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Results for "Ang (4-8) Inhibitors" in MCE Product Catalog:

163

Inhibitors & Agonists

12

Peptides

11

Natural
Products

2

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-130592
    Compound 48/80 trihydrochloride

    C48/80 trihydrochloride

    Phospholipase Neurological Disease
    Compound 48/80 trihydrochloride (C48/80 trihydrochloride) is a mixture of condensation products of N-methyl-p-methoxyphenethylamine with formaldehyde. Compound 48/80 trihydrochloride is also a histamine releaser and a mast cell degranulator. Compound 48/80 inhibits phosphatidylinositol-specific phospholipase C activity from human platelets .
  • HY-131066
    EMI48

    EGFR Cancer
    EMI48, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI48 inhibits EGFR triple mutants.
  • 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-133289
    m-PEG48-OH

    PROTAC Linker Cancer
    m-PEG48-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-133284
    m-PEG48-Br

    PROTAC Linker Cancer
    m-PEG48-Br is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140986
    m-PEG48-Mal

    PROTAC Linker Cancer
    m-PEG48-Mal is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140230
    m-PEG48-amine

    PROTAC Linker Cancer
    m-PEG48-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-18630
    Ro 48-8071

    Others Cancer
    Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
  • HY-126154
    L48H37

    Toll-like Receptor (TLR) Inflammation/Immunology
    L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is used for the research of sepsis or lung injury treatment.
  • HY-18630A
    Ro 48-8071 fumarate

    Others Cancer
    Ro 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
  • HY-121385
    Hydroxy bosentan

    Ro 48-5033

    Endogenous Metabolite Cardiovascular Disease
    Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities.
  • HY-10309
    Sibrafiban

    RO 48-3657

    Integrin Cardiovascular Disease
    Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.
  • HY-129522
    Sulfo-ara-F-NMN

    CZ-48

    Toll-like Receptor (TLR) Neurological Disease
    Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 μM). Sulfo-ara-F-NMN induces intracellular cyclic ADP-ribose (cADPR) production.
  • 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-N6062
    Perivine

    Perivin

    Others Neurological Disease
    Perivine (Perivin) targets protein retinoblastoma-associated proteins (RbAp48) and resolves the instability of the RbAp48-FOG-1 complex. Perivine can be used for the study of Alzheimer's disease.
  • HY-13929
    Isocarboxazid

    Monoamine Oxidase Neurological Disease
    Isocarboxazid is a non-selective and irreversible inhibitor of monoamine oxidase, with an IC50 of 4.8 μM for rat brain monoamine oxidase in vitro.
  • HY-101844
    ML-18

    Bombesin Receptor Cancer
    ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
  • HY-12134
    Poloxin

    Polo-like Kinase (PLK) Cancer
    Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.
  • HY-13005
    Fagomine

    D-Fagomine

    Others Metabolic Disease
    Fagomine is a mild glycosidase inhibitor. The Ki of the iminosugar Fagomine is 4.8 μM, 39 μM, and 70 μM for Amyloglucosidase (A.niger), β-Glucosidase (bovine), and Isomaltase (yeast), respectively.
  • HY-13108
    Bz 423

    BZ48

    Bcl-2 Family Inflammation/Immunology
    Bz 423 is a pro-apoptotic 1,4-benzodiazepine with therapeutic properties in murine models of lupus demonstrating selectivity for autoreactive lymphocytes, and activates Bax and Bak.
  • HY-19568
    Peficitinib

    ASP015K; JNJ-54781532

    JAK Inflammation/Immunology Cancer
    Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
  • HY-15975
    GNF179

    Parasite Infection
    GNF179 is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
  • HY-12663
    AS2521780

    PKC Inflammation/Immunology
    AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
  • HY-100385
    Brevianamide F

    Cyclo(L-Pro-L-Trp)

    PI3K Bacterial Infection
    Brevianamide F (Cyclo(L-Pro-L-Trp)) is a mycotoxin isolated from Colletotrichum gloeosporioides, with antibacterial activity. Brevianamide F shows potent PI3Kα inhibitory activity with an IC50 of 4.8 µM.
  • HY-14559
    PRX-07034 hydrochloride

    5-HT Receptor Neurological Disease
    PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 4-8 nM and an IC50 of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility.
  • HY-120469
    GDC-046

    JAK Inflammation/Immunology
    GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
  • HY-12017
    PF-04217903

    c-Met/HGFR Cancer
    PF-04217903 is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties.
  • HY-11018
    Risperidone

    R 64 766

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-16594
    Lactacystin

    Proteasome Neurological Disease
    Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces neurite outgrowth.
  • HY-112296
    T025

    CDK Cancer
    T025 is an orally available and highly potent Cdc2-like kinase (CLK) inhibitor with Kds of 4.8, 0.096, 6.5, and 0.61 nM for CLK1, CLK2, CLK3, and CLK4, respectively.
  • HY-15980
    GNF179 Metabolite

    Parasite Infection
    GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
  • HY-11018A
    Risperidone hydrochloride

    R 64 766 hydrochloride

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone hydrochloride (R 64 766 hydrochloride) 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-12017A
    PF-04217903 methanesulfonate

    c-Met/HGFR Cancer
    PF-04217903 methanesulfonate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 methanesulfonate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties.
  • HY-12017B
    PF-04217903 phenolsulfonate

    c-Met/HGFR Cancer
    PF-04217903 phenolsulfonate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 phenolsulfonate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties.
  • HY-101769
    UAMC00039 dihydrochloride

    Dipeptidyl Peptidase Cancer
    UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.
  • HY-11018B
    Risperidone mesylate

    R 64 766 mesylate

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-114668
    Camptothecin-20(S)-O-propionate

    Camptothecin-20-O-propionate

    Topoisomerase Cancer
    Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor.
  • 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-100509
    NPS-1034

    TAM Receptor c-Met/HGFR Apoptosis Cancer
    NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.
  • HY-107675
    Desformylflustrabromine hydrochloride

    Deformylflustrabromine hydrochloride; dFBr hydrochloride

    nAChR Neurological Disease
    Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
  • HY-15979A
    H-89 dihydrochloride

    Protein kinase inhibitor H-89 dihydrochloride

    PKA Autophagy Others
    H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.
  • HY-116830
    BRD0705

    GSK-3 Cancer
    BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).
  • HY-135194
    Risperidone E-oxime

    Others Others
    Risperidone E-oxime is an impurity of Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
  • 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-19544
    JAK3-IN-1

    JAK Cancer
    JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
  • HY-N1074
    Warangalone

    Scandenolone

    Parasite PKA Infection Inflammation/Immunology
    Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
  • HY-135881
    OMDM-5

    TRP Channel Endogenous Metabolite Neurological Disease
    OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM).
  • HY-109124
    Taniborbactam

    VNRX-5133

    Bacterial Infection
    Taniborbactam (VNRX-5133) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam is against Gram-negative bacteria.
  • HY-109124A
    Taniborbactam hydrochloride

    VNRX-5133 hydrochloride

    Bacterial Infection
    Taniborbactam hydrochloride (VNRX-5133 hydrochloride) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam hydrochloride has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam hydrochloride is against Gram-negative bacteria.
  • HY-19822
    Elacestrant

    RAD1901

    Estrogen Receptor/ERR Cancer
    Elacestrant (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-19822A
    Elacestrant dihydrochloride

    RAD1901 dihydrochloride

    Estrogen Receptor/ERR Cancer
    Elacestrant dihydrochloride (RAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-18347A
    Conivaptan hydrochloride

    YM 087

    Vasopressin Receptor Cardiovascular Disease Endocrinology
    Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.
  • HY-15979
    H-89

    Protein kinase inhibitor H-89

    PKA Autophagy Neurological Disease
    H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.
  • 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-17356
    Fenofibrate

    PPAR Cytochrome P450 Autophagy Cardiovascular Disease Cancer
    Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
  • HY-111465
    CDK8-IN-4

    CDK Cancer
    CDK8-IN-4 is an inhibitor of CDK8 extracted from patent WO2014090692A1, compound example 16, with an IC50 of 0.2 nM.
  • HY-116830A
    (Rac)-BRD0705

    GSK-3 Cancer
    (Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).
  • HY-12838
    Mirk-IN-1

    Dyrk1B/A-IN-1

    DYRK Cancer
    Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.
  • HY-13455
    LDN-192960

    Haspin Kinase DYRK Cancer
    LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
  • HY-13455A
    LDN-192960 hydrochloride

    Haspin Kinase DYRK Cancer
    LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
  • HY-126242S
    Tyk2-IN-7

    JAK Inflammation/Immunology
    Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 (Compound 48) provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 (Compound 48) provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model.
  • HY-100619
    BMS-986020

    LPL Receptor Metabolic Disease Inflammation/Immunology
    BMS-986020 is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
  • HY-127146
    Platensimycin

