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Results for "Ang (1-4) Inhibitors" in MCE Product Catalog:

505

Inhibitors & Agonists

2

Screening Libraries

4

Dye Reagents

2

Biochemical Assay Reagents

59

Peptides

68

Natural
Products

5

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-P1932
    Cortistatin-14

    Somatostatin Receptor Inflammation/Immunology Neurological Disease Endocrinology
    Cortistatin-14, a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties.
  • HY-P1328
    TAT-14

    Keap1-Nrf2 Others
    TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
  • HY-N4323
    14-Deoxyandrographolide

    Others Metabolic Disease
    14-Deoxyandrographolide, a bioactive compound of Andrographis paniculata, has hepatoprotective efficacy. 14-Deoxyandrographolide desensitizes hepatocytes to TNF-α-mediated apoptosis through the release of TNFRSF1A release.
  • HY-N0358
    1,4-Dicaffeoylquinic acid

    1,4-DCQA

    Others Inflammation/Immunology
    1,4-Dicaffeoylquinic acid (1,4-DCQA) is a phenylpropanoid from Xanthii fructus, inhibits LPS-stimulated TNF-α production.
  • HY-135678
    DHODH-IN-14

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-14 (Compound 7l) is a hydroxyfurazan analog of A771726. DHODH-IN-14 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.49 μM for rat liver DHODH. DHODH-IN-14 can be used for rheumatoid arthritis.
  • HY-Y0496
    1,4-Dichlorobenzene

    Others Others
    1,4-Dichlorobenzene is used as an intermediate product in the manufacture of pigments, pesticides and disinfectants. 1,4-Dichlorobenzene is also employed as a moth control agent.
  • HY-111442
    GC 14

    Others Metabolic Disease
    GC 14 is a selective thyroid hormone receptor antagonist, with IC50 values of 35 nM and 200 nM for hTRβ and hTRα, respectively.
  • HY-111441
    1,4-Chrysenequinone

    Chrysene-1,4-dione

    Aryl Hydrocarbon Receptor Cancer
    1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR).
  • HY-W015780
    1,4-Dimethoxybenzene

    Endogenous Metabolite Metabolic Disease
    1,4-Dimethoxybenzene is an endogenous metabolite.
  • HY-P1932A
    Cortistatin-14 TFA

    Somatostatin Receptor Inflammation/Immunology Neurological Disease Endocrinology
    Cortistatin-14 (TFA), a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 (TFA) shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties.
  • HY-P1328A
    TAT-14 TFA

    Keap1-Nrf2 Others
    TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
  • HY-N7117
    1,4-Cineole

    TRP Channel Endogenous Metabolite Cancer Inflammation/Immunology
    1,4-Cineole is a widely distributed, natural, oxygenated monoterpene. 1,4-Cineole, present in eucalyptus oil, activates both human TRPM8 and human TRPA1.
  • HY-13329
    IRAK-1-4 Inhibitor I

    IRAK-1/4 Inhibitor I

    IRAK Inflammation/Immunology
    IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.
  • HY-N2468
    Xylobiose

    1,4-β-D-Xylobiose; 1,4-D-Xylobiose

    Others Others
    Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is a disaccharide of xylose monomers with a β-1, 4 bond between monomers.
  • HY-Y1781
    1,4-Diaminobutane dihydrochloride

    Endogenous Metabolite Others
    1,4-Diaminobutane dihydrochloride is an endogenous metabolite, acts as an indicator of pollution-induced stress in higher plants: barley and rape stressed with Cr(III) or Cr(VI) . 1,4-Diaminobutane dihydrochloride is an important source of GABA.
  • HY-135008
    J14

    Reactive Oxygen Species Cancer
    J14 is a reversible sulfiredoxin inhibitor with an IC50 of 8.1 μM. J14 induces oxidative stress (intracellular ROS accumulation) by inhibiting sulfiredoxin, leading to cytotoxicity and cancer cell death.
  • HY-16665
    iCRT 14

    Wnt Cancer
    iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase.
  • HY-114454
    INH14

    IKK Cancer Inflammation/Immunology
    INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.
  • HY-111374
    NMDI14

    Others Cancer
    NMDI14 is a nonsense mediated RNA decay (NMD) inhibitor.
  • HY-136584
    2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid

    Others Metabolic Disease Cardiovascular Disease
    2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid is a ketone compound extracted from patent WO2002030860A2, compound example II-9. 2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid can be used for the research of cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders.
  • HY-N1490
    14-Deoxy-11,12-didehydroandrographolide

    14-dehydro Andrographolide; AP10

    NF-κB Inflammation/Immunology Cancer
    14-Deoxy-11,12-didehydroandrographolide is an analogue of Andrographolide that can be isolated from A. paniculata. 14-Deoxy-11,12-didehydroandrographolide inhibits NF-κB activation.
  • HY-100432
    LOC14

    Others Inflammation/Immunology Neurological Disease
    LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding. LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells.
  • HY-118840
    1,4-D-Gulonolactone

    Endogenous Metabolite Metabolic Disease
    1,4-D-Gulonolactone is an endogenous metabolite.
  • HY-P1792
    Angiotensin II (1-4), human

    Angiotensin Receptor Metabolic Disease Endocrinology
    Angiotensin II (1-4), human is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
  • HY-N3505
    14-Hydroxy sprengerinin C

    Others Others
    14-Hydroxy sprengerinin C is a steroidal compound found in Ophiopogon japonicus.
  • HY-N6839
    1,4-b-D-Xylopentaose

    Others Others
    1,4-b-D-Xylopentaose (Xylopentaose) consists of five b-1,4 xylose sugars.
  • HY-107024
    Osteogenic Growth Peptide (10-14)

    OGP(10-14); Historphin

    Src Others
    Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor.
  • HY-W015490
    1,4-Naphthoquinone

    Others Cancer
    1,4-Naphthoquinone is a potential pharmacophore for inhibition of both MAO (monoamine oxidase) and DNA topoisomerase activities, this latter associated with antitumor activity.
  • HY-128811
    E3 ligase Ligand 14

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-W016628
    L-Gulono-1,4-lactone

    Endogenous Metabolite Metabolic Disease
    L-Gulono-1,4-lactone is a substrate of L-gulono-1,4-lactone oxidoreductase, which catalyzes the last step of the biosynthesis of L-ascorbic (Vatamin) C. In other words, L-Gulono-1,4-lactone is a direct precursor of vitamin C in animals, in plants and in some protists.
  • HY-133298
    Amino-PEG14-alcohol

    H2N-PEG14-OH

    PROTAC Linker Cancer
    Amino-PEG14-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-P1792A
    Angiotensin II (1-4), human TFA

    Angiotensin Receptor Endocrinology Metabolic Disease
    Angiotensin II (1-4), human (TFA) is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
  • HY-141022
    Bis-PEG14-acid

    PROTAC Linker Cancer
    Bis-PEG14-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140178
    Amino-PEG14-acid

    PROTAC Linker Cancer
    Amino-PEG14-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140022
    Propargyl-PEG14-acid

    PROTAC Linker Cancer
    Propargyl-PEG14-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-120430
    HO-PEG14-OH

    PROTAC Linker Cancer
    HO-PEG14-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-135822
    m-PEG14-amine

    PROTAC Linker Cancer
    m-PEG14-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140030
    Propargyl-PEG14-Boc

    PROTAC Linker Cancer
    Propargyl-PEG14-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-P1582
    ACTH (1-14)

    Adrenocorticotropic Hormone Fragment 1-14

    Adrenergic Receptor Cancer
    ACTH (1-14) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production.
  • HY-N0157S
    Orotic acid-6-C14

    Endogenous Metabolite Metabolic Disease
    Orotic acid-6-C14 is an endogenous metabolite.
  • HY-12011
    HA14-1

    Bcl-2 Family Cancer
    HA14-1 is a Bcl-2/Bcl-XL antagonist. HA14-1 binds the designated pocket on Bcl-2 with the IC50 of ≈9 μM in competing with the Bcl-2 binding of Flu-BakBH3, and inhibits its function.
  • HY-B1673
    Pharmatose DCL 14

    Pharmatose 200M; Pharmatose 450M

    Endogenous Metabolite Metabolic Disease
    Pharmatose DCL 14 is an endogenous metabolite.
  • HY-W075674
    Butane-1,4-diyldiphosphonic acid

    PROTAC Linker Cancer
    Butane-1,4-diyldiphosphonic acid is an alkyl chain-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-P1524
    Beta-Amyloid(1-14),mouse,rat

    Amyloid-β Neurological Disease
    Beta-Amyloid(1-14),mouse,rat is a 1 to 14 fragment of Amyloid-β peptide.
  • HY-W004661
    1,4-Dioxane-2,5-diol

    Endogenous Metabolite Metabolic Disease
    1,4-Dioxane-2,5-diol is an endogenous metabolite.
  • HY-15481
    KU14R

    Insulin Receptor Metabolic Disease Endocrinology
    KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.
  • HY-15801
    HG-14-10-04

    ALK Cancer
    HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.
  • HY-117889
    PARP14 inhibitor H10

    PARP Apoptosis Cancer
    PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis.
  • HY-U00090
    N-Methylmoranoline

    MOR 14; N-Methyl-1-deoxynojirimycin; N-Methylmoranolin

    Glucosidase Metabolic Disease
    N-Methylmoranoline (MOR 14) is an α-glucosidase inhibitor.
  • HY-P1291
    PKI 14-22 amide,myristoylated

    PKA Cancer
    PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
  • HY-P1582A
    ACTH (1-14) (TFA)

    Adrenocorticotropic Hormone Fragment 1-14 TFA

    Adrenergic Receptor Others
    ACTH (1-14) (TFA) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production.
  • HY-16694
    BAMB-4

    ITPKA-IN-C14

    Others Cancer
    BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 μM in ADP-Glo Assay.
  • HY-125872
    KRAS G12C inhibitor 14

    Ras Cancer
    KRAS G12C inhibitor 14 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 17, has an IC50 of 18 nM.
  • HY-128426
    Trans-​2-​butene-​1,​4-​dicarboxylic acid

    Endogenous Metabolite Metabolic Disease
    Trans-​2-​butene-​1,​4-​dicarboxylic acid is an endogenous metabolite.
  • 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-140003
    Tetraethyl butane-1,4-diylbis(phosphonate)

    PROTAC Linker Cancer
    Tetraethyl butane-1,4-diylbis(phosphonate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-113123
    LysoPC(14:0/0:0)

