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Results for "Ang (1-3) Inhibitors" in MCE Product Catalog:

629

Inhibitors & Agonists

1

Screening Libraries

1

Dye Reagents

2

Biochemical Assay Reagents

57

Peptides

3

Inhibitory Antibodies

73

Natural
Products

15

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-P1497
    Bradykinin (1-3)

    Bradykinin Receptor Cardiovascular Disease Endocrinology
    Bradykinin (1-3) is a 3-amino acid residue peptide. Bradykinin (1-3) is an amino-truncated Bradykinin peptide, cleaved by Prolyl endopeptidase.
  • HY-125827
    13-Methylberberine chloride

    13-Methylberberinium chloride

    Others Cancer Metabolic Disease
    13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS.
  • HY-114421
    FKBP12 PROTAC dTAG-13

    dTAG-13

    PROTAC FKBP Epigenetic Reader Domain Cancer
    FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader. FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
  • HY-P7060
    NT 13

    TPPT

    iGluR Neurological Disease
    NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide. NT 13 is a partial N-methyl-D-aspartate receptor (NMDAR) agonist used in the study of depression, anxiety, and other related diseases.
  • HY-100358
    AQ-13 dihydrochloride

    Parasite Infection
    AQ-13 dihydrochloride is an aminoquinoline antimalarial drug that is effective against drug-resistant strains of Plasmodium falciparum.
  • HY-130255
    BTK inhibitor 13

    Others Inflammation/Immunology
    BTK inhibitor 13 (compound 8) is a potent and selective Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 1.2 nM.
  • HY-135677
    DHODH-IN-13

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-13 (Compound 7a) is a hydroxyfurazan analog of A771726. DHODH-IN-13 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for rat liver DHODH. DHODH-IN-13 can be used for rheumatoid arthritis.
  • HY-15158A
    SBE13

    Polo-like Kinase (PLK) Autophagy Cancer
    SBE13 is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 poorly inhibits Plk2 (IC50>66 μM) or Plk3 (IC50=875 nM).
  • HY-124401
    BT-13

    RET Neurological Disease
    BT-13 is a potent and selective glial cell line-derived neurotrophic factor (GDNF) receptor RET agonist independently of GFLs, promoting neurite growth from sensory neurons in vitro and attenuates experimental neuropathy in the Rat.
  • HY-W008343
    1,3-Dimethyluracil

    Endogenous Metabolite Metabolic Disease
    1,3-Dimethyluracil is a pyrimidone derives from a uracil. 1,3-Dimethyluracil found occasionally in human urine. 1,3-Dimethyluracil shows inhibition activity against hCA I and hCA II (human carbonic anhydrase) with Ki of 316.2 μM and 166.4 μM, respectively.
  • HY-101088
    CeMMEC13

    DNA/RNA Synthesis Cancer
    CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with an IC50 of 2.1 μM.
  • HY-W001189
    1,3-Dithiane

    Bacterial Endogenous Metabolite Infection
    1,3-Dithiane is a protected formaldehyde anion equivalent that could serve as a useful labeled synthon. 1,3-Dithiane is also a sulfur-containing Maillard reaction products (MRPs) found in boiled beef extracts. 1,3-Dithiane shows a potent direct-acting mutagenicity toward S. typhimurium TA98 and TA100.
  • HY-18680
    PU-WS13

    HSP Cancer
    PU-WS13 is a selective Grp94 inhibitor, with an EC50 of 0.22 μM.
  • HY-128810
    E3 ligase Ligand 13

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 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-18009
    LFM-A13

    Btk Polo-like Kinase (PLK) JAK Cancer
    LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
  • HY-125965
    BioA-IN-13

    Bacterial Infection
    BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme.
  • HY-136195
    TL13-110

    ALK Cancer
    TL13-110 is a negative control for TL13-112 (HY-123919) and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells.
  • HY-136194
    TL13-22

    ALK Cancer
    TL13-22 is a negative control for TL13-12 (HY-122582) and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.
  • HY-16728
    Rapastinel

    GLYX-13

    iGluR Neurological Disease
    Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist.
  • HY-131338
    RORγt inverse agonist 13

    ROR Inflammation/Immunology
    RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM.
  • HY-P0251
    Neurotensin(8-13)

    Neurotensin Receptor Neurological Disease
    Neurotensin (8-13) is an active fragment of Neurotensin. Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density.
  • HY-W014993
    1,3-Dimethyluric acid

    Endogenous Metabolite Others
    1,3-Dimethyluric acid is a product of theophylline metabolism in man. 1,3-Dimethyluric acid is one of the purine components in urinary calculi.
  • HY-18850
    MAPK13-IN-1

    p38 MAPK Autophagy Others
    MPAK13-IN-1 is a MAPK13 (p38δ) inhibitor, with an IC50 of 620 nM.
  • HY-129749
    IDO-IN-13

    Indoleamine 2,3-Dioxygenase (IDO) Inflammation/Immunology
    IDO-IN-13 is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an EC50 of 17 nM, extracted from patent WO2019040102A1, example 43.
  • HY-124029
    MMP13-IN-3

    MMP Inflammation/Immunology
    MMP13-IN-3 is a potent, selective, and orally active MMP-13 inhibitor (IC50=1 nM) for the potential treatment of osteoarthritis. MMP13-IN-3 is >1000 selective over other MMPs.
  • HY-122582
    TL13-12

    PROTAC ALK Cancer
    TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the cereblon ligand of Pomalidomide (HY-10984).
  • HY-15158
    SBE13 Hydrochloride

    Polo-like Kinase (PLK) Autophagy Apoptosis Cancer
    SBE13 Hydrochloride is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 Hydrochloride poorly inhibits Plk2 (IC50>66 μM) or Plk3 (IC50=875 nM).
  • HY-A0023AS
    Alogliptin (13CD3)

    SYR-322 (13CD3)

    Dipeptidyl Peptidase Cancer Metabolic Disease
    Alogliptin 13CD3 (SYR-322 13CD3) is the deuterium labeled Alogliptin. Alogliptin is a potent and selective inhibitor of DPP-4.
  • HY-77490
    (R)-(-)-1,3-Butanediol

    Endogenous Metabolite Metabolic Disease
    (R)-(-)-1,3-Butanediol is used to regulate the metabolism of carbohydrate and lipid.
  • 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-126292
    KRAS G12C inhibitor 13

    Ras Cancer
    KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30.
  • HY-141021
    Bis-PEG13-acid

    PROTAC Linker Cancer
    Bis-PEG13-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141266
    Methyltetrazine-PEG13-acid

    PROTAC Linker Cancer
    Methyltetrazine-PEG13-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140021
    Propargyl-PEG13-acid

    PROTAC Linker Cancer
    Propargyl-PEG13-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140041
    Bis-propargyl-PEG13

    PROTAC Linker Cancer
    Bis-propargyl-PEG13 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-124819
    D13-9001

    Bacterial Infection
    D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the KD values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively. D13-9001 exhibits antibiotic activities.
  • HY-140365
    Tos-PEG13-Boc

    PROTAC Linker Cancer
    Tos-PEG13-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140305
    DBCO-PEG13-DBCO

    PROTAC Linker Cancer
    DBCO-PEG13-DBCO is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-130832
    Hydroxy-PEG13-Boc

    PROTAC Linker Cancer
    Hydroxy-PEG13-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-133349
    m-PEG13-Hydrazide

    PROTAC Linker Cancer
    m-PEG13-Hydrazide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141401
    m-PEG13-Boc

    PROTAC Linker Cancer
    m-PEG13-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141281
    Methyltetrazine-PEG13-Boc

    PROTAC Linker Cancer
    Methyltetrazine-PEG13-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141234
    HO-PEG13-OH

    PROTAC Linker Cancer
    HO-PEG13-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-135824
    Propargyl-PEG13-alcohol

    PROTAC Linker Cancer
    Propargyl-PEG13-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-Y0678
    1,3,5-Trimethoxybenzene

    Others Neurological Disease
    1,3,5-Trimethoxybenzene is a key component of the Chinese rose odor. 1,3,5-Trimethoxybenzene is synthesized in three successive methylation steps from phloroglucinol, the initial precursor. 1,3,5-Trimethoxybenzene is an effective sedative.
  • HY-B0389A
    D-Glucose-13C6

    Glucose-13C6

    Endogenous Metabolite Metabolic Disease
    D-Glucose-13C6 is a tracer used to trace glucose-related synthetic catabolism, is a low-cost alternative with the significant advantage that the sixth isotope of natural glucose has virtually zero natural abundance, which facilitates isotopomer analysis with <1% labeled glucose in the infusate.
  • HY-50667S
    Apixaban 13CD3

    BMS-562247-01 13CD3

    Factor Xa Cardiovascular Disease
    Apixaban 13CD3 (BMS-562247-01 13CD3) is a deuterium labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
  • HY-P1337
    Dynorphin B (1-13)

    Opioid Receptor Neurological Disease
    Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.
  • HY-129240S
    13-​cis Acitretin D3

    Isoacitretin D3; Ro 13-7652 D3

    Drug Metabolite Inflammation/Immunology
    13-cis Acitretin D3 (Isoacitretin D3) is a deuterium labeled 13-cis Acitretin. 13-cis Acitretin is the metabolite of Acitretin after chronic administration. Acitretin(Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis.
  • HY-15127
    Isotretinoin

    13-cis-Retinoic acid

    RAR/RXR Endogenous Metabolite Autophagy Cancer
    Isotretinoin(13-cis-Retinoic acid) is a medication used for the treatment of severe acne.
  • HY-N7039
    Mogroside IA-(1-3)-glucopyranoside

    Others Metabolic Disease
    Mogroside IA-(1-3)-glucopyranoside is isolated from Siraitia grosvenorii.
  • HY-N1943
    Ailanthone

    Δ13-Dehydrochaparrinone

    Androgen Receptor Cancer Inflammation/Immunology
    Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
  • HY-N7086
    1,3,5-Trimethylpyrazole

    Others Others
    1,3,5-Trimethylpyrazole is a compound used for chemical synthesis.
  • HY-15005S
    Sofosbuvir 13CD3

    PSI-7977 13CD3; GS-7977 13CD3

    HCV Infection
    Sofosbuvir 13CD3 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
  • HY-N0674
    Dehydrocorydaline

    13-Methylpalmatine

    Bcl-2 Family Caspase PARP p38 MAPK Parasite Autophagy Cancer Infection
    Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
  • HY-P1480
    Neuropeptide Y (13-36), amide, human

    Neuropeptide Y (13-36), human

    Neuropeptide Y Receptor Neurological Disease Endocrinology
    Neuropeptide Y (13-36), amide, human is a neuropeptide Y receptor agonist.
  • HY-10932
    Aniracetam

    Ro 13-5057

    nAChR iGluR Neurological Disease
    Aniracetam(Ro 13-5057) is a nootropics and neuroprotective drug, which is selectively modulates the AMPA receptor and nAChR.
  • HY-141271
    Methyltetrazine-PEG13-NHS ester

    PROTAC Linker Cancer
    Methyltetrazine-PEG13-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141107
    m-PEG13-NHS ester

    PROTAC Linker Cancer
    m-PEG13-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141097
    Acid-PEG13-NHS ester

    PROTAC Linker Cancer
    Acid-PEG13-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140959
    DSPE-PEG13-TFP ester

    PROTAC Linker Cancer
    DSPE-PEG13-TFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141256
    Bis-PEG13-PFP ester

    PROTAC Linker Cancer
    Bis-PEG13-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140270
    DBCO-NHCO-PEG13-acid

    PROTAC Linker Cancer
    DBCO-NHCO-PEG13-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-N1412
    1,3-Dicaffeoylquinic acid

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

    PI3K Akt Reactive Oxygen Species Neurological Disease
    1,3-Dicaffeoylquinic acid is a caffeoylquinic acid derivative that exhibits antioxidant activity and radical scavenging activity.
  • HY-116924
    1,3-Bis-aminooxy propane

    PROTAC Linker Cancer
    1,3-Bis-aminooxy propane is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-130825
    Bis-PEG13-NHS ester

    ADC Linker Cancer
    Bis-PEG13-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-16728B
    Rapastinel Trifluoroacetate

    GLYX-13 Trifluoroacetate

    iGluR Neurological Disease
    Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.
  • HY-P0088
    Porcine dynorphin A(1-13)

    Dynorphin A Porcine Fragment 1-13

    Opioid Receptor Others
    Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
  • 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-77434
    9-Dihydro-13-acetylbaccatin III

    9-DHAB III; 13-Acetyl-9-dihydrobaccatin III

    Others Cancer
    9-Dihydro-13-acetylbaccatin III (9-DHAB III) is an intermediate for taxol analog preparations.
  • HY-14605BS
    Rasagiline 13C3 mesylate racemic

    AGN1135 13C3 racemic; TVP1012 13C3 racemic

    Monoamine Oxidase Neurological Disease
    Rasagiline 13C3 mesylate racemic is the deuterium labeled Rasagiline, which is an irreversible inhibitor of monoamine oxidase.
  • HY-B0779A
    (5E,9E,13E)-Teprenone

    (5E,9E,13E)-Geranylgeranylacetone

    Others Metabolic Disease
    (5E,9E,13E)-Teprenone ((5E,9E,13E)-Geranylgeranylacetone) is an isomer of Teprenone with antiulcer activity. (5E,9E,13E)-Teprenone induces transcriptional activation of HSP genes that may increase gastric mucosal defense at conditions of stress.
  • HY-B0373S
    Tiopronin 13C D3

