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Inhibitors & Agonists


Screening Libraries


Inhibitory Antibodies




Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-N0790

    Clerodol; Monogynol B; Fagarasterol

    Androgen Receptor Apoptosis Cancer
    Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
  • HY-137892

    Epigenetic Reader Domain Inflammation/Immunology
    GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
  • HY-145110
    IGF-1R inhibitor-2

    IGF-1R Cancer
    IGF-1R inhibitor-2 (example 121) is an insulin-like growth factor-1 receptor (IGF-1R) inhibitor. Downregulation of IGF-1R can reverse the transformed phenotype of tumor cells and potentially render them susceptible to apoptosis.
  • HY-100384
    NKL 22

    HDAC Neurological Disease
    NKL 22 (compound 4b) is a potent and selective inhibitor of histone deacetylases (HDAC), with an IC50 of 199 and 69 nM for HDAC1 and HDAC3, respectively. NKL 22 exhibits selectivity over HDAC2/4/5/7/8 (IC50≥1.59 μM). NKL 22 ameliorates the disease phenotype and transcriptional abnormalities in Huntington's disease transgenic mice.
  • HY-N1363
    Royal Jelly acid

    Queen Bee Acid; (E)-10-Hydroxy-2-decenoic acid

    Endogenous Metabolite Neurological Disease
    Royal Jelly acid (Queen Bee Acid) is a fatty acid constituent of royal jelly, promotes the growth and protection of neurons, reduces anxiety-like phenotypes.
  • HY-104026B
    L-Kynurenine sulfate

    Endogenous Metabolite Aryl Hydrocarbon Receptor Inflammation/Immunology
    L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype.
  • HY-139990

    c-Fms Cancer
    CSF1R-IN-3 (compound 21) is a potent and orally active CSF-1R inhibitor (IC50=2.1 nM). CSF1R-IN-3 is a potent antiproliferative activity against colorectal cancer cells. CSF1R-IN-3 inhibits the progression of colorectal cancer by suppressing the migration of macrophages, reprograming M2-like macrophages to the M1 phenotype, and enhancing the antitumor immunity.
  • HY-125331

    Topoisomerase ADC Cytotoxin Cancer
    DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.
  • HY-114250


    Apoptosis Cancer
    Cantrixil (TRX-E-002-1), an active enantiomer of TRX-E-002, is a second-generation super-benzopyran (SBP) compound. Cantrixil increases phosphorylated c-Jun levels resulting in caspase-mediated apoptosis in ovarian cancer cells. Cantrixil has potent pan anti-cancer activity against a broad range of cancer phenotypes.
  • HY-120766

    Histone Demethylase Cancer
    NCDM-32B is a potent and selective KDM4 inhibitor that impaires viability and transforming phenotypes of breast cancer.
  • HY-10996A
    KHS101 hydrochloride

    FGFR Neurological Disease Cancer
    KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).
  • HY-B1378

    Calcium Channel Neurological Disease
    Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
  • HY-121793


    P-glycoprotein Cancer
    Roemerine, an aporphine alkaloid, isolated from the leaves of Annona senegalensis, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells.
  • HY-Y0586
    2,4,5-Trimethoxybenzoic acid

    Others Metabolic Disease
    2,4,5-Trimethoxybenzoic acid is a compound identified in purple perilla extracts. 2,4,5-Trimethoxybenzoic acid inhibits M1 macrophage phenotype-mediated inflammation in diabetes.
  • HY-B1378S1

    Calcium Channel Neurological Disease
    Ethosuximide-d5 is deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
  • HY-B1184

    Cytochrome P450 Neurological Disease
    Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate.
  • HY-12346

    NSC 12407; BRD-K4477

    Others Others
    FH1 (NSC 12407) enhances hepatocyte functions, and promotes the differentiation of induced pluripotent stem (iPS)-derived hepatocytes toward a phenotype more mature and the maturation of well-differentiated cultures of hepatocyte-like cells (iHeps).
  • HY-137206

    Ligands for E3 Ligase Molecular Glues Cancer
    ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment.
  • HY-B1378S

    Calcium Channel Neurological Disease
    Ethosuximide-d3 is the deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
  • HY-125197

    Autophagy Inflammation/Immunology
    BRD5631 is an autophagy enhancer, enhances autophagy through an mTOR-independent pathway. BRD5631 affects several cellular disease phenotypes previously linked to autophagy, including protein aggregation, cell survival, bacterial replication, and inflammatory cytokine production.
  • HY-139059