    Antibiotic Bacterial
    Platensimycin is an antibiotic produced by S. platensis that inhibits gram-positive bacteria by selectively inhibiting cellular lipid biosynthesis (IC50=0.1 μM). Platensimycin targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s=48 nM and 160 nM for S.aureus and E.coli enzymes, respectively). Platensimycin is a promising agent for overcoming antibiotic resistance.
  • HY-116830B
    BRD5648

    (R)-BRD0705

    Others Cancer
    BRD5648 ((R)-BRD0705) is an inactive (R)-enantiomer of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).
  • HY-100619A
    BMS-986020 sodium

    LPL Receptor Metabolic Disease Inflammation/Immunology
    BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
  • HY-B1270
    Isoxsuprine hydrochloride

    Adrenergic Receptor iGluR Neurological Disease Endocrinology
    Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
  • HY-135366
    HPN-01

    IKK Inflammation/Immunology
    HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.
  • HY-120214
    TAS05567

    Syk Inflammation/Immunology
    TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases.
  • HY-120179
    LP-922761

    Others Neurological Disease
    LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with an in vitro IC50 of 4.8 nM and a cellular IC50 of 7.6 nM. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
  • HY-15123
    (S)-Flurbiprofen

    Esflurbiprofen

    COX PGE synthase Inflammation/Immunology
    (S)-Flurbiprofen is an active enantiomer of Flurbiprofen, with IC50 values of 0.48 μM and 0.47 μM for COX-1 and COX-2, respectively.
  • HY-19822D
    Elacestrant S enantiomer

    RAD1901 S enantiomer

    Estrogen Receptor/ERR Cancer
    Elacestrant S enantiomer is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-13227
    SD-208

    TGF-β Receptor Cancer
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
  • HY-19822B
    Elacestrant S enantiomer dihydrochloride

    RAD1901 S enantiomer dihydrochloride; RAD 1901 S enantiomer dihydrochloride; RAD-1901 S enantiomer dihydrochloride

    Estrogen Receptor/ERR Cancer
    Elacestrant S enantiomer dihydrochloride is an low activity enantiomer of elacestrant dihydrochloride. Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-101354
    R-IMPP

    Ser/Thr Protease Cancer Cardiovascular Disease
    R-IMPP is an anti-secretagogue of PCSK9 (IC50=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation.
  • HY-B0790
    TAI-1

    Apoptosis Cancer
    TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.
  • HY-100208
    HC-067047

    TRP Channel Cancer
    HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.
  • 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-10339
    KW-2449

    FLT3 FGFR Bcr-Abl Aurora Kinase Apoptosis Cancer
    KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABL T315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
  • HY-N0112
    Dihydromyricetin

    Ampelopsin; Ampeloptin

    mTOR Autophagy Cancer
    Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2).
  • HY-N5002
    (+)-Viroallosecurinine

    Bacterial Infection
    (+)-Viroallosecurinine, isolated from Securinega virosa as a cytotoxic alkaloid, exhibits a MIC of 0.48 μg/mL for Ps. Aeruginosa and Staph. aureus. Antibacterial activity.
  • HY-136267
    HCV-IN-30

    HCV Infection
    HCV-IN-30 (compound 48) is a HCV NS5A replication complex inhibitor, with IC50s of 901 and 102 nM for genotypes 1a and 1b replicons, respectively.
  • HY-136203
    Resveratrol analog 1

    IKK Autophagy Mitophagy Sirtuin Cancer Inflammation/Immunology
    Resveratrol analog 1 is an analog of Resveratrol (HY-16561), compound 48. Resveratrol is a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties.
  • HY-100984
    HA-100

    PKA PKC Myosin Cancer
    HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50s of 4, 8, 12 and 240 μM, respectively.
  • HY-126320
    EGFR-IN-8

    EGFR c-Met/HGFR Cancer
    EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.
  • HY-123230
    Trifloxystrobin

    CGA 279202

    Fungal Infection
    Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h.
  • 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-13515
    Sirtinol

    Sirtuin Autophagy Apoptosis Cancer
    Sirtinol is a sirtuin (SIRT) inhibitor, with IC50s of 48 μM, 57.7 μM and 131 μM for ySir2, hSIRT2 and hSIRT2, respectively.
  • HY-128832
    Nutlin-C1-amido-PEG4-C2-N3

