  • HY-10458
    PF-562271 besylate

    PF562271 besylate; PF 562271 besylate

    FAK Pyk2 Cancer
    PF-562271 besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.
  • HY-P1439A
    RS 09 TFA

    Toll-like Receptor (TLR) Inflammation/Immunology
    RS 09 TFA is a TLR4 agonist. RS 09 TFA promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 TFA acts as an adjuvant in vivo; RS 09 TFA enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
  • HY-10595
    Ro 28-1675

    Glucokinase Metabolic Disease
    Ro 28-1675 (Ro 0281675) is a potent allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM.
  • HY-10459
    PF-562271

    FAK Pyk2 Cancer
    PF-562271 is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.
  • HY-15414
    Vortioxetine

    Lu AA 21004

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
  • HY-133117A
    (Rac)-BAY-985

    IKK Cancer
    (Rac)-BAY-985 (Compound Example 100.01) is a potent, ATP-competitive and selective TBK1 inhibitor with an IC50 of 1.5 nM. Antitumor efficacy.
  • HY-136259
    ML188

    SARS-CoV Virus Protease Infection
    ML188, a first in class probe, is a selective non-covalent SARS-CoV 3CLpro inhibitor with an IC50 of 1.5 μM. Antiviral activity.
  • HY-131068
    BACE-1 inhibitor 2

    Beta-secretase Neurological Disease
    BACE-1 inhibitor 2 is a potent and CNS permeable BACE-1 inhibitor with an IC50 of 1.5 nM in BACE-1 enzymatic assay.
  • HY-100015
    Mivebresib

    ABBV-075

    Epigenetic Reader Domain Apoptosis Cancer
    Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.
  • HY-13527
    LY310762

    5-HT Receptor Neurological Disease
    LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.
  • HY-104049
    Lanifibranor

    IVA337

    PPAR Metabolic Disease Cancer
    Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.
  • HY-13424
    RITA

    NSC 652287

    MDM-2/p53 Autophagy DNA Alkylator/Crosslinker Cancer
    RITA is an inhibitor of p53-HDM-2 interaction, binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.
  • HY-12283
    Rostafuroxin

    PST 2238

    Na+/K+ ATPase Cardiovascular Disease
    Rostafuroxin(PST 2238) is a antihypertensive compound; Na,K-ATPase antognist;displaced [3H]ouabain from the dogkidney Na+,K+-ATPase with IC50 of 1.5 nM.
  • HY-17453
    Salmeterol xinafoate

    GR 33343X xinafoate

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Salmeterol xinafoate is a long-acting beta-2 adrenergic receptor (β2AR) agonist, with Ki of 1.5 nM for WT β2AR, and used for asthma treatment.
  • HY-124330
    Tripolin A

    (E)-Tripolin A

    Aurora Kinase Others
    Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively.
  • HY-15898
    Y-320

    Interleukin Related Inflammation/Immunology
    Y-320 is a new phenylpyrazoleanilide immunomodulator; inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM.
  • HY-70044
    GSK-1070916

    GSK-1070916A

    Aurora Kinase Apoptosis Cancer
    GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
  • HY-17617
    Nastorazepide

    Z-360

    Cholecystokinin Receptor Cancer Endocrinology
    Nastorazepide (Z-360) is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
  • HY-15414A
    Vortioxetine hydrobromide

    Lu AA21004 hydrobromide

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vortioxetine hydrobromide is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
  • HY-100820
    Sarizotan

    EMD 128130

    5-HT Receptor Dopamine Receptor Neurological Disease
    Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively.
  • HY-A0010
    Eletriptan hydrobromide

    Eletriptan HBr

    5-HT Receptor Neurological Disease
    Eletriptan HBr is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.
  • HY-N2266
    Benzoylgomisin O

    COX Inflammation/Immunology
    Benzoylgomisin O isolated from Schisandra rubriflora, has inhibitory activity against 15-LOX, COX-1 and COX-2 enzymes and anti-inflammatory activity.
  • HY-19758A
    Sirtuin modulator 1

    Sirtuin Cancer
    Sirtuin modulator 1 is a modulator of SIRTl, a homolog of SIRT3, with EC1.5 of < 1 μM, extracted from patent WO 2010071853 A1, Compound No.4.
  • HY-10572
    Efavirenz

    DMP 266; EFV; L-743726

    Reverse Transcriptase HIV Autophagy Infection Cancer
    Efavirenz is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.
  • HY-18976
    UF010

    HDAC Cancer
    UF010 is a potent and selective HDAC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively.
  • HY-107018
    AR-A 2

    AR-A 000002

    5-HT Receptor Neurological Disease
    AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
  • HY-124037
    SRT 1460

    Sirtuin Cancer
    SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues.
  • HY-15304
    Dynasore

    Dynamin Autophagy Virus Protease Metabolic Disease
    Dynasore is a cell-permeable dynamin inhibitor with an IC50 of 15 μM.
  • HY-16294
    LY2090314

    GSK-3 Cancer
    LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
  • HY-18353
    mTOR inhibitor-3

    mTOR Cancer
    mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
  • HY-P1296
    Urocortin, rat

    Urocortin (Rattus norvegicus); Rat urocortin

    CRFR Neurological Disease Endocrinology
    Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF and mouse CRF, respectively.
  • HY-18644
    CWHM-12

    Integrin Cancer
    CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.
  • HY-103131
    PNU-142633

    5-HT Receptor Neurological Disease
    PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy.
  • HY-136146
    SUVN-911

    nAChR Neurological Disease
    SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
  • HY-11079
    A-803467

    Sodium Channel Neurological Disease
    A 803467 is a selective Nav1.8 sodium channel blocker with an IC50 of 8 nM; over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.
  • HY-13270
    ABT-751

    E7010

    Microtubule/Tubulin Autophagy Cancer
    ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.
  • HY-14879A
    Avibactam sodium

    NXL-104

    Bacterial Antibiotic Infection
    Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
  • HY-14879B
    Avibactam sodium hydrate

    NXL-104 hydrate

    Bacterial Antibiotic Infection
    Avibactam sodium hydrate (NXL-104 hydrate) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
  • HY-100342
    Ibrutinib-biotin

    Btk Cancer
    Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC50 of 0.755-1.02 nM for BTK.
  • HY-17429
    Flecainide acetate

    R-818

    Sodium Channel Cardiovascular Disease
    Flecainide acetate (R-818) is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.
  • HY-12177S
    Aliskiren D6 hemifumarate

    CGP 60536 D6 hemifumarate; CGP60536B D6 hemifumarate; SPP 100 D6 hemifumarate

    Renin Autophagy Cancer Cardiovascular Disease
    Aliskiren D6 hemifumarate (CGP 60536 D6 hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM.
  • HY-12285
    Serabelisib

    MLN1117; INK1117

    PI3K Cancer
    Serabelisib (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.
  • HY-130993
    Isatropolone A

    Parasite Infection
    Isatropolone A, a natural product containing a 1,5-diketone moiety, is reisolated from Streptomyces Gö66. Isatropolone A shows potent activity against Leishmania donovani with an IC50 of 0.5 μM.
  • HY-127170
    3-Hydroxycoumarin

    Others Others
    3-hydroxycoumarin is a potent and redox inhibitor of human 15-LOX-1. 3-hydroxycoumarin is recently demonstrated to protect sea urchin reproductive cells against ultraviolet B damage.
  • HY-110346
    AZD5582 dihydrochloride

    IAP Apoptosis Cancer
    AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
  • HY-12600
    AZD5582

    IAP Apoptosis Cancer
    AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
  • HY-P1296A
    Urocortin, rat TFA

    Urocortin (Rattus norvegicus) (TFA); Rat urocortin TFA

    CRFR Endocrinology Neurological Disease
    Urocortin, rat TFA (Urocortin (Rattus norvegicus) TFA) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF and mouse CRF, respectively.
  • HY-15414S
    Vortioxetine D8

    Lu AA 21004 D8

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vortioxetine D8 is a deuterium labeled Vortioxetine. Vortioxetine is an inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
  • HY-101792A
    RG7800 hydrochloride

    RO6885247 hydrochloride

    DNA/RNA Synthesis Neurological Disease
    RG7800 hydrochloride is an orally active SMN2 splicing modulator, with EC1.5xs of 23 nM and 87 nM for SMN2 splicing and SMN protein; RG7800 hydrochloride has the potential to treat spinal muscular atrophy.
  • HY-14403
    ERK5-IN-1

    ERK Cancer
    ERK5-IN-1 is a potent ERK5 inhibitor with an IC50 of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC50 of 26 nM.
  • HY-12048
    Chelerythrine chloride

    PKC Bcl-2 Family Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology
    Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy.
  • HY-13308
    Regorafenib Hydrochloride

    BAY73-4506 hydrochloride

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-14879
    Avibactam free acid

    NXL-104 free acid

    Bacterial Antibiotic Infection
    Avibactam free acid (NXL-104 free acid) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
  • HY-A0195
    Carboprost tromethamine

    Prostaglandin Receptor Endocrinology
    Carboprost tromethamine is the synthetic 15-methyl analogue of prostaglandin F. Carboprost tromethamine can effectively promote law contraction of the uterus and significantly reduce the amount of bleeding during and after delivery.
  • HY-14547
    Bifeprunox

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Bifeprunox is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia.
  • HY-102033
    Oxamflatin

    Metacept-3

    HDAC Cancer
    Oxamflatin (Metacept-3) is a potent HDAC inhibitor with an IC50 of 15.7 nM.
  • HY-101679
    YM-58790

    mAChR Neurological Disease
    YM-58790 is a potent antagonist of M3 muscarinic receptor, with Ki of 15 nM.
  • HY-16968
    SW033291

    15-PGDH Others
    SW033291 is a potent and high-affinity inhibitor of 15-PGDH with a Ki of 0.1 nM. SW033291 increases prostaglandin PGE2 levels in bone marrow and other tissues. SW033291 also promotes tissue regeneration.
  • HY-16687A
    Eltoprazine hydrochloride