    Others Neurological Disease
    ERD03 is a potent disruptor of the EXOSC3-RNA interaction, with a Kd of 17±7 μM . ERD03 induces PCH1B-like phenotype in zebrafish embryo and can be used for neurological disorder disease research.
  • HY-15794

    Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243

    Others Cancer
    Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity.
  • HY-117651
    2-Fluoropalmitic acid

    Acyltransferase Cancer
    2-Fluoropalmitic acid, an acyl-CoA synthetase inhibitor, acts as a candidate anti-glioma agent. 2-Fluoropalmitic acid suppresses the viability and stem-like phenotype of glioma stem cells (GSCs). 2-Fluoropalmitic acid also inhibits proliferation and invasion of glioma cell lines.
  • HY-118134

    Others Cancer
    Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM. Hepln-13 can be used for the research of metastatic prostate cancer.
  • HY-131035
    Lys-CoA TFA

    Histone Acetyltransferase Cancer
    Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation.
  • HY-16706A
    Remodelin hydrobromide

    Histone Acetyltransferase Cancer
    Remodelin, a specific inhibitor of N-acetyltransferase NAT10, can ameliorate Hutchinson-Gilford Progeria Syndrom (HGPS) cellular phenotypes. Remodelin acts in a progerin- and FTI-independent pathway, by targeting and inhibiting NAT10. NAT10 is a protein with histone acetylation activity and primarily identified to be involved in regulation of telomerase activity.
  • HY-N0284

    PI3K Akt Cancer Inflammation/Immunology
    Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.
  • HY-131448

    Others Metabolic Disease
    A3051 is a potent and orally active inhibtor of CXXC5-DVL extracted from patent WO2020079569, has an IC50 of 63.06 nM. A3334 can be used for the research of high fat diet (HFD)-induced and methionine-choline deficient diet (MCD)-induced phenotypes such as obesity, diabetes, and NASH.
  • HY-19987

    Wnt Cancer
    BML-284 is a potent and cell-permeable Wnt signaling activator. BML-284 induces TCF-dependent transcriptional activity with an EC50 of 700 nM.
  • HY-136214
    R-BC154 acetate

    Integrin Cancer Inflammation/Immunology
    R-BC154 acetate is a selective fluorescent α9β1 integrin antagonist. R-BC154 acetate acts as a useful high affinity, activation dependent integrin probe, which can be used to investigate α9β1 and α4β1 integrin binding activity.
  • HY-19987A
    BML-284 hydrochloride

    Wnt Cancer
    BML-284 hydrochloride is a potent and cell-permeable Wnt signaling activator. BML-284 induces TCF-dependent transcriptional activity with an EC50 of 700 nM.
  • HY-144256
    CHD1Li 6.11

    Others Cancer
    CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties.
  • HY-120599

    VERU-111; ABI-231

    Microtubule/Tubulin Apoptosis HPV Cancer
    VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer.
  • HY-101855

    Amyloid-β Neurological Disease
    Anle138b, an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Anle138b strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Anle138b has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology.
  • HY-145848
    ERRγ agonist-1

    Estrogen Receptor/ERR Neurological Disease
    ERRγ agonist-1 is a potent ERRγ agonist. ERRγ agonist-1 increases transcriptional activities of ERRγ. ERRγ agonist-1 has the potential for the research of neuropsychological disorders.
  • HY-150565
    P-gp inhibitor 5

    P-glycoprotein Cancer
    P-gp inhibitor 5 (compound 10) is a potent P-glycoprotein (P-gp) inhibitor with P-gp inhibition fold of 2.5 and 3.0 at 1.25 μM and 2.5 μM. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In TM-293 and KBvin cells by restoring their sensitivity to Vincristine and Paclitaxel.
  • HY-N6711

    HIV Integrase Infection
    Equisetin is an N-methylserine-derived acyl tetramic acid isolated from a terrestrial fungus Fusarium equiseti NRRL 5537. Equisetin is a tetramate-containing natural product with antibiotic and cytotoxic activity. Equisetin inhibits the growth of Gram-positive bacteria and HIV-1 integrase activity but shows no activity against Gram-negative bacteria. Equisetin is a Quorum-sensing inhibitor (QSI) that attenuates QS-regulated virulence phenotypes in P. aeruginosa without affecting the growth of bacterias, serves as a leading compound for the treatment of P. aeruginosa infections.
  • HY-118567


    Phosphatase Metabolic Disease
    Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer.