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Targets Recommended: SNIPER
Results for "

specific

" in MCE Product Catalog:

825

Inhibitors & Agonists

17

Screening Libraries

15

Dye Reagents

5

Biochemical Assay Reagents

92

Peptides

5

MCE Kits

1

Inhibitory Antibodies

89

Natural
Products

128

Recombinant Proteins

20

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-135905
    CL264

    Toll-like Receptor (TLR) Inflammation/Immunology
    CL264 is a TLR7-specific agonist for innate immune signals research.
  • HY-138698
    FT206

    Deubiquitinase Others
    FT206 is an inhibitor of carboxamides as ubiquitin-specific protrase extracted from patent WO 2020033707 A1, example 11-1.
  • HY-141519
    PI-55

    Parasite Others Infection
    PI-55 is a specific cytokinin receptor inhibitor. PI-55 is structurally related to 6-benzylaminopurine (BAP) and was shown to inhibit competitively BAP binding on Arabidopsis-specific receptors CRE1/AHK4 and AHK3. PI-55 inhibits cytokinins induced haustorium formation and increased parasite aggressiveness.
  • HY-112050
    CU-CPT-8m

    TLR8-specific antagonist

    Toll-like Receptor (TLR) Inflammation/Immunology
    CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67 nM.
  • HY-103314
    Gadolinium chloride

    GdCl3

    CaSR Cardiovascular Disease
    Gadolinium chloride is a specific calcium-sensing receptor (CaSR) agonist. Gadolinium chloride can be used for the research of cardiovascular disease.
  • HY-101820A
    Simotinib hydrochloride

    EGFR Cancer
    Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
  • HY-121087
    BCI-215

    Phosphatase Cancer
    BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells.
  • HY-139301
    DDO-5936

    HSP Cancer
    DDO-5936 is a potent and specific Hsp90-Cdc37 PPI inhibitor. DDO-5936 can be used for the research of colorectal cancer.
  • HY-117444
    ONO-9780307

    LPL Receptor Cancer
    ONO-9780307 is a specific synthetic LPA1 (lysophosphatidic acid receptor 1) antagonist with an IC50 value of 2.7 nM.
  • HY-141715
    BRD-8000.3

    Others Infection
    BRD-8000.3, as a specific EfpA inhibitor, is a narrow-spectrum, bactericidal antimycobacterial agent with good wild-type activity. BRD-8000.3 can be used for the research of tuberculosis.
  • HY-133907
    NVS-PI3-4

    PI3K Cancer Inflammation/Immunology
    NVS-PI3-4 is a specific PI3Kγ inhibitor. NVS-PI3-4 can be used for the research of allergies, inflammatory and cancer diseases.
  • HY-B0232
    Dofetilide

    UK 68789

    Potassium Channel Cardiovascular Disease
    Dofetilide (UK 68789), as a class III antiarrhythmic agent, is an orally active, potent and specific IKr blocker. Dofetilide can be used for the research of cardiovascular disease.
  • HY-120019
    Ac-YVAD-CHO

    L-709049

    Interleukin Related Inflammation/Immunology
    Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO can suppress the production of mature IL-lβ.
  • HY-109127
    Berotralstat

    Others Others
    Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.
  • HY-18314
    GW 441756

    Trk Receptor Apoptosis Cancer Neurological Disease
    GW 441756 is a potent and specific nerve growth factor (NGF) receptor tyrosine kinases A (TrkA) inhibitor (IC50=2 nM), which eliminates the BmK NSPK-induced neurite outgrowth.
  • HY-110237
    BX430

    P2X Receptor Calcium Channel Cardiovascular Disease
    BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
  • HY-124424
    VU0071063

    Potassium Channel Neurological Disease Others
    VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential. VU0071063 chemotype has a very steep structure-activity relationships.
  • HY-134595
    SENP1-IN-2

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-2 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 30. SENP1-IN-2 is developed for tumor radiosensitivity enhancement.
  • HY-134594
    SENP1-IN-1

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-1 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 29. SENP1-IN-1 is developed for tumor radiosensitivity enhancement.
  • HY-134597
    SENP1-IN-4

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-4 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 21. SENP1-IN-4 is developed for tumor radiosensitivity enhancement.
  • HY-134596
    SENP1-IN-3

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-3 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 17. SENP1-IN-3 is developed for tumor radiosensitivity enhancement.
  • 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-18303
    AMG-47a

    Src VEGFR p38 MAPK JAK Inflammation/Immunology
    AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.
  • HY-114038
    SB-747651A

    p38 MAPK Inflammation/Immunology
    SB-747651A is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A can be used for inflammation research.
  • HY-110353
    CU-T12-9

    Toll-like Receptor (TLR) Cancer Inflammation/Immunology
    CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
  • HY-17540
    HBX 19818

    Deubiquitinase Cancer
    HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM.
  • HY-102079
    SAFit1

    FKBP Metabolic Disease Neurological Disease
    SAFit1 is a FK506 binding protein 51 (FKBP51)-specific inhibitor with a Ki of 4±0.3 nM.
  • HY-112502B
    MethADP sodium salt

    CD73 Cancer
    MethADP (sodium salt) is a specific CD73 inhibitor.
  • HY-112502
    MethADP

    Adenosine 5'-(α,β-methylene)diphosphate

    CD73 Cancer
    MethADP is a specific CD73 inhibitor.
  • HY-15759A
    Napsagatran hydrate

    Ro 46-6240 hydrate; Ro 46-6240/010 hydrate

    Thrombin Cardiovascular Disease
    Napsagatran hydrate is a novel and specific thrombin inhibitor.
  • HY-120870
    para-Nitroblebbistatin

    Myosin Metabolic Disease
    para-Nitroblebbistatin is a non-cytotoxic, photostable, fluorescent and specific Myosin II inhibitor, usd in the study of the specific role of myosin II in physiological, developmental, and cell biological studies.
  • 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-U00062
    Tarazepide

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    Tarazepide is a potent and specific CCK-A receptor antagonist.
  • HY-126327
    UNC4976

    Histone Methyltransferase Cancer
    UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
  • HY-U00441
    DPBQ

    MDM-2/p53 Apoptosis Cancer
    DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells.
  • HY-101443
    ISCK03

    c-Kit Inflammation/Immunology
    ISCK03 is a specific SCF/c-Kit inhibitor.
  • HY-B1303A
    Mebhydrolin

    Histamine Receptor Inflammation/Immunology Endocrinology
    Mebhydrolin is a specific histamine H1 receptor antagonist.
  • HY-100524
    LRE1

    Adenylate Cyclase Cancer
    LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase.
  • HY-101278
    Thiomyristoyl

    Sirtuin Cancer
    Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM.
  • HY-101550
    HI-TOPK-032

    TOPK Cancer
    HI-TOPK-032 is a potent and specific TOPK inhibitor.
  • HY-B1303
    Mebhydrolin napadisylate

    Mebhydroline 1,5-naphthalenedisulfonate salt

    Histamine Receptor Inflammation/Immunology Endocrinology
    Mebhydrolin napadisylate is a specific histamine H1 receptor antagonist.
  • HY-100592
    Nicaraven

    Others Cancer
    Nicaraven is a novel chemically synthesized hydroxyl radical-specific scavenger.
  • HY-112587
    MC3482

    Sirtuin Cancer
    MC3482 is a specific sirtuin5 (SIRT5) inhibitor.
  • HY-B0263
    Thiabendazole

    2-(4-Thiazolyl)benzimidazole

    Mitochondrial Metabolism Parasite Infection
    Thiabendazole inhibites the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property.
  • HY-P1313A
    PAR 4 (1-6) (TFA)

    GYPGQV TFA

    Protease-Activated Receptor (PAR) Others
    PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is a fragment of protease-activated receptor 4 (PAR4). PAR 4 (1-6) TFA acts as a PAR4-specific agonist.
  • HY-16713A
    (S)-(-)-5-Fluorowillardiine hydrochloride

    (5S)-Fluorowillardiine hydrochloride; (S)-5-Fluorowillardiine hydrochloride

    iGluR Neurological Disease
    (S)-(-)-5-Fluorowillardiine hydrochloride is a potent and specific AMPAR agonist.
  • HY-10544
    Tegobuvir

    GS 333126; GS-9190

    HCV Infection
    Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.
  • HY-W008151
    Diphenyl Phosphate

    DPhP

    Others Metabolic Disease
    Diphenyl Phosphate inhibits growth and energy metabolism of zebrafish in a sex-specific manner.
  • HY-B1016
    Trapidil

    AR-12008

    PDGFR Cardiovascular Disease Cancer
    Trapidil is a vasodilator, is an antiplatelet drug with specific platelet-derived growth factor.
  • HY-110404
    Capzimin

    Proteasome Cancer
    Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
  • HY-15535
    DMAT

    CK2 Inhibitor; Casein kinase II Inhibitor

    Casein Kinase Cancer
    DMAT is a potent and specific CK2 inhibitor with an IC50 value of 130 nM.
  • HY-16713
    (S)-(-)-5-Fluorowillardiine

    (5S)-Fluorowillardiine; (S)-5-Fluorowillardiine

    iGluR Neurological Disease
    (S)-(-)-5-Fluorowillardiine is a potent and specific AMPAR agonist.
  • HY-19695
    (-)-p-Bromotetramisole oxalate

    L-p-Bromotetramisole oxalate; 6-Bromolevamisole oxalate

    Phosphatase Cancer
    (-)-p-Bromotetramisole Oxalate is a potent and non-specific alkaline phosphatase inhibitor.
  • HY-P0136
    SAMS

    AMPK Metabolic Disease
    SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK).
  • HY-16666
    3CAI

    Akt Cancer
    3CAI is a potent and specific AKT1 and AKT2 inhibitor.
  • HY-128921
    Bz-Lys-OMe

    Others Others
    Bz-Lys-Ome is a specific methyl ester substrate of trypsin.
  • HY-101600
    RPR104632

    iGluR Neurological Disease
    RPR104632 is a specific antagonist of NMDA receptor, with potent neuroprotective properties.
  • HY-113283
    Homogentisic acid

    Endogenous Metabolite Metabolic Disease
    Homogentisic acid is a specific metabolite in urine and serum, which is used for diagnosis of alkaptonuria.
  • HY-133870
    Itaconate-alkyne

    ITalk

    Others Inflammation/Immunology
    Itaconate-alkyne (ITalk) is a specific bioorthogonal probe for quantitative and site-specific chemoproteomic profiling of Itaconation in living cells. Itaconate-alkyne, a functional analogue of Itaconate, exhibits comparable antiinflammatory effect with Itaconate and enables the labeling of bona fide targets of Itaconate.
  • HY-P0069A
    L-JNKI-1

    JNK Neurological Disease
    L-JNKI-1 is a cell-permeable peptide inhibitor specific for JNK.
  • HY-10411
    AZ960

    JAK Apoptosis Parasite Virus Protease Cancer
    AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
  • HY-14981
    GSK2334470

    PDK-1 Cancer
    GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
  • HY-50759
    Ispinesib

    SB-715992

    Kinesin Apoptosis Cancer
    Ispinesib is a specific inhibitor of kinesin spindle protein (KSP), with a Ki app of 1.7 nM.
  • HY-16450
    SB 204990

    ATP Citrate Lyase Metabolic Disease
    SB 204990 is a potent and specific inhibitor of ATP citrate lyase (ACLY) enzyme.
  • HY-141810
    MT-134

    Myosin Others
    MT-134 is a SkMII-specific inhibitor and has excellent exposure in muscles.
  • HY-12710A
    Rauwolscine hydrochloride

    α-Yohimbine hydrochloride; Corynanthidine hydrochloride; Isoyohimbine hydrochloride

    Adrenergic Receptor Neurological Disease Endocrinology
    Rauwolscine hydrochloride is a potent and specific α2 adrenergic receptor antagonist with a Ki of 12 nM.
  • HY-118539
    NSC12404

    LPL Receptor Others
    NSC12404 is a weak and specific LPA2 receptor agonist.
  • HY-N0666
    L-Aspartic acid

    Endogenous Metabolite Cardiovascular Disease
    L-Aspartic acid is is an amino acid, shown to be a suitable prodrug for colon-specific drug deliverly.
  • HY-112274
    M443

    Others Cancer
    M443 is an irreversible and specific inhibitor of MRK, with an IC50<125 nM.
  • HY-U00023
    NCX 1000

    Endogenous Metabolite Others
    NCX 1000 is a liver-specific NO donor compound derived from ursodeoxycholic acid (UDCA).
  • HY-12778
    Ivabradine metabolite N-Demethyl Ivabradine hydrochloride

    N-Demethyl ivabradine hydrochloride

    Drug Metabolite Cardiovascular Disease Endocrinology Cancer
    N-Demethyl Ivabradine Hcl is a metabolite of Ivabradine, which is a specific inhibitor of the funny channel.
  • HY-14885
    Eliglustat

    Genz 99067

    Others Metabolic Disease
    Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
  • HY-N9406
    Maltooctaose

    Others Others
    Maltooctaose, a specific-length maltooligosaccharide, can be produced by PFTA (Pyrococcus furiosus).
  • HY-12061
    KU-60019

    ATM/ATR Cancer
    KU-60019 is an improved ATM kinase-specific inhibitor with IC50 of 6.3 nM.
  • HY-102027
    FX1

    Bcl-2 Family Apoptosis Cancer
    FX1 is a potent and specific BCL6 inhibitor, with an IC50 of around 35 μM.
  • HY-P1001
    Ac-DEVD-CHO

    Caspase Cancer
    Ac-DEVD-CHO is a specific Caspase-3 inhibitor with a Ki value of 230 pM.
  • HY-P0248
    Kemptide

    PKA Metabolic Disease
    Kemptide is a synthetic heptapeptide that acts as a specific substrate for cAMP-dependent protein kinase (PKA).
  • HY-100193
    FK-448 Free base

    Proteasome Metabolic Disease
    FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM.
  • HY-P0264
    Avexitide

    Exendin (9-39)

    Glucagon Receptor Metabolic Disease
    Avexitide (Exendin (9-39)) is a specific and competitive GLP-1 receptor antagonist.
  • HY-U00178
    Idoxifene

    CB7432

    Estrogen Receptor/ERR Cancer
    Idoxifene (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM).
  • HY-13261
    A66

    PI3K Cancer
    A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
  • HY-15702
    HJC0350

    Others Cancer
    HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 µM.
  • HY-14885A
    Eliglustat hemitartrate

    Genz-112638; Eliglustat tartrate

    Others Metabolic Disease
    Eliglustat hemitartrate is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
  • HY-122635A
    T-448

    Histone Demethylase Neurological Disease
    T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
  • HY-15468
    IOX2

    HIF/HIF Prolyl-Hydroxylase Cancer
    IOX2 is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM.
  • HY-13688A
    PJ34

    PARP Cancer
    PJ34 is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.
  • HY-100676
    GRI977143

    LPL Receptor Caspase Cancer Inflammation/Immunology
    GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM .
  • HY-112667
    CU-CPT-9a

    Toll-like Receptor (TLR) Inflammation/Immunology
    CU-CPT-9a is a specific TLR8 antagonist, with an IC50 of 0.5 nM.
  • HY-P2286
    D-3

    Phosphatase Cancer
    D-3, a phosphorpeptide, is an efficient, simple, and specific iPSC-eliminating agent.
  • HY-15665
    XMD17-109

    ERK Cancer
    XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.
  • HY-12856
    GSK503

    Histone Methyltransferase Cancer
    GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Ki app values of 3 to 27 nM.
  • HY-B1056
    Procodazole

    Propazol; 2-Benzimidazolepropionic acid

    Bacterial Infection
    Procodazole is a non-specific active immunoprotective agent against viral and bacterial infections, used as a potentiator.
  • HY-15723
    NSC 23766

    Ras Cancer
    NSC 23766 is a cell-permeable, reversible and specific inhibitor of Rac GTPase, used for cancer treatment.
  • HY-15384
    Picoprazole

    Proton Pump Metabolic Disease
    Picoprazole is a specific inhibitor of H +/K +-ATPase with IC50 of 3.1±0.4 μM.
  • HY-13989
    b-AP15

    NSC 687852

    Deubiquitinase Apoptosis Cancer
    b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
  • HY-12758
    YHO-13351

    BCRP Cancer
    YHO-13351 is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  • HY-15878
    LDC000067

    LDC067

    CDK Apoptosis Cancer
    LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.
  • HY-N0379
    D-Mannose

    Endogenous Metabolite Others
    D-Mannose is a carbohydrate, which plays an important role in human metabolism, especially in the glycosylation of specific proteins.
  • HY-15412
    HhAntag

    Smo Cancer
    HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.
  • HY-135140
    Methyltetrazine-Amine

    Others Others
    Methyltetrazine-Amine, a tetrazine compound, is used for the site-specific dual functionalization of the resulting bioconjugates.
  • HY-13252
    MK-5108

    VX-689

    Aurora Kinase Autophagy Cancer
    MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC50 value of 0.064 nM.
  • HY-15700
    PluriSIn 1

    NSC 14613

    Stearoyl-CoA Desaturase (SCD) Apoptosis Cancer
    PluriSIn 1 (NSC 14613) is an inhibitor of stearoyl-coA desaturase (SCD), and is a pluripotent cell-specific inhibitor.
  • HY-131898
    PTIO

    Others Others
    PTIO is a specific scavenger of NO. PTIO reacts with •NO to form the corresponding imino nitroxides and NO2.
  • HY-16587
    Saridegib

    IPI-926; Patidegib

    Smo Cancer
    Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.
  • HY-13950
    S186

    Others Others
    S186 is a kind of sodium salts of calcium-acetylpropylamine phosphonate(APA); a new strontium-specific chelating agent.
  • HY-P2222
    DX600 TFA

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    DX600 TFA is an ACE2 specific inhibitor, and do not cross-react with ACE.
  • HY-N0189
    Aloe emodin

    Rhabarberone; 3-Hydroxymethylchrysazine

    Autophagy Cancer
    Aloe emodin is a hydroxyanthraquinone present in Aloe vera leaves, has a specific in vitro and in vivo antitumor activity.
  • HY-111647
    N2-Methylguanosine

    Nucleoside Antimetabolite/Analog Endogenous Metabolite Others
    N2-methylguanosine is a modified nucleoside that occurs at several specific locations in many tRNA's.
  • HY-121515A
    DPM-1001 trihydrochloride

    Phosphatase Metabolic Disease
    DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property.
  • HY-121515
    DPM-1001

    Phosphatase Metabolic Disease
    DPM-1001 is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 has anti-diabetic property.
  • HY-133869
    cGMP-HTL

    cGMP-HaloTag-ligand

    Autophagy Cancer
    cGMP-HTL contains a HT-ligand, a linker and the Cys-S-cGMP (autophagy tag). cGMP-HTL increases the K63-linked ubiquitination of mitochondria. AUTAC (autophagy-targeting chimera) is a novel targeted-clearance strategy that contains a degradation tag (guanine derivatives) and a warhead to provide target specificity.
  • HY-122635
    T-448 free base

    Histone Demethylase Neurological Disease
    T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons.
  • HY-P0214
    Autocamtide-2-related inhibitory peptide

    CaMK Autophagy Neurological Disease
    Autocamtide-2-related inhibitory peptide is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM.
  • HY-15699A
    SAR7334 hydrochloride

    TRP Channel Neurological Disease
    SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
  • HY-14846
    Litronesib

    LY2523355

    Kinesin Cancer
    Litronesib (LY2523355) is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity.
  • HY-16733
    Verinurad

    RDEA3170

    URAT1 Metabolic Disease
    Verinurad (RDEA3170) is a highly potent and specific URAT1 inhibitor with an IC50 of 25 nM.
  • HY-B1327A
    Chlortetracycline

    7-Chlorotetracycline

    Bacterial Antibiotic Infection
    Chlorotetracycline (7-Chlorotetracycline) is a specific and potent calcium ionophore antibiotic, inhibits binding of aminoacyl-tRNA to ribosomes.
  • HY-119368
    NPB

    Bcl-2 Family Cancer
    NPB is a specific and potent inhibitor of BAD phosphorylation at Ser99, with an IC50 of 0.41 μM.
  • HY-15699
    SAR7334

    TRP Channel Neurological Disease
    SAR7334 is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
  • HY-101073
    Salermide

    Sirtuin Apoptosis Cancer
    Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong cancer-specific apoptotic cell death.
  • HY-10550A
    Tariquidar methanesulfonate, hydrate

    XR9576 methanesulfonate, hydrate

    P-glycoprotein Cancer
    Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.
  • HY-15842
    SF1670

    PTEN Phosphatase Autophagy Cancer
    SF1670 is a potent and specific phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor.
  • HY-120929
    BI8622

    E1/E2/E3 Enzyme Cancer
    BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM.
  • HY-N0666C
    L-Aspartic aicd sodium

    Sodium L-aspartate

    Endogenous Metabolite Others
    L-Aspartic aicd sodium is is an amino acid, shown to be a suitable prodrug for colon-specific drug deliverly.
  • HY-111680
    Nesolicaftor

    PTI-428

    CFTR Autophagy Endocrinology
    Nesolicaftor (PTI-428) is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier.
  • HY-106992
    S 3304

    MMP Cancer
    S 3304 is a novel matrix metalloproteinases (MMP) inhibitor specific for MMP-2 and MMP-9.
  • HY-112680A
    Carboxy pyridostatin trifluoroacetate salt

    Others Cancer
    Carboxy pyridostatin trifluoroacetate salt has the peculiarity to exhibit high molecular specificity for RNA over DNA G4s.
  • HY-12466
    Z-DEVD-FMK

    Caspase Cancer
    Z-DEVD-FMK is a specific and irreversible caspase-3 inhibitor with an IC50 of 18 μM.
  • HY-120204
    BI8626

    E1/E2/E3 Enzyme Cancer
    BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 0.9 μM.
  • HY-12758A
    YHO-13351 free base

    BCRP Cancer
    YHO-13351 free base is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  • HY-101465
    AK-1

    Sirtuin Neurological Disease
    AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor, with an IC50 of 12.5 μM.
  • HY-17551
    NMDA

    N-Methyl-D-aspartic acid

    iGluR Endogenous Metabolite Neurological Disease
    NMDA is a specific agonist for NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor.
  • HY-B1327
    Chlortetracycline hydrochloride

    7-Chlorotetracycline hydrochloride

    Bacterial Antibiotic Infection
    Chlortetracycline hydrochloride (7-Chlorotetracycline hydrochloride) is a specific and potent calcium ionophore antibiotic, inhibits binding of aminoacyl-tRNA to ribosomes.
  • HY-10242
    Ciluprevir

    BILN 2061; BILN 2061ZW

    HCV HCV Protease Infection
    Ciluprevir(BILN 2061) is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease with an IC50 of 3.0 nM.
  • HY-114672
    MBCQ

    Phosphodiesterase (PDE) Cardiovascular Disease
    MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ lacks inhibitory activity toward other PDE isozymes (all IC50s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE.
  • HY-100675
    JTE-013

    LPL Receptor Apoptosis Cancer
    JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively.
  • HY-B0084
    Dienogest

    STS 557

    Progesterone Receptor Autophagy Apoptosis Endocrinology Cancer
    Dienogest(STS-557) is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis.
  • HY-70072
    D609

    Phospholipase Cancer
    D609 is a selective competitive inhibitor of phosphatidyl choline-specific phospholipase C (PC-PLC), with Ki of 6.4 μM.
  • HY-14774
    Monepantel

    AAD1566

    nAChR Cancer
    Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
  • HY-117226A
    GSK 690 Hydrochloride

    Histone Demethylase Others
    GSK 690 (Hydrochloride) is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
  • HY-P0291
    Kemptide Phospho-Ser5

    PKA Others
    Kemptide (Phospho-Ser5) is a phosphate acceptor peptide that serves as a specific substrate for cAMP-dependent protein kinase (PKA).
  • HY-100673
    LM22A-4

    Trk Receptor Neurological Disease
    LM22A-4 is a specific agonist of tyrosine kinase receptor B, used for neurological disease research.
  • HY-128939
    EC0488

    Antifolate Cancer
    EC0488 is used to synthesize EC0531 with folate receptor (FR)-specific and anti-tumor activities.
  • HY-P0214A
    Autocamtide-2-related inhibitory peptide TFA

    CaMK Autophagy Neurological Disease
    Autocamtide-2-related inhibitory peptide (TFA) is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM.
  • HY-103085
    T-3775440 hydrochloride

    Histone Demethylase Cancer
    T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 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-14914
    Azilsartan

    TAK-536

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    Azilsartan(TAK-536) is a specific and potent angiotensin II type 1 receptor antagonist with IC50 of 2.6 nM.
  • HY-101510
    F1063-0967

    Phosphatase Cancer
    F1063-0967 is a Dual-specificity phosphatase 26 (DUSP26) inhibitor with an IC50 of 11.62 μM.
  • HY-117410
    Vipivotide tetraxetan

    PSMA-617

    Drug-Linker Conjugates for ADC Cancer
    Vipivotide tetraxetan (PSMA-617) is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM.
  • HY-12827
    Sortin1

    Others Others
    Sortin1 is a chemical genetic-hit molecule that causes specific mislocalization of plant and yeast-soluble and membrane vacuolar markers.
  • HY-15323
    PRT062607 Hydrochloride

    P505-15 Hydrochloride

    Syk Cancer
    PRT062607 Hydrochloride (P505-15 Hydrochloride) is a highly specific and potent inhibitor of purified Syk (IC50 1-2 nM).
  • HY-113225
    Guanosine triphosphate

    SARS-CoV Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Cancer Infection
    Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
  • HY-128140
    Z-FY-CHO

    Z-Phe-Tyr-CHO

    Cathepsin Metabolic Disease Neurological Disease
    Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor.
  • HY-N2332A
    Methyllycaconitine citrate

    MLA

    nAChR Neurological Disease
    Methyllycaconitine citrate is a specific antagonist of α7 neuronal nicotinic acetylcholine receptor (α7nAChR).
  • HY-137817
    BCH001

    DNA/RNA Synthesis Metabolic Disease
    BCH001, a quinoline derivative, is a specific PAPD5 inhibitor. BCH001 restores telomerase activity and telomere length in dyskeratosis congenita (DC) induced pluripotent stem cells. BCH001 shows no inhibition of poly(A)-specific ribonuclease (PARN) or several other canonical and non-canonical polynucleotide polymerases. BCH001 is used to regulate aging.
  • HY-15798
    UNC2881

    TAM Receptor Cardiovascular Disease
    UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM.
  • HY-10109
    AS-605240

    PI3K Autophagy Cancer
    AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.
  • HY-100546A
    GSK-LSD1 dihydrochloride

    Histone Demethylase Monoamine Oxidase Cancer
    GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
  • HY-15144
    Trichostatin A

    TSA

    HDAC Cancer
    Trichostatin A (TSA) is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.
  • HY-12808
    STF-118804

    NAMPT Apoptosis Cancer
    STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.
  • HY-12635
    SP2509

    Histone Demethylase Apoptosis Cancer
    SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with an IC50 of 13 nM.
  • HY-10590
    TWS119

    GSK-3 Autophagy Neurological Disease Cancer
    TWS119 is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
  • HY-15801
    HG-14-10-04

    ALK Cancer
    HG-14-10-04 (example 10) is a potent and specific ALK inhibitor with an IC50 of 20 nM.
  • HY-13033
    CDK-IN-2

    CDK inhibitor II

    CDK Cancer
    CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4.
  • HY-120007
    JC124

    NOD-like Receptor (NLR) Inflammation/Immunology Neurological Disease
    JC124 is a specific NLRP3 inflammasome inhibitor. JC124 has anti-inflammatory and neuroprotective effects.
  • HY-16931
    SMIFH2

    Others Cancer
    SMIFH2 is a formin specific inhibitor. SMIFH2 inhibits actin polymerization by Formins and affects the actin cytoskeleton.
  • HY-113821
    1-Naphthyl phosphate potassium salt

    Phosphatase Others
    1-Naphthyl phosphate potassium salt is a non-specific phosphatase inhibitor. 1-Naphthyl phosphate potassium salt decreases the splice-correcting effect.
  • HY-101820
    Simotinib

    EGFR Cancer
    Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
  • HY-B0689
    Indinavir

    MK-639; L-735524

    HIV HIV Protease Inflammation/Immunology
    Indinavir(MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
  • HY-P0278
    RGD

    Integrin Cancer
    RGD is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; binds to integrins.
  • HY-17545
    LGK974

    WNT974

    Porcupine Cancer
    LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM.
  • HY-42360
    SMCC

    ADC Linkers Cancer
    SMCC is a protein crosslinker. SMCC-conjugated antigen coupled spleen cells to induce antigen-specific immune responses.
  • HY-113251
    2-Hydroxyestrone

    Catecholestrone

    Endogenous Metabolite Estrogen Receptor/ERR Cancer Endocrinology
    2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic.
  • HY-131904
    POMHEX

    Enolase Apoptosis Cancer Metabolic Disease
    POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX, is a potent, ENO2-specific inhibitor of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis inhibitor.
  • HY-15766A
    GNE-617 hydrochloride

    NAMPT Cancer
    GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
  • HY-B0744
    Eflornithine

    DFMO; MDL71782; RMI71782; α-difluoromethylornithine

    Others Infection
    Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
  • HY-15685
    Ripasudil

    K-115

    ROCK Neurological Disease
    Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
  • HY-50736
    DUB-IN-1

    Deubiquitinase Cancer
    DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8.
  • HY-B0744A
    Eflornithine hydrochloride

    DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; α-difluoromethylornithine hydrochloride

    Others Infection
    Eflornithine hydrochloride is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
  • HY-15698A
    CRT0066101 dihydrochloride

    PKD Cancer
    CRT0066101 dihydrochloride is a potent and specific PKD inhibitor with IC50 values of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.
  • HY-W004206
    2-(4-Methoxyphenyl)acetic acid

    4-Methoxyphenylacetic acid

    Endogenous Metabolite Cancer
    2-(4-Methoxyphenyl)acetic acid is a plasma metabolite, with high sensitivity and specificity value as a biomarker for discriminating between NSCLC and healthy controls.
  • HY-A0122
    Plicamycin

    Mithramycin A

    DNA/RNA Synthesis Bacterial Antibiotic Cancer Infection
    Plicamycin is a selective specificity protein 1 (Sp1) inhibitor. Plicamycin inhibits the growth of various cancers by decreasing Sp1 protein.
  • HY-P0266
    N-Acetyl-Ser-Asp-Lys-Pro

    Ac-SDKP

    Angiotensin-converting Enzyme (ACE) Inflammation/Immunology Cardiovascular Disease
    N-Acetyl-Ser-Asp-Lys-Pro, an endogenous tetrapeptide secreted by bone marrow, is a specific substrate for the N-terminal site of ACE.
  • HY-12642
    Diethylcarbamazine citrate

    Parasite Infection
    Diethylcarbamazine citrate is an inhibitor of arachidonic acid metabolism in filarial microfilaria; is highly specific for several parasites and does not contain any toxic metallic elements.
  • HY-50295
    CI-1040

    PD 184352

    MEK Apoptosis Cancer
    CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
  • HY-107709
    MK-4074

    Acetyl-CoA Carboxylase Metabolic Disease
    MK-4074 is a liver-specific inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC50 values of approximately 3 nM.
  • HY-P0278A
    RGD Trifluoroacetate

    Integrin Cancer
    RGD Trifluoroacetate is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; RGD Trifluoroacetate binds to integrins.
  • HY-N1724
    Concanamycin A

    Antibiotic X 4357B; Concanamycin; X 4357B

    Proton Pump Bacterial Antibiotic Cancer Infection
    Concanamycin A (Antibiotic X 4357B) is a macrolide antibiotic and a specific vacuolar type H +-ATPase (V-ATPase) inhibitor.
  • HY-15766
    GNE-617

    NAMPT Metabolic Disease Cancer
    GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
  • HY-130801
    5-Hydroxy-2'-deoxyuridine

    5-OHdU

    Endogenous Metabolite Metabolic Disease
    5-Hydroxy-2'-deoxyuridine (5-OHdU) is a major stable oxidation product of 2'-Deoxycytidine. 5-Hydroxy-2'-deoxyuridine can be incorporated into DNA in vitro by DNA polymerase.
  • HY-U00346
    DPP-IV-IN-1

    Dipeptidyl Peptidase Metabolic Disease
    DPP-IV-IN-1 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), a highly specific serine protease, with an IC50 of 4.6 nM.
  • HY-100523
    ML385

    Keap1-Nrf2 Ferroptosis Cancer
    ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.
  • HY-50710
    KU-0063794

    mTOR Cancer
    KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC50s of 10 nM.
  • HY-P1505
    C3a (70-77)

    Complement 3a (70-77)

    Complement System Inflammation/Immunology
    C3a (70-77) is an octapeptide corresponding to the COOH terminus of C3a, exhibits the specificity and 1 to 2% biologic activities of C3a.
  • HY-139742
    ADTL-SA1215

    Sirtuin Cancer
    ADTL-SA1215 is a first-in-class specific small-molecule activator of SIRT3 that modulates autophagy in triple negative breast cancer.
  • HY-110164
    AdipoRon hydrochloride

    Adiponectin Receptor Metabolic Disease
    AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with Kds of 1.8 and 3.1 μM, respectively.
  • HY-10502A
    Tipifarnib (S enantiomer)

    IND-58359 S enantiomer; (S)-(-)-R-115777

    Farnesyl Transferase Cancer
    Tipifarnib S enantiomer is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM. Tipifarnib S enantiomer is the less active isomer.
  • HY-106855
    Almokalant

    H 234​/09

    Potassium Channel Cardiovascular Disease
    Almokalant is a class III antiarrhythmic drug, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K + current.
  • HY-P0266A
    N-Acetyl-Ser-Asp-Lys-Pro TFA

    Ac-SDKP TFA

    Angiotensin-converting Enzyme (ACE) Inflammation/Immunology Cardiovascular Disease
    N-Acetyl-Ser-Asp-Lys-Pro (TFA), an endogenous tetrapeptide secreted by bone marrow, is a specific substrate for the N-terminal site of ACE.
  • HY-100350
    CA-074 methyl ester

    CA-074Me

    Cathepsin Neurological Disease Cancer
    CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.
  • HY-N6789
    KT5720

    PKA Bacterial Antibiotic Infection Endocrinology Metabolic Disease
    KT5720 is a cell-permeable, potent, specific, reversible, ATP-competitive inhibitor of protein kinase A (PKA), with a Ki of 60 nM.
  • HY-136583
    28-Epirapamycin

    Others Others
    28-Epirapamycin is an impurity of Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells.
  • HY-B0202S
    Irbesartan D4

    SR-47436 D4; BMS-186295 D4

    Angiotensin Receptor Endocrinology Cardiovascular Disease
    Irbesartan D4 is the deuterium labeled Irbesartan, which is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist.
  • HY-18669
    ML346

    HSP Cancer
    ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 induces specific increases in genes and protein effectors of the heat shock response (HSR), including chaperones such as Hsp70, Hsp40, and Hsp27.
  • HY-W041171
    3-Chloro-L-tyrosine

    Endogenous Metabolite Others
    3-Chloro-L-tyrosine is a specific marker of myeloperoxidase-catalyzed oxidation, and is markedly elevated in low density lipoprotein isolated from human atherosclerotic intima.
  • HY-B0517A
    Mepivacaine hydrochloride

    Sodium Channel Neurological Disease
    Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
  • HY-12782T
    Iadademstat dihydrochloride

    ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride

    Histone Demethylase Cancer
    Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
  • HY-126653
    Atpenin A5

    Potassium Channel Cardiovascular Disease
    Atpenin A5 is a potent and highly specific complex II inhibitor (IC50 ~10 nM), and is an effective mKATP channel agonist and cardioprotective agent.
  • HY-15359
    Episilvestrol

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    Episilvestrol is a derivative of silvestrol, isolated from the fruits and twigs of Aglaia silvestris, and is a specific eIF4A-targeting translation inhibitor, with antitumor activity.
  • HY-110377
    Tariquidar dihydrochloride

    XR9576 dihydrochloride

    P-glycoprotein Cancer
    Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).
  • 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-111376
    Pyrrophenone

    Phospholipase Inflammation/Immunology Cardiovascular Disease
    Pyrrophenone is a potent and specific cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 4.2 nM.
  • HY-19522
    Seladelpar

    MBX-8025

    PPAR Metabolic Disease
    Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.
  • HY-18658
    Siremadlin

    NVP-HDM201; HDM201

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    Siremadlin (NVP-HDM201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
  • HY-112128
    USP7-IN-3

    Deubiquitinase Cancer
    USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor.
  • HY-10550
    Tariquidar

    XR9576

    P-glycoprotein Cancer
    Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).
  • HY-126047A
    (R,S)-Anatabine

    Others Inflammation/Immunology
    (R,S)-Anatabine is a a minor tobacco alkaloid found in the Solanaceae family of plants that can be used as a specific marker for the detection of tobacco use.
  • HY-U00128
    PPA-904

    Parasite Infection Inflammation/Immunology
    PPA-904 is a specific phenothiazine photosensitizer in photodynamic therapy (PDT) research, especially topical application for cutaneous leishmaniasis in vivo.
  • 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-131018
    Jedi2

    Others Inflammation/Immunology Neurological Disease
    Jedi2 is a Piezo1 activator, but not a specific Piezo2 activator. Jedi2 binds to the mouse Piezo1 proteins with a Kd of 2770  μM.
  • 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-B0744B
    Eflornithine hydrochloride hydrate

    DFMO hydrochloride hydrate; MDL-71782 hydrochloride hydrate; RMI-71782 hydrochloride hydrate; α-difluoromethylornithine hydrochloride hydrate

    Others Cancer
    Eflornithine hydrochloride hydrate (DFMO hydrochloride hydrate) is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine hydrochloride hydrate is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
  • HY-N0663
    Talatisamine

    Potassium Channel Neurological Disease
    Talatisamine, a aconitum alkaloid, is specific K + channel blocker. Talatisamine attenuates beta-amyloid oligomers induced neurotoxicity in cultured cortical neurons.
  • HY-114258
    LY3295668

    AK-01

    Aurora Kinase Cancer
    LY3295668 (AK-01) is a potent, orally active and highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively.
  • HY-114415
    AWZ1066S

    Parasite Infection
    AWZ1066S is a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis, with an EC50 of 2.5 nM in cell assay.
  • HY-12325
    GSK2194069

    Others Cancer
    GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM in an assay detecting released CoA.
  • HY-115453
    UBCS039

    Sirtuin Autophagy Cancer
    UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM.
  • HY-17402
    Nisoldipine

    BAY-k 5552

    Calcium Channel Reactive Oxygen Species Cardiovascular Disease
    Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.
  • HY-12444
    Y15

    FAK Inhibitor 14

    FAK Cancer
    Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
  • HY-123600
    SRI-29329

    CDK Others
    SRI-29329 is a specific CLK inhibitor, with IC50 values of 78 nM, 16 nM and 86 nM for CLK1, CLK2 and CLK4, respectively.
  • HY-14560C
    Reboxetine mesylate

    FCE20124 mesylate; PNU155950E mesylate

    Adrenergic Receptor Neurological Disease
    Reboxetine mesylate (FCE20124 mesylate) is a potent, selective, and specific noradrenaline reuptake inhibitor (NARI) for the research of depression. Reboxetine mesylate inhibits the uptake of norepinephrine, with a Ki of 8 nM.
  • HY-P1727
    Super-TDU

    YAP Cancer
    Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model.
  • HY-N1470
    Plantagoside

    Others Metabolic Disease
    Plantagoside, isolated from the seeds of Plantago asiatica, is a specific and non-competitive inhibitor for jack bean α-mannosidase, with an IC50 of 5 μM.
  • HY-15667
    P005091

    P5091

    Deubiquitinase Cancer
    P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.
  • HY-19960
    BCTC

    TRP Channel Cancer
    BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
  • HY-111048
    Corin

    Histone Demethylase HDAC Cancer
    Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
  • HY-18658A
    Siremadlin (R Enantiomer)

    NVP-HDM201 (R Enantiomer); HDM201 (R Enantiomer)

    Others Others
    Siremadlin R Enantiomer (NVP-HDM201 R Enantiomer) is the R enantiomer of Siremadlin. Siremadlin is a potent and highly specific MDM-2/p53 inhibitor.
  • HY-19303
    CRA-2059

    Ser/Thr Protease Inflammation/Immunology
    CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).
  • HY-114380
    Radioprotectin-1

    LPL Receptor Others
    Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA2), with an EC50 value of 25 nM for murine LPA2 subtype.
  • HY-12806
    AG1557

    EGFR Cancer
    AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194.
  • HY-101924
    AVN-492

    5-HT Receptor Neurological Disease
    AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
  • HY-50714
    Quiflapon sodium

    MK-591 sodium

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
  • HY-112623
    Vafidemstat

    ORY-2001

    Histone Demethylase Monoamine Oxidase Neurological Disease
    Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.
  • HY-N7707
    Sandacanol

    Apoptosis Cancer
    Sandacanol is a specific agonist of olfactory receptor (OR10H1). Sandacanol induces cell cycle arrest and some apoptosis in bladder cancer cells.
  • HY-19612B
    DDP-38003 trihydrochloride

    Histone Demethylase Cancer
    DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
  • HY-N3710
    Dehydrocrenatidine

    Kumujian G; O-Methylpicrasidine I

    JAK Apoptosis Cancer Neurological Disease
    Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain.
  • HY-122903B
    (+)-TK216

    DNA/RNA Synthesis Others
    (+)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor.
  • HY-13455
    LDN-192960

    Haspin Kinase DYRK Cancer
    LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
  • HY-19612A
    DDP-38003 dihydrochloride

    Histone Demethylase Cancer
    DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
  • HY-112915
    Eg5 Inhibitor V, trans-24

    Kinesin Cancer
    Eg5 Inhibitor V, trans-24 is a potent and specific kinesin Eg5 inhibitor with an IC50 of 0.65 μM, and can be used in the research of cancer.
  • HY-18632
    GSK2879552

    Histone Demethylase Cancer
    GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.
  • HY-19303B
    CRA-2059 TFA

    Ser/Thr Protease Inflammation/Immunology
    CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).
  • HY-109987
    ISPA-28

    Parasite Infection
    ISPA-28 is a specific plasmodial surface anion channel (PSAC) antagonist. ISPA-28 binds directly and reversibly to CLAG3.
  • HY-19303A
    CRA-2059 hydrochloride

    Ser/Thr Protease Inflammation/Immunology
    CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).
  • HY-10561
    RU 58841

    PSK-3841; HMR-3841

    Androgen Receptor Endocrinology
    RU 58841 (PSK-3841) is a specific androgen receptor antagonist or anti-androgen. RU 58841 (PSK-3841) has a dramatic effect on hair regrowth.
  • HY-13455A
    LDN-192960 hydrochloride

    Haspin Kinase DYRK Cancer
    LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
  • HY-Y1750
    β-Aminopropionitrile

    Monoamine Oxidase Cancer
    β-Aminopropionitrile is a specific and irreversible lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile targets the active site of LOX or LOXL isoenzymes.
  • HY-15685A
    Ripasudil free base

    K-115 (free base)

    ROCK Neurological Disease
    Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
  • HY-16709
    USP7-IN-1

    Deubiquitinase Cancer
    USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, and can be used for the research of cancer.
  • HY-16558
    Butein

    2’,3,4,4’-tetrahydroxy Chalcone

    EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
  • 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-14622A
    Necrostatin 2 racemate

    Necrostatin 1S; Nec-1S; 7-Cl-O-Nec1

    RIP kinase Cancer
    Necrostatin 2 racemate (Nec-1S), the Nec-1 stable, is a potent and specific RIPK1 inhibitor lacking the IDO-targeting effect.
  • HY-101284
    DMU2105