    Endogenous Metabolite Metabolic Disease Neurological Disease
    LysoPC(14:0/0:0) is a lysophospholipid (LyP). It is a monoglycerophospholipid in which a phosphorylcholine moiety occupies a glycerol substitution site. LysoPC(14:0/0:0) has potent antispasmodic effect.
  • 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-P2323
    Lactoferricin B (4-14), bovine TFA

    Bacterial Antibiotic Cancer Inflammation/Immunology
    Lactoferricin B (4-14), bovine (TFA), a peptide corresponding to residues 4-14 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms.
  • HY-103642
    D-myo-Inositol 1,4,5-trisphosphate hexapotassium salt

    Inositol 1,4,5-trisphosphate hexapotassium salt; Ins(1,4,5)-P3 hexapotassium salt

    Others Metabolic Disease
    D-myo-Inositol 1,4,5-trisphosphate hexapotassium salt is the hexapotassium salt of D-myo-Inositol 1,4,5-trisphosphate (1,4,5-IP3), which is a second messenger that stimulates the discharge of calcium from the endoplasmic reticulum.
  • HY-P1291A
    PKI 14-22 amide,myristoylated TFA

    PKA Cancer
    PKI 14-22 amide,myristoylated TFA is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated TFA reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
  • HY-B0238
    Amorolfine hydrochloride

    Ro 14-4767/002

    Fungal Antibiotic Infection
    Amorolfine hydrochloride (Ro 14-4767/002) is a antifungal reagent.
  • HY-P1486
    Angiotensinogen (1-14), human

    Endogenous Metabolite Cardiovascular Disease
    Angiotensinogen (1-14), human is a fragment of the renin substrate angiotensinogen. Angiotensinogen is naturally occurring substrate for renin and a precursor for all angiotensin peptides.
  • HY-141324
    Tetraethyl butane-​1,​4-​diylbis(phosphoramid​ate)

    PROTAC Linker Cancer
    Tetraethyl butane-​1,​4-​diylbis(phosphoramid​ate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-16576
    TCS-PIM-1-4a

    SMI-4a

    Pim Apoptosis Cancer
    TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM).
  • HY-136433
    N,N'-Dinitrosopiperazine

    1,4-Dinitrosopiperazine; DNP

    Others Cancer
    N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine; DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568.
  • HY-P1486A
    Angiotensinogen (1-14), human TFA

    Endogenous Metabolite Cardiovascular Disease
    Angiotensinogen (1-14), human TFA is a fragment of the renin substrate angiotensinogen. Angiotensinogen is naturally occurring substrate for renin and a precursor for all angiotensin peptides.
  • HY-128815
    cIAP1 Ligand-Linker Conjugates 14

    E3 ligase Ligand-Linker Conjugates 36

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 14 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 14 can be used to design SNIPERs.
  • 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-N7116
    Lawsone methyl ether

    2-​Methoxy-​1,​4-​naphthoquinone

    Fungal Bacterial Infection
    Lawsone methyl ether (2-Methoxy-1,4-naphthoquinone), isolated from Impatiens balsamina L. and Swertia calycina, exhibits potent antifungal and antibacterial activities.
  • HY-N5053
    Periplogenin 3-[O-β-glucopyranosyl-(1→4)-β-sarmentopyranoside]

    Others Others
    Periplogenin 3-[O-β-glucopyranosyl-(1→4)-β-sarmentopyranoside] is a cardenolide isolated from the root barks of Periploca sepium.
  • HY-42637
    N3-PEG3-CH2COOH

    PROTAC Linker 14

    PROTAC Linker Cancer
    N3-PEG3-CH2COOH (PROTAC Linker 14) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-136092
    Androsta-1,4,6-triene-3,17-dione

    Aromatase Endocrinology Neurological Disease
    Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor with a Ki of 0.18 μM. Androsta-1,4,6-triene-3,17-dione inhibits estrogen biosynthesis and shows antifertility effects. Androsta-1,4,6-triene-3,17-dione induces impairment of spatial memory.
  • HY-130866
    Mal-NH-PEG14-CH2CH2COOPFP ester

    PROTAC Linker Cancer
    Mal-NH-PEG14-CH2CH2COOPFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-19812
    Acetylene-linker-Val-Cit-PABC-MMAE

    LCB14-0602

    Drug-Linker Conjugates for ADC Cancer
    Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) consists the ADCs linker (Acetylene-linker-Val-Cit-PABC) and potent tubulin inhibitor (MMAE). Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) is a drug-linker conjugate for ADC.
  • 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-N3811
    ent-11β-Hydroxyatis-16-ene-3,14-dione

    RSV Infection
    ent-11β-Hydroxyatis-16-ene-3,14-dione (compound 11) is a diterpenoid from the fresh roots of Euphorbia jolkinii. ent-11β-Hydroxyatis-16-ene-3,14-dione has anti-RSV activity.
  • HY-W017829
    1,7-Bis-Boc-1,4,7-triazaheptane

    PROTAC Linker Cancer
    1,7-Bis-Boc-1,4,7-triazaheptane is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-128976
    10β,17β-dihydroxyestra-1,4-dien-3-one

    DHED

    Estrogen Receptor/ERR Metabolic Disease
    10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor prodrug of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.
  • HY-113463
    CE(20:5(5Z,8Z,11Z,14Z,17Z)

    Endogenous Metabolite Metabolic Disease
    CE(20:5(5Z,8Z,11Z,14Z,17Z) is an endogenous metabolite.
  • HY-N2142
    3-O-beta-Allopyranosyl-(1->4)-beta-oleandropyranosyl-11-O-isobutyryl-12-O-acetyltenacigenin B

    Others Cancer
    3-O-beta-Allopyranosyl-(1->4)-beta-oleandropyranosyl-11-O-isobutyryl-12-O-acetyltenacigenin B is a chemical constituent of the plant Poria cocos .
  • HY-111824
    VH032-thiol-C6-NH2

    VHL Ligand-Linker Conjugates 14; E3 ligase Ligand-Linker Conjugates 29

    E3 Ligase Ligand-Linker Conjugate Cancer
    VH032-thiol-C6-NH2 (VHL Ligand-Linker Conjugates 14) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
  • 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-A0143
    Dihomo-γ-linolenic acid

    all-cis-8,11,14-Eicosatrienoic acid

    Endogenous Metabolite Cancer Inflammation/Immunology Cardiovascular Disease
    Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system.
  • 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-N0902
    Dihydrosanguinarine

    13,14-DihydrosAnguinarine

    Others Infection
    Dihydrosanguinarine is a natural compound isolated from the leaves of Macleaya microcarpa; has antifungal and anticancer activity.
  • HY-N0218
    Benzoylmesaconine

    Mesaconine 14-benzoate

    Others Inflammation/Immunology
    Benzoylmesaconine is the most abundant component of Wutou decoction, which is widely used in China because of its therapeutic effect on rheumatoid arthritis.
  • 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-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-B1106
    Tetrahydroxyquinone

    Tetrahydroxy-1,4-benzoquinone; Tetrahydroxybenzoquinone

    Reactive Oxygen Species Cancer
    Tetrahydroxyquinone is a molecule best known as a primitive anticataract drug, is also a highly redox active molecule that can take part in a redox cycle with semiquinone radicals, leading to the formation of reactive oxygen species (ROS).
  • HY-N2301
    Pleuromutilin

    Drosophilin B; Mutilin 14-glycolate

    Bacterial Antibiotic Infection
    Pleuromutilin (Drosophilin B) inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit of bacteria.
  • HY-N6949
    Juglone

    5-Hydroxy-1,4-naphthalenedione

    Bacterial Infection
    Juglone is a yellow pigment found in black walnut (Juglans regia). Juglone also shows antimicrobial activity.
  • HY-U00262
    ACT 178882

    Renin Metabolic Disease
    ACT 178882 is a new Renin inhibitor with an IC50 of 1.4 nM.
  • HY-B0309
    Felodipine

    Calcium Channel Autophagy Cardiovascular Disease
    Felodipine is a long-acting 1,4-dihydropyridine calcium channel blocker.
  • HY-N0355
    (+)-Catechin hydrate

    COX Cancer
    (+)-Catechin hydrate inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
  • HY-U00034
    PCA50941

    Others Cardiovascular Disease
    PCA50941 is a 1,4-dihydropyridine derivative, used for treatment for cardiovascular disease.
  • HY-100382
    FPTQ

    mGluR Others
    FPTQ is mGluR1 antagonist with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1 respectively.
  • HY-N0898
    Catechin

    (+)-Catechin; Cianidanol; Catechuic acid

    COX Apoptosis Influenza Virus Endogenous Metabolite Cancer
    Catechin ((+)-Catechin) inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
  • HY-18336
    GlyH-101

    CFTR Cardiovascular Disease
    GlyH-101 is a cell-permeable glycinyl hydrazone compound that blocks CFTR with Ki of 1.4 uM.
  • HY-12298
    Setanaxib

    GKT137831; GKT831

    NADPH Oxidase Ferroptosis Cardiovascular Disease
    Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with Kis of 140 and 110 nM, respectively.
  • HY-N7526
    Naphthazarin

    DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone

    Apoptosis Cancer Neurological Disease
    Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects.
  • HY-B1160
    Bitoscanate

    p-Phenylene diisothiocyanate; 1,4-Diisothiocyanatobenzene; PDITC

    Parasite Infection
    Bitoscanate (p-Phenylene diisothiocyanate) is an organic chemical compound used in the treatment of hookworms.
  • HY-P1039
    R18

    PHCVPRDLSWLDLEANMCLP

    Others Cancer
    R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1.
  • HY-112945
    MLS0315771

    Others Metabolic Disease
    MLS0315771 is a potent and biologically active competitive phosphomannose isomerase (MPI) inhibitor, with an IC50 ~1 μM and a Ki of 1.4 μM.
  • HY-P1275
    Tertiapin-Q

    Potassium Channel Cardiovascular Disease
    Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1).
  • HY-N2024
    Maltose

    Endogenous Metabolite Metabolic Disease
    Maltose is a disaccharide formed from two units of glucose joined with an α(14) bond. Maltose is a reducing sugar.
  • HY-19664
    Pranidipine

    OPC-13340

    Calcium Channel Cardiovascular Disease
    Pranidipine (OPC-13340) is a potent, long acting 1,4-dihydropyridine calcium channel blocker with antihypertensive activity.
  • HY-N2041
    Myristic acid