    DU 28853 hydrochloride

    5-HT Receptor Neurological Disease
    Eltoprazine hydrochloride (DU 28853 hydrochloride) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.
  • HY-10331A
    Regorafenib monohydrate

    BAY 73-4506 monohydrate

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib monohydrate is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-15320
    NBI-74330

    CXCR Inflammation/Immunology Endocrinology
    NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of ( 125I)CXCL10 and ( 125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
  • HY-19627
    Naldemedine

    S-297995

    Opioid Receptor Neurological Disease
    Naldemedine (S-297995) is an orally active, peripherally acting µ-opioid receptor antagonist. Naldemedine shows potent binding affinities (IC50s = 1.15, 1.11, and 1.5 nM, repectively) and antagonist activities (IC50s= 25.57, 7.09, 16.1 nM, repectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine tempers opioid-induced constipation (OIC) without compromising opioid analgesia.
  • HY-12047
    Ponatinib

    AP24534

    Bcr-Abl PDGFR VEGFR FGFR Src Autophagy Cancer
    Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-16986
    EPZ011989

    Histone Methyltransferase Cancer
    EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
  • HY-16687
    Eltoprazine

    DU 28853

    5-HT Receptor Neurological Disease
    Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.
  • 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-16986A
    EPZ011989 trifluoroacetate

    EPZ-011989 trifluoroacetate

    Histone Methyltransferase Cancer
    EPZ011989 trifluoroacetate is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
  • HY-B1213
    Trimipramine maleate

    5-HT Receptor Bacterial Neurological Disease
    Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively.
  • HY-14274
    Anastrozole

    ZD1033

    Aromatase Cancer
    Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
  • HY-13269
    BMS-707035

    HIV HIV Integrase Infection
    BMS-707035 is an HIV-1 integrase (IN) inhibitor with an IC50 value of 15 nM.
  • HY-P1818
    Neuropeptide Y (22-36)

    Neuropeptide Y Receptor Neurological Disease Endocrinology
    Neuropeptide Y (22-36), a 15 amino acid peptide, is a fragment of Neuropeptide Y.
  • HY-13946
    BML-277

    Chk2 Inhibitor II

    Checkpoint Kinase (Chk) Apoptosis Cancer
    BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.
  • HY-14181A
    Cinaciguat hydrochloride

    BAY 58-2667 hydrochloride

    Guanylate Cyclase Cardiovascular Disease
    Cinaciguat hydrochloride is a potent soluble guanylate cyclase (GC) activator with EC50 of 15 nM in platelets.
  • HY-12294
    PEAQX

    NVP-AAM077

    iGluR Neurological Disease
    PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).
  • HY-P1179
    Guanylin(human)

    Guanylate Cyclase Endogenous Metabolite Cancer Endocrinology
    Guanylin(human), a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.
  • HY-10331
    Regorafenib

    BAY 73-4506

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
  • HY-12235
    PI-3065

    PI3K Inflammation/Immunology Cancer
    PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.
  • HY-111639
    2’-O,4’-C-Methyleneuridine

    Nucleoside Antimetabolite/Analog Infection
    2’-O,4’-C-Methyleneuridine (Compound 15a) is a bicyclic nucleoside.
  • HY-B0500
    Alverine citrate

    NSC 35459

    5-HT Receptor Metabolic Disease
    Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.
  • HY-100166
    AP521

    5-HT Receptor Neurological Disease
    AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
  • HY-13760
    Tasidotin hydrochloride

    ILX651

    Microtubule/Tubulin Cancer
    Tasidotin hydrochloride is a peptide analog of the antimitotic depsipeptide dolastatin 15, as an inhibitor of microtubule assembly and microtubule dynamics.
  • HY-117407
    ALLO-2

    Smo Cancer
    ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.
  • HY-P1179A
    Guanylin(human) TFA

    Guanylate Cyclase Endogenous Metabolite
    Guanylin(human) TFA, a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) TFA is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.
  • HY-15296
    Cabergoline

    FCE-21336

    Dopamine Receptor Autophagy Endocrinology
    Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
  • HY-P1236
    Atrial Natriuretic Peptide (ANP) (1-28), rat

    Atrial natriuretic factor (1-28) (rat)

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Atrial Natriuretic Peptide (ANP) (1-28), rat is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
  • HY-133121
    WDR5-IN-1

    Histone Methyltransferase Apoptosis Cancer
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.
  • HY-15066
    CNQX

    FG9065

    iGluR Neurological Disease
    CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist. CNQX blocks the expression of fear-potentiated startle in rats.
  • HY-P1219
    Jingzhaotoxin-III

    Sodium Channel Neurological Disease
    Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype.
  • HY-121653
    Flesinoxan

    5-HT Receptor Neurological Disease
    Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects.
  • HY-12294A
    PEAQX tetrasodium hydrate

    NVP-AAM077 tetrasodium hydrate

    iGluR Apoptosis Neurological Disease
    PEAQX tetrasodium hydrate (NVP-AAM077 tetrasodium hydrate) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).
  • HY-120738
    p-MPPI hydrochloride

    5-HT Receptor Neurological Disease
    p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects.
  • HY-14785
    Befiradol

    NLX-112; F13640

    5-HT Receptor Neurological Disease
    Befiradol (NLX-112) is a selective 5-HT1A receptor agonist.
  • HY-14785A
    Befiradol hydrochloride

    NLX-112 hydrochloride; F 13640 hydrochloride

    5-HT Receptor Neurological Disease
    Befiradol hydrochloride (NLX-112 hydrochloride) is a selective 5-HT1A receptor agonist.
  • HY-B1517A
    Alprenolol hydrochloride

    (RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochloride

    5-HT Receptor Cancer
    Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist.
  • HY-19313
    LLY-507

    Histone Methyltransferase Cancer
    LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2 with an IC50 of 15 nM.
  • HY-B0716
    Urapidil

    5-HT Receptor Adrenergic Receptor Neurological Disease Endocrinology
    Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.
  • HY-B1517
    Alprenolol

    (RS)-Alprenolol; dl-Alprenolol

    5-HT Receptor Cancer
    Alprenolol is a non-selective beta blocker as well as 5-HT1A receptor antagonist.
  • HY-108414
    (R)-Equol

    (+)-Equol

    Estrogen Receptor/ERR Cancer
    (R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
  • HY-13788B
    LY 344864 hydrochloride

    5-HT Receptor Neurological Disease
    LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM.
  • HY-13314
    Tesevatinib

    XL-647; EXEL-7647; KD-019

    EGFR VEGFR Ephrin Receptor Cancer
    Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.
  • HY-N3513
    Mulberrin

    Kuwanon C

    Others Cardiovascular Disease
    Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
  • HY-N7489
    β-Hederin

    Parasite Infection Inflammation/Immunology
    β-Hederin, a saponin isolated from Hedera helix L.(Araliaceae), possesses antileishmanial activity. β-Hederin exhibits IC50 values of 1.5 μM, 68 nM and 4.57 μM in L. Mexicana promastigotes, L. mexicana amastigotes and THP1 cells, respectively.
  • HY-19630
    ML289

    VU0463597

    mGluR Neurological Disease
    ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5.
  • HY-P1236A
    Atrial Natriuretic Peptide (ANP) (1-28), rat TFA

    Atrial natriuretic factor (1-28) (rat) TFA

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Atrial Natriuretic Peptide (ANP) (1-28), rat (TFA) is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
  • HY-P1219A
    Jingzhaotoxin-III TFA

    Sodium Channel Neurological Disease
    Jingzhaotoxin-III TFA is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III TFA can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype.
  • HY-12185
    BRD7389

    Ribosomal S6 Kinase (RSK) Cancer Metabolic Disease
    BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells.
  • HY-I0678
    Regorafénib N-oxyde (M2)

    Drug Metabolite Cancer
    Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-136128
    H3B-120

    Potassium Channel Cancer
    H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity.
  • HY-N0925
    Tetrahydroberberine

    Canadine

    Dopamine Receptor Neurological Disease
    Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00).
  • HY-W017511
    5,6-Dimethyl-1H-benzo[d]imidazole

    Endogenous Metabolite Metabolic Disease
    5,6-Dimethyl-1H-benzo[d]imidazole is an endogenous metabolite.
  • HY-101853
    STAT5-IN-1

    STAT Cancer
    STAT5-IN-1 is a STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform.
  • HY-18977
    KML29

    MAGL Metabolic Disease
    KML29 is a potent and selective MAGL inhibitor with IC50 = 5.9, 15, and 43 nM in human, mouse, and rat brain proteomes, respectively.
  • HY-16691
    AK-7

    Sirtuin Neurological Disease
    AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
  • HY-103107
    LY334370

    5-HT Receptor Neurological Disease
    LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.
  • HY-101772
    Ziritaxestat

    GLPG1690

    Phosphodiesterase (PDE) Inflammation/Immunology
    Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and a Ki of 15 nM.
  • HY-101111
    PF-06840003

    EOS200271

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor with IC50s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively.
  • HY-19759
    SRT 2183

    Sirtuin Apoptosis Cancer
    SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.
  • HY-15066A
    CNQX disodium

    FG9065 disodium

    iGluR Neurological Disease
    CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist. CNQX disodium blocks the expression of fear-potentiated startle in rats.
  • HY-100545
    BAPTA-AM

    Potassium Channel Cardiovascular Disease
    BAPTA-AM is a well-known membrane permeable Ca 2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.
  • HY-12047S
    Ponatinib D8

    AP24534 D8

    Bcr-Abl PDGFR VEGFR FGFR Src Autophagy Cancer
    Ponatinib D8 (AP24534 D8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-15945
    DBeQ

    JRF 12

    p97 Autophagy Apoptosis Cancer
    DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
  • HY-14546
    Aripiprazole

    OPC-14597

    5-HT Receptor Neurological Disease
    Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
  • HY-14261
    Vilazodone Hydrochloride

    EMD 68843 Hydrochloride; SB659746A Hydrochloride

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  • HY-12201
    TAK-901

    Aurora Kinase Cancer
    TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.
  • HY-14394
    TBB

    NSC 231634; Casein Kinase II Inhibitor I

    Casein Kinase Cancer
    TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
  • HY-101105A
    SB-224289 hydrochloride

    SB-224289A

    5-HT Receptor Neurological Disease
    SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
  • HY-101609
    Lesopitron dihydrochloride

    E4424

    5-HT Receptor Neurological Disease
    Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
  • HY-100256
    Trifarotene

    CD5789

    RAR/RXR Autophagy Inflammation/Immunology
    Trifarotene (CD5789) is a retinoic acid receptor (RAR) agonist with Kd app of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively.
  • HY-110195
    Smurf1-IN-A01

    A01

    Others Others
    Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.
  • HY-10847
    SB-277011

    SB-277011A

    Dopamine Receptor Neurological Disease
    SB-277011 is a potent and delective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively); brain penetrant.
  • HY-A0007
    Rotigotine Hydrochloride

    N-0923 Hydrochloride

    Dopamine Receptor Adrenergic Receptor 5-HT Receptor Neurological Disease
    Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
  • HY-101698
    Alniditan

    Alnitidan

    5-HT Receptor Neurological Disease
    Alniditan is a potent 5-HT1B/1D receptors agonist, with IC50 of 1.7 and 1.3 nM in HEK 293 cells, and pKi value of 8.96 and 9.40 for 5-HT1B/1D receptors, respectively.
  • HY-19417A
    Wf-516

    Serotonin Transporter 5-HT Receptor Neurological Disease
    Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.
  • HY-14541
    Olanzapine

    LY170053

    5-HT Receptor Dopamine Receptor mAChR Adrenergic Receptor Autophagy Mitophagy Apoptosis Neurological Disease Cancer
    Olanzapine (LY170053) is a selective monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-12481
    SAR405

    PI3K Autophagy Cancer
    SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.
  • HY-14264
    Cyamemazine

    5-HT Receptor Neurological Disease
    Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity.
  • HY-P2244A
    YAP-TEAD-IN-1 TFA

    YAP Cancer
    YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM).
  • HY-P0111
    Z-WEHD-FMK

    Caspase Cathepsin Cancer
    Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis.
  • HY-15768
    Ilomastat

    GM6001; Galardin

    MMP Cancer
    Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC50s, 1.5 nM for MMP-1; 1.1 nM for MMP-2; 1.9 nM for MMP-3; 0.5 nM for MMP-9), with a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1).
  • HY-120947
    AV-105

    Others Neurological Disease
    AV-105 is a Florbetapir ( 18F)-radiolabeled slyrylpyridine tosylate precursor extracted from patent WO2010078370A1, example 1.5. AV-105 can synthesize 18F-radiolabeled compounds, which are used for positron emission tomography (PET) imaging of neurodegenerative diseases of the brain.
  • HY-P2244
    YAP-TEAD-IN-1

    YAP Cancer
    YAP-TEAD-IN-1 is a potent and competitive inhibitor of YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM).
  • HY-10216
    Refametinib R enantiomer

    BAY 869766 R enantiomer; RDEA119 R enantiomer

    MEK Cancer
    Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM.
  • HY-128351
    SHR1653

    Oxytocin Receptor Neurological Disease Endocrinology
    SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC50 of 15 nM for hOTR.
  • HY-B0526
    Flumequine

    R-802

    Bacterial Topoisomerase Antibiotic Infection Cancer
    Flumequine (R-802) is a quinolone antibiotic, and acts as a topoisomerase II inhibitor, with an IC50 of 15 μM (3.92 μg/mL).
  • HY-13788
    LY 344864

    5-HT Receptor Neurological Disease
    LY 344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
  • HY-B0354A
    Urapidil hydrochloride

    5-HT Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    Urapidil HCl is an α1-adrenoceptor antagonist and 5-HT1A receptor agonist.
  • HY-13788C
    LY 344864 racemate

    5-HT Receptor Neurological Disease
    LY 344864 racemate is a 5-HT1F receptor agonist extracted from patent US 5708187 A.
  • HY-14348
    GSK163090

    5-HT Receptor Dopamine Receptor Neurological Disease
    GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.
  • HY-75502
    Rotigotine

    N-0437; N-0923

    Dopamine Receptor Adrenergic Receptor 5-HT Receptor Neurological Disease Endocrinology
    Rotigotine (N-0437; N-0923) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
  • HY-103046
    UbcH5c-IN-1

    E1/E2/E3 Enzyme Inflammation/Immunology
    UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent.
  • HY-131140
    BD750

    JAK STAT Cancer Inflammation/Immunology
    BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
  • HY-13909
    RGFP966

    HDAC Cancer
    RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM.
  • HY-101986
    BIIE-0246

    AR-H 053591

    Neuropeptide Y Receptor Metabolic Disease Endocrinology
    BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 of 15 nM.
  • HY-10804
    CCT 137690

    Aurora Kinase Apoptosis Cancer
    CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.
  • HY-13788A
    LY 344864 S-enantiomer

    5-HT Receptor Others
    LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist.
  • HY-B0383A
    Almotriptan

    5-HT Receptor Neurological Disease
    Almotriptan is a 5-HT1B/1D-receptor agonist used to treat migraine.
  • HY-19863
    F-15599

    NLX-101

    5-HT Receptor Neurological Disease
    F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
  • HY-101976
    JAK3-IN-6

    JAK Inflammation/Immunology
    JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.
  • HY-100036
    MK-4101

    Smo Apoptosis Hedgehog Cancer
    MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 µM for mouse cells; IC50 of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.
  • HY-10510
    BI-D1870

    Ribosomal S6 Kinase (RSK) Autophagy Cancer
    BI-D1870 is an ATP-competitive, cell permeable inhibitor of RSK isoforms, with IC50s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively.
  • HY-N0747
    Oxypeucedanin

    Potassium Channel Cancer Cardiovascular Disease
    Oxypeucedanin is a furocoumarin derivative isolated from Angelica dahurica. Oxypeucedanin is a selective open-channel blocker, inhibits the hKv1.5 current with an IC50 value of 76 nM. Oxypeucedanin prolongs cardiac action potential duration (APD), is a potential antiarrhythmic agent for atrial fibrillation. Oxypeucedanin induces cell apoptosis through inhibition of cancer cell migration.
  • HY-126429
    Nav1.1 activator 1

    Sodium Channel Neurological Disease
    Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant τ of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.
  • HY-116175
    BIBB 515

    Others Metabolic Disease
    BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED50 values of 0.2-0.5 mg/kg and 0.36-33.3 mg/kg in rats and mice (1-5 hours), respectively. BIBB 515 exerts lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL).
  • HY-10847A
    SB-277011 dihydrochloride

    SB-277011A dihydrochloride

    Dopamine Receptor Neurological Disease
    SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
  • HY-103142
    AS19

    5-HT Receptor Neurological Disease
    AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia.
  • HY-14541S
    Olanzapine D3

    LY170053 D3

    5-HT Receptor Dopamine Receptor mAChR Adrenergic Receptor Autophagy Mitophagy Apoptosis Cancer Neurological Disease
    Olanzapine D3 (LY170053 D3) is the deuterium labeled Olanzapine. Olanzapine is a selective monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic.
  • HY-14782
    Adoprazine

    SLV313

    5-HT Receptor Dopamine Receptor Neurological Disease
    Adoprazine, a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.
  • HY-14443
    XMD8-92

    ERK Cancer
    XMD8-92 is a highly selective ERK5/BMK1 inhibitor with dissociation constant (Kd) value of 80 nM.
  • HY-16615
    SIRT-IN-1

    Sirtuin Metabolic Disease Neurological Disease Cancer Inflammation/Immunology
    SIRT-IN-1 is a potent inhibitor of SIRT1/2/3, with IC50s of 15, 10, 33 μM, respectively.
  • HY-111539
    BAY-1316957

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    BAY-1316957 is a highly potent and selective EP4 receptor antagonist with an IC50 of 15.3 nM. Good oral bioavailability.
  • HY-124861
    Malic enzyme inhibitor ME1

    ME1

    Others Cancer Metabolic Disease
    Malic enzyme inhibitor ME1 (ME1; compound 1) is a potent inhibitor of Malic enzyme (ME1) with an IC50 of 0.15 μM.
  • HY-12528
    DBPR108

    Dipeptidyl Peptidase Metabolic Disease
    DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9.
  • HY-B0383
    Almotriptan malate

    PNU180638

    5-HT Receptor Neurological Disease
    Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.
  • HY-13948
    Angiotensin II human

    Angiotensin II; Ang II; DRVYIHPF

    Angiotensin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Angiotensin II human (Angiotensin II) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis.
  • HY-128342
    Complement C5-IN-1

    Complement System Inflammation/Immunology
    Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM.
  • HY-103171
    BAY 60-6583

    Adenosine Receptor Inflammation/Immunology Cardiovascular Disease
    BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50 = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model.
  • HY-117048
    PF-4191834

    PF-04191834

    Lipoxygenase Inflammation/Immunology
    PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain.
  • HY-126010
    Dooku1

    Others Cardiovascular Disease
    Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca 2+-entry with IC50 values of 1.3 μM (in HEK 293 cells) and 1.5 μM (in HUVECs). Dooku1 inhibits Yoda1-induced relaxation of aorta.
  • HY-16697
    CID 16020046

    GPR55 Cancer
    CID 16020046 is a potent and selective GPR55(LPI receptor) antagonist; inhibitsGPR55 constitutive activity with IC50 of 0.15 uM.
  • HY-19134
    EMD 56551

    5-HT Receptor Neurological Disease
    EMD 56551 is a potent and selective 5-HT1A receptor agonist. EMD 56551 exerts anxiolytic activity.
  • HY-19946
    Eptapirone