    Others Metabolic Disease
    Tiopronin 13C D3 is deuterium labeled Tiopronin.
  • HY-P1337A
    Dynorphin B (1-13) (TFA)

    Opioid Receptor Neurological Disease
    Dynorphin B (1-13) TFA acts as an agonist on opioid κ-receptor.
  • HY-P1317
    Nociceptin (1-13), amide

    Opioid Receptor Neurological Disease
    Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.
  • HY-18739
    Phorbol 12-myristate 13-acetate

    PMA

    PKC SPHK Inflammation/Immunology
    Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator.
  • HY-101953
    β-Apo-13-carotenone

    D'Orenone

    Others Others
    β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
  • HY-140276
    DBCO-NHCO-PEG13-NHS ester

    PROTAC Linker Cancer
    DBCO-NHCO-PEG13-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-Y0786
    1,3-Dibromo-5,5-dimethylhydantoin

    PROTAC Linker Cancer
    1,3-Dibromo-5,5-dimethylhydantoin is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-15236S
    PSI-6206 13CD3

    RO-2433 13CD3; GS-331007 13CD3; Sofosbuvir metabolite GS-331007 13CD3

    HCV Others
    PSI-6206 13CD3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
  • HY-133328
    Amino-PEG13-amine

    H2N-PEG13-CH2CH2NH2

    PROTAC Linker Cancer
    Amino-PEG13-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-125828
    1-(3,4-Dimethoxycinnamoyl)piperidine

    Others Infection
    1-(3,4-Dimethoxycinnamoyl)piperidine, a synthesized piperidine analog, possesses antimicrobial and antioxidant activity.
  • HY-N6926
    1,3,5-Tricaffeoylquinic acid

    HIV Infection
    1,3,5-Tricaffeoylquinic acid is a tricaffeoylquinic acid derivative isolated from H. populifolium with anti-HIV effect.
  • HY-N7506
    13-Hydroxyisobakuchiol

    Delta3,2-Hydroxylbakuchiol

    Monoamine Transporter Dopamine Transporter Neurological Disease
    Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) isolated from Psoralea corylifolia (L.), is a potent monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50=0.58 μM) and norepinephrine transporter (NET) (IC50=0.69 μM) than for the serotonin transporter (SERT) (IC50=312.02 μM). 13-Hydroxyisobakuchiol has the potential for the research of disorders such as Parkinson's disease, depression, and cocaine addiction.
  • HY-N2050
    1,3,5,8-Tetrahydroxyxanthone

    Desmethylbellidifolin

    Others Inflammation/Immunology Neurological Disease
    1,3,5,8-Tetrahydroxyxanthone (Desmethylbellidifolin) is a natural xanthone extracted from Gentianella acuta. 1,3,5,8-Tetrahydroxyxanthone has antispasmodic effect and anti-inflammatory activity.
  • HY-13619A
    Efaproxiral sodium

    RSR13 sodium

    Reactive Oxygen Species Cancer
    Efaproxiral sodium (RSR13 sodium) is a synthetic allosteric modifier of haemoglobin (Hb), decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy.
  • HY-133781S
    cis-Clopidogrel-MP Derivative 13CD3

    Clopidogrel-MP-AM 13CD3

    Others Others
    cis-Clopidogrel-MP Derivative 13CD3 (Clopidogrel-MP-AM 13CD3) is a deuterium labele cis-Clopidogrel-MP Derivative. cis-Clopidogrel-MP Derivative is a 3’-methoxyacetophenone derivative of Clopidogrel active metabolite. Clopidogrel is a well-known and orally active platelet inhibitor that targets P2Y12 receptor.
  • HY-W014316
    5-Bromo-5-nitro-1,3-dioxane

    Bacterial Fungal Infection
    5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol.
  • HY-N0078
    Ginkgolic Acid C13:0

    Ginkgolic acid (13:0); Ginkgoneolic Acid; 6-Tridecylsalicylic acid

    Others Infection
    Ginkgolic Acid (C13:0) is a natural anticariogenic agent in that it exhibits antimicrobial activity against S.
  • HY-14218
    Ditolylguanidine

    1,3-Di-o-tolylguanidine; DTG

    Sigma Receptor Neurological Disease
    Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor).
  • HY-135330
    Lamivudine 13C,15N2

    HIV Reverse Transcriptase Infection
    Lamivudine 13C,15N2 is a labelled impurity of Lamivudine (BCH-189). Lamivudine is a nucleoside reverse transcriptase inhibitors (NRTIs), and can inhibit HIV reverse transcriptase 1/2 and the reverse transcriptase of hepatitis B virus.
  • HY-23212
    2-Amino-1,3-bis(carboxylethoxy)propane

    PROTAC Linker Cancer
    2-Amino-13-bis(carboxylethoxy)propane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-N0674A
    Dehydrocorydaline chloride

    13-Methylpalmatine chloride

    Bcl-2 Family Caspase PARP p38 MAPK Parasite Autophagy Cancer Infection
    Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline chloride shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
  • HY-N4238
    Dehydrocorydaline nitrate

    13-Methylpalmatine nitrate

    Bcl-2 Family Caspase PARP p38 MAPK Parasite Autophagy Cancer Infection
    Dehydrocorydaline nitrate (13-Methylpalmatine nitrate) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline nitrate elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline nitrate shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
  • HY-U00264
    2-γ-Linolenoyl-1,3-dilinoleoyl-sn-glycerol

    Others Metabolic Disease
    2-γ-Linolenoyl-1,3-dilinoleoyl-sn-glycerol is a triglyceride.
  • HY-W008474
    Boc-NH-PEG2-C2-NH2

    PROTAC Linker 13

    PROTAC Linker Cancer
    Boc-NH-PEG2-C2-NH2 (PROTAC Linker 13) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-126355
    4,7,10,13,16-Docosapentaenoic acid

    Endogenous Metabolite Metabolic Disease
    4,7,10,13,16-Docosapentaenoic acid is an endogenous metabolite.
  • HY-N5097
    13-Oxo-9E,11E-octadecadienoic acid

    PPAR Metabolic Disease
    13-Oxo-9E,11E-octadecadienoic acid, an isomer of 9-oxo-ODA, is a potent PPARα activator derived from tomato juice. 13-Oxo-9E,11E-octadecadienoic acid decreases plasma and hepatic triglyceride in obese diabetic mice.
  • HY-128822
    cIAP1 Ligand-Linker Conjugates 13

    E3 ligase Ligand-Linker Conjugates 43

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 13 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 13 can be used to design SNIPERs.
  • HY-101953S
    β-Apo-13-carotenone D3

    D'Orenone D3

    Others Cancer
    β-Apo-13-carotenone D3 is the deuterium labeled β-Apo-13-carotenone. β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
  • HY-N6006
    1,3,6-Tri-O-galloyl-beta-D-glucose

    1,3,6-Tri-O-galloyl-β-D-glucose

    Others Others
    1,3,6-Tri-O-galloyl-beta-D-glucose (1,3,6-Tri-O-galloyl-β-D-glucose) is a phenolic compound in Black Walnut Kernels.
  • HY-133706S
    2-Nitrobenzaldehyde semicarbazone 13C,15N2

    Others Others
    2-Nitrobenzaldehyde semicarbazone 13C,15N2 is used for analysis of semicarbazide in the LC-MS/MS method.
  • HY-141248
    2-(Azido-PEG2-amido)-1,3-propandiol

    PROTAC Linker Cancer
    2-(Azido-PEG2-amido)-13-propandiol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-18985
    Phorbol 12,13-dibutyrate

    Phorbol dibutyrate; PDBu

    PKC Cancer
    Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter.
  • HY-P1320
    [Nphe1]Nociceptin(1-13)NH2

    Opioid Receptor Inflammation/Immunology
    [Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
  • HY-140527
    1,3-bis(carboxyethoxy)-2,2-bis(carboxyethoxy)propane

    PROTAC Linker Cancer
    1,3-bis(carboxyethoxy)-2,2-bis(carboxyethoxy)propane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-13619
    Efaproxiral

    RSR13

    Reactive Oxygen Species Cancer
    Efaproxiral is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
  • HY-P1300
    [(pF)Phe4]Nociceptin(1-13)NH2

    Opioid Receptor Neurological Disease
    [(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).
  • HY-P1320A
    [Nphe1]Nociceptin(1-13)NH2 TFA

    Opioid Receptor Inflammation/Immunology
    [Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
  • HY-140865
    2-(Azido-PEG3-amido)-1,3-bis(NHS ester)

    PROTAC Linker Cancer
    2-(Azido-PEG3-amido)-1,3-bis(NHS ester) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-18638
    TCID

    4,5,6,7-Tetrachloroindan-1,3-dione

    Deubiquitinase Neurological Disease
    TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective neuronal ubiquitin C-terminal hydrolase (UCH-L3) inhibitor with an IC50 of 0.6 μM. TCID diminishes glycine transporter GlyT2 ubiquitination in brainstem and spinal cord primary neurons.
  • HY-125392
    2-(Biotin-amido)-1,3-bis-(C1-PEG1-acid)

    PROTAC Linker Cancer
    2-(Biotin-amido)-13-bis(carboxylethoxy)propane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-P1300A
    [(pF)Phe4]Nociceptin(1-13)NH2 TFA

    Opioid Receptor Neurological Disease
    [(pF)Phe4]Nociceptin(1-13)NH2 TFA is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 TFA displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).
  • HY-140828
    m-PEG4-azide

    13-Azido-2,5,8,11-tetraoxatridecane

    PROTAC Linker Cancer
    m-PEG4-azide (13-Azido-2,5,8,11-tetraoxatridecane) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • 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-N0903
    Dihydrochelerythrine

    12,13-Dihydrochelerythrine

    Fungal Infection
    Dihydrochelerythrine is a natural compound isolated from the leaves of Macleaya microcarpa; has antifungal activity.
  • HY-W011120
    Ethyl docosa-4,7,10,13,16,19-hexaenoate

    Others Metabolic Disease
    Ethyl cis-4,7,10,13,16,19-Docosahexaenoate, the ethyl ester of Docosahexaenoate (DHA), is enriched in the ethyl ester fraction by the selective alcoholysis of fatty acid ethyl esters originating from tuna oil with lauryl alcohol.
  • HY-P1019A
    [Ala1,​3,​11,​15]​-​Endothelin (53-63) (TFA)

    Endothelin Receptor Cardiovascular Disease Endocrinology
    [Ala1,3,11,15]-Endothelin (53-63) (TFA), a linear peptide analog of endothelin (ET)-1, is a highly selective endothelin B (ETB) receptor.
  • HY-101408
    Docosatrienoic Acid

    cis-13,16,19-docosatrienoic acid; (13Z,16Z,19Z)-13,16,19-Docosatrienoic acid

    Endogenous Metabolite Cardiovascular Disease
    Docosatrienoic acid is a rare ω-3 fatty acid; inhibits LTB4 binding to pig neutrophil membranes with an Ki of 5 μM.
  • HY-P9970
    Infliximab

    Avakine; CT-P13

    TNF Receptor Metabolic Disease Inflammation/Immunology Neurological Disease
    Infliximab (Avakine) is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α. Infliximab has the potential for autoimmune, chronic inflammatory diseases and diabetic neuropathy research.
  • HY-B1324
    Oxiconazole nitrate

    Ro 13-8996

    Fungal Antibiotic Infection
    Oxiconazole nitrate is a broad spectrum antifungal which can inhibit the growth of T. tonsurans and T. rubrum with MIC90s of 0.25 and 0.5 μg/mL, respectively.
  • HY-12022
    3-Aminobenzamide

    PARP-IN-1

    PARP Cancer
    3-Aminobenzamide (PARP-IN-1) is a potent inhibitor of PARP with IC50 of appr 50 nM in CHO cells, and acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion.
  • HY-U00233
    FG8119

    NNC13-8119

    GABA Receptor Neurological Disease
    FG8119 is a novel benzodiazepine agonist extracted from patent US 4745112 A.
  • HY-W015818
    2-Benzoxazolinone

    2-Benzoxazolone; 1,3-Benzoxazol-2(3H)-one; 2-Hydroxybenzoxazole

    Parasite Infection
    2-Benzoxazolinone is an anti-leishmanial agent with an LC50 of 40 μg/mL against L. donovani. A building block in chemical synthesis. 1,3-Benzoxazol-2(3H)-one derivatives have antimicrobial activity against a selection of Gram-positive, Gram-negative bacteria and yeasts. Derivatives as anti-quorum sensing agent.
  • HY-108712
    TDCPP

    Tris(1,3-dichloroisopropyl)phosphate

    Others Cancer
    TDCPP is a chlorinated analog of tris(2,3-dibromopropyl)phosphate (Tris) which is one of the most detected organophosphorus flame retardants (OPFRs) in the environment.
  • HY-N4328
    Pasakbumin B

    13α-(21)-Epoxyeurycomanone

    Others Inflammation/Immunology
    Pasakbumin B, a bioactive compound from Eurycoma longifolia Jack, exhibits potent antiulcer activity.
  • HY-B0809
    Theophylline