    Cytochrome P450 Cancer
    DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
  • HY-128113
    AG-09/1

    Others Inflammation/Immunology
    AG-09/1 is a specific formyl peptide receptor 1 (FPR1) agonist. N-formyl peptide receptors (FPR) are important in host defense.
  • HY-108522
    PA452

    RAR/RXR Metabolic Disease
    PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.
  • 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-12424A
    42-(2-Tetrazolyl)rapamycin

    Others Cancer
    42-(2-Tetrazolyl)rapamycin is a prodrug compound of a rapamycin analog extracted from patent US 20080171763 A1, Example 1. Rapamycin is a specific mTOR inhibitor.
  • HY-103087
    FIN56

    Ferroptosis Others
    FIN56 is a specific inducer of ferroptosis. FIN56 induces ferroptosis by inducing degradation of GPX4. FIN56 also binds to and activates squalene synthase.
  • HY-110063
    4-IPP

    4-Iodo-6-phenylpyrimidine

    Others Metabolic Disease
    4-IPP (4-Iodo-6-phenylpyrimidine) is a specific suicide substrate and irreversible inhibitor of macrophage migration inhibitory factor (MIF).
  • HY-P1727A
    Super-TDU TFA

    YAP Cancer
    Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model.
  • HY-N8460
    Cortisol sulfate

    Cortisol 21-sulfate

    Endogenous Metabolite Endocrinology
    Cortisol sulfate (Cortisol 21-sulfate) is a metabolite of Cortisol (HY-N0583). Cortisol sulfate is a specific ligand for intracellular transcortin.
  • HY-101285
    DMU2139

    Cytochrome P450 Cancer
    DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
  • HY-W018161
    Hexadecanedioic acid

    Endogenous Metabolite Others
    Hexadecanedioic acid is covalently linked to Sepharose 4B, shows better performance in terms of specificity than dye-based resins and could be used for depletion of SA from plasma samples.
  • HY-17446
    Icatibant

    HOE 140

    Bradykinin Receptor Endocrinology
    Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM 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-14261S
    Vilazodone D8

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.
  • HY-110277
    S2101

    Histone Demethylase Cancer
    S2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.
  • HY-108896
    Icatibant acetate

    HOE 140 acetate

    Bradykinin Receptor Inflammation/Immunology
    Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with an IC50 and Ki of 1.07 nM and 0.798 nM respectively.
  • HY-13299A
    MK-8033 hydrochloride

    c-Met/HGFR Cancer
    MK8033 Hcl is a novel and specific dual ATP competitive c-Met/Ron inhibitor (IC50=1 nM Wt c-Met) under investigation as a treatment for cancer.
  • HY-15027
    5-Aminosalicylic Acid

    Mesalamine; 5-ASA; Mesalazine

    PPAR PAK NF-κB Endogenous Metabolite Inflammation/Immunology Cancer
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-103591
    DUPA(OtBu)-OH

    Others Cancer
    DUPA(OtBu)-OH is a DUPA precursor. DUPA is used as the targeting moiety to actively deliver Docetaxel (DTX) for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.
  • HY-16663
    ITX3

    Others Others
    ITX3 is a specific and nontoxic inhibitor of the TrioN (N-terminal GEF domain of the multidomain Trio protein) with IC50 of 76 uM; inhibits TrioN-stimulated RhoG exchange in vitro.
  • HY-70083
    SPK-601

    LMV-601

    Phospholipase Reverse Transcriptase Infection
    SPK-601 (LMV-601) is an inhibitor of the phosphatidylcholine-specific phospholipase C (PC-PLC). SPK-601 also can be used as an antimicrobial agent.
  • HY-W001909
    Myosmine

    nAChR Metabolic Disease
    Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM.
  • HY-14566
    Donepezil

    E2020 free base

    AChE Neurological Disease
    Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively.
  • HY-14841
    Gisadenafil

    UK-369003

    Phosphodiesterase (PDE) Neurological Disease
    Gisadenafil (UK-369003) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).
  • 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-15969
    Sal003

    Phosphatase Apoptosis Cancer
    Sal003 is a potent, specific and cell-permeable inhibitor of the eukaryotic translation initiation factor 2α (eIF2α) phosphatase. Sal003 is a derivative of salubrinal.
  • HY-14914S
    Azilsartan D5

    TAK-536 D5

    Angiotensin Receptor Others
    Azilsartan D5 (TAK-536 D5) is the deuterium labeled Azilsartan(TAK-536), which is a specific and potent angiotensin II type 1 receptor antagonist.
  • HY-124330
    Tripolin A

    (E)-Tripolin A

    Aurora Kinase Others
    Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively.
  • HY-141677
    INCB059872

    Histone Demethylase Cancer
    INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia.
  • HY-13299
    MK-8033

    c-Met/HGFR Cancer
    MK-8033 is a novel and specific dual ATP competitive c-Met/Ron inhibitor (IC50=1 nM Wt c-Met) under investigation as a treatment for cancer.
  • HY-15613
    Maritoclax

    Marinopyrrole A

    Bcl-2 Family Cancer
    Maritoclax (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).
  • HY-100927
    Ro 20-1724

    Ro 20-174

    Phosphodiesterase (PDE) Neurological Disease
    Ro 20-1724 (Ro 20-174) is a potent inhibitor of cAMP-specific phosphodiesterase (PDE4/PDE IV) with a Ki of 1930 nM. Neuroprotective effect.
  • HY-U00449
    AGN 193109

    RAR/RXR Autophagy Cancer
    AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.
  • HY-125934
    Allocholic acid

    Others Cancer
    Allocholic acid is a typically fetal bile acid found in vertebrates and reappears during liver regeneration and carcinogenesis. Allocholic acid is also a potent and specific stimulant of the adult olfactory system.
  • 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-101325
    BRL 37344 sodium

    BRL 37344A

    Adrenergic Receptor Metabolic Disease Endocrinology
    BRL 37344 sodium (BRL 37344A) is a specific β3-adrenergic receptor agonist. BRL 37344 sodium treatment significantly lowers the body weight of obese mice.
  • HY-132599
    Lademirsen

    SAR339375; RG-012

    MicroRNA Inflammation/Immunology
    Lademirsen (SAR339375; RG-012) is a highly specific antisense oligonucleotide (ASO) targeting miR-21. Lademirsen has the potential for Alport nephropathy research.
  • HY-P2287
    Cortagine

    CRFR Neurological Disease
    Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.
  • HY-111939
    Amiprofos methyl

    BAY-NTN 6867

    Microtubule/Tubulin Others
    Amiprofos methyl (BAY-NTN 6867) is a phosphoric amide herbicide. Amiprofos methyl is a specific and potent antimicrotubule agent. Amiprofos methyl directly poisons microtubule dynamics in plant cells.
  • HY-B1978
    Iprodione

    Fungal Reactive Oxygen Species Infection
    Iprodione, a dicarboximide fungicide, has a highly specific action, with a capacity to cause oxidative damage through production of free oxygen radicals (ROS). Iprodione does not appear to be species selective.
  • HY-W024604
    4,4-Dimethyl-2-cyclopenten-1-one

    4,4-Dimethylcyclopent-2-enone

    Others Cancer
    4,4-Dimethyl-2-cyclopenten-1-one, a natural compound from Apocyniveneti Folium, displays higher tumor-specific cytotoxicity.
  • HY-20349
    Monobehenin

    Bacterial Infection
    Monobehenin, an bacterial biofilm formation inhibitor, has strong inhibitory activity toward bacterial biofilm formation of S. mutans, X. oryzae, and Y. enterocolitica in a strain specific manner.
  • HY-15594
    Phen-DC3

    DNA/RNA Synthesis Cancer
    Phen-DC3 is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65±6 and 50±10 nM, respectively.
  • HY-100437
    HA15

    HSP Autophagy Apoptosis Cancer
    HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.
  • HY-18719B
    Endoxifen hydrochloride

    Estrogen Receptor/ERR Drug Metabolite Parasite Aromatase Cancer
    Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study.
  • HY-131252
    Dihydro Donepezil

    Dihydro E2020

    AChE Neurological Disease
    Dihydro Donepezil (Dihydro E2020) is a metabolite of Donepezil. Donepezil is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bAChE and hAChE, respectively.
  • HY-111605
    Macropa-NCS

    Others Cancer
    Macropa-NCS is conjugated to trastuzumab as well as to the prostate-specific membrane antigen-targeting compound RPS-070. A promising therapeutic radionuclide applied in the treatment of soft-tissue metastases.
  • HY-N8493
    Mycalolide B

    Others Others
    Mycalolide-B is a specific inhibitor of actomyosin ATPase isolated from marine sponge. Mycalolide-B inhibits ATP-induced contraction and Mg 2+-ATPase activity in the absence of Ca 2+.
  • HY-17038S
    Agomelatine-d6

    S-20098-d6

    Melatonin Receptor 5-HT Receptor Neurological Disease
    Agomelatine-d6 (S-20098-d6) is deuterium labeled Agomelatine. Agomelatine is a specific agonist of MT1 and MT2 receptors .
  • HY-P3066
    SKF 100398

    d(CH2)5Tyr(Et)VAVP

    Vasopressin Receptor Metabolic Disease
    SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP.
  • HY-128578
    KPLH1130

    PDHK Metabolic Disease Inflammation/Immunology
    KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice.
  • HY-12828
    KH-CB19

    CDK Cancer
    KH-CB19 is a potent and highly specific inhibitor of the CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4).
  • HY-108619
    Gisadenafil besylate

    UK 369003-26

    Phosphodiesterase (PDE) Neurological Disease
    Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).
  • HY-114702
    M77976

    PDHK Metabolic Disease
    M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes.
  • HY-18719E
    Endoxifen

    Estrogen Receptor/ERR Aromatase Drug Metabolite Parasite Cancer
    Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study.
  • HY-18632A
    GSK2879552 dihydrochloride

    Histone Demethylase Cancer
    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
  • HY-107051
    GW 766994

    GW 994

    CCR Inflammation/Immunology Endocrinology
    GW 766994 (GW 994) is an orally active and specific chemokine receptor-3 (CCR3) antagonist. GW 766994 has the potential for asthma and eosinophilic bronchitis research.
  • HY-13917A
    PND-1186 hydrochloride

    VS-4718 hydrochloride; SR-2516 hydrochloride

    FAK Apoptosis Cancer
    PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis.
  • HY-13865
    P 22077

    Deubiquitinase Cancer
    P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. P 22077 also inhibits USP47 with an EC50 of 8.74 μM.
  • HY-15564
    AR 231453

    GPR119 Metabolic Disease
    AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s.
  • HY-15845
    STF-083010

    IRE1 Cancer
    STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
  • HY-B0517
    Mepivacaine

    Sodium Channel Neurological Disease
    Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
  • HY-129111
    EACC

    Autophagy Infection Neurological Disease
    EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion.
  • HY-P1674A
    Murepavadin TFA

    POL7080 TFA

    Bacterial Antibiotic Infection
    Murepavadin (TFA), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic for the treatment of bacterial infections caused by Pseudomonas aeruginosa. Murepavadin (TFA) targets the lipopolysaccharide transport portin D .
  • HY-134452
    MeAIB

    α-(Methylamino)isobutyric acid

    Others Others
    MeAIB (α-(Methylamino)isobutyric acid) is a specific substrate for amino acid transport system A (ATA1). ATA mediate the uptake of short-chain neutral amino acids in a Na +-dependent manner.
  • HY-15594A
    Phen-DC3 Trifluoromethanesulfonate

    Phen-DC3 Triflate

    G-quadruplex Cancer
    Phen-DC3 Trifluoromethanesulfonate is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65±6 and 50±10 nM, respectively.
  • HY-100690
    NSC16168

    Others Cancer
    NSC16168 is a specific inhibitor of ERCC1-XPF, with an IC50 value of 0.42 μM. NSC16168 inhibits DNA repair and potentiates CDDP efficacy in cancer.
  • HY-128522
    ARS-1323-alkyne

    Ras Cancer
    ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRAS G12C nucleotide state in living cells.
  • HY-138641
    Bavdegalutamide

    ARV-110

    Androgen Receptor Cancer
    Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer.
  • HY-125006
    TRi-1

    Others Cancer
    TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.
  • HY-13917
    PND-1186

    VS-4718; SR-2516

    FAK Apoptosis Cancer
    PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis.
  • HY-Y0520
    Itaconic acid

    Endogenous Metabolite Inflammation/Immunology
    Itaconic acid, a precursor of polymers, chemicals, and fuels, can be synthesized by many fungi. Itaconic acid also is a macrophage-specific metabolite. Itaconic acid mediates crosstalk between macrophage metabolism and peritoneal tumors.
  • HY-D0144
    Resorufin methyl ether

    Methoxyresorufin

    Cytochrome P450 Others
    Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate. Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents.
  • HY-19541
    I-CBP112

    Histone Acetyltransferase Epigenetic Reader Domain Cancer
    I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.
  • HY-107615
    TC LPA5 4

    LPL Receptor Cancer
    TC LPA5 4 is a LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 displays selectivity for LPA5 over 80 other screened drug targets. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells.
  • HY-B0713
    Amlexanox

    AA673; Amoxanox; CHX3673

    IKK Metabolic Disease
    Amlexanox (AA673; Amoxanox; CHX3673) is a specific inhibitor of IKKε and TBK1, and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM.
  • HY-B1218
    Sulfaphenazole

    Bacterial Infection
    Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
  • HY-13272
    Dacomitinib

    PF-00299804; PF-299804

    EGFR Apoptosis Cancer
    Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
  • HY-139056
    SU0268

    Others Cancer Infection Inflammation/Immunology
    SU0268 is a potent and specific inhibitor of 8-Oxoguanine DNA glycosylase 1 (OGG1). SU0268 regulates inflammatory responses during Pseudomonas aeruginosa infection.
  • HY-136595
    3,5-Difluoro-L-tyrosine

    Phosphatase Others
    3,5-Difluoro-L-tyrosine is a functional, tyrosinase-resistant mimetic of tyrosine. 3,5-Difluoro-L-tyrosine can be used to analyze the substrate specificity of protein tyrosine phosphatases (PTPs).
  • HY-111351
    MLK-IN-1

    Mixed Lineage Kinase Neurological Disease
    MLK-IN-1 is a potent, brain penetrant and specific mixed lineage kinase 3 (MLK-3) inhibitor, compound 68, extracted from patent US20140256733A1.
  • HY-18749
    SC79

    Akt Cancer Inflammation/Immunology Neurological Disease
    SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt.
  • HY-102076
    0990CL

    Others Others
    0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP.
  • HY-103473A
    Boc-MLF TFA

    Boc-Met-Leu-Phe-OH (TFA)

    Others Inflammation/Immunology
    Boc-MLF (TFA) is a peptide, used as a specific formyl peptide receptor (FPR) antagonist, also inhibits the signaling through formyl peptide receptor like 1 (FPRL1) at higher concentrations.
  • HY-N6910
    Pseudolaric Acid C2

    Others Metabolic Disease
    Pseudolaric Acid C2, a diterpenoid isolated from Pseudolarix kaempferi, is identified as the specific metabolite of Pseudolaric acid B in plasma, urine, bile and feces after both oral and intravenous administration to rats.
  • HY-101945
    A-69412

    Lipoxygenase Inflammation/Immunology
    A-69412 is a reversible, specific inhibitor of the 5-lipoxygenase (5-LO). A-69412 has the potential to treat asthma and ulcerative colitis, and possibly other inflammatory and allergic conditions.
  • HY-112951
    ChX710

    STING Cancer
    ChX710 could prime the type I interferon response to cytosolic DNA, which induces the ISRE promoter sequence, specific cellular Interferon-Stimulated Genes (ISGs), and the phosphorylation of Interferon Regulatory Factor (IRF) 3.
  • HY-U00462
    D-Mannoheptulose

    Others Metabolic Disease
    D-Mannoheptulose is a major non-structural carbohydrate in avocado. D-mannoheptulose is a specific inhibitor of D-glucose phosphorylation. D-Mannoheptulose can block insulin release and utilization of carbohydrate in rat.
  • HY-105917
    Endovion

    NS3728

    Chloride Channel Others
    Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
  • HY-135232
    MMP-9-IN-1

    MMP Cancer
    MMP-9-IN-1 is a specific matrix metalloproteinase-9 (MMP-9) inhibitor, which selectively target the hemopexin (PEX) domain of MMP-9, but not other MMPs.
  • HY-141729
    Biotin-NH-PSMA-617

    Others Cancer
    Biotin-NH-PSMA-617 is a biotin-tagged PSMA-617. PSMA-617 is a small molecule targeting the prostate-specific membrane antigen (PSMA), which is directly expressed by the tumor cells .
  • HY-W014081
    Ethyl 3-coumarincarboxylate

    Ethyl 2-oxo-2H-chromene-3-carboxylate

    Others Others
    Ethyl 3-coumarincarboxylate is a coumarin derivative. Ethyl 3-coumarincarboxylate can be used as a pseudo-template to give a molecularly imprinted polymer (MIP) that has a fairly specific recognition capability for aflatoxins.
  • HY-15469
    GW791343 dihydrochloride

    P2X Receptor Neurological Disease
    GW791343 dihydrochloride is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-120838
    Heptelidic acid

    Koningic acid

    Caspase Cancer Infection
    Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM.
  • HY-122903A
    (-)-TK216

    DNA/RNA Synthesis Cancer
    (-)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. (-)-TK216 has anti-cancer activity.
  • HY-13977A
    PKR-IN-C16

    Others Neurological Disease
    PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.
  • HY-101213
    OSW-1

    Others Cancer
    OSW-1, isolated from Ornithogalum caudatum, is a specific antagonist of osterol-binding protein (OSBP) and OSBP-related protein 4 (ORP4) with GI50s in the nanomolar range in human cancer lines.
  • HY-131256
    Cetirizine Impurity C

    Histamine Receptor Endocrinology Inflammation/Immunology
    Cetirizine Impurity C is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist[1] [2] .
  • HY-N2019
    Chaetocin

    Histone Methyltransferase Bacterial Antibiotic Cancer Infection
    Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC50 of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 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-128678
    ORM-10103

    Na+/Ca2+ Exchanger Cardiovascular Disease
    ORM-10103 is a specific inhibitor of the Na+/Ca2+ exchanger (NCX), which decreases the NCX current with estimated IC50s of 55 and 67 nM at -80 and at 20 mV, respectively.
  • HY-N1150
    Thymidine

    DThyd; NSC 21548

    DNA/RNA Synthesis Endogenous Metabolite Others
    Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
  • HY-P1505A
    C3a (70-77) (TFA)

    Complement 3a (70-77) (TFA)

    Complement System Inflammation/Immunology
    C3a (70-77) TFA (Complement 3a (70-77) TFA) is an octapeptide corresponding to the COOH terminus of C3a, exhibits the specificity and 1 to 2% biologic activities of C3a.
  • HY-129168
    USP7-IN-5

    Deubiquitinase Cancer
    USP7-IN-5 is a potent ubiquitin specific protease 7 (USP7) inhibitor extracted from patent WO2017212012A1, example 40, has an IC50 of 49.9 nM.
  • HY-129169
    USP7-IN-6

    Deubiquitinase Cancer
    USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM.
  • HY-128938
    EC1167

    Others Cancer
    EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC).
  • HY-P0224
    N-Formyl-Met-Leu-Phe

    fMLP; N-Formyl-MLF

    TNF Receptor Inflammation/Immunology
    N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.
  • HY-W007324
    Maleimide

    Others Cancer
    Maleimide can be used for production of antibody-drug conjugate (ADC) which is used in cancer research. Maleimide also be leveraged for the preparation of fluorogenic probe, which is mainly used for the specific detection of thiol analytes.
  • HY-18006
    NKP608

    Neurokinin Receptor Neurological Disease Endocrinology
    NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.
  • HY-15470
    GW791343 trihydrochloride

    P2X Receptor Neurological Disease
    GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-108697A
    (Rac)-PT2399

    HIF/HIF Prolyl-Hydroxylase Cancer
    (Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM.
  • HY-14823
    Sobetirome

    GC-1; QRX-431

    Thyroid Hormone Receptor Metabolic Disease Endocrinology
    Sobetirome (GC-1) is a thyroid hormone receptor β (TRβ)-specific agonist which bind selectively to TRβ-1 with an EC50 of 0.16 μM.
  • HY-101370
    2-Methylthio-ATP tetrasodium

    Others Metabolic Disease
    2-Methylthio-ATP tetrasodium is a non-specific P2-receptor agonist. 2-Methylthio-ATP tetrasodium causes noncompetitive inhibition of ADP-induced human platelet aggregation.
  • HY-19529
    Ro 46-2005

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.
  • HY-14902
    Tofogliflozin

    CSG452

    SGLT Metabolic Disease
    Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.
  • HY-106406
    Benzylacyclouridine

    BAU; 5-Benzylacyclouridine

    Others Cancer
    Benzylacyclouridine (BAU) is a potent and specific inhibitor of uridine phosphorylase, the first enzyme in the catabolism of uridine. Benzylacyclouridine can modulate the cytotoxic side effects of 5-fluorouracil (5-FU) and its derivatives.
  • HY-D0843
    N-Ethylmaleimide

    NEM

    Cathepsin Deubiquitinase Others
    N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
  • HY-126583
    Nemadipine-A

    Calcium Channel Cancer
    Nemadipine-A is a specific inhibitor of the EGL-19 L-type Ca 2+ channel. Nemadipine-A, a cell-permeable L-type calcium channel inhibitor, sensitizes TRAIL-resistant cancer cells to this ligand.
  • HY-15777A
    Ribociclib hydrochloride

    LEE011 hydrochloride

    CDK Cancer
    Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-100816
    Rbin-1

    Ribozinoindole-1

    Phosphatase Metabolic Disease
    Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
  • HY-111149A
    PS372424 hydrochloride