    F 11440

    5-HT Receptor Neurological Disease
    Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
  • HY-10223
    CUDC-101

    EGFR HDAC Cancer
    CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4, 2.4, and 15.7 nM, respectively.
  • HY-15030A
    Naproxen sodium

    Autophagy COX Inflammation/Immunology Cancer
    Naproxen sodium is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
  • HY-U00117
    Lusaperidone

    R107474

    Adrenergic Receptor Neurological Disease Endocrinology
    Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.
  • HY-10501
    SU14813

    PDGFR VEGFR c-Kit Cancer
    SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
  • HY-19477
    SB-616234A

    5-HT Receptor Neurological Disease
    SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.
  • HY-15030
    Naproxen

    (S)-Naproxen

    COX Autophagy Inflammation/Immunology Cancer
    Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
  • HY-10501A
    SU14813 maleate

    PDGFR VEGFR c-Kit Cancer
    SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
  • HY-18955
    BI-847325

    MEK Aurora Kinase Apoptosis Cancer
    BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.
  • HY-B0121
    Sumatriptan succinate

    GR 43175

    5-HT Receptor Neurological Disease
    Sumatriptan succinate (GR 43175) is a serotonin1 (5-HT1) receptor agonist, which is effective in the acute treatment of migraine headache.
  • HY-108938
    SDZ285428

    Cytochrome P450 Fungal Parasite Infection
    SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h).
  • HY-112061
    8-OH-DPAT

    8-Hydroxy-DPAT

    5-HT Receptor Neurological Disease
    8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
  • HY-120081A
    Metixene hydrochloride hydrate

    mAChR Neurological Disease
    Metixene hydrochloride hydrate is an anticholinergic antiparkinsonian agent, potently inhibits binding of quinuclidinyl benzilate (QNB) to the muscarinic receptor in rat brain cortical tissue, with an IC50 of 55 nM and a Kd of 15 nM.
  • HY-15338
    TG003

    CDK Cancer
    TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
  • HY-76981
    5-Hydroxy-1-tetralone

    Others Others
    5-hydroxy-1-tetralone can be used as a fluorescent labeling reagent for the determination of glycosphingolipid from biological samples.
  • HY-13701
    Nelarabine

    506U78; GW 506U78; Nelzarabine

    Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Nelarabine (Arranon, 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
  • HY-120081B
    Metixene hydrochloride

    mAChR Neurological Disease
    Metixene hydrochloride is an anticholinergic antiparkinsonian agent, potently inhibits binding of quinuclidinyl benzilate (QNB) to the muscarinic receptor in rat brain cortical tissue, with an IC50 of 55 nM and a Kd of 15 nM.
  • HY-10349
    WAY-100635

    5-HT Receptor Dopamine Receptor Neurological Disease
    WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist.
  • HY-N2359
    Chelerythrine

    PKC Bcl-2 Family Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology
    Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.
  • HY-P1318
    Ac-RYYRIK-NH2

    Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
  • HY-107417
    Hypothemycin

    VEGFR MEK FLT3 PDGFR ERK Cancer
    Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.
  • HY-114263
    NXT629

    PPAR Cancer
    NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.
  • HY-P1318A
    Ac-RYYRIK-NH2 TFA

    Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-18670
    HQ-415

    Others Neurological Disease
    HQ-415 is a class of clinically relevant bioactive metal chelators related to clioquinol. The effective concentration eliciting a EC50 for HQ-415 is 15 μM.
  • HY-50866
    NVP-AEW541

    AEW541

    IGF-1R Insulin Receptor Autophagy Cancer Endocrinology
    NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 0.15 μM, also inhibits InsR, with IC50 of 0.14 μM.
  • HY-14261S
    Vilazodone D8

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.
  • HY-100416A
    LY2365109 hydrochloride

    GlyT Neurological Disease
    LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a.
  • HY-10497
    BMS-794833

    c-Met/HGFR VEGFR Cancer
    BMS-794833 is a VEGFR2 and Met inhibitor extracted from patent WO2009094417, compound example 1; has IC50s of 15 and 1.7 nM, respectively.
  • HY-18595
    BI 224436

    HIV HIV Integrase Infection
    BI 224436 is a novel HIV-1 noncatalytic site integrase inhibitor with EC50 values of less than 15 nM against different HIV-1 laboratory strains.
  • HY-111594
    Homo-PROTAC cereblon degrader 1

    PROTAC Cancer
    Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.
  • HY-103464
    5'-Fluoroindirubinoxime

    5'-FIO

    FLT3 Cancer
    5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
  • HY-101125
    L-45

    L-Moses

    Epigenetic Reader Domain Cancer
    L-45 is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126±15 nM.
  • HY-101430
    PGD2-IN-1

    Others Inflammation/Immunology
    PGD2-IN-1 is an antagonist of DP extracted from patent WO 2006044732 A2, example 15 (d); has an IC50 of 0.3 nM.
  • HY-126140
    MDRTB-IN-1

    Bacterial Infection
    MDRTB-IN-1 (5aα) is an antibiotic which is against Mycobacterium tuberculosis H37Rv with a MIC90 value of 10.5 μM.
  • HY-136311
    NCT-504

    Others Neurological Disease
    NCT-504 is a selective allosteric inhibitor of PIP4Kγ, with an IC50 of 15.8 μM. NCT-504 is potential for the research of Huntington's disease.
  • HY-19752A
    VU0357017 hydrochloride

    CID-25010775

    mAChR Neurological Disease
    VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).
  • HY-133012
    GFB-8438

    TRP Channel Neurological Disease
    GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.
  • HY-116594A
    OPC-14523 hydrochloride

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.
  • HY-135960
    BO-264

    FGFR Apoptosis Cancer
    BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity.
  • HY-U00347
    COX/5-LO-IN-1

    Atreleuton analog

    COX Lipoxygenase Inflammation/Immunology
    COX/5-LO-IN-1 (Atreleuton analog) is an inhibitor of cylooxygenase and 5-lipoxygenase (5-LO), used for the research of inflammatory and allergic disease states.
  • HY-113951
    Prolyl Endopeptidase Inhibitor 1

    Boc-Pro-prolinal; (Boc)-Prolyl-prolinal; BPP

    Dipeptidyl Peptidase Neurological Disease
    Prolyl Endopeptidase Inhibitor 1 (Boc-Pro-prolinal) is a potent prolyl endopeptidase (PEP; PE) inhibitor, with a Ki value of 15 nM. Prolyl Endopeptidase Inhibitor 1 has anti-amnesic effect.
  • HY-101947
    SMI-16a

    PIM1/2 Kinase Inhibitor VI

    Pim Cancer
    SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively.
  • HY-18361
    TMP195

    HDAC Cancer
    TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with Kis of 59, 60, 26, 15 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
  • HY-B0115
    Pizotifen

    BC-105; Pizotyline

    5-HT Receptor Neurological Disease
    Pizotifen (BC-105) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
  • HY-12558
    LY3009120

    DP-4978

    Raf Autophagy Cancer
    LY3009120 is a pan RAF inhibitor which inhibits BRAF V600E, BRAF WT and CRAF WT with IC50s of 5.8, 9.1 and 15 nM, respectively.
  • HY-12335
    UNC0379

    Histone Methyltransferase Cancer
    UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM; selective over 15 other methyltransferases.
  • HY-110244
    Tilfrinib

    Others Cancer
    Tilfrinib (compound 4f) is a potent and selective inhibitor of breast tumor kinase (Brk) with an IC50 of 3.15 nM, which displays anti-proliferative activity and acts as a promising antitumor agent.
  • HY-109112
    Brilaroxazine

    RP5063

    Dopamine Receptor 5-HT Receptor Inflammation/Immunology Neurological Disease
    Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
  • HY-100719
    BRD-6929

    HDAC HIV Infection Cardiovascular Disease
    BRD-6929 (Cpd-60) is a brain-penetrant, selective inhibitor of HDAC1 and HDAC2 (IC50= 1 and 8 nM), extracted from patent US2018360927. BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively. BRD-6929 (TPB) potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1.
  • HY-10349A
    WAY-100635 Maleate

    5-HT Receptor Dopamine Receptor Neurological Disease
    WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 maleate has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D4 receptor agonist.
  • HY-116594
    OPC-14523 free base

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity.
  • HY-103152
    GR 113808

    5-HT Receptor Inflammation/Immunology Neurological Disease
    GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.
  • HY-123824
    GNE-0439

    Others Neurological Disease
    GNE-0439 is a novel Nav1.7-selective inhibitor with IC50 of 0.34 uM and inhibits Nav1.5 with an IC50 of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC50=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders.
  • HY-114312
    MD-224

    PROTAC MDM-2/p53 E1/E2/E3 Enzyme Cancer
    MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
  • HY-15555
    EPZ005687

    Histone Methyltransferase Cancer
    EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
  • HY-10527
    Telatinib

    Bay 57-9352

    c-Kit PDGFR VEGFR Cancer
    Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
  • HY-106157
    Donitriptan

    5-HT Receptor Neurological Disease
    Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively.
  • HY-16679
    Helioxanthin derivative 5-4-2

    Helioxanthin 5-4-2

    HBV Infection
    Helioxanthin derivative 5-4-2 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV activity with EC50 of 0.08 uM in HepG2.2.15 cells.
  • HY-12335A
    UNC0379 TFA

    Histone Methyltransferase Cancer
    UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM; selective over 15 other methyltransferases.
  • HY-114301
    PF-06305591

    Sodium Channel Neurological Disease
    PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.
  • HY-B0716S
    Urapidil D6

    5-HT Receptor Adrenergic Receptor Endocrinology Neurological Disease
    Urapidil D6 is a deuterium labeled Urapidil. Urapidil is an α1-adrenoreceptor antagonist and a 5-HT1A receptor agonist.
  • HY-101125A
    L-45 dihydrochloride

    L-Moses dihydrochloride

    Epigenetic Reader Domain Cancer
    L-45 dihydrochloride (L-Moses dihydrochloride) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126±15 nM.
  • HY-112441
    Prolyl Hydroxylase inhibitor 1

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM. Antianemia agent.
  • HY-10527C
    Telatinib mesylate

    Bay 57-9352 mesylate

    VEGFR PDGFR c-Kit Cancer
    Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.
  • HY-16680
    Helioxanthin 8-1

    Helioxanthin analogue 8-1

    HBV Infection
    Helioxanthin 8-1 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV/HCV/HSV-1/HIV activity with EC50 of >5/10/1.4/15 uM.
  • HY-106025
    Radequinil

    AC-3933

    GABA Receptor Neurological Disease
    Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively.
  • HY-B0744C
    L-Eflornithine

    L-DFMO; L-RMI71782; L-α-difluoromethylornithine

    Others Cancer
    L-Eflornithine (L-DFMO) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min -1.
  • HY-B0115A
    Pizotifen malate

    BC-105 malate; Pizotyline malate

    5-HT Receptor Neurological Disease
    Pizotifen malate (BC-105 malate) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
  • HY-U00037
    Ecopladib

    PLA 725

    Phospholipase Inflammation/Immunology
    Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
  • HY-14546S
    Aripiprazole (D8)

    OPC-14597 D8

    5-HT Receptor Neurological Disease
    Aripiprazole D8 (OPC-14597 D8) is the deuterium labeled Aripiprazole, which is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
  • HY-136568
    Stafia-1-dipivaloyloxymethyl ester

    STAT Others
    Stafia-1-dipivaloyloxymethyl ester (compound 27, 0-200 μM) decreases pSTAT5a expression significantly, and has no obvious inhibition on pSTAT5b.
  • HY-111419
    DSP-1053

    Serotonin Transporter Neurological Disease
    DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.
  • HY-P1218
    Phrixotoxin 3

    Sodium Channel Neurological Disease
    Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
  • HY-16961
    Sitravatinib

    MGCD516; MG-516

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-116941
    A-381393

    Dopamine Receptor Neurological Disease
    A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM).
  • HY-P1218A
    Phrixotoxin 3 TFA

    Sodium Channel Neurological Disease
    Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
  • HY-108496
    Sphingosine-1-phosphate

    S1P

    Endogenous Metabolite LPL Receptor Endocrinology
    Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca 2+ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids.
  • HY-P1205A
    MCH(human, mouse, rat) TFA

    MCHR1 (GPR24) Neurological Disease
    MCH (human, mouse, rat) TFA is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively.
  • HY-P1205
    MCH(human, mouse, rat)

    MCHR1 (GPR24) Neurological Disease
    MCH (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-101516
    CYP17-IN-1

    Cytochrome P450 Cancer
    CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM.
  • HY-B1626A
    Demecarium Bromide

    BC-48

    AChE Neurological Disease
    Demecarium Bromide (BC-48) is a potent cholinesterase inhibitor, with an apparent affinity (Kiapp) of 0.15 μM. Demecarium Bromide (BC-48) is used as a glaucoma agent.
  • HY-N6968
    α-Humulene

    Humulene; α-Caryophyllene

    NO Synthase COX Inflammation/Immunology
    α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 µg/mL). α-Humulene inhibits COX-2 and iNOS expression.
  • HY-14175
    Begacestat

    GSI-953

    γ-secretase Neurological Disease
    Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC5040=15 nM) for the treatment of Alzheimer's disease.
  • HY-14262
    Vilazodone

    EMD 68843; SB659746A

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone (EMD 68843; SB 659746A) is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression.
  • HY-B0744D
    L-Eflornithine monohydrochloride

    L-DFMO monohydrochloride; L-RMI71782 monohydrochloride; L-α-difluoromethylornithine monohydrochloride

    Others Cancer
    L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min -1.
  • HY-10133
    β-Secretase Inhibitor IV

    Beta-secretase Neurological Disease
    β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.
  • HY-B0982
    Pindolol

    LB-46

    5-HT Receptor Adrenergic Receptor Neurological Disease Endocrinology
    Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33nM).
  • HY-15141
    Staurosporine

    Antibiotic AM-2282; STS; AM-2282

    PKC PKA Apoptosis Bacterial Fungal Antibiotic Cancer Infection
    Staurosporine is a potent and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine is an apoptosis inducer.
  • HY-14604
    Xaliproden hydrochloride

    SR57746A; SR57746 hydrochloride

    5-HT Receptor Dopamine Receptor Neurological Disease
    Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases.
  • HY-16961A
    Sitravatinib malate

    MGCD516 malate; MG-516 malate

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-15196
    TAK-285

    EGFR Cancer
    TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
  • HY-111545
    BSc5371

    FLT3 Cancer
    BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines.
  • HY-114429
    CB-6644

    Others Cancer
    CB-6644 is a selective inhibitor of RUVBL1/2 complex with anti-cancer activity. CB-6644 blocks the ATPase activity of RUVBL1/2 with an IC50 of 15 nM.
  • HY-109586
    BRL-50481

    Phosphodiesterase (PDE) Neurological Disease
    BRL-50481 is a novel and selective inhibitor of PDE7 with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.
  • HY-135914
    JBJ-02-112-05

    EGFR Cancer
    JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFR L858R/T790M.
  • HY-130639
    Thalidomide-NH-C4-NH-Boc

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-NH-C4-NH-Boc (compound 15) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
  • HY-15573
    EI1

    KB-145943

    Histone Methyltransferase Apoptosis Cancer
    EI1 (KB-145943) is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
  • HY-106080A
    Furegrelate sodium

    U-63557A

    Others Cardiovascular Disease
    Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent.
  • HY-19540
    GSK864

    Isocitrate Dehydrogenase (IDH) Cancer
    GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
  • HY-120012
    AZD9567

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    AZD9567 (compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC50 of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation.
  • HY-112437
    PF-06737007

    Trk Receptor Neurological Disease
    PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.
  • HY-14848
    Naluzotan

    PRX 00023

    5-HT Receptor Potassium Channel Neurological Disease
    Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K + channel blocker, with IC50 of 3800 nM.
  • HY-133019
    ATX inhibitor 5

    Phosphodiesterase (PDE) Inflammation/Immunology
    ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 has anti-hepatofibrosis effect, and reduces CCl4-induced hepatic fibrosis level prominently.
  • HY-111540B
    (S)-IDO1-IN-5

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    (S)-IDO1-IN-5 (Example 1B) is an active S-isomer of IDO1-IN-5. (S)-IDO1-IN-5 binds to IDOL with an IC50 value less than 1.5 µΜ. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
  • HY-126291
    GNE-616

    Sodium Channel Neurological Disease
    GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively.
  • HY-100014
    KDM5A-IN-1

    Histone Demethylase Cancer
    KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
  • HY-112461A
    NF449 octasodium

    P2X Receptor Cardiovascular Disease
    NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a G-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-111455
    LP-211

    5-HT Receptor Neurological Disease
    LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
  • HY-116474
    Viridicatol

    Fungal Infection
    Viridicatol, a quinolinone alkaloid, is isolated from the fermentation of an endophytic fungus Penicillium sp. R22 in Nerium indicum. Viridicatol has strong antifungal activity against Staphylococcus aureus with MIC value of 15.6 μg/mL.
  • HY-112136
    TAO Kinase inhibitor 1

    Others Cancer
    TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.
  • HY-10329
    JNJ-7706621

    Aurora Kinase CDK Apoptosis Cancer
    JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC50s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.
  • HY-N2411
    Geissoschizine methyl ether

    5-HT Receptor Neurological Disease
    Geissoschizine methyl ether, a major indole alkaloid found in Uncaria hook, is a major active component of Yokukansan with psychotropic effects. Geissoschizine methyl ether is potent 5-HT1A receptor agonist.
  • HY-128573
    RORγt Inverse agonist 3

    ROR Neurological Disease
    RORγt Inverse agonist 3 is a potent, selective and orally active RORγ inverse agonist, with EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively.
  • HY-70013
    Abiraterone

    CB-7598

    Cytochrome P450 Cancer
    Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
  • HY-N1581
    Quassin

    Nigakilactone D

    Parasite Infection Endocrinology
    Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC50 of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity.
  • HY-13271
    Tubastatin A Hydrochloride

    Tubastatin A HCl; TSA HCl

    HDAC Autophagy Apoptosis Cancer
    Tubastatin A (Hydrochloride) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
  • HY-112134
    CSN5i-3

    Others Cancer
    CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM.
  • HY-112908
    RTS-V5

    HDAC Proteasome Cancer
    RTS-V5 is a dual HDAC/proteasome inhibitor with IC50s of 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.
  • HY-13271A
    Tubastatin A

    HDAC Autophagy Apoptosis Cancer
    Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
  • HY-19754
    CRA-026440

    HDAC Cancer Cardiovascular Disease
    CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively.
  • HY-18991
    CCG215022

    PKA Cancer
    CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-124322
    NB-360

    Beta-secretase Inflammation/Immunology Neurological Disease
    NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E.
  • HY-B0032S
    Lurasidone D8 Hydrochloride

    SM-13496 D8

    Others Neurological Disease
    Lurasidone D8 Hydrochloride is the deuterium labeled Lurasidone, which is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C.
  • HY-N6057
    Obtusin

    Monoamine Oxidase Neurological Disease
    Obtusin, isolated from Cassia obtusifolia Linn seed, is a highly selective and competitive human monoamine oxidase-A (hMAO-A) inhibitor with an IC50 of 11.12 μM and a Ki of 6.15 μM. Obtusin plays a preventive role in neurodegenerative diseases, especially anxiety and depression.
  • HY-N0096
    Rotundine

    (-)-Tetrahydropalmatine; L-Tetrahydropalmatine

    5-HT Receptor Dopamine Receptor Neurological Disease
    Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of 5-HT1A with an IC50 of 370 nM.
  • HY-107367
    Epertinib

    S-22611

    EGFR Cancer
    Epertinib (S-22611) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity.
  • HY-14958A
    Pardoprunox hydrochloride