    1,3-Dimethylxanthine; Theo-24

    Adenosine Receptor Phosphodiesterase (PDE) Autophagy Endogenous Metabolite Cancer
    Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
  • HY-W040240
    (3S,4R,5S)-1,3,4,5,6-Pentahydroxyhexan-2-one

    Endogenous Metabolite Metabolic Disease
    (3S,4R,5S)-1,3,4,5,6-Pentahydroxyhexan-2-one is an endogenous metabolite.
  • HY-N0157
    Orotic acid

    6-Carboxyuracil; Vitamin B13

    Nucleoside Antimetabolite/Analog Endogenous Metabolite Apoptosis Cancer
    Orotic acid (OA) is an intermediate in pyrimidine metabolism.
  • HY-B0367
    Lornoxicam

    Chlortenoxicam; Ro 13-9297; TS110

    COX Endogenous Metabolite Inflammation/Immunology
    Lornoxicam, a COX-1 and COX-2 inhibitor, is a new nonsteroidal anti-inflammatory drug (NSAID).
  • HY-B1169
    Timonacic

    1,3-Thiazolidine-4-carboxylic acid

    Others Cardiovascular Disease Cancer
    Timonacic is used as an adjuvant in the treatment of acute and hepatic disorders. It has also been used for the treatment of some cases of cancer, through the induction of the reverse transformation.
  • 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-15682
    TTNPB

    Ro 13-7410; Arotinoid acid; AGN191183

    RAR/RXR Autophagy Apoptosis Cancer
    TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
  • HY-42680
    (3S,4S,5R)-1,3,4,5,6-Pentahydroxyhexan-2-one

    Tagatose, D- (8CI)

    Endogenous Metabolite Metabolic Disease
    (3S,4S,5R)-1,3,4,5,6-Pentahydroxyhexan-2-one is an endogenous metabolite.
  • HY-W013215
    Adrenic Acid

    cis-7,10,13,16-Docosatetraenoic acid

    Endogenous Metabolite Metabolic Disease Inflammation/Immunology
    Adrenic Acid is an inflammation enhancer in non-alcoholic fatty liver disease.
  • HY-112077
    13-cis-N-[4-(Ethoxycarbonyl)phenyl]retinamide

    Ethyl 4-((2Z,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohex-1-en-1-yl)nona-2,4,6,8-tetraenamido)benzoate

    Others Inflammation/Immunology
    13-cis-N-[4-(Ethoxycarbonyl)phenyl]retinamide is a derivative of Retinoic acid.
  • HY-125843
    Pomalidomide-PEG1-C2-N3

    Cereblon Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 50

    E3 Ligase Ligand-Linker Conjugate Cancer
    Pomalidomide-PEG1-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology. Pomalidomide-PEG1-C2-N3 can be used to design a selective CDK6 PROTAC degrader CP-10. CP-10 induces the degradation of CDK6 with an DC50 of 2.1 nM.
  • HY-103599
    (S,R,S)-AHPC-PEG2-N3

    VH032-PEG2-N3; VHL Ligand-Linker Conjugates 6; E3 ligase Ligand-Linker Conjugates 13

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in PROTAC technology.
  • 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-114176
    (S,R,S)-AHPC-C4-NH2 hydrochloride

    VH032-C4-NH2 hydrochloride; VHL Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 28

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.
  • HY-B0708
    β-Estradiol 17-acetate

    1,3,5(10)-Estratriene-3,17β-diol 17-acetate

    Estrogen Receptor/ERR Endocrinology
    β-Estradiol 17-acetate is a metabolite of estradiol.
  • 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-140733
    Dioxoisoindolin-O-PEG-OMe (MW 2000)

    (1,3-dioxoisoindolin-2-yl)-O-PEG-OMe (MW 2000)

    PROTAC Linker Cancer
    Dioxoisoindolin-O-PEG-OMe (MW 2000) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140790
    Azide-PEG9-amido-C12-Boc

    13-(Azide-PEG9-ethylcarbamoyl)tridecanoic t-butyl ester

    PROTAC Linker Cancer
    Azide-PEG9-amido-C12-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140732
    Dioxoisoindolin-O-PEG-OH (MW 2000)

    (1,3-dioxoisoindolin-2-yl)-O-PEG-OH (MW 2000)

    PROTAC Linker Cancer
    Dioxoisoindolin-O-PEG-OH (MW 2000) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • 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-W000434
    Fmoc-NH-PEG4-CH2CH2COOH

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

    ADC Linker Cancer
    Fmoc-NH-PEG4-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-101023
    MK-8617

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.
  • HY-14588
    Lopinavir

    ABT-378

    HIV HIV Protease SARS-CoV Infection
    Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM.
  • HY-100359
    CL-82198

    MMP Cancer Inflammation/Immunology
    CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression.
  • HY-18958
    CCT245737

    Checkpoint Kinase (Chk) Cancer
    CCT245737 is an orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM.
  • HY-100518
    T-26c

    MMP Inflammation/Immunology
    T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes.
  • HY-19981A
    Derazantinib Racemate

    ARQ-087 Racemate

    FGFR Cancer
    Derazantinib Racemate (ARQ-087 Racemate) is the racemate of Derazantinib; Derazantinib is a potent inhibitor of FGFR1-3.
  • 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-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-P1036
    Compstatin

    Complement System Others
    Compstatin is a 13-residue cyclic peptide and a potent inhibitor of the complement system, and has species specificity.
  • HY-19966
    K858 (Racemic)

    Kinesin Apoptosis Cancer
    K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM.
  • HY-100190
    Amphethinile

    Amphetinile; CRC 82-07

    Microtubule/Tubulin Cancer
    Amphethinile is an anti-tubulin agent. The affinity constant for the association (Ka) of Amphethinile with tubulin is 1.3 μM.
  • HY-17006
    Caspofungin Acetate

    MK-0991 Acetate; L-743872 Acetate

    Fungal Antibiotic Infection
    Caspofungin Acetate (MK-0991 Acetate) is an antifungal drug, and noncompetitively inhibits 1,3-β-d glucan synthase activity.
  • HY-100545
    BAPTA-AM

    Potassium Channel Cardiovascular Disease
    BAPTA-AM is a well-known membrane permeable Ca 2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.
  • HY-112166
    PRN1008

    Btk Cancer Metabolic Disease
    PRN1008 is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
  • HY-B0202
    Irbesartan

    SR-47436; BMS-186295

    Angiotensin Receptor Apoptosis Cardiovascular Disease Endocrinology
    Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.
  • HY-17579
    Micafungin

    FK463

    Fungal Antibiotic Infection
    Micafungin (Mycamine; FK463) is an echinocandin antifungal drug which can inhibit 1,3-beta-D-glucan synthase.
  • HY-50904
    Nintedanib

    BIBF 1120

    PDGFR VEGFR FGFR Cancer
    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
  • HY-119109
    Laminaran

    Others Cancer
    Laminaran is a neutral water-soluble β-1-3-glucan and a typical ligand for Dectin-1 isolated from the brown alga D. dichotoma, has potent immunomodulating, radioprotective, and anticancer activities. Laminaran is made up of β (13)-glucan with β (1→6)-branches and can be catalyzed by enzymes such as laminarinase (EC 3.2.1.6) that breaks the β (1→3) bonds. Laminaran is a promising immune stimulatory molecule for use in cancer immunotherapy.
  • HY-11106
    Nintedanib esylate

    BIBF 1120 esylate

    PDGFR VEGFR FGFR Cancer
    Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
  • HY-115496
    7-BIA

    Phosphatase Neurological Disease
    7-BIA is a receptor-type protein tyrosine phosphatase D (PTPRD) inhibitor with an IC50 of ~1-3 μM.
  • HY-131166
    Curdlan

    Others Others
    Curdlan is a polysaccharide produced by bacteria and a homopolymer of glucose with β-1,3-glucosidic linkage.
  • HY-100506
    GLPG0187

    Integrin Cancer
    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
  • HY-101782
    HSK0935

    HSK-0935; HSK 0935

    SGLT Metabolic Disease
    HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic activities.
  • HY-101872
    GSK-872

    RIP kinase Inflammation/Immunology
    GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM.
  • HY-126332
    NED-3238

    Arginase Metabolic Disease
    NED-3238 is a highly potent arginase I and II inhibitor with IC50 values of 1.3 nM and 8.1 nM, respectively.
  • HY-16122A
    CAL-130

    PI3K Cancer
    CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
  • HY-16122B
    CAL-130 Hydrochloride

    PI3K Cancer
    CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
  • HY-16582A
    Sonidegib

    Erismodegib; LDE225; NVP-LDE225

    Smo Cancer
    Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.
  • HY-128523
    Kgp-IN-1

    Others Inflammation/Immunology
    Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.
  • HY-128523A
    Kgp-IN-1 hydrochloride

    Others Inflammation/Immunology
    Kgp-IN-1 hydrochloride is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.
  • HY-10857
    Vipadenant

    BIIB-014; CEB-4520

    Adenosine Receptor Neurological Disease
    Vipadenant (BIIB-014; CEB-4520) is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively.
  • HY-B1643
    Ethyl Vanillate

    Fungal Infection
    Ethyl Vanillate is a fungicidal agent. Ethyl Vanillate inhibits 17β-HSD2 with an IC50 1.3 µM.
  • HY-13283
    MF63

    PGE synthase Inflammation/Immunology
    MF63 is a selective mPGES-1 inhibitor with an IC50 of 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively.
  • HY-112439
    PI3Kdelta inhibitor 1

    PI3K Cancer Inflammation/Immunology
    PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM.
  • HY-16582
    Sonidegib diphosphate

    Erismodegib diphosphate; LDE225 diphosphate; NVP-LDE225 diphosphate

    Smo Cancer
    Sonidegib diphosphate (Erismodegib diphosphate) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, 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-50905
    Dovitinib

    TKI258; CHIR-258

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib (TKI258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
  • HY-10285A
    Saxagliptin hydrate

    BMS-477118 hydrate

    Dipeptidyl Peptidase Metabolic Disease
    Saxagliptin H2O(BMS477118 H2O) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.
  • HY-107723
    CGP71683 hydrochloride

    CGP71683A

    Neuropeptide Y Receptor Neurological Disease Endocrinology
    CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes.
  • HY-15704
    LH846

    Casein Kinase Cancer
    LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
  • HY-14248
    Letrozole

    CGS 20267

    Aromatase Autophagy Cancer
    Letrozole is an aromatase inhibitor with an IC50 of 1-13 nM.
  • HY-U00304
    Aurora B inhibitor 1

    Aurora Kinase Cancer
    Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor extracted from patent WO2007059299A1, compound 1-3, has a Ki value of <0.010 uM.
  • HY-10011
    SCH 563705

    CXCR Inflammation/Immunology Endocrinology
    SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.
  • HY-P1043A
    NGR peptide Trifluoroacetate

    Aminopeptidase Cancer
    NGR peptide Trifluoroacetate containing the asparagine-glycine-arginine (NGR) motif is recognized by CD13/aminopeptidase N (APN) receptor isoforms that are selectively overexpressed in tumor neovasculature.
  • HY-10193
    AZD-1480

    JAK Cancer
    AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 1.3 nM and <0.4 nM, respectively.
  • HY-10207
    Dovitinib lactate

    CHIR-258 lactate; TKI-258 lactate

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
  • 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-19818A
    NAN-190 hydrobromide

    5-HT Receptor Neurological Disease
    NAN-190 hydrobromide is a serotonin receptor 5-HT antagonist. NAN-190 is a selective antagonist of 5-HT1A.
  • HY-P1282
    Agitoxin-2

    Potassium Channel Neurological Disease
    Agitoxin-2 is a K+ channel inhibitor, with IC50 values of 201 pM and 144 pM for mKV1.3 and mKV1.1, respectively).
  • HY-108689
    Broflanilide

    GABA Receptor Neurological Disease
    Broflanilide is a potential insecticide and metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.
  • HY-100933
    MY-5445

    Phosphodiesterase (PDE) Cardiovascular Disease
    MY-5445 is a specific phosphodiesterase type 5 (PDE5) inhibitor. MY-5445 selectively inhibits cGMP PDE with a Ki of 1.3 μM.
  • HY-13493
    AC710

    PDGFR c-Kit FLT3 Cancer
    AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
  • HY-10805A
    Almorexant hydrochloride

    ACT-078573 hydrochloride

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Almorexant hydrochloride (ACT 078573 hydrochloride) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
  • HY-128669
    Abemaciclib Metabolites M2

    CDK Cancer
    Abemaciclib Metabolites M2 is a metabolite of abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity.
  • HY-P2228
    Chlamydocin

    HDAC Apoptosis Cancer
    Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3.
  • HY-10805
    Almorexant

    ACT 078573

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
  • HY-P1282A
    Agitoxin-2 TFA

    Potassium Channel Neurological Disease
    Agitoxin-2 TFA is a K+ channel inhibitor, with IC50 values of 201 pM and 144 pM for mKV1.3 and mKV1.1, respectively).
  • HY-13781
    Pemetrexed disodium hemipenta hydrate

    LY231514 disodium hemipenta hydrate

    Antifolate Autophagy Apoptosis Cancer
    Pemetrexed disodium hemipenta hydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-13493A
    AC710 Mesylate

    PDGFR Cancer
    AC710 Mesylate is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
  • HY-17002
    Suplatast (Tosilate)