    CXCR Inflammation/Immunology
    PS372424 hydrochloride, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 hydrochloride prevents human T-cell migration in a humanized model of arthritic inflammation.
  • HY-15802
    WZ4003

    AMPK Cancer
    WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1 (ARK5)/NUAK2, without significant inhibition on other 139 kinases.
  • HY-W062696
    BC-1382

    E1/E2/E3 Enzyme Inflammation/Immunology
    BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity.
  • HY-122445
    Resorcinolnaphthalein

    Angiotensin-converting Enzyme (ACE) Inflammation/Immunology Cardiovascular Disease
    Resorcinolnaphthalein is a specific angiotensin-converting enzyme 2 (ACE2) enhancer and activates ACE2 activity with an EC50 value of 19.5 μM. Resorcinolnaphthalein can be used for the investigation of hypertension and renal fibrosis.
  • HY-137067
    IMT1B

    LDC203974

    Others Cancer
    IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.
  • HY-120140
    Ganoderic acid DM

    Apoptosis PI3K Cancer Metabolic Disease Inflammation/Immunology
    Ganoderic acid DM, a natural triterpenoid isolated from Ganoderma lucidum, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells. Ganoderic acid DM as a specific inhibitor of osteoclastogenesis.
  • HY-101253
    AM-92016 hydrochloride

    Others Cardiovascular Disease
    AM-92016 hydrochloride is a specific blocker of rectifier potassium current (IK). AM-92016 hydrochloride delays rectifier potassium channel (IK), repolarizes the membrane thereby restricting the duration of the nerve impulse thereby restricting the duration of the nerve impulse.
  • HY-111149
    PS372424

    CXCR Inflammation/Immunology
    PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 prevents human T-cell migration in a humanized model of arthritic inflammation.
  • HY-110182
    SP-141

    MDM-2/p53 Cancer
    SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells.
  • 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-W016087
    Monoethyl pimelate

    PROTAC Linkers Cancer
    Monoethyl pimelate is a PROTAC linker, which refers to the alkyl/ether composition. Monoethyl pimelate can be used in the synthesis of (S,R,S)-AHPC-Me-C7 ester, a specific BCL-XL PROTAC degrader.
  • HY-P1124
    AS2034178 free base

    GPR40 Metabolic Disease
    AS2034178 free base, a specific and orally active GPR40 agonist, exhibits glucose-dependent insulin secretion enhancement. AS2034178 free base has potential for type 2 diabetes mellitus research.
  • HY-15320
    NBI-74330

    CXCR Inflammation/Immunology Endocrinology
    NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of ( 125I)CXCL10 and ( 125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
  • HY-137655
    BMS-P5

    Protein Arginine Deiminase Cancer
    BMS-P5 is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model.
  • HY-12757
    YHO-13177

    BCRP Cancer
    YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.
  • HY-19522A
    Seladelpar sodium salt

    MBX-8025 sodium salt; RWJ-800025 sodium salt

    PPAR Metabolic Disease
    Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.
  • HY-118716
    PhIP

    Others Cancer
    PhIP is the most abundant of generation of heterocyclic amines (HCA), resulted in the cooking of meat. DNA damaging and mutagenic activities. PhIP also has oestrogenic activity that could contribute to its tissue specific carcinogenicity.
  • HY-121018
    Daltroban

    BM-13505; SKF 96148

    Prostaglandin Receptor Cardiovascular Disease
    Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury.
  • HY-136433
    N,N'-Dinitrosopiperazine

    1,4-Dinitrosopiperazine; DNP

    Others Cancer
    N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine; DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568.
  • HY-139245
    MC-Ala-Ala-Asn-PAB

    Others Cancer
    MC-Ala-Ala-Asn-PAB is a linker extracted from patent CN104147612A, page 14. MC-Ala-Ala-Asn-PAB can be used to synthesis the tumor microenvironment specific activated micromolecular targeted conjugate.
  • HY-101033
    GPR35 agonist 1

    Others Cancer Endocrinology
    GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
  • HY-B0461
    Trospium chloride

    mAChR Neurological Disease
    Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors.
  • HY-10588
    Bay K 8644

    Calcium Channel Neurological Disease
    Bay K 8644, a dihydropyridine compound, is a specific L-type Ca 2+ channel agonist. Bay K 8644 increases Ca2+ influx through sarcolemmal Ca 2+ channels by increasing the open time of the channel.
  • HY-B0503
    2-Thiouracil

    Thiouracil

    NO Synthase Endocrinology Cancer
    2-Thiouracil (Thiouracil) is an antithyroid compound. 2-Thiouracil can function as a highly specific melanoma seeker. 2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS) with a Ki of 20 μM.
  • HY-121381
    Kuraridine

    Phosphodiesterase (PDE) Others
    Kuraridine is a prenylated flavonol extract from the roots of Sophora flavescens. Kuraridine has an inhibitory effect on cGMP specific phosphodiesterase type 5 (PDE5) (IC50=0.64 μM).
  • HY-108477
    TMPyP4 tosylate

    TMP 1363

    G-quadruplex Telomerase Cancer
    TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines.
  • HY-112051
    CU-CPT9b

    Toll-like Receptor (TLR) Inflammation/Immunology
    CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM. CU-CPT9b shows high binding affinity towards TLR8 with a Kd of 21 nM.
  • HY-W011417
    Cinnabarinic acid

    mGluR Apoptosis Others
    Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.
  • HY-N1462
    Atractyloside potassium salt

    Others Cardiovascular Disease
    Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart.
  • HY-N7765
    Oenothein B

    HCV Bacterial Apoptosis Fungal Cancer Infection Inflammation/Immunology
    Oenothein B is a dimeric macrocyclic ellagitannin and has widely pharmacological activities, including antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor properties. Oenothein B is a potent and specific inhibitor of poly(ADP-ribose) glycohydrolase.
  • HY-123892
    RK-287107

    PARP Cancer
    RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.
  • HY-100596
    AS1842856

    Autophagy Metabolic Disease
    AS1842856, a specific Foxo1 inhibitor (IC50=30 nM), potently suppresses autophagy. AS1842856 only reduces the activity of FoxO1 by binding with it, without affecting its transcription and protein expression.
  • HY-107406
    Antimycin A1

    Mitochondrial Metabolism Cancer
    Antimycin A1 is a specific electron transfer inhibitor of ubiquinol-cytochrome c oxidoreductase. Antimycin A1 inhibits angiogenesis through decrease in VEGF production caused by inhibition of HIF-1α activation.
  • HY-107981
    LSN 3213128

    Antifolate Cancer
    LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.
  • HY-100737
    ML349

    Phospholipase Cancer
    ML349 is a potent and specific acyl protein thioesterase 2(APT2)/lysophospholipase 2 (LYPLA2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
  • HY-123979
    ζ-Stat

    NSC37044

    PKC Apoptosis Cancer
    ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
  • HY-115684
    2-Undecanol

    Undecan-2-ol

    Others Others
    2-Undecanol (Undecan-2-ol) is a male specific volatile identified from the sap beetle Lobiopa insularis. 2-undecanol is a flower emitted volatile, used by various species of Hymenoptera as a pheromone component.
  • HY-15777
    Ribociclib

    LEE011

    CDK Cancer
    Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • 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-W008129
    H-D-cis-Hyp-OH

    Endogenous Metabolite Metabolic Disease
    cis-4-Hydroxy-D-proline is a precursor of conformationally restricted PNA adenine monomer. cis-4-Hydroxy-D-proline can be used to study the specificity and kinetics of D-alanine dehydrogenase.
  • HY-15777C
    Ribociclib succinate hydrate

    LEE011 succinate hydrate

    CDK Cancer
    Ribociclib succinate hydrate (LEE011 succinate hydrate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-15777B
    Ribociclib succinate

    LEE011 succinate

    CDK Cancer
    Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-111066A
    JNJ-37822681 dihydrochloride

    Dopamine Receptor Neurological Disease
    JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2L receptor (Ki =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder.
  • HY-135280
    CB1 inverse agonist 1

    Cannabinoid Receptor Metabolic Disease
    CB1 inverse agonist 1 is a highly potent, orally active, and specific inverse agonist of CB1 receptor with IC50s of 7.5 nM and 4100 nM for CB1 and CB2 receptors, respectively. Anorexigenic effects.
  • HY-128900
    11-cis-Vaccenyl acetate

    Endogenous Metabolite Others
    11-cis-Vaccenyl acetate is male-specific lipid that mediates aggregation behavior in both male and female flies, which activates a few dozen olfactory neurons located in T1 sensilla on the antenna of both male and female flies.
  • HY-120072
    PF-3450074

    PF-74

    HIV Infection
    PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
  • HY-12684
    CH-223191

    Aryl Hydrocarbon Receptor Cancer
    CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM.
  • HY-108555
    FR-171113

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM..
  • HY-128347
    M‑89

    Epigenetic Reader Domain Cancer Inflammation/Immunology
    M-89 is a highly potent and specific menin inhibitor, with a Kd of 1.4 nM for binding to menin. M-89 inhibits the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction and has potential to treat MLL leukemia.
  • HY-12345
    ML365

    Potassium Channel Cardiovascular Disease
    ML365 is a selective two-pore domain potassium channel KCNK3/TASK1 inhibitor, with an IC50 of 4 nM. ML365 acts as a pharmacological tool that can be used to examine the specific roles of TASK1 channels.
  • HY-123846
    MLS-0437605

    Phosphatase Cardiovascular Disease
    MLS-0437605 is a selective dual-specificity phosphatase 3 (DUSP3) inhibitor with an IC50 of 3.7 μM. MLS-0437605 is more selective for DUSP3 than DUSP22 and other protein tyrosine phosphatases (PTPs).
  • HY-123604A
    TH1834 dihydrochloride

    Histone Acetyltransferase Apoptosis Cancer
    TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
  • HY-111895B
    Macropa-NH2 TFA

    Others Others
    Macropa-NH2 TFA is the precursor of Macropa-NCS. Macropa-NCS is conjugated to trastuzumab as well as to the prostate-specific membrane antigen-targeting compound RPS-070 and is a promising therapeutic radionuclide applied in the treatment of soft-tissue metastases.
  • HY-134809
    Cyclotriazadisulfonamide

    CADA

    HIV Infection Inflammation/Immunology
    Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way.
  • HY-101266B
    Milademetan tosylate hydrate

    DS-3032b; DS-3032 tosylate hydrate

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.
  • HY-111532
    (3R,4R)-A2-32-01

    Bacterial Infection
    (3R,4R)-A2-32-01 (compound 2), an anti-virulence drug, is a specific caseinolytic protein proteases (ClpP) inhibitor with an EC50 of 4.5 μM, and shows a tolerable cytotoxicity.
  • HY-13487
    USP7/USP47 inhibitor

    Deubiquitinase Cancer
    USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.
  • HY-10219
    Rapamycin

    Sirolimus; AY-22989

    mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Cancer
    Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-115521
    Jarin-1

    Others Others
    Jarin-1 is a jasmonic acid-amido synthetase (JAR1) inhibitor with an IC50 of 3.8 μM. Jarin-1 specific inhibits bioactive JA (jasmonoyl-isoleucine, JA-Ile) biosynthesis in Arabidopsis and other plants.
  • HY-128758
    DYRKs-IN-1