    SLV-308 hydrochloride; DU-126891 hydrochloride

    5-HT Receptor Adrenergic Receptor Dopamine Receptor Neurological Disease Endocrinology
    Pardoprunox (SLV-308) hydrochloride is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC50s of 8, 9.2, and 6.3, respectively.
  • HY-14958
    Pardoprunox

    SLV-308; DU-126891

    5-HT Receptor Adrenergic Receptor Dopamine Receptor Neurological Disease Endocrinology
    Pardoprunox (SLV-308) is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC50s of 8, 9.2, and 6.3, respectively.
  • HY-119934
    NaV1.7 inhibitor-1

    Sodium Channel Neurological Disease
    NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5.
  • HY-14435
    Pyridone 6

    JAK Cancer
    Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.
  • HY-129357
    CCK-B Receptor Antagonist 2

    Cholecystokinin Receptor Metabolic Disease
    CCK-B Receptor Antagonist 2, compound 15b, is a potent and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.43 nM. CCK-B Receptor Antagonist 2 also inhibits gastrin/CCK-A activity with an IC50 of 1.82 μM.
  • HY-19675
    Naproxen etemesil

    LT-NS 001; MX 1094

    COX Inflammation/Immunology
    Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
  • HY-13948A
    Angiotensin II human acetate

    Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate

    Angiotensin Receptor Apoptosis Cancer Endocrinology Cardiovascular Disease
    Angiotensin II human acetate (Angiotensin II acetate) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis.
  • HY-14763A
    Cariprazine hydrochloride

    RGH188 hydrochloride

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Cariprazine hydrochloride is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
  • HY-100290
    5-HT1A modulator 1

    5-HT Receptor Neurological Disease
    5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.
  • HY-W062835
    CGP77675

    Src Cancer
    CGP77675 is a potent inhibitor of Src family kinases. CGP77675 inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity.
  • HY-10204
    OSI-930

    c-Fms c-Kit VEGFR Apoptosis Cancer
    OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.
  • HY-15273
    UNC0638

    Histone Methyltransferase Autophagy Influenza Virus Cancer Infection
    UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively. UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities.
  • HY-14763
    Cariprazine

    RGH-188

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
  • HY-13290
    KN-62

    CaMK P2X Receptor Autophagy Metabolic Disease Cancer
    KN-62 is a selective and potent inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with IC50 of 0.9 μM, KN-62 also displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
  • HY-107367A
    Epertinib hydrochloride

    S-22611 hydrochloride

    EGFR Cancer
    Epertinib hydrochloride (S-22611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride shows potent antitumor activity.
  • HY-135795
    1-Cyclohexyl-3-dodecyl urea

    CDU; N-Cyclohexyl-N-dodecyl urea; NCND

    Epoxide Hydrolase Metabolic Disease Cardiovascular Disease
    1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor. 1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) increases epoxyeicosatrienoic acids (EETs) levels and lowers blood pressure in angiotensin II (Ang II) hypertension.
  • HY-A0095S
    Flibanserin D4

    BIMT-17 D4; BIMT-17BS D4

    5-HT Receptor Neurological Disease
    Flibanserin D4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM).
  • HY-15780
    Brexpiprazole

    OPC-34712

    5-HT Receptor Dopamine Receptor Neurological Disease
    Brexpiprazole (OPC-34712), an atypical antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM.
  • HY-W013636
    2-Ketoglutaric acid

    Alpha-Ketoglutaric acid

    Tyrosinase Endogenous Metabolite Others
    2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM).
  • HY-111820
    CK1-IN-1

    Casein Kinase Inflammation/Immunology
    CK1-IN-1 is a casein kinase 1 (CK1) inhibitor extracted from patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.
  • HY-131246
    DM-01

    Histone Methyltransferase Cancer
    DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors.
  • HY-19533
    SCH 58261

    Adenosine Receptor Cancer
    SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively.
  • HY-N2795
    9-Hydroxycalabaxanthone

    Xanthone I

    Parasite Bacterial Infection
    9-Hydroxycalabaxanthone (Xanthone I) is a known xanthone isolated from Garcinia mangostana Linn. 9-Hydroxycalabaxanthone has quorum-sensing inhibitory, anti-microbial, and anti-malarial activities (IC50=1.2-1.5 µM).
  • HY-112443
    AZD3458

    PI3K Cancer Metabolic Disease Inflammation/Immunology
    AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively.
  • HY-111383
    LX2343

    Beta-secretase PI3K Amyloid-β Autophagy Neurological Disease
    LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of clearance.
  • HY-P0027
    Jasplakinolide

    Arp2/3 Complex Fungal Cancer Infection
    Jasplakinolide is a potent actin polymerization inducer and stabilizes pre-existing actin filaments. Jasplakinolide binds to F-actin competitively with phalloidin with a Kd of 15 nM. Jasplakinolide, a naturally occurring cyclic peptide from the marine sponge, has both fungicidal and anti-cancer activity.
  • HY-133776
    Rivastigmine carbamate impurity

    3-Nitrophenyl ethyl(methyl)carbamate

    AChE Neurological Disease
    Rivastigmine carbamate impurity (3-Nitrophenyl ethyl(methyl)carbamate) is an impurity of Rivastigmine. Rivastigmine is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively.
  • HY-10015
    PAP-1

    5-(4-Phenoxybutoxy)psoralen

    Potassium Channel Inflammation/Immunology
    PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects.
  • HY-W013636A
    2-Ketoglutaric acid Sodium

    Alpha-Ketoglutaric acid Sodium

    Tyrosinase Endogenous Metabolite Metabolic Disease
    2-Ketoglutaric acid Sodium (Alpha-Ketoglutaric acid Sodium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM).
  • HY-100862
    BRCA1-IN-2

    PARP Cancer
    BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions.
  • HY-15338A
    (E/Z)-TG003

    CDK Cancer
    (E/Z)-TG003 is a racemic compound of (Z)-TG003 and (E)-TG003. (Z)-TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
  • HY-13221
    BRL 54443

    5-HT Receptor Cardiovascular Disease
    BRL 54443 is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.
  • HY-N0781
    Linderalactone

    Apoptosis Cancer
    Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM.
  • HY-115470
    CLK-IN-T3

    CDK DYRK Cancer
    CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-19805
    STO-609

    CaMK AMPK Autophagy Metabolic Disease
    STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
  • HY-W013636B
    Calcium 2-oxoglutarate

    Tyrosinase Endogenous Metabolite Metabolic Disease
    Calcium 2-oxoglutarate is an intermediate in the production of ATP or GTP in the Krebs cycle. Calcium 2-oxoglutarate also acts as the major carbon skeleton for nitrogen-assimilatory reactions. Calcium 2-oxoglutarate is a reversible inhibitor of tyrosinase (IC50=15 mM).
  • HY-N6027
    Cyclosporin C

    Fungal Bacterial
    Cyclosporin C is a fungal metabolite that has been found in T. inflatum and has diverse biological activities, including antifungal, antiviral, and immunosuppressant properties. Cyclosporin C is active against isolates of B. cinerea, A. niger, and Alternaria, Mucor, and Penicillium species (MICs=0.1-5 μg/ml).
  • HY-128778
    DBPR112

    EGFR Cancer
    DBPR112 (compound 78) is an orally active Furanopyrimidine-Based Epidermal Growth Factor Receptor inhibitor with IC50s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M, respectively. DBPR112 has significant antitumor efficacy.
  • HY-10847B
    SB-277011 hydrochloride

    SB-277011A hydrochloride

    Dopamine Receptor 5-HT Receptor Neurological Disease
    SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
  • HY-77293
    (E)-[6]-Dehydroparadol

    Apoptosis Cancer
    (E)-[6]-Dehydroparadol, extracted from patent US 9272994, compound M15, shows growth inhibition and induction of apoptosis against human cancer cells with IC50 values of 43.02 μM in HCT-116 cell and 41.59 μM in H-1299 cell, respectively.
  • HY-B0061
    Tandospirone citrate

    SM-3997 citrate

    5-HT Receptor Neurological Disease
    Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).
  • HY-100656
    Desmethyl cariprazine

    Dopamine Receptor 5-HT Receptor Drug Metabolite Neurological Disease
    Desmethyl cariprazine is an active metabolite of Cariprazine. Cariprazine, an antipsychotic drug candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM).
  • HY-135122
    DC10SMe

    ADC Cytotoxin DNA Alkylator/Crosslinker Cancer
    DC10SMe is a DNA alkylator, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC10SMe exhibits IC50s of 15 pM, 12 pM, and 12 pM for Ramos, Namalwa, and HL60/s cancer cells, respectively.
  • HY-15477
    YS-49

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-15314
    Ranirestat

    AS-3201

    Aldose Reductase Metabolic Disease Neurological Disease
    Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC50s of 11 nM and 15 nM for rat lens AR and recombinant human AR, respectively, and a Ki of 0.38 nM for recombinant human AR. Ranirestat has the potential for diabetic sensorimotor polyneuropathy treatment. Ranirestat also has a neuroprotective effect on diabetic retinas.
  • HY-B0032A
    Lurasidone

    SM-13496

    5-HT Receptor Dopamine Receptor Neurological Disease
    Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
  • HY-B0032
    Lurasidone Hydrochloride

    SM-13496 Hydrochloride

    5-HT Receptor Dopamine Receptor Neurological Disease
    Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
  • HY-U00322
    5-HT3 antagonist 3

    5-HT Receptor Neurological Disease
    5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. 5-HT3 antagonist 3 binds to 5-HT3 receptors in rat brain cortical membranes with Ki of 0.25 nM.
  • HY-129910
    FABP5-IN-1

    FABP Inflammation/Immunology
    FABP5-IN-1(Compounds 4j) is a selective and high affinity fatty acid binding protein 5 (FABP5) inhibitor with a Ki value of 1.7 μM, and does not bind to both FABP3 and FABP7. FABP5-IN-1 shows potent antinociceptive effects.
  • HY-B0824
    Bifenthrin

    Sodium Channel
    Bifenthrin is a synthetic pyrethroid insecticide that prolongs opening of sodium channels resulting in membrane depolarization and conductance block in the insect nervous system. Bifenthrin is effective against A. gambiae and C. quinquefasciatus mosquitos (LD50s = 0.15 and 0.16 ng/mg, respectively) and increases O. insidiosus mortality in treated corn and sorghum plants.
  • HY-104012
    Islatravir

    MK-8591

    HIV Reverse Transcriptase Infection
    Islatravir (MK-8591) is a potent anti-HIV-1 agent, acting as a nucleoside reverse transcriptase inhibitor, with EC50s of 0.068 nM, 3.1 nM and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively.
  • HY-14763S
    Cariprazine D6

    RGH-188 D6

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Cariprazine D6 (RGH-188 D6) is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM).
  • HY-14940
    Volinanserin

    MDL100907; M 100907

    5-HT Receptor Neurological Disease
    Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
  • HY-14558
    Tandospirone

    SM-3997

    5-HT Receptor Neurological Disease
    Tandospirone(SM-3997) is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).
  • HY-109571
    HZ-1157

    HCV Protease Infection Inflammation/Immunology
    HZ-1157 inhibits HCV NS3/4A protease with an IC50 of 1.0 μmol/L. HZ-1157 (4a) has a high dengue virus inhibitory activity (EC50 = 0.15 μM) and is a relatively nontoxic (CC50 > 10 μM) dengue antiviral agent.
  • HY-103353
    SID 26681509

    Cathepsin Parasite Cancer Infection
    SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.
  • HY-114181
    IRAK4-IN-4

    IRAK Inflammation/Immunology
    IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.
  • HY-108587
    ICA 110381

    Potassium Channel Neurological Disease
    ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 is a KCNQ2/Q3 agonist (EC50=0.38 μM) as well as KCNQ1 antagonist (IC50=15 μM).
  • HY-101489
    GZD856

    PDGFR Bcr-Abl Cancer
    GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities. Also a Bcr-Abl T315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant.
  • HY-N6061
    Ophiopogonin C

    Others Cancer
    Ophiopogonin C, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin C shows cytotoxic activity against two human tumor cell lines MG-63 and SNU387 with IC50s of 19.76 μM and 15.51 μM, respectively.
  • HY-130244
    BACE1-IN-5

    Beta-secretase Neurological Disease
    BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux.
  • HY-124819
    D13-9001

    Bacterial Infection
    D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the KD values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively. D13-9001 exhibits antibiotic activities.
  • HY-100658
    Didesmethyl cariprazine

    5-HT Receptor Dopamine Receptor Neurological Disease
    Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic drug candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor.
  • HY-103319
    Calmidazolium chloride

    R 24571

    CaMK Autophagy Cancer Neurological Disease
    Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to CaMK with a Kd of 3 nM.
  • HY-P1597
    Malantide

    PKA PKC Cancer
    Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-15477A
    YS-49 monohydrate

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-15298C
    Grazoprevir sodium salt

    MK-5172 (sodium salt)

    HCV HCV Protease Infection
    Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
  • HY-15298B
    Grazoprevir hydrate

    MK-5172 (hydrate)

    HCV HCV Protease
    Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
  • HY-19120
    KB-5492 anhydrous

    Sigma Receptor Inflammation/Immunology
    KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent.
  • HY-N6785
    Okadaic acid

    Phosphatase Parasite Apoptosis Infection
    Okadaic acid is extracted from black sponges of the genus Halichondria. Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A and PP3 inhibitor with IC50s of 10-15 nM, 0.5 nM and 4 nM, respectively. Okadaic acid eliminate metazoan symbionts/parasites by apoptosis.
  • HY-10987A
    ENMD-2076

    Aurora Kinase FLT3 VEGFR FGFR PDGFR Src Apoptosis Cancer
    ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
  • HY-15298
    Grazoprevir

    MK-5172

    HCV Protease HCV Infection
    Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
  • HY-122337
    Streptolydigin

    Portamycin

    DNA/RNA Synthesis Bacterial Infection
    Streptolydigin (Portamycin) is a 3-acetyltetramic acid antibiotic and a potent bacterial RNA polymerase inhibitor with a Ki of 18 μM and a Kd of 15 μM. Streptolydigin inhibits RNA synthesis by binding to RNA polymerase and does not inhibit eukaryotic RNA polymerases. Streptolydigin possess potent antibacterial activity, particularly against anaerobes and some Gram-positive aerobes.
  • HY-111925
    BI-749327

    TRP Channel Cardiovascular Disease
    BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.
  • HY-N0288
    Lycorine

    Fatty Acid Synthase (FASN) Virus Protease Bacterial Apoptosis Cancer Inflammation/Immunology
    Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a Kd value 15.24 nM. Lycorine downregulates the SCAP protein level without changing its transcription. Lycorine is also a melanoma vasculogenic inhibitor. Lycorine can be used for the study of prostate cancer and metabolic diseases.
  • HY-10987
    ENMD-2076 Tartrate

    Aurora Kinase FLT3 VEGFR FGFR Src PDGFR Apoptosis Cancer
    ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
  • HY-18056
    PF-915275

    Others Metabolic Disease
    PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively.
  • HY-15298A
    Grazoprevir potassium salt

    MK-5172 (potassium salt)

    HCV HCV Protease Infection
    Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
  • HY-17372
    Rofecoxib

    MK 966

    COX Inflammation/Immunology Cancer
    Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).
  • HY-15394
    (Rac)-Rotigotine hydrochloride

    Dopamine Receptor Adrenergic Receptor 5-HT Receptor Endocrinology Neurological Disease
    (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
  • HY-13200A
    BRL-15572 hydrochloride

    5-HT Receptor Neurological Disease
    BRL-15572 hydrochloride is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 hydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses.
  • HY-16489A
    Terodiline hydrochloride

    mAChR Calcium Channel Neurological Disease
    Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence.
  • HY-P1597A
    Malantide TFA

    PKA PKC Cancer
    Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM.
  • HY-13200
    BRL-15572 dihydrochloride

    BRL-15572

    5-HT Receptor Neurological Disease
    BRL-15572 dihydrochloride is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 dihydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses.
  • HY-122537A
    Arotinolol

    Adrenergic Receptor 5-HT Receptor Cardiovascular Disease
    Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-135902
    Synucleozid

    NSC 377363

    DNA/RNA Synthesis Neurological Disease
    Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
  • HY-B0274
    Chlorprothixene

    Dopamine Receptor Bacterial Neurological Disease
    Chlorprothixene has strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.
  • HY-135902A
    Synucleozid hydrochloride

    NSC 377363 hydrochloride

    DNA/RNA Synthesis Neurological Disease
    Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
  • HY-12164
    Mocetinostat

    MGCD0103

    HDAC Autophagy Apoptosis Cancer
    Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.
  • HY-122560A
    VU0134992 hydrochloride

    Potassium Channel Cardiovascular Disease
    VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
  • HY-B1826
    Adefovir

    GS-0393; PMEA

    HBV Reverse Transcriptase Infection
    Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses.
  • HY-107407
    SB-218078

    Checkpoint Kinase (Chk) CDK PKC Apoptosis Cancer
    SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest.
  • HY-122560
    VU0134992

    Potassium Channel Cardiovascular Disease
    VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
  • 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-17368
    Rivastigmine

    S-Rivastigmine

    AChE Neurological Disease
    Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
  • HY-P1206A
    CH 275 TFA

    Somatostatin Receptor Neurological Disease
    CH 275 TFA is a potent and selective somatostatin receptor 1 (sst1) agonist and display IC50 values of 30.9 nM, 345 nM, >1 μM, >10 μM for human human sst1, sst3, sst4, sst2 and sst5 respectively. CH 275 can be used for the research of Alzheimer’s disease.
  • HY-A0095
    Flibanserin

    BIMT-17; BIMT-17BS

    5-HT Receptor Neurological Disease
    Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD).
  • HY-P1206
    CH 275

    Somatostatin Receptor Neurological Disease
    CH 275 is a potent and selective somatostatin receptor 1 (sst1) agonist and display IC50 values of 30.9 nM, 345 nM, >1 μM, >10 μM for human human sst1, sst3, sst4, sst2 and sst5 respectively. CH 275 can be used for the research of Alzheimer’s disease.
  • HY-N0173
    Cinchonidine

    α-Quinidine

    Serotonin Transporter Parasite Infection
    Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
  • HY-102064
    SR 57227A

    5-HT Receptor Neurological Disease
    SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
  • HY-W008364
    Olivetol

    Cytochrome P450 Cannabinoid Receptor Neurological Disease
    Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.
  • HY-B0731A
    Perospirone

    SM-9018 free base

    5-HT Receptor Dopamine Receptor Neurological Disease
    Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic drug and has the potential for schizophrenic disease.
  • HY-15780S
    Brexpiprazole D8

    OPC-34712 D8

    5-HT Receptor Dopamine Receptor Neurological Disease
    Brexpiprazole D8 (OPC-34712 D8) is a deuterium labeled Brexpiprazole (OPC-34712). Brexpiprazole, an atypical antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine receptor (Ki=0.12 nM and 0.3 nM, respectively). Brexpiprazole is also a 5-HT2A receptor antagonist (Ki=0.47 nM).
  • HY-10930
    UNC0321

    Histone Methyltransferase Cancer
    UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
  • HY-10929
    UNC0224

    Histone Methyltransferase Cancer
    UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-N0515
    Ophiopogonin D

    PPAR NF-κB Calcium Channel Inflammation/Immunology Cardiovascular Disease
    Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
  • HY-10211
    Tanespimycin

    17-AAG; NSC 330507; CP 127374

    HSP Autophagy Mitophagy Bacterial Apoptosis Antibiotic Cancer Infection
    Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.
  • HY-119706
    Barbadin