    MDM2 Ligand-Linker Conjugates 1; E3 ligase Ligand-Linker Conjugates 48

    E3 Ligase Ligand-Linker Conjugate Cancer
    Nutlin-C1-amido-PEG4-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Nutlin 3 based MDM2 ligand and 4-unit PEG linker used in PROTAC technology.
  • HY-136430
    JCN037

    JGK037

    EGFR Cancer
    JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.
  • HY-15044
    NU1025

    PARP Cancer Neurological Disease
    NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity.
  • HY-P1132
    Galanin (1-29)(rat, mouse)

    Neuropeptide Y Receptor Neurological Disease
    Galanin (1-29)(rat, mouse) is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3 respectively. Anticonvulsant effect.
  • HY-113514
    6-Phosphogluconic acid

    Endogenous Metabolite Metabolic Disease
    6-Phosphogluconic acid is a potent and competitive phosphoglucose isomerase (PGI) inhibitor with Kis of 48 μM for glucose 6-phosphate and 42 μM for fructose 6-phosphate. 6-Phosphogluconic acid is an endogenous metabolite.
  • HY-16026
    Ricolinostat

    ACY-1215; Rocilinostat

    HDAC Apoptosis Cancer
    Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.
  • HY-P1132A
    Galanin (1-29)(rat, mouse) TFA

    Neuropeptide Y Receptor Neurological Disease
    Galanin (1-29)(rat, mouse) TFA is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3, respectively. Anticonvulsant effect.
  • HY-B0760
    Fenofibric acid

    FNF acid

    PPAR COX Metabolic Disease
    Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 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-P1249
    Neuropeptide SF(mouse,rat)

    Neuropeptide Y Receptor Neurological Disease
    Neuropeptide SF (mouse,rat) is a potent neuropeptide FF receptor agonist with Ki values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .
  • HY-101641
    NRA-0160

    Dopamine Receptor 5-HT Receptor Adrenergic Receptor Neurological Disease Endocrinology
    NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2A receptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).
  • HY-122295
    Dehydroleucodine

    Apoptosis Cancer Inflammation/Immunology
    Dehydroleucodine is a sesquiterpene lactone isolated from Gynoxys verrucosa. Dehydroleucodine is a mast cell stabilizer that inhibits tmast cell degranulation induced by compound 48/80. Dehydroleucodine inudces cells apoptosis, and has gastric ulcer inhibition and antileukemic effects.
  • HY-12057
    Vemurafenib

    PLX4032; RG7204; RO5185426

    Raf Autophagy Cancer
    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
  • HY-N6256
    Ilexsaponin B2

    Phosphodiesterase (PDE) Cardiovascular Disease
    Ilexsaponin B2 is a saponin isolated from the root of Ilex pubescens Hook. et Arn. Ilexsaponin B2 is a potent phosphodiesterase 5 (PDE5) and PDEI inhibitor with IC50 values of 48.8 μM and 477.5 μM, respectively.
  • HY-100488
    Bay 59-3074

    Cannabinoid Receptor Cancer
    Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. Bay 59-3074 has analgesic properties.
  • 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-P1249A
    Neuropeptide SF(mouse,rat) TFA

    Neuropeptide Y Receptor Neurological Disease
    Neuropeptide SF (mouse,rat) TFA is a potent neuropeptide FF receptor agonist with Ki values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF TFA increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .
  • HY-128602
    c-Kit-IN-2

    c-Kit Cancer
    c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively.
  • HY-122825
    SNIPER(ER)-110

    SNIPER Estrogen Receptor/ERR Cancer
    SNIPER(ER)-110 consists of a cIAP1 ligand and an estrogen ligand, connected by a linker. SNIPER(ER)-51 induces estrogen receptor (ER) protein degradation with DC50s of <3 nM and 7.7 nM after 4 h and 48 h, respectively.
  • HY-12930
    SPR719

    VXc-486

    Topoisomerase Bacterial Infection
    SPR719 (VXc-486) is a gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively.
  • 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-136342
    Antitumor agent-23

    Others Cancer
    Antitumor agent-23 is a potent anti-cancer agent with GI50s of 38, 48, 5, 27, 80, and 28 nM for lymphoma cell line GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI, respectively. Antitumoral activity.
  • HY-P1202
    CYN 154806

    Somatostatin Receptor Endocrinology
    CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
  • HY-130119
    Integrin-IN-2

    Integrin Cancer
    Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively.
  • HY-P1202A
    CYN 154806 TFA

    Somatostatin Receptor Endocrinology
    CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
  • HY-12305
    Q-VD-OPh

    QVD-OPH; Quinoline-Val-Asp-Difluorophenoxymethylketone

    Caspase HIV Cancer Infection
    Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.
  • HY-16210
    Forodesine

    BCX-1777; Immucillin-H

    Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels.
  • HY-10197
    Wortmannin

    SL-2052; KY-12420

    PI3K Polo-like Kinase (PLK) Autophagy Cancer
    Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively.
  • HY-16209
    Forodesine hydrochloride

    BCX-1777 hydrochloride; Immucillin-H hydrochloride

    Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Forodesine hydrochloride (BCX-1777 hydrochloride) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels.
  • HY-14722C
    NVP-BSK805 trihydrochloride

    JAK Cancer
    NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
  • HY-14722A
    NVP-BSK805 dihydrochloride

    JAK Cancer
    NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
  • HY-14722
    NVP-BSK805

    JAK Cancer
    NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
  • HY-N5005
    Guanfu base H

    Atisinium chloride

    Parasite Infection
    Guanfu base H (Atisinium chloride) is a diterpenoid alkaloid isolated from Aconitum coreanum and has antiplasmodial activity against the malarial Plasmodium falciparum strains TM4/8.2 (wild type) and K1CB1 with IC50 values of 4 μM and 3.6 μM, respectively.
  • 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-18161
    CCT241736

    FLT3 Aurora Kinase Cancer
    CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
  • HY-15039
    SSR240612

    Bradykinin Receptor Metabolic Disease Inflammation/Immunology Endocrinology
    SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
  • HY-106161
    Rupintrivir

    AG7088

    Virus Protease Enterovirus Infection Inflammation/Immunology
    Rupintrivirvr (AG7088), an antiviral drug, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC50 of 0.023 μM. Rupintrivirvr shows immune-modulatory effect.
  • 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-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-B0623A
    Ropinirole hydrochloride

    SKF 101468 hydrochloride

    Dopamine Receptor Neurological Disease
    Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.
  • HY-101121
    NI-42

    Epigenetic Reader Domain Cancer
    NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins.
  • HY-124308
    PS315

    PKC Cancer
    PS315, a derivative of PS48, is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCι (IC50=30 μM). PS315 has anti-cancer activity.
  • HY-103050
    ML-030

    Phosphodiesterase (PDE) Inflammation/Immunology
    ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively.
  • HY-136573
    5-Hydroxytoluene-2,4-disulphonic acid diammonium

    Virus Protease Infection
    5-Hydroxytoluene-2,4-disulphonic acid diammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
  • HY-136575
    4-Hydroxy-2-methylbenzenesulfonic acid ammonium

    Virus Protease Infection
    4-Hydroxy-2-methylbenzenesulfonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
  • HY-136574
    2-Hydroxy-4-methylbenzenesulphonic acid ammonium

    Virus Protease Infection
    2-Hydroxy-4-methylbenzenesulphonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-10115
    PI-103

    PI3K mTOR DNA-PK Autophagy Apoptosis Cancer
    PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.
  • HY-10115A
    PI-103 Hydrochloride

    PI3K mTOR DNA-PK Autophagy Apoptosis Cancer
    PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.
  • 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-111977
    ZEN-3219

    Epigenetic Reader Domain Cancer
    ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4.
  • HY-124662
    IHVR-19029

    Glucosidase Infection
    IHVR-19029 is a potent endoplasmic reticulum (ER) α-glucosidases I and II inhibitor, with an IC50 of 0.48 μM for ER a-glucosidase I. IHVR-19029 efficiently blocks the replication of several hemorrhagic fever viruses, such as Dengue virus (DENV), Ebola virus (EBOV) and Rift Valley fever virus. The combination of IHVR-19029 with Favipiravir (HY-14768) improves the antiviral efficacy.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-128717A
    GSK3368715 dihydrochloride

    EPZ019997 dihydrochloride

    Histone Methyltransferase Cancer
    GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
  • HY-128717
    GSK3368715

    EPZ019997

    Histone Methyltransferase Cancer
    GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
  • HY-122720
    SEC inhibitor KL-1

    KL-1

    Others Cancer
    SEC inhibitor KL-1 (KL-1), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-1 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 3.48 μM.
  • HY-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-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-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-121638A
    (5Z,2E)-CU-3

    Apoptosis Cancer
    (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
  • 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-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-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-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-121638
    CU-3

    Apoptosis Cancer Inflammation/Immunology
    CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
  • 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-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-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-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-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-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-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.