    Endogenous Metabolite Others
    Myristic acid is a saturated 14-carbon fatty acid occurring in most animal and vegetable fats, particularly butterfat and coconut, palm, and nutmeg oils.
  • HY-19528
    SAH

    SAH (S-Adenosylhomocysteine)

    Endogenous Metabolite Metabolic Disease
    SAH is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM.
  • HY-18729A
    L-NAME hydrochloride

    NG-Nitroarginine methyl ester hydrochloride

    NO Synthase Cancer
    L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM.
  • HY-112444
    BACE1-IN-2

    Beta-secretase Neurological Disease
    BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC50 of 22 nM.
  • HY-10401
    VX-702

    p38 MAPK Autophagy Inflammation/Immunology
    VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.
  • HY-102003
    Rucaparib Camsylate

    PARP Cancer
    Rucaparib Camsylate is an inhibitor of PARP with a Ki of 1.4 nM for PARP1. Rucaparib Camsylate also shows binding affinity to eight other PARP domains.
  • HY-135218
    AV-153

    DNA/RNA Synthesis Cancer
    AV-153, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 has anti-cancer activity.
  • HY-B1008
    4-Aminobenzoic acid

    PABA; Vitamin Bx; Vitamin H1

    Endogenous Metabolite Others
    4-Aminobenzoic acid is an intermediate in the synthesis of folate by bacteria, plants, and fungi.
  • HY-15292A
    S107 hydrochloride

    Others Cardiovascular Disease
    S107 hydrochloride is a RyR-selective 1,4-benzothiazepine derivative that stabilizes RyR2 channels by enhancing the binding affinity of calstabin2 to mutant and/or PKA-phosphorylated channels.
  • 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-16704
    ESI-09

    Virus Protease Cancer
    ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.
  • HY-108708
    GeA-69

    PARP Cancer
    GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM.
  • HY-19532
    ZM241385

    Adenosine Receptor Neurological Disease Cancer
    ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM.
  • HY-14595
    Biochanin A

    4-Methylgenistein; Olmelin

    FAAH Autophagy Neurological Disease Cancer
    Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC50s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.
  • HY-15767
    TAK-632

    Raf Aurora Kinase Cancer
    TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF V600E, BRAF WT, respectively.
  • HY-112622
    GSK3186899

    DDD-853651

    Parasite Cancer
    GSK3186899 (DDD-853651) is an inhibitor of cdc-2-related kinase 12 (CRK12), with an EC50 of 1.4 μM for L. donovani in an intra-macrophage assay.
  • HY-P1380A
    Difopein TFA

    Apoptosis Cancer
    Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to induction of apoptosis and enhances the ability of cisplatin to kill cells.
  • HY-122502
    Pyrazofurin

    DNA/RNA Synthesis Cancer
    Pyrazofurin, a pyrimidine nucleoside analogue with antineoplastic activity, inhibits cell proliferation and DNA synthesis in cells by inhibiting uridine 5'-phosphate (UMP) synthase. Pyrazofurin is an active, sensitive orotate-phosphoribosyltransferase inhibitor with IC50s between 0.06-0.37 µM in the three squamous cell carcinoma (SCC) cell lines Hep-2, HNSCC-14B and HNSCC-14C.
  • HY-D0713
    7ACC2

    Monocarboxylate Transporter Cancer
    7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.
  • HY-N7266
    Obtusifoliol

    Cytochrome P450 Cancer Infection
    Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with Kd values of 1.2 µM and 1.4 µM for Trypanosoma brucei (TB) and human CYP51, respectively.
  • HY-135218A
    AV-153 free base

    DNA/RNA Synthesis Cancer
    AV-153 free base, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 free base intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 free base interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 free base has anti-cancer activity.
  • HY-10393
    Eperezolid

    PNU-100592

    Bacterial Antibiotic Infection
    Eperezolid(PNU-100592) is a oxazolidinone antibacterial agent, Eperezolid demonstrated good in vitro inhibitory activity, regardless of methicillin susceptibility for staphylococci(MIC90= 1-4 mg/ml).
  • HY-101441
    ST-193

    Arenavirus Infection
    ST-193 is a potent broad-spectrum arenavirus inhibitor; inhibits Guanarito, Junin, Lassa and Machupo virus with IC50 values of 0.44, 0.62, 1.4 and 3.1 nM, respectively.
  • HY-13438
    AZD3839 free base

    Beta-secretase Cancer
    AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.
  • HY-101441A
    ST-193 hydrochloride

    Arenavirus Infection
    ST-193 hydrochloride is a potent broad-spectrum arenavirus inhibitor; inhibits Guanarito, Junin, Lassa and Machupo virus with IC50 values of 0.44, 0.62, 1.4 and 3.1 nM, respectively.
  • HY-112534
    GSTO-IN-2

    Gutathione S-transferase Cancer
    GSTO-IN-2 is a glutathione S-transferase inhibitor with IC50s of 3.6, 16.3, and 1.4 μM for GSTA2, GSTM1, and GSTP1-1.
  • HY-112108
    Chitosan oligosaccharide

    COS

    AMPK Cancer Metabolic Disease
    Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.
  • HY-10981A
    Lenvatinib mesylate

    E7080 mesylate

    VEGFR FGFR PDGFR RET c-Kit Cancer
    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-109040
    Quilseconazole

    VT-1129

    Fungal Cytochrome P450 Infection
    Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.
  • HY-P1674A
    Murepavadin TFA

    POL7080 TFA

    Bacterial Antibiotic Infection
    Murepavadin (TFA), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic for the treatment of bacterial infections caused by Pseudomonas aeruginosa. Murepavadin (TFA) targets the lipopolysaccharide transport portin D .
  • HY-10617
    Rucaparib phosphate

    AG-014699 phosphate; PF-01367338 phosphate

    PARP Cancer
    Rucaparib phosphate (AG-014699 phosphate) is an orally active and potent PARP inhibitor, with a Ki of 1.4 nM for PARP1 in cell-free assay. Rucaparib phosphate shows binding affinity to eight other PARP domains.
  • HY-10981
    Lenvatinib

    E7080

    VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-10617A
    Rucaparib

    AG014699; PF-01367338

    PARP Cancer
    Rucaparib (AG014699) is an orally active and potent inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay. Rucaparib shows binding affinity to eight other PARP domains.
  • HY-N2913
    Ayanin

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology
    Ayanin is a bioflavonoid isolated from Croton schiedeanus Schlecht. Ayanin is a non-selective phosphodiesterase1-4 inhibitor and can be used for the study of respiratory disease,such as allergic asthma et al.
  • HY-N2464
    Maltotetraose

    Amylotetraose; Fujioligo 450; α-1,4-Tetraglucose

    Endogenous Metabolite Metabolic Disease
    Maltotetraose can be used as a substrate for the enzyme-coupled determination of amylase activity in biological fluids.
  • HY-135954A
    PDK4-IN-1 hydrochloride

    PDHK Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.
  • HY-135954
    PDK4-IN-1

    PDHK Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.
  • HY-135307
    SSF-109

    Huanjunzuo

    Fungal Infection
    SSF-109 is a broad-spectrum fungicide which has protective activity against plant disease. SSF-109 inhibits the biosynthesis of ergosterol at the 14α-demethylation step in Botrytis cinerea.
  • HY-10061
    Lesogaberan

    AZD-3355

    GABA Receptor Metabolic Disease
    Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively.
  • HY-B2054
    Tebufenozide

    Apoptosis Others
    Tebufenozide is a nonsteroidal ecdysone agonist used to control pest. Tebufenozide has cytotoxic and induces apoptosis in HeLa and insect Tn5B1-4 cells.
  • HY-13495
    ML281

    Others Cancer
    ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM.
  • HY-11000
    GSK429286A

    ROCK Cancer
    GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
  • HY-122815
    Fusicoccin

    Fusicoccin A

    Apoptosis Cancer
    Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.
  • HY-13311A
    Infigratinib phosphate

    BGJ-398 phosphate; NVP-BGJ398 phosphate

    FGFR Cancer
    Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) is a potent inhibitor of the FGFR family with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
  • HY-127104
    FMF-04-159-2

    CDK Cancer
    FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively.
  • HY-P1107
    Antisauvagine-30

    aSvg-30

    CRFR Neurological Disease
    Antisauvagine-30 (aSvg-30) is a potent, competitive and selective CRF2 receptor antagonist with Kd values of 1.4 nM and 153.6 nM for mouse CRF and rat CRF1 receptors, respectively.
  • HY-10440
    Vismodegib

    GDC-0449

    Hedgehog Autophagy Cancer
    Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively.
  • HY-13817
    IU1

    Deubiquitinase Autophagy Cardiovascular Disease
    IU1 is a special Usp14 inhibitor with an IC50 of 4-5 μM.
  • HY-128347
    M‑89

    Epigenetic Reader Domain Cancer Inflammation/Immunology
    M-89 is a highly potent and specific menin inhibitor, with a Kd of 1.4 nM for binding to menin. M-89 inhibits the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction and has potential to treat MLL leukemia.
  • HY-13311
    Infigratinib

    BGJ-398; NVP-BGJ398

    FGFR Cancer
    Infigratinib (BGJ-398; NVP-BGJ398) is a potent inhibitor of the FGFR family with IC50s of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
  • HY-N4097
    Incensole

    Others Neurological Disease
    Incensole, a 14-membered diterpenoid, is isolated from both essential oils and resins of frankincense. Incensole has shown anti-inflammatory and anti-depression activities due to their ability to activate ion channels in the brain to alleviate anxiety or depression.
  • HY-N0898A
    (-)-Catechin

    (-)-Cianidanol; (-)-Catechuic acid

    COX Cancer
    (-)-Catechin, isolated from green tea, is an isomer of Catechin having a trans 2S,3R configuration at the chiral center. Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
  • HY-P2272
    NLS-StAx-h

    Wnt β-catenin Cancer
    NLS-StAx-h is a selective, stapled peptide inhibitor of Wnt signaling with an IC50 of 1.4 μM. NLS-StAx-h efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h inhibits proliferation and migration of colorectal cancer cells.
  • HY-108682
    EMPA

    Orexin Receptor (OX Receptor) Neurological Disease
    EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [ 3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM 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-15199
    Agerafenib hydrochloride

    CEP-32496 (hydrochloride); RXDX-105 hydrochloride

    Raf Cancer
    Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
  • HY-13989
    b-AP15

    NSC 687852

    Deubiquitinase Apoptosis Cancer
    b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
  • 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-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-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-19624
    NVP-ACC789