    Others Others
    Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors.
  • HY-10201
    Sorafenib

    Bay 43-9006

    Raf VEGFR FLT3 Autophagy Apoptosis Ferroptosis Cancer
    Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
  • HY-11017
    Rivastigmine tartrate

    ENA 713; SDZ-ENA 713

    AChE Neurological Disease
    Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
  • HY-124697
    BMP signaling agonist sb4

    TGF-β Receptor Cancer
    BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.
  • HY-13650
    Indisulam

    E 7070

    Carbonic Anhydrase Cancer
    Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15.
  • HY-12546
    Brevetoxin B

    Brevetoxin-2; PbTx-2

    Sodium Channel
    Brevetoxin B (Brevetoxin-2; PbTx-2) is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. Brevetoxin B binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50=15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively. Brevetoxin B is ichthyotoxic at nanomolar concentrations and is responsible for an illness described as neurotoxic shellfish poisoning.
  • HY-121222
    alpha-Bisabolol

    Apoptosis Cancer
    alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells.
  • HY-119037
    UK-101

    Proteasome Apoptosis Cancer
    UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey. UK-101 induces cell apoptosis and can be used for the study of prostate cancer.
  • HY-133152
    Brexpiprazole S-oxide

    DM-3411

    5-HT Receptor Dopamine Receptor Neurological Disease
    Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM.
  • HY-10201A
    Sorafenib Tosylate

    Bay 43-9006 Tosylate

    Raf VEGFR FLT3 Autophagy Ferroptosis Apoptosis Cancer
    Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator.
  • HY-123076
    Pifithrin-α, p-Nitro, Cyclic

    PFN-α

    MDM-2/p53 Neurological Disease
    Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
  • HY-12119
    GW274150

    NO Synthase Inflammation/Immunology Neurological Disease
    GW274150 is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation.
  • HY-12119A
    GW274150 phosphate

    NO Synthase Inflammation/Immunology Neurological Disease
    GW274150 phosphate is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 phosphate displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 phosphate exerts a protective role in an acute model of lung injury inflammation.
  • HY-13456
    LY-404187

    iGluR Neurological Disease
    LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases.
  • HY-135855
    SARS-CoV-IN-1

    SARS-CoV Parasite Infection
    SARS-CoV-IN-1 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-1 shows anti-Coronavirus activity with an EC50 of 4.9 μM in Vero cells. SARS-CoV-IN-1 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 15.4 and 133.2 nM; and IC90s of 25.7 and 459.1 nM; respectively. Antimalarial and antiviral activities.
  • HY-13807
    UNC0646

    Histone Methyltransferase Cancer
    UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-13866
    Ro 31-8220 mesylate

    Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate

    PKC Neurological Disease Cardiovascular Disease Cancer
    Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
  • HY-123023
    12(S)-HETE D8

    Others
    12(S)-HETE D8 contains eight deuterium atoms at the 5, 6, 8, 9, 11, 12, 14 and 15 positions. It is intended for use as an internal standard for the quantification of 12(S)-HETE by GC- or LC-mass spectrometry (MS). 12(S)-HETE D8 is the predominant lipoxygenase product of mammalian platelets. It enhances tumor cell adhesion to endothelial cells, fibronectin, and the subendothelial matrix at 0.1 µM.
  • HY-13233A
    Talabostat mesylate

    Val-boroPro mesylate; PT100 mesylate

    Dipeptidyl Peptidase Cancer Inflammation/Immunology
    Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
  • HY-103712A
    Samuraciclib hydrochloride

    CT7001 hydrochloride; ICEC0942 hydrochloride

    CDK Apoptosis Cancer
    Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects.
  • HY-14544
    Quetiapine

    ICI204636

    5-HT Receptor Dopamine Receptor Neurological Disease
    Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
  • HY-13233
    Talabostat

    Val-boroPro; PT100

    Dipeptidyl Peptidase Cancer Inflammation/Immunology
    Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
  • HY-13866A
    Ro 31-8220

    Bisindolylmaleimide IX

    PKC Neurological Disease Cardiovascular Disease
    Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
  • HY-N6792
    T-​2 Toxin

    T-2 Mycotoxin

    Apoptosis DNA/RNA Synthesis Metabolic Disease
    T-2 Toxin (T-2 Mycotoxin) is a toxic trichothecene mycotoxin produced by various Fusarium species in feedstuffs and cereal grains, LD50 values of T-2 Toxin in mice and rats are 5.2 and 1.5 mg/kg BW a,respectively . T-2 Toxin (T-2 Mycotoxin) can be transformed into a variety of metabolite, the typical metabolites of T-2 toxin in animals are HT-2 toxin and T-2-triol, which are hydrolysates. T-2 Toxin (T-2 Mycotoxin) is an inhibitor of protein synthesis resulting from binding peptidyltransferase, which is an integral part of the 60s ribosomal subunit. T-2 Toxin (T-2 Mycotoxin) inhibits the synthesis of DNA and RNA, interferes with the metabolism of membrane phospholipids, and increases the level of liver lipid peroxides. T-2 Toxin (T-2 Mycotoxin) induces apoptosis in the immune system, gastrointestinal tissues, and fetal tissues.
  • HY-40178
    NH2-C4-NH-Boc

    PROTAC Linker Cancer
    NH2-C4-NH-Boc (compound 15) is a PROTAC linker, which refers to the Alkyl/ether composition. NH2-C4-NH-Boc can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-112345
    PD-089828

    FGFR PDGFR EGFR Src Cancer
    PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.
  • HY-12304
    IOX1

    Histone Demethylase Cancer
    IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively. IOX1 also inhibits ALKBH5.
  • HY-B1658A
    Frovatriptan succinate hydrate

    5-HT Receptor Neurological Disease
    Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT1B, HT1D receptor agonist and a moderately potent 5-HT7 receptor agonist, with pKi values of 8.6, 8.4, and 6.7, respectively. Frovatriptan succinate hydrate is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine.
  • HY-116214
    Cyprodinil

    Fungal Androgen Receptor
    Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
  • HY-B0031
    Quetiapine hemifumarate

    5-HT Receptor Dopamine Receptor Neurological Disease
    Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
  • HY-101514
    β3-AR agonist 1

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).
  • HY-B0879
    Suramin

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase Parasite Apoptosis Cancer Infection Cardiovascular Disease
    Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-133152S
    Brexpiprazole S-oxide D8

    DM-3411 D8

    5-HT Receptor Dopamine Receptor Neurological Disease
    Brexpiprazole S-oxide D8 (DM-3411 D8) is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM.
  • HY-100769
    YL0919

    5-HT Receptor Neurological Disease
    YL0919 is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). YL0919 inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. YL0919 shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.
  • HY-19336
    BAZ2-ICR

    Epigenetic Reader Domain Cancer
    BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.
  • HY-N3032
    Xanthatin

    Apoptosis VEGFR Lipoxygenase Bacterial Cancer Infection Inflammation/Immunology
    Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer.
  • HY-B0879A
    Suramin sodium salt

    Suramin hexasodium salt

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase Parasite Apoptosis Cancer Infection Cardiovascular Disease
    Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-101044
    PPADS tetrasodium

    P2X Receptor Na+/Ca2+ Exchanger Neurological Disease
    PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca²⁺exchanger in guinea pig airway smooth muscle.
  • HY-101094
    Ocaperidone

    R79598

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
  • HY-108359
    Alsterpaullone

    9-Nitropaullone; NSC 705701

    CDK GSK-3 Cancer
    Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders.
  • HY-133124
    PARP/PI3K-IN-1

    PARP PI3K Apoptosis Cancer
    PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.
  • HY-135906
    CK2/ERK8-IN-1

    Casein Kinase ERK Pim DYRK Apoptosis Cancer
    CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.
  • HY-130612
    PROTAC BRD2/BRD4 degrader-1

    Epigenetic Reader Domain PROTAC Cancer
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.
  • HY-B1101
    Pimethixene

    Pimetixene

    5-HT Receptor Histamine Receptor Neurological Disease Endocrinology
    Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
  • HY-107738
    Guggulsterone

    Z/E-Guggulsterone

    Apoptosis JNK Akt Caspase FXR Autophagy Cancer
    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.
  • HY-B1101A
    Pimethixene maleate

    Pimetixene maleate

    5-HT Receptor Histamine Receptor Neurological Disease Endocrinology
    Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
  • HY-112544
    IK1 inhibitor PA-6

    PA-6

    Potassium Channel Cardiovascular Disease
    IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia.
  • HY-101308
    MRS2179 tetrasodium

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium inhibits platelet aggregation.
  • HY-108400
    SCH-23390 maleate

    R-(+)-SCH-23390 maleate

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-105285
    Piromelatine

    Neu-P11

    Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel Neurological Disease
    Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
  • HY-115687
    PDE4B-IN-2

    Phosphodiesterase (PDE)
    PDE4B-IN-2 is an orally active and selective PDE4B inhibitor (IC50=15 nM) and exhibits >100-fold selectivity for PDE4B over 4D. PDE4B-IN-2 regulates cAMP in inflammatory cells and inhibits LPS-induced TNF-α production and neutrophil accumulation in mouse lungs. PDE4B-IN-2 reduces microglial and neutrophil activation, and improves behavioral deficits in a traumatic brain injury model in vivo. PDE4B-IN-2 also exhibits antidepressant-like effects.
  • HY-19545A
    SCH-23390 hydrochloride

    R-(+)-SCH-23390 hydrochloride

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-130619
    Boc-C1-PEG3-C4-OBn

    PROTAC Linker Cancer
    Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-107836
    Methiothepin mesylate

    Metitepine mesylate; Ro 8-6837 mesylate

    5-HT Receptor Neurological Disease
    Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-N0049
    Nuciferine

    5-HT Receptor Dopamine Receptor Neurological Disease
    Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
  • HY-18137
    PF-04995274

    5-HT Receptor Neurological Disease
    PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
  • HY-19974
    TAK-220

    CCR HIV Infection Endocrinology
    TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.