    IPD 1151T

    Interleukin Related Inflammation/Immunology
    Suplatast Tosilate (IPD 1151T) is a Th2 cytokine inhibitor that attenuates IL-2, IL-5 and IL-13 production and has no effect on IFN-γ production.
  • HY-120934
    C25-140

    TNF Receptor E1/E2/E3 Enzyme Inflammation/Immunology
    C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.
  • 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-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-10820
    Pemetrexed

    LY231514

    Antifolate Autophagy Cancer
    Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-131064
    RIPK3-IN-1

    RIP kinase Inflammation/Immunology
    RIPK3-IN-1 is a RIPK3 type II DFG-out inhibitor with an IC50 of 9.1 nM. RIPK3-IN-1 inhibits RIPK1 and RIPK2 with IC50s of 5.5 and >10 μM. RIPK3-IN-1 is also a c-Met kinase inhibitor with an IC50 of 1.1 μM.
  • HY-10820A
    Pemetrexed disodium

    LY231514 disodium

    Antifolate Autophagy Apoptosis Cancer
    Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-117288A
    S55746 hydrochloride

    BLC201 (hydrochloride)

    Bcl-2 Family Cancer
    S55746 hydrochloride (BLC201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 hydrochloride (BLC201 hydrochloride) has antitumor activity with low toxicity.
  • HY-W008449
    1-Methylxanthine

    Endogenous Metabolite Cancer
    1-Methylxanthine, a caffeine derivative, is an essential human urinary metabolite of caffeine and theophylline (1,3-dimethylxanthine, TP). 1-Methylxanthine enhances the radiosensitivity of tumor cells.
  • HY-11079
    A-803467

    Sodium Channel Neurological Disease
    A 803467 is a selective Nav1.8 sodium channel blocker with an IC50 of 8 nM; over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.
  • HY-19981
    Derazantinib

    ARQ-087

    FGFR Cancer
    Derazantinib (ARQ-087) is an ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
  • HY-B1730
    Phensuximide

    Others Metabolic Disease Neurological Disease
    Phensuximide is an orally active succinimide antiepileptic and anticonvulsant agent. Phensuximide inhibits cyclic AMP and cyclic GMP accumulation in depolarized brain tissue. Phensuximide can be used for the study of seizure and petit mal.
  • HY-13016
    Cabozantinib

    XL184; BMS-907351

    VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
  • HY-117288
    S55746

    BLC201

    Bcl-2 Family Cancer
    S55746 (BLC201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BLC201) has antitumor activity with low toxicity.
  • HY-15404
    Darusentan

    Lu-135252

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Darusentan is a selective endothelin A (ETA) receptor antagonist. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki=13 nM.
  • HY-101549
    MRX-2843

    UNC2371

    FLT3 Cancer
    MRX-2843 (UNC2371) is an orally active dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively.
  • HY-13704
    SN-38

    NK012

    Topoisomerase ADC Cytotoxin Autophagy Cancer
    SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
  • HY-N2380
    N-Benzoyl-(2R,3S)-3-phenylisoserine

    Others Cancer
    N-Benzoyl-(2R,3S)-3-phenylisoserine is a Taxol C-13 Side Chain and crucial for the strong antitumor activity of Taxol.
  • HY-125166
    DB04760

    MMP Cancer Neurological Disease
    DB04760 (compound 4) is a potent, highly selective, non-zinc-chelating MMP-13 inhibitor with an IC50 of 8 nM. DB04760 significantly reduces paclitaxel neurotoxicity and has anticancer activity.
  • HY-11100
    Asenapine maleate

    Org 5222 maleate

    5-HT Receptor Neurological Disease
    Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.
  • HY-U00256
    ZD8321

    Elastase Inflammation/Immunology Cancer
    ZD8321 is a potent inhibitor of human Neutrophil elastase (NE) with a Ki of 13±1.7 nM.
  • HY-12280
    THZ2

    CDK Cancer
    THZ2 is a potent and selective CDK7 inhibitor with an IC50 of 13.9 nM.
  • HY-12653
    LDC4297

    CDK HSV Infection
    LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.
  • HY-12875
    BQU57

    Ras Cancer
    BQU57 shows selective inhibition for Ral relative to Ras or Rho and inhibit xenograft tumor growth similar to depletion of Ral by siRNA. The IC50 for BQU57 of 2.0 μM in H2122 and 1.3 μM in H358.
  • 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-130250
    SR-4835

    CDK Apoptosis Cancer
    SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.
  • HY-135250B
    Thalidomide-O-C6-NH2 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-O-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12 F36V and BET.
  • HY-P9926
    Dupilumab

    REGN-668; SAR-231893

    Interleukin Related Inflammation/Immunology
    Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis.
  • HY-135250
    Thalidomide-O-C6-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-O-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12 F36V and BET.
  • HY-136535
    hTrkA-IN-1

    Trk Receptor Inflammation/Immunology
    hTrkA-IN-1 is a potent and orally active inhibitor of TrkA kinase with an IC50 of 1.3 nM, compound 2. extracted from patent WO2015175788. hTrkA-IN-1 can be used for the study of inflammatory disease, such as prostatitis, pelvic, et al.
  • HY-112703
    AMG 333

    TRP Channel Neurological Disease Cardiovascular Disease
    AMG 333 is a potent and highly selective TRPM8 antagonist with an IC50 of 13 nM.
  • HY-P1595
    CREBtide

    PKA Metabolic Disease
    CREBtide, a synthetic 13 amino acid peptide, has been reported as a PKA substrate.
  • HY-50864
    GDC-0879

    Raf Cancer
    GDC-0879 is a potent and selective B-Raf inhibitor with an IC50 of 0.13 nM.
  • HY-102038
    PC786

    RSV Infection
    PC786 is an inhaled respiratory syncytial virus (RSV) L protein polymerase inhibitor. PC786 demonstrates potent antiviral activity against RSV-A (IC50 <0.09 to 0.71 nM) and RSV-B (IC50, 1.3 to 50.6 nM).
  • HY-117604
    THPP-1

    Phosphodiesterase (PDE) Neurological Disease
    THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
  • HY-108411
    Emedastine

    Histamine Receptor Inflammation/Immunology
    Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
  • HY-12044
    Cabozantinib S-malate

    XL184 S-malate; BMS-907351 S-malate

    VEGFR Apoptosis Cancer
    Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
  • HY-135250A
    Thalidomide-O-C6-NH2 TFA

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-O-C6-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12 F36V and BET.
  • HY-116819
    VU0453379

    Glucagon Receptor Metabolic Disease
    VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM.
  • HY-117970
    MMPI-1154

    MMP Cardiovascular Disease
    MMPI-1154 is a promising novel cardio-cytoprotective imidazole-carboxylic acid (ICA) MMP-2 inhibitor(IC50=6.6 μM) and can be used for the study of acute myocardial infarction. MMPI-1154 also inhibits the activity of MMP-13, MMP-1 and MMP-9 with IC50s of 1.8 μM,10 μM, and 13 μM, respectively.
  • HY-113974
    trans-AUCB

    t-AUCB

    Epoxide Hydrolase Cancer
    trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity.
  • HY-12753S1
    Debutyldronedarone D6 hydrochloride

    SR35021 D6 hydrochloride

    Others Cardiovascular Disease
    Debutyldronedarone D6 hydrochloride (SR35021 D6 hydrochloride) is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans. Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent.
  • HY-115446A
    Lenalidomide-C4-NH2 hydrochloride

    Cereblon ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively.
  • HY-N1753
    3-(4-Hydroxyphenyl)-1-propanol

    Dihydro-p-coumaryl alcohol; 3-(p-Hydroxyphenyl)propyl alcohol

    Others Others
    3-(4-Hydroxyphenyl)-1-propanol is used in the synthesis of (-)-centrolobine.
  • HY-U00411
    PSN-GK1

    Glucokinase Metabolic Disease
    PSN-GK1 is a potent glucokinase activator with an EC50 of 0.13 μM.
  • HY-B0852
    Tebuconazole

    Cytochrome P450 Fungal Infection
    Tebuconazole is an agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively.
  • HY-13816
    NU6027

    CDK ATM/ATR Cancer
    NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 µM and 1.3 µM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.
  • HY-12753S
    Debutyldronedarone D7

    SR35021 D7

    Others Cardiovascular Disease
    Debutyldronedarone D7 (SR35021 D7) is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans.Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent.
  • HY-B2178
    Emedastine difumarate

    Histamine Receptor Inflammation/Immunology
    Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
  • HY-103254
    ML221

    Others Neurological Disease
    ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
  • HY-103460
    IRL 2500

    Endothelin Receptor Cardiovascular Disease
    IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
  • HY-15335
    Nutlin-3b

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    Nutlin-3b is a p53/MDM2 inhibitor with an IC50 of 13.6 μM. Nutlin-3b is 150 times less potent in binding to MDM2 than Nutlin-3a.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-16321
    Micafungin sodium

    FK 463 sodium

    Fungal Antibiotic Infection
    Micafungin sodium (FK 463 sodium) is an antifungal agent which inhibits 1, 3-beta-D-glucan synthesis.
  • HY-10483
    SCH-1473759 hydrochloride

    Aurora Kinase Cancer
    SCH-1473759 hydrochloride is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively.
  • HY-10179
    Danusertib

    PHA-739358

    Aurora Kinase Autophagy Cancer
    Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
  • HY-10482
    SCH-1473759

    Aurora Kinase Cancer
    SCH-1473759 is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively.
  • HY-10015
    PAP-1

    5-(4-Phenoxybutoxy)psoralen

    Potassium Channel Inflammation/Immunology
    PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects.
  • HY-N1454
    Apigenin-7-glucuronide

    Apigenin 7-O-glucuronide

    MMP Cancer
    Apigenin-7-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 12.87, 22.39, 17.52, 0.27 μM for MMP-3, MMP-8, MMP-9, MMP-13, respectively.
  • HY-12068
    PI3K-IN-1

    XL-147 derivative 1

    PI3K Cancer
    PI3K-IN-1 (XL-147 derivative 1) is a potent inhibitor of PI3K. PI3K-IN-1 (25 μM) blocks PI3K/Akt signaling pathways.
  • HY-W013014
    3-Methyl-2-cyclopenten-1-one

    Endogenous Metabolite Metabolic Disease
    3-Methyl-2-cyclopenten-1-one is an endogenous metabolite.
  • HY-114460
    SHP2 IN-1

    Phosphatase Others
    SHP2 IN-1 (compound 13) is an allergic inhibitor of SHP2 (PTPN11), with an IC50 of 3 nM.
  • HY-12635
    SP2509

    Histone Demethylase Apoptosis Cancer
    SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with IC50 of 13 nM.
  • HY-W013035
    3-Methyl-2-buten-1-ol

    Endogenous Metabolite Metabolic Disease
    3-Methyl-2-buten-1-ol is an endogenous metabolite.
  • HY-113527
    3-Carbamoyl-1-methylpyridin-1-ium chloride

    Endogenous Metabolite Metabolic Disease
    3-Carbamoyl-1-methylpyridin-1-ium chloride is an endogenous metabolite.
  • HY-B0134B
    Bestatin trifluoroacetate

    Ubenimex trifluoroacetate

    Aminopeptidase Bacterial Antibiotic Cancer Infection
    Bestatin trifluoroacetate is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer treatment.
  • HY-13873
    IKK-IN-1

    IKK Inflammation/Immunology
    IKK-IN-1 is an inhibitor of IKK extracted from patent WO2002024679A1, compound example 18-13.
  • HY-B0134A
    Bestatin hydrochloride

    Ubenimex hydrochloride

    Aminopeptidase Bacterial Antibiotic Cancer Infection
    Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer treatment.
  • HY-111506
    Aurora inhibitor 1

    Aurora Kinase Cancer
    Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, respectively.
  • 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-117145
    Thiophene-2

    TP2

    Bacterial Infection
    Thiophene-2 (TP2) is a specific polyketide synthase 13 (Pks13) inhibitor. Thiophene-2 inhibits mycolic acid biosynthesis and rapidly leads to mycobacterial cell death. Thiophene-2 is active against Mycobacterium tuberculosis with a MIC value of 1 μM, and has potent anti-tuberculosis activity.
  • HY-114404
    SJFα

    PROTAC p38 MAPK Autophagy Cancer
    SJFα is a 13-atom linker PROTAC. SJFα degrades p38α with a DC50 of 7.16  nM, but is far less effective at degrading p38δ (DC50=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 µM.
  • HY-112154
    CXCR7 modulator 2

    CXCR Cardiovascular Disease Endocrinology
    CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), with a Ki of 13 nM.
  • HY-100739
    RA190

    Proteasome Cancer
    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
  • HY-16107
    BMS-303141

    ATP Citrate Lyase Metabolic Disease
    BMS-303141 is a potent, cell-permeable ATP-citrate lyase (ACL) inhibitor with an IC50 of 0.13 μM.
  • HY-109020
    Acrizanib

    VEGFR Others
    Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR.
  • HY-16696
    SN 2

    TRP Channel Others
    SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8±0.13 μM.
  • HY-101143
    PGMI-004A

    Phosphatase Cancer
    PGMI-004A is a potent phosphoglycerate mutase 1 (PGAM1) inhibitor with an IC50 of 13.1 μM.
  • HY-14731
    VE-821

    ATM/ATR Cancer
    VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
  • 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-15536
    Cebranopadol

    GRT6005

    Opioid Receptor Neurological Disease
    Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.
  • HY-136072
    QPX7728-OH disodium

    Bacterial Infection
    QPX7728-OH disodium (compound 13) is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 13. QPX7728-OH disodium inhibits cleavage of Nitrocefin (HY-108913) by purified class A, C and D enzymes, with Kis less than 0.1 µΜ.
  • HY-101698
    Alniditan

    Alnitidan

    5-HT Receptor Neurological Disease
    Alniditan is a potent 5-HT1B/1D receptors agonist, with IC50 of 1.7 and 1.3 nM in HEK 293 cells, and pKi value of 8.96 and 9.40 for 5-HT1B/1D receptors, respectively.
  • HY-18773
    Oct3/4-inducer-1

    Oct3/4 Inflammation/Immunology
    Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer. Oct3/4-inducer-1 promotes expression and stabilization of Oct3/4, and enhances its transcriptional activity in diverse human somatic cells.
  • HY-16567
    Asenapine hydrochloride

    5-HT Receptor Dopamine Receptor Neurological Disease
    Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
  • HY-N1463
    Luteolin 7-O-glucuronide

    Luteolin 7-glucuronide

    MMP Others
    Luteolin 7-O-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 17.63, 7.99, 11.42, 12.85, 0.03 μM for MMP-1, MMP-3, MMP-8, MMP-9, MMP-13, respectively.
  • HY-W012126
    2,6-Dichlorodiphenylamine

    2,6-Dichloro-N-phenylaniline

    Bacterial Cancer Infection
    2,6-Dichlorodiphenylamine is an analogue of Diclofenac Sodium (HY-15037) and has anti-Candida albicans activity. Diclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells.
  • 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-100131
    GSK481

    RIP kinase Inflammation/Immunology
    GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser 166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM.
  • HY-19544
    JAK3-IN-1

    JAK Cancer
    JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
  • HY-100658
    Didesmethyl cariprazine

    5-HT Receptor Dopamine Receptor Neurological Disease
    Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic drug candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor.
  • HY-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-N7363
    Isolongifolene

    (-)-Isolongifolene

    Others Cancer Inflammation/Immunology Neurological Disease
    Isolongifolene ((-)-Isolongifolene) is a tricyclic sesquiterpene isolated from Murraya koenigii. Isolongifolene attenuates Rotenone-induced oxidative stress, mitochondrial dysfunction and apoptosis through the regulation of P13K/AKT/GSK-3β signaling pathways. Isolongifolene has antioxidant, anti-inflammatory, anticancer and neuroprotective properties.
  • HY-124738
    BI 01383298

    Sodium Channel Metabolic Disease
    BI 01383298 is a potent inhibitor of the sodium-citrate co-transporter (SLC13A5) that is highly expressed in the liver.
  • HY-13452
    CID-1067700

    ML282

    Ras Inflammation/Immunology
    CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
  • HY-19775
    GNE-6468

    ROR Inflammation/Immunology
    GNE-6468 is a potent and selective RORγ(RORc) agonists with an EC50 value of 13 nM for HEK-293 cell.
  • 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-19120
    KB-5492 anhydrous

    Sigma Receptor Inflammation/Immunology
    KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent.
  • HY-112801
    F-1

    ALK ROS Cancer
    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively.
  • HY-P1978
    CysHHC10

    Bacterial Infection
    CysHHC10 is a synthetic antimicrobial peptide (AMP), and exhibits strong anti-microbial properties against both Gram-positive and Gram-negative bacteria. The MIC values of CysHHC10 against E. coli, P. aeruginosa, S. aureus and S. epidermidis are 10.1 mM, 20.2 mM, 2.5 mM and 1.3 mM, respectively.
  • HY-109523
    Cerivastatin sodium

    HMG-CoA Reductase (HMGCR) Ferroptosis Cancer Cardiovascular Disease
    Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.
  • HY-15610
    GDC-0623

    RG 7421; MEK inhibitor 1

    MEK Apoptosis Cancer
    GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
  • HY-129458
    Cerivastatin

    HMG-CoA Reductase (HMGCR) Ferroptosis Cancer Cardiovascular Disease
    Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.
  • HY-15736
    Sodium Channel inhibitor 1

    Sodium Channel Neurological Disease
    Sodium Channel inhibitor1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.
  • HY-111365
    TES-1025

    Others Metabolic Disease
    TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13 nM.
  • HY-101565
    AMG-176

    Bcl-2 Family Cancer
    AMG-176 is a potent, selective and orally active MCL-1 inhibitor, with a Ki of 0.13 nM.
  • HY-101921
    PI3Kδ-IN-1

    PI3K Inflammation/Immunology
    PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.
  • 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-15491
    AG-024322

    COX Cancer
    AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis.
  • HY-112055
    DIM-C-pPhOH

    Apoptosis Cancer
    DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
  • HY-101121
    NI-42

    Epigenetic Reader Domain Cancer
    NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins.
  • HY-124634
    PZ-2891

    Others Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
  • HY-19485
    XL-784

    MMP Cardiovascular Disease
    XL-784 is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively.
  • HY-19801
    CVT-10216

    Aldehyde Dehydrogenase (ALDH) Neurological Disease
    CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.
  • HY-B0011
    Docetaxel

    RP-56976

    Microtubule/Tubulin Apoptosis Endogenous Metabolite Cancer
    Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity.
  • 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-P1978A
    CysHHC10 TFA

    Bacterial Infection
    CysHHC10 TFA is a synthetic antimicrobial peptide (AMP), and exhibits strong anti-microbial properties against both Gram-positive and Gram-negative bacteria. The MIC values of CysHHC10 TFA against E. coli, P. aeruginosa, S. aureus and S. epidermidis are 10.1 mM, 20.2 mM, 2.5 mM and 1.3 mM, respectively.
  • HY-B1604
    Chloroprocaine hydrochloride

    2-Chloroprocaine hydrochloride

    Na+/K+ ATPase Neurological Disease
    Chloroprocaine hydrochloride (2-Chloroprocaine hydrochloride) is a potent inhibitor of Na,K-ATPase activity with an IC50 of 13 mM. Chloroprocaine hydrochloride blocks peripheral nerve.
  • HY-102075B
    TMP780

    ROR Inflammation/Immunology
    TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.
  • HY-19713
    LJI308

    Ribosomal S6 Kinase (RSK) Cancer
    LJI308 is a new and potent pan-RSK inhibitor, with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.
  • HY-109044
    Tapinarof

    GSK2894512; Benvitimod; WBI 1001

    Aryl Hydrocarbon Receptor Inflammation/Immunology
    Tapinarof (GSK2894512) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.
  • HY-U00231
    KF 13218

    Prostaglandin Receptor Cardiovascular Disease Endocrinology
    KF 13218 is a potent, selective and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.
  • HY-103618
    THZ531

    CDK Cancer
    THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.
  • 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-100383
    BH3I-1

    BHI1; BH 3I1

    Bcl-2 Family MDM-2/p53 E1/E2/E3 Enzyme Cancer
    BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
  • HY-136153
    Amphotericin X1

    Fungal Infection
    Amphotericin X1 is an 13-O-methyl derivative of Amphotericin B with good antifungal activity. Amphotericin X1 inhibits Candida albicans 33/079, C.parapsilosis 937A, Cryptococcus neoformans 451, Aspergillus niger 57A and A.fumigatus with MIC values of 1 μg/mL, 8 μg/mL, 1 μg/mL, 2 μg/mL and 2 μg/mL, respectively.
  • HY-126010
    Dooku1

    Others Cardiovascular Disease
    Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca 2+-entry with IC50 values of 1.3 μM (in HEK 293 cells) and 1.5 μM (in HUVECs). Dooku1 inhibits Yoda1-induced relaxation of aorta.
  • HY-112160
    XL-784 free base

    MMP Cardiovascular Disease
    XL-784 free base is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively.
  • HY-78131
    Ibuprofen

    (±)-Ibuprofen

    COX Inflammation/Immunology Cancer
    Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-107379
    AKR1C3-IN-1

    Others Others
    AKR1C3-IN-1 is a potent, highly selective inhibitor of AKR1C3, with an IC50 of 13 nM.
  • HY-W020215
    Tricarballylic acid

    Mitochondrial Metabolism Inflammation/Immunology
    Tricarballylic acid, a conjugate acid of a tricarballylate, is a competitive inhibitor of the enzyme aconitate hydratase (aconitase; EC 4.2.1.3) with a Ki value of 0.52 mM.
  • HY-N4320
    3-​Feruloyl-​1-​Sinapoyl sucrose

    Others Others
    3-Feruloyl-1-Sinapoyl sucrose (compound 1) is a glycoside isolated from the aerial parts of Polygala chamaebuxus.
  • HY-10458
    PF-562271 besylate

    PF562271 besylate; PF 562271 besylate

    FAK Pyk2 Cancer
    PF-562271 besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.
  • HY-U00117
    Lusaperidone

    R107474

    Adrenergic Receptor Neurological Disease Endocrinology
    Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.
  • HY-15719
    NU 7026

    LY293646

    DNA-PK Apoptosis Cancer
    NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.
  • HY-128661
    IDH1 Inhibitor 2

    Isocitrate Dehydrogenase (IDH) Metabolic Disease
    IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM.
  • HY-12168
    Tanomastat

    BAY 12-9566

    MMP Cancer
    Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models.
  • HY-19834
    Fenebrutinib

    GDC-0853

    Btk Cancer
    Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.
  • HY-11109
    Resatorvid

    TAK-242; CLI-095

    Toll-like Receptor (TLR) TNF Receptor Interleukin Related Autophagy Inflammation/Immunology Cancer
    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-R and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.
  • HY-112804
    SGC-iMLLT

    Epigenetic Reader Domain Cancer
    SGC-iMLLT is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC50 of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with Kds of 0.129 and 0.077 μM, respectively.
  • HY-12270
    T-5224

    MMP Others
    T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
  • HY-P1432
    K-(D-1-Nal)-FwLL-NH2

    GHSR
    K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-B0011A
    Docetaxel Trihydrate

    RP-56976 Trihydrate

    Microtubule/Tubulin Apoptosis Cancer
    Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis.
  • HY-130258
    LC3-mHTT-IN-AN1

    Autophagy Neurological Disease
    LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN1 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
  • HY-104065
    Pyrotinib

    SHR-1258

    EGFR Cancer
    Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
  • HY-13967
    AMG 837

    GPR40 Metabolic Disease
    AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
  • HY-11006
    KU-57788

    NU7441

    DNA-PK CRISPR/Cas9 Cancer
    KU-57788 is a potent and selective inhibitor of DNA-PK with an IC50 of 13 nM, with selectivity over a range of kinases including mTOR, PI 3-K, ATM and ATR.
  • HY-15542A
    FRAX597

    PAK Cancer
    FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
  • HY-13245
    PF-4136309

    INCB8761

    CCR Inflammation/Immunology Endocrinology
    PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
  • HY-10459
    PF-562271

    FAK Pyk2 Cancer
    PF-562271 is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.
  • HY-13967A
    AMG 837 sodium salt

    GPR40 Metabolic Disease
    AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
  • HY-112522A
    HS80

    Fatty Acid Synthase (FASN) Cancer
    HS-80 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-80 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 7.13 μM.
  • HY-100733
    4E2RCat

    Eukaryotic Initiation Factor (eIF) Autophagy Virus Protease Neurological Disease
    4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

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

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-P1432A
    K-(D-1-Nal)-FwLL-NH2 TFA

    GHSR
    K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-111552
    PIM1-IN-1

    Pim Cancer
    PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity.
  • HY-U00444
    DDR1-IN-2

    Discoidin Domain Receptor Inflammation/Immunology
    DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM.
  • HY-P1749
    Influenza HA (307-319)

    Influenza Virus Infection
    Influenza HA (307-319) is 13 amino acids 307 to 319 fragment of Influenza HA. Influenza HA is a glycoprotein found on the surface of influenza viruses.
  • HY-128352
    SMYD3-IN-1

    Histone Methyltransferase Cancer
    SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM.
  • HY-14894
    Ipragliflozin

    ASP1941

    SGLT Metabolic Disease
    Ipragliflozin (ASP1941) is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
  • HY-112737
    LY223982

    CGS23131; SKF107324

    Leukotriene Receptor Inflammation/Immunology
    LY223982 is a potent and specific inhibitor of leukotriene B4 receptor, with an IC50 of 13.2 nM against [ 3H]LTB4 binding to LTB4 receptor.
  • HY-13967B
    AMG 837 calcium hydrate

    GPR40 Metabolic Disease
    AMG 837 calcium hydrate is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
  • HY-100325
    NHE3-IN-1

    Sodium Channel Neurological Disease
    NHE3-IN-1 is a sodium/proton exchanger type 3 (NHE-3) inhibitor extracted from patent WO 2011019784 A1.
  • HY-B1270
    Isoxsuprine hydrochloride

    Adrenergic Receptor iGluR Neurological Disease Endocrinology
    Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
  • HY-14894A
    Ipragliflozin L-Proline

    SGLT Metabolic Disease
    Ipragliflozin (L-Proline) is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
  • HY-129057
    2',5-Difluoro-2'-deoxycytidine