    ACC-789; ZK202650

    VEGFR PDGFR Cancer
    NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.
  • HY-12987
    Pimozide

    R6238

    Dopamine Receptor Adrenergic Receptor STAT Cancer Neurological Disease Endocrinology
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-128582
    PI3K/HDAC-IN-1

    PI3K HDAC Cancer
    PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC50s of 8.1 nM and 1.4 nM, respectively.
  • HY-107440
    Thalidomide-O-amido-PEG3-C2-NH2

    Cereblon Ligand-Linker Conjugates 3 ; E3 Ligase Ligand-Linker Conjugates 14

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
  • HY-15456
    NVP-BVU972

    c-Met/HGFR Cancer
    NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.
  • HY-15150
    Bemcentinib

    R428; BGB324

    TAM Receptor Cancer
    Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM.
  • HY-123242
    FTI-2153

    Farnesyl Transferase Cancer
    FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity.
  • HY-14740
    Elvitegravir

    GS-9137; JTK-303; D06677

    HIV Integrase HIV Infection
    Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
  • HY-P1107A
    Antisauvagine-30 TFA

    aSvg-30 TFA

    CRFR Neurological Disease
    Antisauvagine-30 TFA (aSvg-30 TFA) is a potent, highly selective and competitive CRF2 receptor peptidic antagonist. Antisauvagine-30 TFA exhibits a Kd of 1.4 nM and 150 nM for mCRFR2β and CRFR1, respectively.
  • HY-101708
    N-(2-Chloro-6-methylphenyl)-N'-4-pyridinylurea

    Others Neurological Disease
    N-[(1R)-4-[(Aminoiminomethyl)amino]-1-[[[(1R)-1-(4-hydroxyphenyl)ethyl]amino]carbonyl]butyl]-α-phenylbenzeneacetamide is an anticonvulsant agent with potential for the treatment of generalized tonic-clonic and partial seizures.
  • HY-100332
    CP 375

    Others Others
    CP 375 is a Fe 3+ chelating agent, with a log K1 value of 14.50.
  • HY-101071A
    Monastrol

    (±)-Monastrol

    Kinesin Apoptosis Cancer
    Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.
  • HY-19919
    BMS-779788

    EXEL04286652; XL-652; BMS-788

    LXR Metabolic Disease
    BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
  • HY-100631
    FGFR4-IN-1

    FGFR Neurological Disease
    FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.
  • HY-123037
    Triadimefon

    Fungal
    Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis.
  • 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-118916
    FTI-2148

    Farnesyl Transferase Cancer
    FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
  • HY-14552
    Talnetant

    SB 223412

    Neurokinin Receptor Neurological Disease Endocrinology
    Talnetant (SB 223412) is a potent and selective NK3 receptor antagonist (ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.
  • HY-B0240
    Disulfiram

    Tetraethylthiuram disulfide; TETD

    Aldehyde Dehydrogenase (ALDH) Interleukin Related Metabolic Disease Cancer
    Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1-4].
  • 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-19831A
    (Z)-4EGI-1

    Eukaryotic Initiation Factor (eIF) Cancer
    (Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity.
  • HY-15521
    ETP-46464

    mTOR ATM/ATR Cancer
    ETP-46464 is an effective mTOR and ATR inhibitor with IC50s of 0.6 and 14 nM, respectively.
  • HY-102044
    BET-IN-2

    Epigenetic Reader Domain Cancer
    BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.
  • HY-13503
    Epothilone A

    Epo A

    Microtubule/Tubulin Apoptosis Cancer
    Epothilone A is a competitive inhibitor of the binding of [ 3H] paclitaxel to tubulin polymers, with a Ki of 0.6-1.4 μM.
  • HY-12043
    SB 525334

    TGF-β Receptor Cancer
    SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
  • HY-13867
    Bisindolylmaleimide I

    GF109203X; Go 6850

    PKC Metabolic Disease Cancer
    Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
  • HY-14809
    Amenamevir

    ASP2151

    HSV Infection
    Amenamevir is a helicase-primase inhibitor which has potent antiviral activity against HSVs with an EC50 of 14 ng/mL.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-118916A
    FTI-2148 diTFA

    Farnesyl Transferase Cancer
    FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
  • HY-14552A
    Talnetant hydrochloride

    SB 223412 hydrochloride; SB 223412-A

    Neurokinin Receptor Neurological Disease Endocrinology
    Talnetant Hcl(SB 223412 Hcl) is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.
  • HY-107201
    β-Cyclodextrin

    Influenza Virus Infection
    β-Cyclodextrin is a cyclic polysaccharide composed of seven units of glucose (α-D-glucopyranose) linked by α-(1,4) type bonds. β-Cyclodextrin has often been used to enhance the solubility of drugs. β-Cyclodextrin has anti-influenza virus H1N1 activities.
  • HY-12980
    Batefenterol

    GSK961081; TD-5959

    Adrenergic Receptor mAChR Inflammation/Immunology Endocrinology
    Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
  • HY-127106
    VU0810464

    Potassium Channel Neurological Disease
    VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration.
  • HY-124373
    ND-336

    MMP Metabolic Disease
    ND-336 is a selective inhibitor of matrix metalloproteinase (MMP)-2, MMP-9, and MMP-14, with Kis of 85, 150, and 120 nM, respectively. ND-336 accelerates diabetic wound healing in mice by lowering inflammation and by enhancing angiogenesis and re-epithelialization of the wound.
  • HY-118743
    KMN-80

    Prostaglandin Receptor Metabolic Disease
    KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors.
  • HY-101922
    IRAK4-IN-1

    IRAK Inflammation/Immunology
    IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
  • HY-A0014
    Ramelteon

    TAK-375

    Melatonin Receptor Neurological Disease Endocrinology Cancer
    Ramelteon is a highly potent and selective melatonin receptor agonist with Ki values of 14 and 112 pM for human melatonin1 and melatonin2.
  • HY-124373A
    (R)-ND-336

    MMP Metabolic Disease
    (R)-ND-336 is a potent and selective MMP-9 inhibitor with a Ki of 19 nM. (R)-ND-336 inhibits MMP-2 (Ki=127 nM) and MMP-14 (Ki=119 nM). (R)-ND-336 has the potential for diabetic foot ulcers (DFUs) research.
  • HY-101768
    PRN1371

    FGFR c-Fms Cancer
    PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively.
  • HY-17514
    Itraconazole

    R51211

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects.
  • HY-14282
    Lanoconazole

    Fungal Infection Inflammation/Immunology
    Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis.
  • HY-108645
    AL 8697

    p38 MAPK Autophagy Inflammation/Immunology
    AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity.
  • HY-107394
    UK 356618

    MMP Cancer Inflammation/Immunology
    UK 356618 (Compound 4j) is a potent and selective inhibitor of matrix metalloprotease-3 (MMP-3) with an IC50 of 5.9 nM. UK 356618 is less potent against MMP-1, MMP-2, MMP-9, MMP-13 and MMP-14 compared with MMP-3.
  • HY-N2273
    Gymnestrogenin

    LXR Metabolic Disease
    Gymnestrogenin is a pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br. Gymnestrogenin is a LXR antagonist with IC50s of 2.5 and 1.4 μM for LXRα and LXRβ transactivation, respectively. Gymnestrogenin reduces the transcriptional activity of LXR even on its own promoter, thus reducing the mRNA expression.
  • HY-103611
    Thalidomide-O-amido-PEG3-C2-NH2 (TFA)

    Cereblon Ligand-Linker Conjugates 3 (TFA); E3 ligase Ligand-Linker Conjugates 14 (TFA)

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-O-amido-PEG3-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
  • HY-P1164
    Urotensin II (114-124), human

    Urotensin Receptor Cardiovascular Disease
    Urotensin II (114-124), human, an 11-amino acid residue peptide, is a potent vasoconstrictor and agonist for the orphan receptor GPR14.
  • HY-19512
    ACH-806

    GS9132

    HCV Protease HCV Infection
    ACH-806 is an NS4A antagonist which can inhibit Hepatitis C Virus (HCV) replication with an EC50 of 14 nM.
  • HY-N0083
    Betulin

    Trochol

    Fatty Acid Synthase (FASN) Apoptosis Endogenous Metabolite Cancer
    Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line.
  • HY-104009A
    GSK2807 Trifluoroacetate

    Histone Methyltransferase Others
    GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM.
  • HY-U00299
    LTB4-IN-1

    Leukotriene Receptor Inflammation/Immunology
    LTB4-IN-1 (Compound 6) is a leukotriene synthesis (LTB4) inhibitor with an IC50 of 70 nM.
  • HY-135675
    DHODH-IN-11

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-11 (Compound 14b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.03.
  • HY-117632
    ABX-1431

    MAGL Neurological Disease
    ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
  • 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-128780
    SPR206

    Bacterial Cancer Infection
    SPR206 is a polymyxin analogue and an important class of antibiotic for the treatment of bacterial infections due to multidrug resistant Gram-negative pathogen. The MIC values of SPR206 against Pseudomonas aeruginosa Pa14 (MIC value of for Pa14) and Acinetobacter baumannii NCTC13301 are 0.125 mg/L and 0.125 mg/L, respectively.
  • HY-19676
    Pralnacasan

    VX-740; HMR 3480

    Caspase Inflammation/Immunology
    Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment.
  • HY-B0492
    Paroxetine hydrochloride

    BRL29060 hydrochloride; BRL29060A

    Serotonin Transporter Autophagy Neurological Disease Cancer
    Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an antidepressant and has GRK2 inhibitory ability with IC50 of 14 μM.
  • HY-112588
    dBET6

    PROTAC Epigenetic Reader Domain Apoptosis Cancer
    dBET6 is a highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.
  • HY-B1948
    Diniconazole

    Rac-diniconazole

    Bacterial Infection
    Diniconazole is a newly developed fungicide strongly inhibited lanosterol 14 alpha-demethylation catalyzed by a yeast cytochrome P-450.
  • HY-P1164A
    Urotensin II (114-124), human TFA

    Urotensin Receptor Cardiovascular Disease
    Urotensin II (114-124), human TFA, an 11-amino acid residue peptide, is a potent vasoconstrictor and agonist for the orphan receptor GPR14.
  • HY-100681
    GSK2837808A

    Lactate Dehydrogenase Cancer
    GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 1.9 and 14 nM for LDHA and LDHB, respectively.
  • HY-B0457
    Clomipramine hydrochloride

    Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) and dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
  • HY-B0492A
    Paroxetine hydrochloride hemihydrate

    BRL29060 hydrochloride hemihydrate; BRL29060A hemihydrate

    Serotonin Transporter Autophagy Neurological Disease
    Paroxetine hydrochloride hemihydrate is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an antidepressant and has GRK2 inhibitory ability with IC50 of 14 μM.
  • HY-15200
    Agerafenib

    CEP-32496; RXDX-105

    Raf Cancer
    Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
  • HY-128693
    BpV(HOpic)

    PTEN Cancer Neurological Disease
    BpV(HOpic) is a potent and selective inhibitor of PTEN with an IC50 of 14 nM. Nanocarrier-BpV(HOpic) has neuroprotective activity.
  • HY-109562A
    GRK2-IN-1 hydrochloride

    Others Cardiovascular Disease
    GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
  • HY-12680
    PRN694

    Itk Inflammation/Immunology
    PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo.
  • HY-103463
    SA57

    FAAH MAGL Neurological Disease
    SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases.
  • HY-12333
    G-749

    FLT3 Apoptosis Cancer
    G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants with IC50s of 0.4/0.6/3.5/7.5 nM for Wt Flt3/D835Y/MV4-11/Molm-14 respectively.
  • HY-109562
    GRK2-IN-1

    Others Cardiovascular Disease
    GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
  • HY-15490
    PF-670462

    Casein Kinase Cancer
    PF-670462 is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.
  • HY-12744
    Genz-123346 free base

    Others Metabolic Disease Cancer
    Genz-123346 (free base) is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1; inhibits GM1 with IC50 value of 14 nM.
  • HY-13068
    Golvatinib

    E-7050

    c-Met/HGFR VEGFR Cancer
    Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
  • HY-111416
    WY-135

    ALK ROS Cancer
    WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
  • HY-15755
    RKI-1447

    ROCK Cancer
    RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
  • HY-128848
    Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH

    Cereblon Ligand-Linker Conjugates 14; E3 ligase Ligand-Linker Conjugates 49

    E3 Ligase Ligand-Linker Conjugate Cancer
    Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
  • HY-12987S
    Pimozide D4

    R6238 D4

    Dopamine Receptor Adrenergic Receptor STAT Cancer Endocrinology Neurological Disease
    Pimozide D4 (R6238 D4) is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-N0828
    Pterostilbene

    Autophagy Cancer Inflammation/Immunology
    Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium. Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties. Pterostilbene blocks ROS production, also exhibits inhibitory activity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide.
  • HY-128345
    UDM-001651

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP).
  • HY-W014078
    4-(3-Methyl-5-oxo-2-pyrazolin-1-yl)benzoic acid

    Others Metabolic Disease
    4-(3-Methyl-5-oxo-2-pyrazolin-1-yl)benzoic acid has hypoglycaemic activity. 4-(3-Methyl-5-oxo-2-pyrazolin-1-yl)benzoic acid follows a mechanism based on the response to the oral glucose overcharge.
  • HY-N0603
    20(S)-Ginsenoside Rg3

    20(S)-Propanaxadiol; S-ginsenoside Rg3

    Sodium Channel Potassium Channel NF-κB COX Amyloid-β Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    20(S)-Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na + and hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits levels, NF-κB activity, and COX-2 expression.
  • HY-20685
    Impulsin

    AM 3112; Loramine P 256; Mackpeart DR 14V

    Influenza Virus Endogenous Metabolite Infection
    Impulsin (AM 3112) is an active endogenous compound which can used for preventing virus infection of the respiratory tract.
  • HY-16312
    MDL-29951

    iGluR Neurological Disease
    MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [ 3H]glycine binding in vitro and in vivo.
  • HY-109877
    Ro 22-3581

    4'-(Imidazol-1-yl) acetophenone

    Others Cardiovascular Disease
    Ro 22-3581 (4'-(Imidazol-1-yl) acetophenone) is a selective thromboxane (Tx) synthetase inhibitor.
  • HY-11102
    RO4929097

    RG-4733

    γ-secretase Notch Neurological Disease Cancer
    RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.
  • HY-P0179
    β-Casomorphin, bovine

    β-Casomorphin-7 (bovine); Bovine β-casomorphin-7

    Opioid Receptor Metabolic Disease Neurological Disease
    β-Casomorphin, bovine (β-Casomorphin-7 (bovine) ) is a opioid peptide with an IC50 of 14 μM in an Opioid receptors binding assay.
  • HY-10792
    Eplivanserin

    SR-46349

    5-HT Receptor Neurological Disease
    Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM.
  • HY-12340
    ETP-46321

    PI3K Cancer
    ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
  • HY-112583
    MIV-247

    Cathepsin Neurological Disease
    MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.
  • HY-N0610A
    Cinnamic acid

    3-Phenylacrylic acid; β-Phenylacrylic acid

    Endogenous Metabolite Cancer
    Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-15098
    Apoptozole

    Apoptosis Activator VII

    HSP Apoptosis Cancer
    Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
  • HY-B2193
    α-Amylase

    Others Others
    α-Amylase is a hydrolase enzyme that catalyses the hydrolysis of internal α-1, 4-glycosidic linkages in starch to yield products like glucose and maltose.
  • HY-12332
    JW 642

    MAGL Neurological Disease
    JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
  • HY-101261
    ATPA

    iGluR Neurological Disease
    ATPA is a selective glutamate receptor GluR5 activator with EC50s of 0.66, 9.5, 1.4, 23, 32, 18, and 14 μM for GluR5wt, GluR5(S741M), GluR5(S721T), GluR5(S721T, S741M), GluR5(S741A), GluR5(S741L), and GluR5(S741V), 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-15149
    Romidepsin

    FK 228; FR 901228; NSC 630176

    HDAC Apoptosis Cancer
    Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
  • HY-117766
    PC945

    Fungal Cytochrome P450 Infection
    PC945, a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. PC945 is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively.
  • HY-12688A
    Succinyl phosphonate trisodium salt

    Endogenous Metabolite Reactive Oxygen Species Cancer Metabolic Disease Neurological Disease
    Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
  • HY-10221
    Vorinostat

    SAHA; Suberoylanilide hydroxamic acid

    HDAC Autophagy Mitophagy Filovirus Cancer Infection
    Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.
  • HY-10372
    PP121

    mTOR PDGFR VEGFR Src Apoptosis Cancer
    PP121 is a multi-targeted kinase inhibitor with IC50s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively.
  • 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-124587
    MLT-747

    MALT1 Inflammation/Immunology
    MLT-747 is a potent, selective, allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 14 nM.
  • HY-133029
    PI3K-IN-9

    PI3K Cancer
    PI3K-IN-9 (compound 1-14) is a potent and selective PI3Kδ inhibitor with an IC50 of 8.9 nM.
  • HY-12032
    AG14361

    PARP Cancer
    AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively.
  • HY-10237
    Boceprevir

    EBP 520; SCH 503034

    HCV Protease HCV Infection
    Boceprevir is a novel, potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with Ki of 14 nM in both enzyme assay and EC90 of 350 nM in cell-based replicon assay.
  • HY-B0970
    Diphenylpyraline hydrochloride

    4-Diphenylmethoxy-1-methylpiperidine hydrochloride

    Histamine Receptor Neurological Disease Endocrinology
    Diphenylpyraline hydrochloride (4-Diphenylmethoxy-1-methylpiperidine hydrochloride) is a first-generation antihistamine with anticholinergic effects, acts as a dopamine reuptake inhibitor, shows to be useful in the treatment of Parkinsonism.
  • HY-P0179A
    β-Casomorphin, bovine TFA

    β-Casomorphin-7 (bovine) (TFA); Bovine β-casomorphin-7 TFA

    Opioid Receptor Metabolic Disease Neurological Disease
    β-Casomorphin, bovine TFA (β-Casomorphin-7 (bovine) TFA) is a opioid peptide with an IC50 of 14 μM in an Opioid receptors binding assay.
  • HY-103484
    GATA4-NKX2-5-IN-1

    Others Cardiovascular Disease
    GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.
  • HY-133136
    PROTAC BRD4 Degrader-2

    PROTAC Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-2 is an efficacious PROTAC BRD4 degrader with an IC50 of 14.2 nM against BRD4 BD1.
  • HY-15542B
    FRAX486

    PAK Cancer
    FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
  • HY-102000B
    IACS-9571 Hydrochloride

    ASIS-P040 Hydrochloride

    Epigenetic Reader Domain Cancer
    IACS-9571 Hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1, with an IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
  • HY-18602
    FIIN-2

    FGFR Cancer
    FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
  • HY-18874
    p38-α MAPK-IN-1

    p38 MAPK Autophagy Others
    p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
  • HY-16928
    Cytochalasin B

    Phomin

    Arp2/3 Complex Cancer
    Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, disrupting the formation of actin polymers, with Kd value of 1.4-2.2 nM for F-actin.
  • HY-15466
    CH5132799

    PI3K Cancer
    CH5132799 is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
  • HY-128574
    GLUT4 activator 1

    GLUT Metabolic Disease
    GLUT4 activator 1 (Compound 26b) is a potent glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM.
  • HY-101913
    IL-17A antagonist 1

    Interleukin Related Inflammation/Immunology
    IL-17A antagonist 1 (compound 1) is an IL-17A antagonist, with a Kd of 0.66 μM and an IC50 of 1.14 μM.
  • HY-102000
    IACS-9571

    ASIS-P040

    Epigenetic Reader Domain Cancer
    IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
  • HY-102011
    BMS-1166

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-P1045
    187-1, N-WASP inhibitor

    Arp2/3 Complex Others
    187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-102011A
    BMS-1166 hydrochloride

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-12599
    URMC-099

    Mixed Lineage Kinase Autophagy Neurological Disease Cancer
    URMC-099 is an orally bioavailable and potent mixed lineage kinase type 3 (MLK3) (IC50=14 nM) inhibitor with with excellent blood-brain barrier penetration properties.
  • HY-103088
    E7046

    Prostaglandin Receptor Cancer Endocrinology
    E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. E7046 exhibits anti-tumor activities.
  • HY-135893
    SGK1-IN-2

    SGK Inflammation/Immunology
    SGK1-IN-2 (14h) is a selective SGK1 (serum and glucocorticoid regulated kinase 1) inhibitor, with an IC50 of 5 nM at 10 μM ATP concentration.
  • HY-110322A
    PPTN

    P2Y Receptor Inflammation/Immunology
    PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. Anti-inflammatory and immune activity.
  • HY-15498
    Rimegepant

    BMS-927711

    CGRP Receptor Neurological Disease
    Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor.
  • 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-13638
    GDC-0152

    IAP Cancer
    GDC-0152 is a potent IAPs inhibitor, and binds to the BIR3 domains of XIAP, cIAP1, cIAP2 and the BIR domain of ML-IAP with Ki values of 28 nM, 17 nM, 43 nM and 14 nM, respectively.
  • HY-12338
    ON 146040

    PI3K Bcr-Abl Cancer
    ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
  • HY-P1599
    Valorphin

    Opioid Receptor Cancer Neurological Disease
    Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM; Valorphin also shows anti-tumor activity.
  • HY-100370
    MRK-016

    GABA Receptor Cancer
    MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
  • HY-15813
    FIIN-1

    FGFR irreversible inhibitor-1

    FGFR Cancer
    FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively.
  • HY-13246
    Apitolisib

    GDC-0980; GNE 390; RG 7422

    PI3K mTOR Apoptosis Cancer
    Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
  • HY-103045
    CMPD101

    PKC ROCK Cardiovascular Disease
    CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
  • HY-P1045A
    187-1, N-WASP inhibitor TFA

    Arp2/3 Complex Others
    187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-112831
    BI-409306

    Phosphodiesterase (PDE) Neurological Disease
    BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); BI-409306 can be used in the research of memory enhancement in CNS disorders.
  • HY-P1274A
    ShK-Dap22 TFA

    Potassium Channel Inflammation/Immunology
    ShK-Dap22 TFA is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 TFA is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.
  • HY-P1220
    Huwentoxin-IV

    Sodium Channel Neurological Disease
    Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain[1] [2] .
  • HY-P1274
    ShK-Dap22

    Potassium Channel Inflammation/Immunology
    ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.
  • HY-B0845
    Prochloraz

    BTS 40542

    Fungal Estrogen Receptor/ERR Androgen Receptor Aryl Hydrocarbon Receptor
    Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s = 25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50 = 1 μM).
  • HY-101928
    KDM4D-IN-1

    Histone Demethylase Cancer
    KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
  • HY-16965
    TH287

    DNA/RNA Synthesis Cancer
    TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.
  • HY-15065
    Chembridge-5861528

    TCS 5861528

    TRP Channel Neurological Disease
    Chembridge-5861528 is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7μM 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-16617
    Auglurant

    VU0424238

    mGluR Neurological Disease
    Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.
  • HY-16965A
    TH287 hydrochloride

    DNA/RNA Synthesis Cancer
    TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.
  • 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-108370
    N33-TEG-COOH

    N3-TEG-COOH; 14-Azido-3,6,9,12-tetraoxatetradecanoic acid

    PROTAC Linker Cancer
    N33-TEG-COOH (N3-TEG-COOH) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-P1483
    Urotensin II, mouse

    Urotensin Receptor Neurological Disease Cardiovascular Disease
    Urotensin II, mouse is an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse is a potent vasoconstrictor. Urotensin II, mouse plays a physiological role in the central nervous system.
  • HY-50706
    Selumetinib

    AZD6244; ARRY-142886

    MEK Apoptosis Cancer
    Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
  • 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-B0820
    Nitenpyram

    nAChR Neurological Disease
    Nitenpyram is a calss of neonicotinoid and an insect nicotinic acetylcholine receptor (nAChR) agonist with an IC50 of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals.
  • HY-12744A
    Genz-123346

    Others Metabolic Disease
    Genz-123346 is a potent, orally available glucosylceramide synthase inhibitor. Genz-123346 blocks the conversion of ceramide to glucosylceramide (GL1) and inhibits GM1 with an IC50 value of 14 nM.
  • HY-B0745
    Ramatroban

    BAY u3405

    Prostaglandin Receptor Inflammation/Immunology Endocrinology Cancer
    Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
  • HY-P1483B
    Urotensin II, mouse acetate

    Urotensin Receptor Neurological Disease Cardiovascular Disease
    Urotensin II, mouse acetate is an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse acetate is a potent vasoconstrictor. Urotensin II, mouse acetate plays a physiological role in the central nervous system.
  • HY-14902
    Tofogliflozin

    CSG452

    SGLT Metabolic Disease
    Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.
  • 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[1] .
  • HY-126257
    AKT-IN-3

    Akt Apoptosis Cancer
    AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells.
  • 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[1] .
  • 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-P1220A
    Huwentoxin-IV TFA

    Sodium Channel Neurological Disease
    Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain[1] [2] .
  • HY-50706A
    Selumetinib sulfate

    AZD6244 sulfate; ARRY-142886 sulfate

    MEK Apoptosis Cancer
    Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
  • HY-B0457AS
    Clomipramine D3

    Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine D3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
  • HY-129180
    XY028-133

    PROTAC CDK Cancer
    XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, extracted from patent WO2018106870A1.
  • HY-19719
    Miransertib

    ARQ-092

    Akt Cancer
    Miransertib (ARQ-092) is an orally bioavailable, selective, and potent allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.
  • HY-10009
    Semagacestat

    LY450139

    γ-secretase Amyloid-β Notch Neurological Disease
    Semagacestat is a γ-secretase inhibitor, inhibits β-amyloid (Aβ42), Aβ38 and Aβ40 with IC50 of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with IC50 of 14.1 nM.
  • HY-12286
    PI-1840

    Proteasome Cancer
    PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome.
  • HY-B0457S
    Clomipramine D3 hydrochloride

    Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine D3 hydrochloride is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
  • HY-14649
    Retinoic acid

    Vitamin A acid; all-trans-Retinoic acid; ATRA

    RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM.
  • HY-10095A
    Olcegepant hydrochloride

    BIBN-4096 hydrochloride; BIBN4096BS hydrochloride

    CGRP Receptor Neurological Disease
    Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.
  • HY-128340
    Autogramin-2

    Autophagy Cancer
    Autogramin-2 potently inhibits autophagy induced by either starvation (IC50=0.27 μM) or mTORC1 inhibition (Rapamycin; IC50=0.14 μM).
  • HY-10095
    Olcegepant

    BIBN-4096; BIBN 4096BS

    CGRP Receptor Neurological Disease
    Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.
  • HY-W016645
    4-Diethylaminobenzaldehyde

    Aldehyde Dehydrogenase (ALDH) Cancer
    4-Diethylaminobenzaldehyde is a reversible aldehyde dehydrogenases (ALDHs) inhibitor, with a Ki of 4 nM for ALDH1. 4-Diethylaminobenzaldehyde displays potent anti-androgenic effect (IC50= 1.71μM).
  • 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-125990
    SLC13A5-IN-1

    Sodium Channel Metabolic Disease Cardiovascular Disease
    SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of  14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5.
  • HY-10108
    LY294002

    PI3K Casein Kinase DNA-PK Autophagy Apoptosis Cancer Infection
    LY294002 (NSC 697286; SF 1101) is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
  • 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-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase Infection Inflammation/Immunology Neurological Disease
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway.
  • HY-P1483A
    Urotensin II, mouse TFA

    Urotensin Receptor Neurological Disease Cardiovascular Disease
    Urotensin II, mouse TFA is an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse TFA is a potent vasoconstrictor. Urotensin II, mouse TFA plays a physiological role in the central nervous system.
  • HY-P1418
    DPC-AJ1951

    Thyroid Hormone Receptor Endocrinology
    DPC-AJ1951, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR) , and characterized its activity in ex vivo and in vivo assays of bone resorption.
  • HY-N0906
    Ginsenoside Rk3

    NF-κB Inflammation/Immunology Cardiovascular Disease
    Ginsenoside Rk3 is present in the roots Panax notoginseng herbs. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 14.24±1.30 μM in HepG2 cells.
  • HY-19567
    PK 11195

    RP 52028

    Parasite Infection
    PK 11195 (RP 52028) is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.
  • HY-101564
    JNJ-64619178

    Histone Methyltransferase Cancer
    JNJ-64619178 is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. JNJ-64619178 has potent activity In lung cancer.
  • HY-133149
    Lp-PLA2-IN-3

    Phospholipase Cardiovascular Disease
    Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2).
  • HY-P1418A
    DPC-AJ1951 TFA

    Thyroid Hormone Receptor Endocrinology
    DPC-AJ1951 TFA, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR) , and characterized its activity in ex vivo and in vivo assays of bone resorption.
  • HY-15506
    TAK-593

    PDGFR VEGFR Cancer
    TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
  • HY-125012
    MAP4K4-IN-3

    MAP4K Metabolic Disease
    MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay. Antidiabetic agent.
  • HY-117491
    BRD4 Inhibitor-10

    Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM.
  • HY-107361
    AZD4205

    JAK Cancer
    AZD4205 is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM).
  • HY-41076
    Ca2+ channel agonist 1

    Calcium Channel CDK Neurological Disease
    Ca 2+ channel agonist 1 is an agonist of N-type Ca 2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
  • HY-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-111052
    AZD7325

    GABA Receptor Cytochrome P450 Inflammation/Immunology Neurological Disease
    AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
  • 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-B0850
    Difenoconazole

    Fungal
    Difenoconazole is a broad-spectrum triazole fungicide that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Difenoconazole inhibits the growth of F. graminearum isolates in vitro (EC50s = 1.69-19.6 mg/L for mycelial growth). Difenoconazole also inhibits growth of A. sonali, F. fulva, B. cinerea, and R. solani (EC50s = 0.131 mg/L, 0.069 mg/L, 0.297 mg/L, and 0.252 mg/L, respectively).
  • HY-107639
    UK-370106

    MMP Inflammation/Immunology
    UK-370106 is a potent and highly selective MMP-3 (IC50 of 23 nM) and MMP-12 (IC50 of 42 nM) inhibitor with >1200-fold higher potency than MMP-1, MMP-2, MMP-9, and MMP-14, and about 100-fold than MMP-13 and MMP-8. UK-370106 potently inhibits cleavage of [ 3H]-fibronectin by MMP-3 (IC50 of 320 nM) and has little effect on keratinocyte migration in vitro.
  • HY-100818
    Futibatinib

    TAS-120

    FGFR Cancer
    Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM).
  • HY-111787
    CSF1R-IN-2

    Src c-Met/HGFR c-Fms Cancer
    CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
  • HY-13264
    Degrasyn

    WP1130

    Deubiquitinase Bcr-Abl Autophagy Apoptosis Cancer
    Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
  • HY-136123
    Tubulin inhibitor 8

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
  • HY-21292
    SU5214

    SU4949

    VEGFR Cancer
    SU5214 is a potent VEGFR2 inhibitor extracted from patent US5834504A, SU5214, has the IC50s of 14.8 µM (FLK-1) and 36.7 µM (EGFR), respectively.
  • HY-136121
    Tubulin inhibitor 6

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
  • 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-123892
    RK-287107

    PARP Cancer
    RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.
  • HY-110339
    RKI 1447 dihydrochloride

    ROCK Apoptosis Cancer
    RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis.
  • HY-129636A
    GABAB receptor antagonist 1

    GABA Receptor Neurological Disease
    GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
  • 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-105940
    IQB-782

    Others Cardiovascular Disease
    IQB-782 is a cysteine derivative. IQB-782 has inhibition for thrombin activatable fibrinolysis inhibitor (TAFI), with an Ki(app) of 0.14 μM. IQB-782 shows a potent mucolytic-expectorant 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-107522
    DL-TBOA

    EAAT2 Neurological Disease
    DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.
  • HY-18971
    TG4-155

    Prostaglandin Receptor Inflammation/Immunology Neurological Disease Endocrinology Cancer
    TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1. TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor.
  • 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-12169
    Marimastat

    BB2516; TA2516

    MMP Cancer
    Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM) and MMP-7 (IC50=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes.
  • HY-117959
    TAK-615

    LPL Receptor Inflammation/Immunology
    TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).
  • HY-N7015
    Zerumbone

    HSV Infection
    Zerumbone is a monocyclic sesquiterpene compound isolated from the rhizomes of Zingiber zerumbet Smith. Zerumbone potently inhibits the activation of Epstein-Barr virus with an IC50 of 0.14 mM. Zerumbone has anti-cancer, antioxidant, anti-inflammatory and anti-proliferative activity.
  • HY-112272
    Lerociclib

    G1T38

    CDK Cancer
    Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
  • HY-126741
    Azadirachtin

    Apoptosis Others
    Azadirachtin, one of the most promising botanical insecticides, is widely used for pest control. Azadirachtin induces apoptosis in insect cell lines, including Sf9, SL-1 and BTI-Tn-5B1-4.
  • HY-13102
    UK-383367

    Procollagen C Proteinase Others
    UK-383367 (UK 383367) is a potent and selective inhibitor of BMP-1 (procollagen C-proteinase) with IC50 of 44 nM; Selective for BMP-1 over MMPs 1, 2, 3, 9 and 14 (IC50 values are >10,000 nM for listed MMPs).
  • HY-114267
    Cbz-B3A

    mTOR Others
    Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
  • HY-103394
    TC HSD 21

    Others Cancer
    TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
  • HY-133234
    BMVC-8C3O

    G-quadruplex Others
    BMVC-8C3O is a DNA G-quadruplexe (G4) ligand which can induce topological conversion of non-parallel to parallel forms in human telomeric DNA G4s.
  • HY-12842
    UC-112

    IAP Cancer
    UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
  • HY-112820
    Chlorantraniliprole

    Others Others
    Chlorantraniliprole is an insecticide that potently and selectively activates insect ryanodine receptor, with EC50s of 40 nM and 50 nM for Drosophila melanogaster and H. virescens ryanodine receptor, and ∼300-fold more potent than that in the mouse myoblast cell line, C2C12 (EC50, 14 μM).
  • HY-101964
    SPI-112

    Phosphatase Cancer
    SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively.
  • 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-12275
    FR 180204

    ERK Apoptosis Cancer
    FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC50s of 0.51 μM (Ki=0.31 μM) and 0.33 μM (Ki=0.14 μM), respectively.
  • HY-10261A
    Afatinib dimaleate

    BIBW 2992MA2

    EGFR Autophagy Cancer
    Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
  • 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-122243
    IU1-47

    Deubiquitinase Neurological Disease
    IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 inhibits IsoT/USP5 with an IC50 of 20 μM. IU1-47 induces tau elimination in cultured neurons.
  • HY-P1440
    BeKm-1

    Potassium Channel
    BeKm-1 is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 dose-dependently prolongs QTc interval in isolated rabbit heart.
  • HY-106254
    Vapendavir

    BTA798

    Enterovirus Infection
    Vapendavir (BTA798) is a potent enteroviral capsid binder (CB). Vapendavir (BTA798) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains.
  • HY-103061
    Dehydro-ZINC39395747

    Others Cardiovascular Disease
    Dehydro-ZINC39395747 is a derivative of ZINC39395747. ZINC39395747 is a potent cytochrome b5 reductase 3 (CYB5R3) inhibitor with an IC50 of 9.14 μM and a Kd of 1.11 μM. ZINC39395747 can increase NO bioavailability in vascular cells.
  • HY-N7389B
    GDP-​α-D-​mannose disodium

    Endogenous Metabolite Metabolic Disease
    GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM).
  • HY-112272A
    Lerociclib dihydrochloride

    G1T38 dihydrochloride

    CDK Cancer
    Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
  • HY-131187
    BMS-1166-N-piperidine-COOH

    Ligand for Target Protein for PROTAC Cancer
    BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-10261
    Afatinib

    BIBW 2992

    EGFR Autophagy Cancer
    Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
  • HY-14658
    Thalidomide

    Ligand for E3 Ligase Autophagy Apoptosis Cancer Inflammation/Immunology
    Thalidomide is initially promoted as a sedative, inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties.
  • HY-108341
    PF-06424439

    Acyltransferase Metabolic Disease
    PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
  • HY-101930B
    (R)-BMS-816336

    Others Metabolic Disease
    (R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .
  • HY-N7032
    Uridine 5′-diphosphoglucose disodium salt

    UDP-D-Glucose disodium salt

    Endogenous Metabolite P2Y Receptor Neurological Disease
    Uridine 5′-diphosphoglucose disodium salt (UDP-D-Glucose disodium salt) is the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine-5′-diphosphoglucose is an agonist of the P2Y14 receptor, a neuroimmune system GPCR.
  • 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-N4205
    Tetrahydropiperine

    Cytochrome P450 Cancer
    Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum. Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM).
  • HY-135750
    VAF347

    Aryl Hydrocarbon Receptor Inflammation/Immunology
    VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14 +CD11b + monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects.
  • HY-120877
    MRT199665

    Salt-inducible Kinase (SIK) AMPK Apoptosis Cancer
    MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
  • HY-P1440A
    BeKm-1 TFA

    Potassium Channel
    BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.
  • HY-126321
    RORγt agonist 1

    ROR Cancer
    RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy.
  • HY-100352
    BI-9564

    Epigenetic Reader Domain Cancer
    BI-9564 is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 μM and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 μM for BET family.
  • HY-129769
    CMLD012073

    Eukaryotic Initiation Factor (eIF) Cancer
    CMLD012073 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012073 against NIH/3T3 cells with an IC50 of 10 nM. CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A).
  • HY-111370
    mTOR inhibitor-2

    mTOR Cancer
    mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.
  • HY-103258
    TC ASK 10

    MAP3K Apoptosis Cancer
    TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM).
  • HY-108341A
    PF-06424439 methanesulfonate

    Acyltransferase Metabolic Disease
    PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
  • HY-18332C
    DOV-216,303 Free Base

    Serotonin Transporter Dopamine Transporter Neurological Disease
    DOV-216,303 (Free Base) is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats.
  • HY-114370
    Selpercatinib

    LOXO-292

    RET Cancer
    Selpercatinib (LOXO-292) is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 163, has an IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively. Antineoplastic activity.
  • HY-129636
    (E)-GABAB receptor antagonist 1

    GABA Receptor Neurological Disease
    (E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
  • HY-70059
    LY341495

    mGluR Neurological Disease
    LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC50s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively.
  • HY-106254A
    Vapendavir diphosphate

    BTA798 diphosphate

    Enterovirus Infection Inflammation/Immunology
    Vapendavir diphosphate (BTA798 diphosphate) is a potent enteroviral capsid binder (CB). Vapendavir diphosphate (BTA798 diphosphate) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains.
  • 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-N2609
    7,4'-Dihydroxyflavone

    CCR NF-κB Inflammation/Immunology Endocrinology
    7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid isolated from Glycyrrhiza uralensis, the eotaxin/CCL11 inhibitor, has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production. 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2. 7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM.
  • HY-10683
    PKI-402

    PI3K mTOR Cancer
    PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
  • HY-135791
    T-705RTP sodium

    DNA/RNA Synthesis Influenza Virus SARS-CoV Infection
    T-705RTP sodium is a selective and GTP-competitive influenza virus RNA polymerase inhibitor with an IC50 of 0.14 μM and a Ki of 1.52 μM. T-705RTP sodium is the active triphosphate metabolite of T-705 and has potent anti-influenza virus activity.
  • HY-135803
    T-705RTP

    DNA/RNA Synthesis Influenza Virus SARS-CoV Infection
    T-705RTP is a selective and GTP-competitive influenza virus RNA polymerase inhibitor with an IC50 of 0.14 μM and a Ki of 1.52 μM. T-705RTP is the active triphosphate metabolite of T-705 and has potent anti-influenza virus activity.
  • HY-W016584
    4,5-Dichlorocatechol

    Others Infection
    4,5-Dichlorocatechol is a substrate of the broad-spectrum chlorocatechol 1,2-dioxygenase of pseudomonas chlororaphis RW71. The Ki values for 4,5-dichlorocatechol is 30 nM for the dioxygenase of the Chlorobenzoate-degrading strain Pseudomonas putida AC27 and 4 nM for the dioxygenase of Acidovorax sp. strain PS14.
  • HY-124729
    BL-918

    ULK Autophagy Neurological Disease
    BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.
  • HY-N2181
    Acetylshikonin

    Cytochrome P450 AChE Cancer Inflammation/Immunology
    Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity. Acetylshikonin is a non-selective cytochrome P450 inhibitor against all P450s (IC50 values range from 1.4-4.0 μM). Acetylshikonin is an AChE inhibitor and exhibits potent antiapoptosis activity.
  • HY-13413
    Tofogliflozin (hydrate)

    CSG-452 hydrate

    SGLT Reactive Oxygen Species Metabolic Disease
    Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells.
  • HY-111139
    MS417

    GTPL7512

    Epigenetic Reader Domain HIV Infection Inflammation/Immunology
    MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).
  • HY-111978
    ZEN-3862

