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Inhibitors & Agonists



Cat. No. Product Name Target Research Areas
  • HY-16100
    BI 99179

    Fatty Acid Synthase (FASN) Cancer Metabolic Disease
    BI 99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats.
  • HY-130609A
    Aβ42-IN-1 free base

    γ-secretase Neurological Disease
    Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
  • HY-W014075

    Endogenous Metabolite Metabolic Disease
    1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes.
  • HY-113247
    trans-trans-Muconic acid

    Endogenous Metabolite Metabolic Disease
    trans-trans-Muconic acid is a urinary metabolite of benzene and has been used as a biomarker of exposure to benzene in human.
  • HY-B1178

    (-)-Cotinine; (S)-Cotinine; NIH-10498

    Endogenous Metabolite Others
    Cotinine is an alkaloid found in tobacco and is also the predominant metabolite of nicotine, used as a biomarker for exposure to tobacco smoke.
  • HY-117290

    Factor Xa Cardiovascular Disease
    BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity.
  • HY-W010255
    Phenylglyoxylic acid

    Benzoylformic acid

    Endogenous Metabolite Metabolic Disease
    Phenylglyoxylic acid (Benzoylformic acid) is a metabolite of ethylbenzene and styrene (EB/S) and can be used as a biomarker of exposure to EB/S in human.
  • HY-W011848
    Monobenzyl phthalate

    2-((Benzyloxy)carbonyl)benzoic acid

    Endogenous Metabolite Metabolic Disease
    Monobenzyl phthalate (2-((Benzyloxy)carbonyl)benzoic acid) is the urinary metabolite exposuring to phthalates, such as, diethylhexyl phthalate (DEHP).
  • HY-133668
    Monoethyl phthalate

    Others Cancer
    Monoethyl phthalate is a metabolite of diethyl phthalate. Monoethyl phthalate acts as a urinary biomarker of phthalates exposure indicating the risks of thyroid cancer and benign nodule.
  • HY-136612

    Drug Metabolite Others
    DCBA is a metabolite of insect repellent N-N-diethyl-meta-toluamide (DEET). The concentration of DCBA in urine can assess exposure to DEET.
  • HY-Y1097
    Monomethyl phthalate

    2-(Methoxycarbonyl)benzoic acid

    Endogenous Metabolite Cancer
    Monomethyl phthalate is a phthalate metabolite. Monomethyl phthalate acts as a urinary biomarker of phthalates exposure and can be used as a standard for the determination of thyroid cancer and benign nodule.
  • HY-B1444
    Isoconazole nitrate

    Bacterial Fungal Antibiotic Infection
    Isoconazole nitrate is a broad-spectrum antimicrobial agent with a highly effective antimycotic and gram-positive antibacterial activity, exhibiting a rapid rate of absorption and low systemic exposure potential.
  • HY-18237

    Src Others
    KX1-004 is a potent and non-ATP competitive Src-PTK inhibitor with an IC50 of 40 μM. KX1-004 protects the cochlea from hazardous noise and prevents noise-induced hearing loss (NIHL).
  • HY-130609

    γ-secretase Neurological Disease
    Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
  • HY-15234
    Fluticasone furoate

    Glucocorticoid Receptor Inflammation/Immunology
    Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment.
  • HY-126316

    FKBP Others
    Zapalog is a photocleavable small-molecule heterodimerizer that can be used to repeatedly initiate, and instantaneously terminate, a physical interaction between two target proteins. Zapalog dimerizes any two proteins tagged with the FKBP and DHFR domains until exposure to light causes its photolysis.
  • HY-14375
    CB 300919

    NAMPT Cancer
    CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft.
  • HY-B0815

    AChE Neurological Disease
    Chlorpyrifos is an organophosphate insecticide that is classified as a phosphorothionate. The oxon metabolite of Chlorpyrifos is an inhibitor of acetylcholinesterase (AChE), affecting neurological function in insects, humans, and other animals. The Chlorpyrifos oxon (CPO) metabolite is hydrolyzed by the plasma enzyme paraoxonase 1 (PON1), and susceptibility to neurotoxicity associated with CPO exposure is mitigated by PON1 overexpression.
  • HY-109587A
    BM635 hydrochloride

    Bacterial Infection
    BM635 hydrochloride is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 hydrochloride has an MIC50 of 0.08 μM against M.tuberculosis H37Rv. BM635 hydrochloride doubles the in vivo exposure with respect to the free base BM635.
  • HY-136924

    Others Others
    FP-biotin is a potent organophosphorus toxicant, well-suited for searching for new biomarkers of organophosphorus toxicants exposure. FP-Biotin quantifies FAAH, ABHD6, and MAG-lipase activity. FP-biotin is used for studies with plasma because biotinylated peptides are readily purified by binding to immobilized avidin beads.
  • HY-130602

    PROTACs MEK Cancer
    MS432 is a first-in-class and highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
  • HY-N4192

    Others Cancer Cardiovascular Disease
    Toringin, a bioflavonoid, is isolated from the bark of Docyniopsis tschonoski. Toringin progressively decreases not only the cis-effect of the expanded CTG repeats but cytotoxicity as well. Exposure to isosakuranetin, Toringin rescues PC12 neuronal cells. Flavonoids are efficacious for ameliorating the RNA gain of function caused by expanded CTG repeats, and have various biological activities and beneficial actions against cancers, coronary heart disease, among other pathologies.
  • HY-123349
    5α-Hydroxy-6-keto cholesterol

    Drug Metabolite Cardiovascular Disease
    5α-Hydroxy-6-keto cholesterol is major metabolite of β-epoxide (5α,6β-epoxycholesterol) during direct exposure of intact cultured human bronchial epithelial cells (16-HBE) to ozone. 5α-Hydroxy-6-keto cholesterol inhibits cholesterol synthesis with an IC50 of 350 nM.
  • HY-12545


    Sodium Channel Inflammation/Immunology
    Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
  • HY-107353
    Gadopentetic acid

    Gd-DTPA; gadolinium complex

    Others Others
    Gadopentetic acid (Gd-DTPA) is an paramagnetic contrast agent commonly implemented by a bolus intravenous injection (i.v.) in Dynamic contrast-enhanced MRI (DCE-MRI) studies. The initial concentration of Gadopentetic acid (Gd-DTPA) in the plasma ([Gd-DTPA0]) is an important parameter for DCE-MRI. [Gd-DTPA0] is related to the administered bolus dose and varies with subjects. A bolus of 0.025 mmol/kg Gd-DTPA offers shorter acquisition time and less exposure of subjects, with a half-life of 37.3 mins, a mean residence time of 53.8 mins, and an AUC of 3.37 ± 0.47 mmol/min/L.