    HCV Infection
    2',5-Difluoro-2'-deoxycytidine, compound 13, has potent anti-HCV activity and toxicity to ribosomal RNA (rRNA).
  • HY-15036
    Diclofenac

    COX Apoptosis Inflammation/Immunology
    Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-P1280
    Margatoxin

    Potassium Channel Neurological Disease
    Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research.
  • HY-15038
    Diclofenac potassium

    COX Apoptosis Inflammation/Immunology
    Diclofenac potassium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac potassium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • 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-15716
    Kobe0065

    Ras Apoptosis Cancer
    Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
  • HY-103464
    5'-Fluoroindirubinoxime

    5'-FIO

    FLT3 Cancer
    5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
  • HY-12090
    Anacetrapib

    MK-0859

    CETP Cardiovascular Disease
    Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.
  • HY-12469
    Decernotinib

    VX-509; VRT-831509

    JAK Inflammation/Immunology
    Decernotinib is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively.
  • HY-112066
    SHIN1

    RZ-2994

    Others Cancer
    SHIN1 (RZ-2994) is a human serine hydroxymethyltransferse 1 and 2 (SHMT1/2) inhibitor with IC50s of 5 and 13 nM, respectively, in an in vitro assay.
  • HY-104065B
    Pyrotinib dimaleate

    SHR-1258 dimaleate

    EGFR Cancer
    Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
  • 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-15036A
    Diclofenac diethylamine

    COX Apoptosis Inflammation/Immunology
    Diclofenac diethylamine is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-15342
    Timapiprant

    OC000459

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant (OC000459) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils.
  • HY-107625A
    SNAP 94847 hydrochloride

    MCHR1 (GPR24) Neurological Disease
    SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
  • HY-15342A
    Timapiprant sodium

    OC000459 sodium

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils.
  • HY-107625
    SNAP 94847

    MCHR1 (GPR24) Neurological Disease Endocrinology
    SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
  • HY-15037
    Diclofenac Sodium

    GP 45840

    COX Apoptosis Inflammation/Immunology
    Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-109067
    Opiranserin

    GlyT 5-HT Receptor P2X Receptor Neurological Disease
    Opiranserin, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.
  • HY-100398
    PF-04979064

    PI3K mTOR Cancer
    PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
  • HY-B0790
    TAI-1

    Apoptosis Cancer
    TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.
  • HY-136073
    Wnt pathway activator 2

    Wnt Cancer
    Wnt pathway activator 2 is a potent Wnt activator extracted from patent WO2012024404A1, compound 2, has an IC50s of 13 nM.
  • HY-136567
    TBAP-001

    Raf Cancer
    TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay.
  • 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-112219A
    H3R-IN-1 Hydrochloride

    Histamine Receptor Inflammation/Immunology Endocrinology
    H3R-IN-1 Hydrochloride is a histamine receptor 3 (H3R) inverse agonist extracted from patent WO2013107336A1, compound example 2.
  • HY-12990
    Spautin-1

    Autophagy Apoptosis Cancer
    Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.
  • HY-78131S
    Ibuprofen D3

    (±)-Ibuprofen D3

    COX Inflammation/Immunology
    Ibuprofen D3 is a deuterium labeled Ibuprofen. Ibuprofen is a COX-1 and COX-2 inhibitor with IC50s of 13 μM and 370 μM.
  • HY-18603
    FIIN-3

    EGFR FGFR Cancer
    FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
  • HY-112145
    FLT3-IN-3

    FLT3 Cancer
    FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.
  • HY-10013
    Taranabant

    MK-0364

    Cannabinoid Receptor Metabolic Disease
    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
  • HY-15166
    SB1317

    TG02

    CDK JAK FLT3 Cancer
    SB1317 is a potent inhibitor of CDK2, JAK2, and FLT3 for the treatment of cancer, with IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.
  • HY-117977
    FCPR03

    Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease
    FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effects.
  • HY-105231
    Bryostatin 1

    PKC HIV Cancer Infection Inflammation/Immunology Neurological Disease
    Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties.
  • HY-100719
    BRD-6929

    HDAC HIV Infection Cardiovascular Disease
    BRD-6929 (Cpd-60) is a brain-penetrant, selective inhibitor of HDAC1 and HDAC2 (IC50= 1 and 8 nM), extracted from patent US2018360927. BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively. BRD-6929 (TPB) potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1.
  • HY-135887
    ZX-29

    ALK Apoptosis Autophagy Cancer
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
  • 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.
  • 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-114396
    BR351

    MMP Cancer
    BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively.
  • HY-111468
    Mcl1-IN-3

    Bcl-2 Family Cancer
    Mcl1-IN-3 is an inhibitor of Mcl1 extracted from patent WO2015153959A2, compound example 57; has an IC50 and Ki of 0.67 and 0.13 μM, respectively.
  • HY-12030
    PIK-90

    PI3K DNA-PK Cancer
    PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
  • HY-B0662
    Imidafenacin

    KRP-197; ONO-8025

    mAChR Neurological Disease
    Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).
  • 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-50943
    AT7519 Hydrochloride

    CDK Apoptosis Cancer
    AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
  • HY-12593
    GS967

    Sodium Channel Cardiovascular Disease
    GS967 (GS-458967) is a potent, and selective inhibitor of cardiac late sodium current (late INa ) with IC50 values of 0.13 and 0.21 μM for ventricular myocytes and isolated hearts, respectively.
  • HY-50940
    AT7519

    CDK Apoptosis Cancer
    AT7519 as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
  • HY-10644
    Lck inhibitor 2

    Src Inflammation/Immunology
    Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively
  • HY-50940A
    AT7519 trifluoroacetate

    CDK Cancer
    AT7519 trifluoroacetate as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
  • HY-15790
    Elobixibat

    A 3309; AZD 7806

    Others Metabolic Disease
    Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
  • HY-123601
    DHQZ 36

    Parasite Infection
    DHQZ 36 is a potent inhibitor of retrograde trafficking. DHQZ 36 inhibits Leishmania amazonensis infection in macrophages with an EC50 of 13.63 μM. DHQZ 36 has potent anti-parasite activity.
  • HY-P1596
    Gluten Exorphin C

    Opioid Receptor Neurological Disease
    Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.
  • HY-16962A
    CC-115 hydrochloride

    DNA-PK mTOR Cancer
    CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
  • HY-18937
    WEHI-345

    RIP kinase Cancer
    WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.
  • HY-B0744C
    L-Eflornithine

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

    Others Cancer
    L-Eflornithine (L-DFMO) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min -1.
  • HY-16962
    CC-115

    DNA-PK mTOR Cancer
    CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
  • HY-126121
    2-Hydroxy Ibuprofen

    (±)-2-Hydroxy Ibuprofen

    COX Cancer Inflammation/Immunology
    2-Hydroxy Ibuprofen is a metabolite of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-112218
    MIK665

    S-64315

    Bcl-2 Family Cancer
    MIK665 (S-64315) is a special Mcl-1 inhibitor extracted from patent WO2016207225A1, compound Preparation 13, has an IC50 of 1.81 nM.
  • HY-10244
    MK-0608

    HCV Infection
    MK-0608 is a potent and orally bioavailable inhibitor of HCV replication in vitro with an EC50 of 0.3 μM (EC90=1.3 μM) in the subgenomic-replicon assay.
  • HY-P1218
    Phrixotoxin 3

    Sodium Channel Neurological Disease
    Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
  • HY-P1218A
    Phrixotoxin 3 TFA

    Sodium Channel Neurological Disease
    Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
  • HY-131061
    BET bromodomain inhibitor 1

    Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
  • 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.
  • HY-131259
    Ibuprofen Impurity F

    COX Inflammation/Immunology
    Ibuprofen Impurity F is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-P0289
    CEF3

    Influenza Virus Infection
    CEF3 (SIIPSGPLK) corresponds to aa 13-21 of the influenza A virus M1 protein. The matrix (M1) protein of influenza A virus is a multifunctional protein that plays essential structural and functional roles in the virus life cycle.
  • HY-U00201
    KRN4884

    Potassium Channel Cardiovascular Disease
    KRN4884 is a K + channel opener. In the presence of intracellular ATP (1 mM), KRN4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM).
  • HY-P1296
    Urocortin, rat

    Urocortin (Rattus norvegicus); Rat urocortin

    CRFR Neurological Disease Endocrinology
    Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF and mouse CRF, respectively.
  • HY-80013A
    THZ1 Hydrochloride

    CDK Cancer
    THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • HY-N6649
    Isotanshinone I

    Glucosidase Infection
    Isotanshinone I has inhibitory activity against α-glucosidase and formation of AGE, with IC50s of 1.13 μM and 0.432 μM for α-glucosidase and AGE, respectively.
  • HY-131258
    Ibuprofen impurity 1

    COX Inflammation/Immunology
    Ibuprofen impurity 1 is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-131260
    Ibuprofen Impurity K

    COX Inflammation/Immunology
    Ibuprofen Impurity K is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-10875
    LRRK2-IN-1

    LRRK2 Apoptosis Neurological Disease Cancer
    LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.
  • HY-14305A
    BMS-582949 hydrochloride

    p38 MAPK Autophagy Inflammation/Immunology
    BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.
  • HY-80013
    THZ1

    CDK Cancer
    THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • 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-125801
    3-Oxo-5β-cholanoic acid

    Dehydrolithocholic acid; 3-oxoLCA

    ROR Inflammation/Immunology
    3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
  • HY-B0744D
    L-Eflornithine monohydrochloride

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

    Others Cancer
    L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min -1.
  • HY-121832
    DDX3-IN-1

    HIV HCV Infection
    DDX3-IN-1 (Compound 16f) is a DEAD-box polypeptide 3 (DDX3) inhibitor with CC50s of 50 and 36 μM for HIV and HCV, respectively. Antiviral activity.
  • HY-12433
    BMS-819881

    MCHR1 (GPR24) Cytochrome P450 Metabolic Disease Endocrinology
    BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM. BMS-819881 also is selective and potent for CYP3A4 activity with an EC50 of 13 μM.
  • HY-109053
    Delgocitinib

    JTE-052

    JAK Inflammation/Immunology
    Delgocitinib (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
  • HY-114208
    BI-9321

    Histone Methyltransferase Cancer
    BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
  • HY-110105
    NS8593 hydrochloride

    Potassium Channel Neurological Disease
    NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
  • HY-108672
    NF157

    P2Y Receptor Inflammation/Immunology
    NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).
  • HY-114208A
    BI-9321 trihydrochloride

    Histone Methyltransferase Cancer
    BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
  • HY-118152
    Org-12962

    5-HT Receptor Neurological Disease
    Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.
  • HY-101198
    Clobenpropit dihydrobromide

    Histamine Receptor Cancer Neurological Disease
    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
  • HY-111545
    BSc5371

    FLT3 Cancer
    BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines.
  • HY-N2503
    Ginsenoside F4

    Apoptosis MMP Inflammation/Immunology
    Ginsenoside F4 (GF4), ginseng saponinis, isolated from notoginseng or red ginseng. Ginsenoside F4 (GF4) has inhibitory effect on human lymphocytoma JK cell by inducing its apoptosis. Ginsenoside F4 (GF4) inhibits matrix metalloproteinase 13 (MMP 13) expression in IL-1β-treated chondrocytes and blocks cartilage breakdown in rabbit cartilage tissue culture, shows therapeutic potential for preventing cartilage collagen matrix breakdown in diseased tissues.
  • HY-12871
    Atuveciclib Racemate

    BAY-1143572 Racemate

    CDK Cancer
    Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
  • HY-10398
    CTS-1027

    Ro 1130830; RS 130830

    MMP Cancer
    CTS-1027 is a potent small molecule inhibitor of MMPs, with IC50s of 0.3 nM, 0.5 nM for MMP2, MMP13, respectively, and has > 1,000 fold selectivity over MMP1.
  • HY-127170
    3-Hydroxycoumarin

    Others Others
    3-hydroxycoumarin is a potent and redox inhibitor of human 15-LOX-1. 3-hydroxycoumarin is recently demonstrated to protect sea urchin reproductive cells against ultraviolet B damage.
  • HY-133122
    UCB-9260

    TNF Receptor Inflammation/Immunology
    UCB-9260, an orally active compound, inhibits TNF signalling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar Kd of 13 nM.
  • HY-P1296A
    Urocortin, rat TFA

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

    CRFR Endocrinology Neurological Disease
    Urocortin, rat TFA (Urocortin (Rattus norvegicus) TFA) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF and mouse CRF, respectively.
  • HY-15573
    EI1

    KB-145943

    Histone Methyltransferase Apoptosis Cancer
    EI1 (KB-145943) is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
  • HY-101032
    RIPA-56

    RIP kinase Inflammation/Immunology
    RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM. RIPA-56 can be used for the treatment of systemic inflammatory response syndrome.
  • 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-12871B
    Atuveciclib

    BAY-1143572

    CDK Cancer
    Atuveciclib (BAY-1143572) is a potent and highly selective, oral PTEFb/CDK9 inhibitor. Atuveciclib (BAY-1143572) inhibits CDK9/CycT1 with an IC50 of 13 nM.
  • HY-10205
    Cediranib

    AZD2171

    VEGFR Autophagy PDGFR Cancer
    Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  • 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-100781A
    L-APB

    L-AP 4

    mGluR Neurological Disease
    L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
  • HY-13308
    Regorafenib Hydrochloride

    BAY73-4506 hydrochloride

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-115502
    BCI

    (E)-BCI

    Phosphatase Cancer Inflammation/Immunology
    BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.
  • HY-100548
    GSK621

    AMPK Autophagy Apoptosis Cancer
    GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
  • HY-13049
    Cediranib maleate

    AZD-2171 maleate

    VEGFR Autophagy PDGFR Cancer
    Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  • HY-103436
    NSC624206

    E1/E2/E3 Enzyme Cancer
    NSC624206 is an inhibitor of ubiquitin E1 (UBA1), with an IC50 of ~9 μM. NSC624206 specifically blocks ubiquitin-thioester formation (IC50=13 μM) but has no effect on ubiquitin adenylation.
  • HY-19312
    3-Methyladenine

    3-MA

    PI3K Autophagy Mitophagy Endogenous Metabolite Cancer
    3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K.
  • 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-10122
    Silodosin

    KAD 3213; KMD 3213

    Adrenergic Receptor Cancer Endocrinology
    Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.
  • 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-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-W011053
    Neotame

    Others Others
    Neotame is a derivative of Aspartame and is a low-caloric and high-intensity artificial sweetener that is 7000-13,000 times sweeter than sugar. Neotame is a non-nutritive sweetener and flavor enhancer that can be used in a variety of foods.
  • HY-111950
    (-)-Ibuprofenamide

    (R)-Ibuprofenamide

    Others Inflammation/Immunology
    (-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-111234
    IDO-IN-11

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-11 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50s of 0.18 μM (Kinase) and 0.014 μM (Hela Cell), extracted from patent WO 2016041489 A1, compound 13.
  • HY-N4119
    Neoeriocitrin

    AChE Neurological Disease
    Neoeriocitrin, isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor.
  • HY-103632
    PROTAC BRD9 Degrader-1

    PROTAC Epigenetic Reader Domain Cancer
    PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.
  • HY-N2821
    (+)-Afzelechin

    Glucosidase Metabolic Disease
    (+)-Afzelechin, isolated from rhizomes of Bergenia ligulata, is an alpha-glucosidase activity inhibitor with an ID50 (50% inhibition dose) value of 0.13 mM. (+)-Afzelechin can delay the absorption of carbohydrates in food to suppress postprandial hyperglycemia and hyperinsulinemia.
  • HY-12429
    Beclabuvir

    BMS-791325

    HCV Infection
    Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM. 
  • HY-10331A
    Regorafenib monohydrate

    BAY 73-4506 monohydrate

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib monohydrate is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-43586
    BR351 precursor

    MMP Cancer
    BR351 precursor is a precursor of BR351. BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively.
  • 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-115502A
    BCI hydrochloride

    (E)-BCI hydrochloride

    Phosphatase Cancer Inflammation/Immunology
    BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI hydrochloride specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5.
  • HY-U00287
    BACE-IN-1

    Beta-secretase Neurological Disease
    BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease.
  • 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-108648
    2-Methylthioadenosine diphosphate trisodium

    2-Methylthio-ADP trisodium

    P2Y Receptor Neurological Disease
    2-Methylthioadenosine diphosphate trisodium is a potent purinergic P2Y receptors agonist, with EC50s of 19, 6.2, and 5 nM for human P2Y13, mouse P2Y13 and human P2Y12, respectively. 2-Methylthioadenosine diphosphate trisodium has pEC50s of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. 2-Methylthioadenosine diphosphate trisodium induces platelet aggregation and shape change, and inhibits cyclic AMP accumulation in platelets exposed to prostaglandin E1.
  • HY-N7041
    11-Oxomogroside IIa

    HSV Infection
    11-Oxomogroside IIa (11-oxomogroside II A1) is a cucurbitane glycoside extracted from the fruits of Siraitia grosVenorii. 11-Oxomogroside IIa has inhibitory effects against the Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), shows weak inhibitory effects on activation of (+/-)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexemide (NOR 1), a nitric oxide (NO) donor.
  • HY-N6840
    Xylotetraose

    Others Others
    Xylotetraose is a hydrolysis product of Xylan. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose. Xylotetraose can be used for enzyme biochemical analysis.
  • HY-130603
    DCZ0415

    NF-κB Apoptosis Cancer
    DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.
  • HY-126130
    LysRs-IN-2

    Aminoacyl-tRNA Synthetase Infection
    LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively.
  • HY-15897
    LDN-212854

    TGF-β Receptor Cancer
    LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.
  • HY-107457
    AZD-8529

    mGluR Neurological Disease
    AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-10331
    Regorafenib

    BAY 73-4506

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
  • HY-109619
    D4-abiraterone

    Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite

    Androgen Receptor Cytochrome P450 Cancer
    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
  • 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-N2350
    Cynaropicrin

    MMP NF-κB TNF Receptor Cancer
    Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
  • HY-12678
    Entrectinib

    NMS-E628; RXDX-101

    ROS Trk Receptor ALK Autophagy Cancer
    Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.
  • HY-130122
    MG-277

    PROTAC Apoptosis Cancer
    MG-277 is a molecular glue compound transformed from PROTAC degradation agent. MG-277 induces moderate MDM2 degradation. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. MG-277 effectively induces degradation of a translation termination factor, GSPT1, with a DC50 of 1.3 nM. MG-277 has potent anticancer activity.
  • HY-111400
    SR-4370

    HDAC Cancer
    SR-4370 is an inhibitor of HDAC, with IC50s of 0.13 μM, 0.58 μM, 0.006 μM, 2.3 μM, and 3.4 μM for HDAC1, HDAC2, HDAC3, HDAC8, and HDAC6, respectively.
  • HY-114177
    PF-06873600

    CDK Cancer
    PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. PF-06873600 has potential antineoplastic activity.
  • HY-135666
    DHODH-IN-8

    Parasite Dihydroorotate Dehydrogenase DNA/RNA Synthesis Infection
    DHODH-IN-8 (Compound 27) is an inhibitor of human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) with IC50s of 0.13 μM and 47.4 μM, and Kis of 0.016 μM and 5.6 μM, respectively. DHODH-IN-8 has antimalarial activity.
  • HY-N2230
    N-p-trans-Coumaroyltyramine

    AChE Infection Neurological Disease
    N-p-trans-Coumaroyltyramine is a cinnamoylphenethyl amide isolated from polygonum hyrcanicum, acts as an acetylcholinesterase (AChE) inhibitor with an an IC50 of 122 μM. N-p-trans-Coumaroyltyramine exhibits anti-trypanosomal activity with an IC50 of 13.3 µM for T. brucei rhodesiense.
  • HY-100369A
    DMCM hydrochloride

    GABA Receptor Neurological Disease
    DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5  receptors, respectively.
  • HY-114334
    Glutaminase-IN-1

    CB839 derivative

    Glutaminase Cancer
    Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
  • HY-113973
    LPA2 antagonist 2

    LPL Receptor Cancer
    LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM).
  • HY-128781
    Glucagon receptor antagonists-5

    Glucagon Receptor Metabolic Disease
    Glucagon receptor antagonists-5 (compound 13K) is a potent and orally bioavailable indazole-based glucagon receptor antagonist (Ki=32 nM). Glucagon receptor antagonists-5 has potential for the treatment of type 2 diabetes mellitus (T2DM).
  • HY-10446
    Pralatrexate

    Antifolate Apoptosis Cancer
    Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment.
  • HY-107457A
    AZD-8529 mesylate

    mGluR Neurological Disease
    AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-136592
    1-Hydroxy-ibuprofen

    COX Cancer Inflammation/Immunology
    1-Hydroxy Ibuprofen is a metabolite of Ibuprofen in P. australis. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, 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-19826
    Isofistularin-3

    DNA Methyltransferase ADC Cytotoxin Autophagy Apoptosis Cancer
    Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
  • HY-121899
    1-Oxo Ibuprofen

    Ibuprofen EP impurity J

    Others Others
    1-Oxo Ibuprofen (Ibuprofen EP impurity J) is a degradation product and a potential impurity in preparations of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-N3523
    3-O-Beta-D-Glucopyranosylplatycodigenin

    Others Cancer
    3-O-Beta-D-Glucopyranosylplatycodigenin is an oleanane-type triterpenoid isolated from roots of Platycodon grandiflorum. 3-O-Beta-D-Glucopyranosylplatycodigenin exhibits anti-proliferative activities against HSC-T6 cell line with an IC50 of 13.36 μM.
  • HY-135279
    CFTR corrector 4

    CFTR Inflammation/Immunology
    CFTR corrector 4 (Compound 13), an active (R,R)-form enantiomer, is a highly potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 4 can increase CFTR levels at the cell surface and have the potential for treatment of cystic fibrosis.
  • HY-111678
    ML230

    CID44640177; SID 88095709

    Others Cancer
    ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively.
  • HY-G0025
    Tetrabenazine Metabolite

    (-)-β-Dihydrotetrabenazine; (-)-β-HTBZ

    Monoamine Transporter Drug Metabolite Neurological Disease
    Tetrabenazine Metabolite is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite is a vesicular monoamine transporter 2 (VMAT2) inhibitor with a high affinity (Ki=13.4 nM). Tetrabenazine Metabolite is be developed for the treatment of chorea associated with Huntington’s disease and other hyperkinetic disorders.
  • HY-I0678
    Regorafénib N-oxyde (M2)

    Drug Metabolite Cancer
    Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-U00326
    PI3Kα/mTOR-IN-1

    PI3K mTOR Cancer
    PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.
  • HY-B0335
    Tolfenamic Acid

    GEA 6414

    COX Inflammation/Immunology Cancer
    Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
  • HY-14670
    Firocoxib

    ML 1785713

    COX Inflammation/Immunology
    Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects.
  • HY-129656
    GLP-1 receptor agonist 3

    Glucagon Receptor Metabolic Disease
    GLP-1 receptor agonist 3 is a GLP-1 receptor agonist extracted from patent WO2018109607A1, Example 4A-1, has EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.
  • HY-100726
    GNE-272

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.
  • HY-P1028
    Hexa-D-arginine

    Furin Inhibitor II

    Others Infection
    Hexa-D-arginine (Furin Inhibitor II) is a stable furin inhibitor with Ki values 106 nM, 580 nM and 13.2 μM for furin, PACE4 and prohormone convertase-1 (PC1), respectively. Hexa-D-arginine blocks Pseudomonas exotoxin A and anthrax toxins toxicity in vitro and in vivo.
  • 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-12305
    Q-VD-OPh

    QVD-OPH; Quinoline-Val-Asp-Difluorophenoxymethylketone

    Caspase HIV Cancer Infection
    Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.
  • HY-13404
    Capmatinib

    INC280; INCB28060

    c-Met/HGFR Apoptosis Cancer
    Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib (INC280; INCB28060) potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity.
  • HY-P9805
    Anti-MERS-3A1 mAb

    MERS-3A1; MERS Antibody-3A1

    SARS-CoV Infection
    Anti-MERS-3A1 mAb (MERS-3A1) is a human monoclonal IgG1 antibody with the high binding affinity produced in CHO cells. Anti-MERS-3A1 mAb bocks the binding of MERS-CoV spike protein to DPP4 receptor.
  • 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-17589
    Chloroquine phosphate

    Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Antibiotic Cancer Infection Inflammation/Immunology
    Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
  • HY-101523
    Cdc7-IN-1

    CDK Cancer
    Cdc7-IN-1 (Compound 13) is a highly potent, selective and ATP competitive inhibitor of Cdc7 kinase, with an IC50 value of 0.6 nM at 1 mM ATP and with slow off-rate characteristics. Cdc7-IN-1 potently inhibits Cdc7 activity in cancer cells, and effectively induces cell death.
  • HY-A0077
    Perphenazine

    5-HT Receptor Adrenergic Receptor Dopamine Receptor Histamine Receptor Neurological Disease Endocrinology
    Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
  • HY-17589B
    Chloroquine dihydrochloride

    Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Antibiotic Cancer Infection Inflammation/Immunology
    Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
  • HY-136563
    RA375

    Proteasome Apoptosis Reactive Oxygen Species Cancer
    RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead.
  • HY-122906
    JTE-952

    c-Fms Inflammation/Immunology
    JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis.
  • HY-108006
    Mirogabalin besylate

    DS 5565 besylate

    Calcium Channel Neurological Disease
    Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
  • HY-108264
    TCS 21311

    NIBR3049

    JAK PKC GSK-3 Cancer
    TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.
  • HY-131179
    Influenza A virus-IN-1

    Influenza Virus Infection
    Influenza A virus-IN-1 is a dihydropyrrolidones derivative and is a potent inhibitor against wide subtypes of influenza A virus (IAV) with IC50 values from 3.11 μM to 7.13 μM. Influenza A virus-IN-1 efficiently inhibits replication of IAV, up-regulates the expression of key antiviral cytokines IFN-β and antiviral protein MxA.
  • 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-101517
    PI3K-IN-2

    PI3K Cancer
    PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively).
  • HY-117383
    NGI-1

    ML414

    Virus Protease Cancer
    NGI-1 (ML414) is a potent oligosaccharyltransferase (OST) inhibitor, directly targeting and blocking the function of the OST catalytic subunits STT3A and STT3B. NGI-1 is a cell permeable inhibitor and can effectively reduce virus infectivity without affecting cell viability.
  • HY-17589A
    Chloroquine

    Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Antibiotic Cancer Infection Inflammation/Immunology
    Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
  • HY-129707
    AMG 837 hemicalcium

    GPR40 Metabolic Disease
    AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1, inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents.
  • HY-50101A
    Mavorixafor trihydrochloride

    AMD-070 trihydrochloride

    CXCR HIV Infection Endocrinology
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-12344
    UNC2025

    FLT3 Cancer
    UNC2025 is a potent and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.
  • HY-113039
    L-2-Hydroxyglutaric acid

    (S)-2-Hydroxyglutaric acid

    Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
  • HY-128338
    CETP-IN-3

    CETP Cardiovascular Disease
    CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively.
  • HY-111925
    BI-749327

    TRP Channel Cardiovascular Disease
    BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.
  • HY-50101
    Mavorixafor

    AMD-070

    CXCR HIV Infection Endocrinology
    Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-12344A
    UNC2025 hydrochloride

    FLT3 Cancer
    UNC2025 hydrochloride is a potent and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.
  • 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-100935S
    Cimaterol-D7

    Adrenergic Receptor
    Cimaterol-D7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
  • HY-W015114
    L-2-Hydroxyglutaric acid disodium

    (S)-2-Hydroxyglutaric acid disodium

    Histone Demethylase Mitochondrial Metabolism Cancer
    L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
  • HY-17444
    Tesaglitazar

    PPAR Cancer Metabolic Disease
    Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively, and approximately 0.2 μM for both rat and human PPARγ. Tesaglitazar induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats.
  • HY-10185
    TG 100572 Hydrochloride

    Src VEGFR FGFR PDGFR Inflammation/Immunology
    TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-111501
    H4R antagonist 1

    Histamine Receptor Inflammation/Immunology Endocrinology
    H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.
  • HY-10184
    TG 100572

    Src VEGFR PDGFR FGFR Cancer
    TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-101761
    TM5441

    PAI-1 Apoptosis Cancer
    TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence.
  • HY-105189
    Meclinertant

    SR 48692

    Neurotensin Receptor Neurological Disease
    Meclinertant (SR 48692) is a potent, selective, nonpeptide and orally active neurotensin receptor 1 (NTS1) antagonist. In human colon carcinoma (HT-29) cells, Meclinertant competitively antagonizes neurotensin-induced intracellular Ca 2+ mobilization with a pA2 values of 8.13. Meclinertant has anxiolytic, anti-addictive and memory-impairing effects.
  • HY-130608
    Mutated EGFR-IN-3

    EGFR Cancer
    Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
  • HY-123348
    Sampatrilat

    UK-81252

    Angiotensin-converting Enzyme (ACE) Neprilysin Inflammation/Immunology Cardiovascular Disease
    Sampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase (NEP). Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM). Sampatrilat (UK-81252) can be used for the study of chronic heart failure and blood pressure regulation.
  • HY-111544
    EML741

    Histone Methyltransferase Cancer
    EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.
  • HY-10249
    GSK-690693

    Akt AMPK Autophagy Cancer
    GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.
  • HY-N6743
    Cercosporin

    PKC Cancer
    Cercosporin is produced by a plant pathogen, Cercosporakikuchii, and the elsinochromes, pigments of the elsinoe family of fungi. Cercosporin is a potent photosensitizer with a short activation wavelength, mostly suitable for superficial photodynamic therapy (PDT) treatments, especially when it is necessary to avoid perforations. Cercosporin contains the perylenequinone structural features necessary to PKC activity with an IC50 of 0.6-1.3 μM.
  • HY-112714
    GSK3532795

    BMS-955176

    HIV Infection
    GSK3532795 (BMS-955176) is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively.
  • HY-17589AS
    Chloroquine D5

    Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Cancer Infection Inflammation/Immunology
    Chloroquine D5 is deuterium labeled Chloroquine. Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
  • HY-N1457
    Chrysosplenetin

    P-glycoprotein Cytochrome P450 Ferroptosis Metabolic Disease
    Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A.
  • HY-D0128
    4-Methylherniarin

    7-Methoxy-4-methylcoumarin

    Bacterial Infection
    4-Methylherniarin (7-Methoxy-4-methylcoumarin) is a coumarin derivative and fluorescent label, has an antimicrobial activitiy against both gram positive and gram negative bacterial stains. 4-Methylherniarin displays good activity against B. subtilis and S.sonnei with IC50 values of 11.76 μg/ml and 13.47 μg/ml.
  • HY-12354
    SB-3CT

    MMP Cancer
    SB-3CT is a potent and competitive matrix metalloproteinase MMP-2 and MMP-9 inhibitor with Ki values of 13.9 and 600 nM, respectively. SB-3CT has high selectivity for gelatinases. SB-3CT shows blood-brain barrier permeability and has neuroprotective effects and anticancer activity.
  • HY-10581A
    Gatifloxacin hydrochloride

    AM-1155 hydrochloride; BMS-206584 hydrochloride; PD135432 hydrochloride

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
  • HY-126318
    Demethoxydeacetoxypseudolaric acid B analog

    Others Cancer
    Demethoxydeacetoxypseudolaric acid B analog (Compound 13b) is semi-synthesized by efficient routines from Pseudolaric acid B. It has potent activities against HMEC-1, HL-60, A-549, MB-MDA-468, BEL-7402, HCT116, and Hela cells with IC50s ranging from 0.136 to 1.162 μM.
  • HY-124652
    TBK1/IKKε-IN-4

    IKK Cancer
    TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR.
  • HY-10581B
    Gatifloxacin mesylate

    AM-1155 mesylate; BMS-206584 mesylate; PD135432 mesylate

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin mesylate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin mesylate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin mesylate can be used to treat bacterial conjunctivitis in vivo.
  • HY-12883B
    PF 05089771 tosylate

    Sodium Channel Neurological Disease
    PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
  • HY-108742A
    Abaloparatide TFA

    BA 058 TFA; BIM 44058 TFA

    Thyroid Hormone Receptor Metabolic Disease Endocrinology
    Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue selected to be a potent and selective activator of the PTHR1 signaling pathway. Abaloparatide TFA enhances Gs/cAMP signaling (EC50 of 0.3 nM) and β-arrestin recruitment (EC50 of 0.9 nM) in MC3T3-E1 osteoblast cells.
  • HY-103110A
    ST1936 oxalate

    5-HT Receptor Neurological Disease
    ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human α2 adrenergic receptor.
  • HY-P1340
    [Ala11,D-Leu15]-Orexin B(human)

    Orexin Receptor (OX Receptor) Neurological Disease
    [Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM).
  • HY-12883
    PF 05089771

    Sodium Channel Neurological Disease
    PF 05089771 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
  • HY-P1340A
    [Ala11,D-Leu15]-Orexin B(human) TFA

    Orexin Receptor (OX Receptor) Neurological Disease
    [Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM).
  • HY-16708A
    ZLN024 hydrochloride

    AMPK Metabolic Disease
    ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
  • HY-N0678
    Icaritin

    Anhydroicaritin

    Autophagy Apoptosis Cancer
    Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium Genusis and potently inhibits proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis[3.
  • HY-10581
    Gatifloxacin

    AM-1155; BMS-206584; PD135432

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50=0.109 μg/ml). Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
  • HY-W008947
    SEW​2871

    LPL Receptor Inflammation/Immunology Neurological Disease
    SEW2871 is a highly selective, orally active S1P1 agonist with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood and has therapeutic implications in contexts of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses.
  • HY-10297
    Omipalisib

    GSK2126458; GSK458

    PI3K mTOR Autophagy Cancer
    Omipalisib (GSK2126458) is an orally active and highly selective inhibitor of PI3K with Kis of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. Omipalisib has anti-cancer activity.
  • HY-10581C
    Gatifloxacin sesquihydrate

    AM-1155 sesquihydrate; BMS-206584 sesquihydrate; PD135432 sesquihydrate

    Bacterial Topoisomerase Antibiotic Infection Inflammation/Immunology
    Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis in vivo.
  • HY-51424
    PLX-4720

    Raf Cancer
    PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
  • HY-16708
    ZLN024

    AMPK Metabolic Disease
    ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
  • HY-130484
    2,3-Dehydro-3,4-dihydro ivermectin

    Parasite
    2,3-Dehydro-3,4-dihydro ivermectin is an analog of ivermectin (HY-15310) and an anthelmintic. 2,3-Dehydro-3,4-dihydro ivermectin has activity against L. amazonensis promastigotes and amastigotes (IC50s=13.8 and 3.6 µM, respectively) without inducing cytotoxicity to macrophages (IC50= 65.5 µM).
  • HY-17624
    Framycetin

    Neomycin B; Fradiomycin B

    Bacterial Infection
    Framycetin (Neomycin B), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
  • HY-108263A
    (S)-3-Hydroxy Midostaurin

    (S)-CGP52421

    FLT3 Drug Metabolite Cancer
    (S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nM for 13 kinases (VEGFR-2, TRK-A, FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML).
  • HY-125878
    PROTAC SGK3 degrader-1

    SGK3-PROTAC1

    PROTAC SGK Cancer
    PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on PROTAC. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).
  • HY-P1420
    TAT-cyclo-CLLFVY

    HIF/HIF Prolyl-Hydroxylase
    TAT-cyclo-CLLFVY is a selective HIF-1 dimerization inhibitor. TAT-cyclo-CLLFVY blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50=1.3 μM). TAT-cyclo-CLLFVY inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. TAT-cyclo-CLLFVY also reduces tubularization of hypoxic HUVECs.
  • HY-13317S
    Oseltamivir D3

    Influenza Virus Infection
    Oseltamivir D3 is a deuterium labeled Oseltamivir. Oseltamivir is an influenza virus neuraminidase inhibitor (NAI). Oseltamivir inhibits influenza A/H3N2, A/H1N2, A/H1N1, and B viruses with mean IC50s of 0.67, 0.9, 1.34 and 13 nM, respectively. Anti-influenza A and B agent.
  • HY-107420
    AY 9944

    Others Metabolic Disease
    AY 9944 is a specific cholesterol biosynthesis inhibitor. AY 9944 inhibits the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50=13 nM). AY 9944 causes hypocholesterolemia and accumulation of 7DHC. At high doses, AY 9944 inhibits also in cultured embryos sterol Δ7-Δ8 isomerase, which causes the accumulation of cholest-8-en-3β-ol.
  • HY-13281
    PIK-75 hydrochloride

    DNA-PK PI3K Apoptosis Cancer
    PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis.
  • HY-10187
    TG 100801 Hydrochloride

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 Hydrochloride is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-17624A
    Framycetin sulfate

    Neomycin B sulfate; Fradiomycin B sulfate

    Bacterial Infection
    Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin sulfate, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
  • HY-14183
    Vernakalant Hydrochloride

    RSD1235 hydrochloride

    Potassium Channel Cardiovascular Disease
    Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
  • HY-101562
    GDC-0077

    RG6114

    PI3K Apoptosis Cancer
    GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα.
  • HY-107834
    PIK-75

    DNA-PK PI3K Apoptosis Cancer
    PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis.
  • HY-10186
    TG 100801

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-P0172A
    ATI-2341 TFA

    CXCR Cancer Inflammation/Immunology Endocrinology
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
  • HY-13811
    NSC697923

    E1/E2/E3 Enzyme Apoptosis Cancer
    NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
  • HY-P1420A
    TAT-cyclo-CLLFVY TFA

    HIF/HIF Prolyl-Hydroxylase
    TAT-cyclo-CLLFVY TFA is a selective HIF-1 dimerization inhibitor. TAT-cyclo-CLLFVY TFA blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50=1.3 μM). TAT-cyclo-CLLFVY TFA inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. TAT-cyclo-CLLFVY TFA also reduces tubularization of hypoxic HUVECs.
  • HY-P0172
    ATI-2341

    CXCR Inflammation/Immunology Endocrinology Cancer
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
  • HY-117163
    FzM1.8

    Wnt β-catenin Cancer
    FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
  • HY-111553
    TAS0728

    EGFR Cancer
    TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity.
  • HY-130241
    Reverse transcriptase-IN-1

    HIV Infection
    Reverse transcriptase-IN-1 (Compound 12z) is a diarylbenzopyrimidine (DABP) analogue and a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50 value of 13.7 nM against HIV-1 reverse transcriptase enzyme.
  • 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-133124
    PARP/PI3K-IN-1

    PARP PI3K Apoptosis Cancer
    PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.
  • HY-19408
    Pyr10

    TRP Channel Others
    Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels.
  • HY-P2264
    KYL peptide

    Ephrin Receptor
    KYL peptide is an EphA4 receptor tyrosine kinase inhibitor (Kd=0.8 μM). KYL peptide inhibits EphA4-EphrinA5 interactions (IC50=6.34 μM). KYL peptide prevents AβO induced synaptic damage, dendritic spine loss and prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. KYL peptide also exhibits a long half life in cell culture media (8 and 12 hours in PC3 and C2C12 media respectively).
  • 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-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-101257B
    YKL-5-124 TFA

    CDK Cancer
    YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-131183
    PROTAC PD-1/PD-L1 degrader-1

    PROTAC PD-1/PD-L1 Inflammation/Immunology
    PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 degrader, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
  • 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.