    Epigenetic Reader Domain Cancer
    ZEN-3862 is a BET inhibitor with IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4.
  • HY-133780
    Afatinib impurity 11

    EGFR Autophagy Cancer
    Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
  • HY-125035
    LCH-7749944

    GNF-PF-2356

    PAK Apoptosis Cancer
    LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis.
  • HY-17371
    Oxaliplatin

    DNA Alkylator/Crosslinker Autophagy Cancer
    Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death. Oxaliplatin time-dependently inhibits human melanoma cell lines C32 and G361 with IC50 values of 0.98 μM and 0.14 μM, respectively. Oxaliplatin induces cell autophagy.
  • HY-100753
    STAT3-IN-1

    STAT Apoptosis Cancer
    STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis.
  • HY-110266
    GN44028

    HIF/HIF Prolyl-Hydroxylase Cancer
    GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.
  • 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-125820
    Sigma-1 receptor antagonist 3

    Sigma Receptor Potassium Channel Neurological Disease
    Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain.
  • 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-112294
    TIE-2/VEGFR-2 kinase-IN-1

    VEGFR Cancer Inflammation/Immunology Cardiovascular Disease
    TIE-2/VEGFR-2 kinase-IN-1 is used for the synthesis of TIE-2 and/or VEGFR-2 inhibitors, extracted from patent WO2003022852, example 14. TIE-2/VEGFR-2 kinase-IN-1 is used for the study of diseases associated with inappropriate angiogenesis.
  • 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-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-14658S
    Thalidomide D4

    Ligand for E3 Ligase Autophagy Apoptosis Cancer Inflammation/Immunology
    Thalidomide D4 is a deuterium labeled Thalidomide. Thalidomide is initially promoted as a sedative, inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties.
  • HY-17397
    Strontium Ranelate

    Distrontium renelate; S12911

    CaSR Metabolic Disease
    Strontium Ranelate (S12911) is an antiosteoporotic agent that acts by reducing bone resorption and promoting bone formation, thereby inducing a positive bone balance. Strontium Ranelate also can activate the calcium-sensing receptor (CaSR) in non skeletal cells, resulting in the activation of inositol 1, 4, 5-triphosphate production and mitogen-activated protein kinase signaling.
  • HY-107818
    4-Hydroxychalcone

    NF-κB Inflammation/Immunology Cardiovascular Disease
    4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice.
  • HY-10405
    Pamapimod

    Ro4402257; R1503

    p38 MAPK Autophagy Inflammation/Immunology
    Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.
  • HY-12993
    RSV604

    (S)-1-(2-Fluorophenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea

    RSV Infection
    RSV604 is a novel inhibitor of respiratory syncytial virus replication(EC50=0.86 uM); a putative RSV nucleoprotein(N) inhibitor in phase 2 clinical trials.
  • HY-101507
    Pico145

    HC-608

    TRP Channel Cancer
    Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
  • HY-107123
    TMC310911

    HIV Protease Infection
    TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity.
  • HY-102070
    NS13001

    Potassium Channel Neurological Disease
    NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.
  • HY-N0761
    Isoferulic acid

    3-Hydroxy-4-methoxycinnamic acid

    Adrenergic Receptor Influenza Virus Infection Endocrinology Metabolic Disease
    Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is a cinnamic acid derivative that has antidiabetic activity. Isoferulic acid binds to and activates α1-adrenergic receptors (IC50=1.4 µM) to enhance secretion of β-endorphin (EC50=52.2 nM) and increase glucose use. Isoferulic acid also has anti-influenza virus activities.
  • HY-15478
    WZ811

    CXCR Cancer Endocrinology
    WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM).
  • HY-76569
    Desfesoterodine

    PNU-200577; 5-Hydroxymethyl Tolterodine

    mAChR Neurological Disease
    Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.
  • HY-100809
    Guvacine hydrochloride

    GABA Receptor Neurological Disease
    Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
  • 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-12001
    WZ-3146

    EGFR Cancer
    WZ3146 is a mutant selective EGFR inhibitor with IC50s of 2, 2, 5, 14 and 66 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750, EGFR E746_A750/T790M and EGFR, respectively.
  • HY-105064D
    Zoniporide hydrochloride hydrate

    CP-597396 hydrochloride hydrate

    Sodium Channel Cardiovascular Disease
    Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM).
  • HY-19827
    Aeroplysinin 1

    (+)-Aeroplysinin-1

    Bacterial HIV Apoptosis Cancer Infection
    Aeroplysinin 1 ((+)-Aeroplysinin-1), a secondary metabolite isolated from marine sponges, shows potent antibiotic effects on Gram-positive bacteria and exerts antiviral activity against HIV-1 (IC50=14.6 μM). Aeroplysinin 1 has anti-inflammatory, anti-angiogenic and anti-tumor activities. Aeroplysinin 1 induces apoptosis in endothelial cells.
  • HY-W010820
    Uridine 5'-diphosphate sodium salt

    P2Y Receptor DNA/RNA Synthesis Endogenous Metabolite Metabolic Disease Inflammation/Immunology
    Uridine 5'-diphosphate sodium salt is a potent, selective P2Y6 receptor native agonist (EC50=300 nM; pEC50=6.52) and a potent P2Y14 antagonist (pEC50=7.28). Uridine 5'-diphosphate sodium salt, an endogenous metabolite, catalyzes the glucuronidation of a wide array of substrates and is used in nucleic acid (RNA) biosynthesis.
  • HY-103371
    DCPIB

    Chloride Channel Potassium Channel Neurological Disease
    DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK and inhibits TRESK, TASK1 and TASK3 (IC50s of 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM in CPAE cells.
  • HY-111979
    ZEN-3411

    Epigenetic Reader Domain Cancer
    ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4.
  • HY-19824
    3PO

    Others Cancer
    3PO is a novel small-molecule inhibitor of the PFKFB3 isozyme, 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) IC50 value Target: PFKFB3 isozyme in vitro: 3PO inhibits recombinant PFKFB3 activity, suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
  • HY-125269
    TED-347

    YAP Cancer
    TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity.
  • 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-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-117626
    LP-935509

    Others Inflammation/Immunology Neurological Disease
    LP-935509 is a selective, ATP-competitive and brain-penetrant inhibitor of adapter protein-2 associated kinase 1 (AAK1) with an IC50 and a Ki of 3.3 nM and 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure.
  • HY-W010832
    Uridine-5'-diphosphate disodium salt

    P2Y Receptor DNA/RNA Synthesis Endogenous Metabolite Metabolic Disease Inflammation/Immunology
    Uridine-5'-diphosphate disodium salt is a potent, selective P2Y6 receptor native agonist (EC50=300 nM; pEC50=6.52) and a potent P2Y14 antagonist (pEC50=7.28). Uridine-5'-diphosphate disodium salt, an endogenous metabolite, catalyzes the glucuronidation of a wide array of substrates and is used in nucleic acid (RNA) biosynthesis.
  • HY-104036
    IDH-305

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)).
  • HY-100609
    4-P-PDOT

    Melatonin Receptor Neurological Disease
    4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity).
  • HY-18346
    Mozavaptan

    OPC-31260

    Vasopressin Receptor Cancer Endocrinology Metabolic Disease
    Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.
  • HY-123593
    Mozavaptan hydrochloride

    OPC-31260 hydrochloride

    Vasopressin Receptor Cancer Endocrinology Metabolic Disease
    Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.
  • 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-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-14945
    Remogliflozin etabonate

    GSK189075

    SGLT Metabolic Disease
    Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a prodrug based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.
  • HY-130538
    1-Naphthohydroxamic acid

    HDAC Cancer
    1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity.1-Naphthohydroxamic acid can induce tubulin acetylation.
  • HY-103409
    ABT-724 trihydrochloride

    Dopamine Receptor Neurological Disease
    ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.
  • 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-123919
    TL13-112

    PROTAC ALK Cancer
    TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib (HY-15656) and the cereblon ligand of Pomalidomide (HY-10984).
  • HY-126750
    GNF362

    Phosphatase Inflammation/Immunology
    GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca 2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4].
  • HY-14330
    ABT-724

    Dopamine Receptor Neurological Disease
    ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.
  • HY-122720
    SEC inhibitor KL-1

    KL-1

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

    KL-2

    Others Cancer
    SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM.
  • HY-101513
    eIF4A3-IN-1

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD.
  • HY-104040
    MKC8866

    IRE1 Cancer
    MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.
  • 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-120000
    MS402

    Epigenetic Reader Domain Cancer Inflammation/Immunology
    MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice.
  • HY-114091
    PF-00356231 hydrochloride

    MMP Inflammation/Immunology
    PF-00356231 hydrochloride is a specific, non-peptidic, non-zinc chelating ligand and inhibitor of matrix metalloproteinase MMP-12 (IC50=1.4 μM). PF-00356231 hydrochloride binds to MMP-12 and forms PF-00356231/MMP-12 complex. PF-00356231 hydrochloride shows potency against MMP-13, MMP-8, MMP-9, MMP-3 with IC50s of 0.00065, 1.7, 0.98, 0.39 μM, respectively.
  • HY-110368
    BS-181 dihydrochloride

    CDK Cancer
    BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy.
  • HY-13266
    BS-181

    CDK Cancer
    BS-181 is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy.
  • 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-100858
    PP7

    Influenza Virus Infection
    PP7 is a potent PB1-PB2 interaction inhibitor with an IC50 of 8.6 μM, and their inhibition against viral polymerase activity (IC50=9.5 μM). PP7 shows antiviral activities against influenza A virus (IAV), including A(H1N1)pdm09 (EC50=1.4 μM), A(H7N9) and A(H9N2) subtypes.
  • 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-104042
    Vorasidenib

    AG-881

    Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.
  • 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-B0846
    Dimethomorph

    Fungal Androgen Receptor
    Dimethomorph is a morpholine fungicide that inhibits fungal cell wall formation. Dimethomorph inhibits mycelial growth of the oomycete fungi P. citrophthora, P. parasitica, P. capsici, and P. infestans (EC50s=0.14 µg/mL, 0.38 µg/mL, <0.1 µg/mL, and 0.16-0.3 µg/mL, respectively) but is less active against the green algae species C. vulgaris or S. obliquus in vitro (EC50s=47.46 µg/mL and 44.87 µg/mL, respectively). Dimethomorph inhibits androgen receptor (AR) activity in a reporter assay in MDA-kb2 human breast cancer cells but not in a yeast antiandrogen screen (IC20s=0.263 µM and 38.5 µM, respectively).
  • 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.