    DYRK Cancer
    DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity.
  • HY-128758A
    DYRKs-IN-1 hydrochloride

    DYRK Cancer
    DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity.
  • HY-B0392
    (S)-(+)-Rolipram

    (+)-Rolipram; (S)-Rolipram

    Phosphodiesterase (PDE) Apoptosis Cancer Inflammation/Immunology Neurological Disease
    (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells.
  • HY-139099
    Diguanosine 5′-triphosphate

    Gp3G

    Others Infection
    Diguanosine 5′-triphosphate (Gp3G) is a kind of homodinucleotide from by GTP:GTP guanylyltransferase. Diguanosine 5′-triphosphate is a virus-specific oligonucleotide, can be used to prime reovirus transcription and inhibit RNA methylation.
  • HY-19792
    Mertansine

    DM1; Maytansinoid DM1

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC).
  • HY-101266
    Milademetan

    DS-3032

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.
  • 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-123604
    TH1834

    Histone Acetyltransferase Apoptosis Cancer
    TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
  • HY-123054
    BTSA1

    Bcl-2 Family Apoptosis Cancer
    BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.
  • HY-13030
    (+)-JQ-1

    JQ1

    Epigenetic Reader Domain Autophagy Ligand for Target Protein for PROTAC Cancer
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
  • HY-138936
    SSK1

    p38 MAPK Apoptosis Inflammation/Immunology
    SSK1, a senescence-specific killing compound, is a β-galactosidase-targeted prodrug attenuates inflammation. SSK1 is activated by lysosomal β-galactosidase and selectively killed senescent cells through the activation of p38 MAPK and induction of apoptosis.
  • HY-50937
    ST 2825

    MyD88 Inflammation/Immunology
    ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity.
  • HY-103380
    NSC 625987

    CDK Cancer
    NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2.
  • HY-112885A
    nor-NOHA acetate

    Nω-Hydroxy-nor-L-arginine acetate

    Arginase Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a specific and reversible arginase inhibitor, induces apoptosis in ARG2-expressing cells under hypoxia but not normoxia. Anti-leukemic activity, effective in endothelial dysfunction, immunosuppression and metabolism.
  • HY-120855
    CCG-100602

    Ras Cardiovascular Disease
    CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF.
  • HY-108589
    PNU 37883 hydrochloride

    PNU 37883A

    Potassium Channel Neurological Disease
    PNU 37883 hydrochloride (PNU 37883A) is a selective vascular ATP-sensitive potassium (Kir6, KATP) channels blocker. PNU 37883 hydrochloride has diuretic effects with specific binding in kidney and vascular smooth muscle rather than in brain or pancreatic beta cells.
  • HY-17042A
    Cetirizine dihydrochloride

    P071

    Histamine Receptor Inflammation/Immunology Endocrinology
    Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-P0215
    Autocamtide-2-related inhibitory peptide, myristoylated

    CaMK Autophagy Neurological Disease
    Autocamtide-2-related inhibitory peptide, myristoylated is the myristoylated Autocamtide-2-related inhibitory peptide. Autocamtide-2-related inhibitory peptide is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM.
  • HY-N3522
    Platycoside E

    Others Inflammation/Immunology
    Platycoside E is a platycodigenin-type saponin isolated from the root of Platycodon grandiflorum with haemolytic activity and adjuvant potential. Platycoside E promotes the production of the sera OVA-specific IgG2a and IgG2b antibody in the ovalbumin (OVA)-immunized mice.
  • HY-137655A
    BMS-P5 free base

    Protein Arginine Deiminase Cancer
    BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 free base blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model.
  • HY-17042
    Cetirizine

    Histamine Receptor Inflammation/Immunology Endocrinology
    Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-13682B
    Mifamurtide sodium

    MTP-PE sodium; L-MTP-PE sodium; CGP 19835 sodium

    Others Cancer Inflammation/Immunology
    Mifamurtide sodium (MTP-PE sodium), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide sodium, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide sodium has the potential for osteosarcoma research.
  • HY-P0215A
    Autocamtide-2-related inhibitory peptide, myristoylated TFA

    CaMK Autophagy Neurological Disease
    Autocamtide-2-related inhibitory peptide, myristoylated TFA is the myristoylated Autocamtide-2-related inhibitory peptide. Autocamtide-2-related inhibitory peptide is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM.
  • HY-105040
    Pomaglumetad methionil

    LY2140023 hydrate

    mGluR Neurological Disease
    Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used for schizophrenia.
  • HY-B0689A
    Indinavir sulfate

    MK-639 sulfate; L735524 sulfate

    HIV HIV Protease SARS-CoV Infection
    Indinavir sulfate(MK-639 sulfate; L735524 sulfate ) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability. Indinavir sulfate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.71 μM.
  • HY-13682
    Mifamurtide

    MTP-PE; L-MTP-PE; CGP 19835

    Others Cancer Inflammation/Immunology
    Mifamurtide (MTP-PE), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide has the potential for osteosarcoma research.
  • HY-123979A
    ζ-Stat trisodium

    NSC37044 trisodium

    PKC Apoptosis Cancer
    ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
  • HY-112038A
    GSK2983559

    RIP kinase Inflammation/Immunology
    GSK2983559 (compound 3) is a potent, specific and oral active receptor interacting protein 2 (RIP2) kinase inhibitor, which has excellent activity in blocking many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
  • HY-100442
    Paquinimod

    ABR 25757

    Others Metabolic Disease Inflammation/Immunology
    Paquinimod (ABR 25757) is a specific inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice.
  • HY-130644
    iRucaparib-AP6

    PARP Cancer
    iRucaparib-AP6 is a highly efficient and specific PARP1 degrader based on Rucaparib by using the PROTAC approach. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1.
  • HY-131265
    Mesalamine impurity P

    PPAR PAK NF-κB Cancer Inflammation/Immunology
    Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-122632
    Ciliobrevin D

    Hedgehog Cancer
    Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.
  • HY-N0927
    (-)-Isocorypalmine

    Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine

    Dopamine Receptor Others
    (-)-Isocorypalmine (Tetrahydrocolumbamine), isolated from the crude base fraction of Corydalis chaerophylla, is a dopamine receptor ligand. Recombinant CYP719A21 displays strict substrate specificity and high affinity (Km=4.63 ± 0.71 μM) for (-)-Isocorypalmine.
  • HY-110249
    CINPA1

    Others Metabolic Disease
    CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.
  • HY-18963
    Lavendustin A

    RG-14355

    EGFR Cancer
    Lavendustin A (RG-14355), isolated from Streptomyces Griseolavendus, is a potent, specific and ATP-competitive inhibitor of tyrosine kinase, with an IC50 of 11 ng/mL for EGFR-associated tyrosine kinase. It suppresses VEGF-induced angiogenesis and blocks the induction of LTPGABA-A.
  • HY-131045
    HADA hydrochloride

    HCC-Amino-D-alanine hydrochloride

    Others Infection
    HADA hydrochloride (HCC-Amino-D-alanine hydrochloride) is a blue (λem~450 nm) fluorescent D-amino acid (FDAA). FDAAs are efficiently incorporated into the peptidoglycans (PGs) of diverse bacterial species at the sites of PG biosynthesis, allowing specific and covalent probing of bacterial growth with minimal perturbation.
  • HY-15322
    PRT062607

    P505-15; PRT-2607; BIIB-057

    Syk Inflammation/Immunology
    PRT062607(P505-15; PRT-2607; BIIB-057) is a highly specific and potent inhibitor of Syk with IC50 of 1-2 nM; >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.
  • HY-17596A
    Closantel sodium

    Parasite Infection
    Closantel sodium is a halogenated salicylanilide with a potent anti-parasitic activity. Closantel sodium is a potent and highly specific Onchocerca volvulus chitinase (OvCHT1) inhibitor with an IC50 of 1.6 μM and a Ki of 468 nM. Closantel sodium inhibits the O. volvulus L3 to L4 molt of developing.
  • HY-141644
    PY-60

    YAP Inflammation/Immunology
    PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a Kd of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity.
  • HY-103194
    KH7

    Adenylate Cyclase Others
    KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.
  • HY-128760
    COH34

    Others Cancer
    COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors.
  • HY-17596
    Closantel

    Parasite Infection
    Closantel is a halogenated salicylanilide with a potent anti-parasitic activity. Closantel is a potent and highly specific Onchocerca volvulus chitinase (OvCHT1) inhibitor with an IC50 of 1.6 μM and a Ki of 468 nM. Closantel inhibits the O. volvulus L3 to L4 molt of developing.
  • HY-100660A
    Cetirizine Impurity B dihydrochloride

    Others Others
    Cetirizine Impurity B dihydrochloride is an impurity of Cetirizine dihydrochloride. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-123032
    Sorivudine

    BV-araU

    DNA/RNA Synthesis Infection
    Sorivudine (BV-araU) is an orally active synthetic pyrimidine nucleoside antimetabolite drug. Sorivudine derives its antiviral activity from selective conversion by a specific thymidine kinase present in certain DNA viruses to nucleotides, which can in turn interfere with viral DNA synthesis.
  • HY-19711
    STING agonist-1

    G10

    STING Virus Protease Infection
    STING agonist-1 (G10) is human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses. G10 potently blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC90 of 24.57 μM.
  • HY-W006230
    Anthraflavic acid

    Others Cancer
    Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
  • HY-125510
    UNC2541

    TAM Receptor Others
    UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC50 of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM).
  • HY-12759
    CARM1-IN-1

    Histone Methyltransferase Cancer
    CARM1-IN-1 is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM).
  • HY-12759A
    CARM1-IN-1 hydrochloride

    Histone Methyltransferase Cancer
    CARM1-IN-1 hydrochloride is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM).
  • HY-100661
    Cetirizine Impurity D

    Histamine Receptor Endocrinology Inflammation/Immunology
    Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-109169
    Bomedemstat

    IMG-7289

    Histone Demethylase Cancer
    Bomedemstat (IMG-7289) is an orally active and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity.
  • HY-109169A
    Bomedemstat ditosylate

    IMG-7289 ditosylate

    Histone Demethylase Cancer
    Bomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity.
  • HY-15164A
    Icotinib

    BPI-2009

    EGFR Cancer
    Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q.
  • HY-P1052
    Myelin Basic Protein(87-99)

    Others Inflammation/Immunology
    Myelin Basic Protein(87-99) is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein(87-99) causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS).
  • HY-103023
    CLP290

    Potassium Channel Neurological Disease
    CLP290 is an orally available activator of the neuron-specific K +-Cl cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats.
  • HY-108323
    CCR2 antagonist 4

    Teijin compound 1

    CCR Inflammation/Immunology
    CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
  • HY-100781B
    L-AP4 monohydrate

    L-APB monohydrate

    mGluR Neurological Disease
    L-AP4 (L-APB) monohydrate 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-103362
    CCR2 antagonist 4 hydrochloride

    Teijin compound 1 hydrochloride

    CCR Inflammation/Immunology
    CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
  • HY-13945
    NVP 231

    Apoptosis Cancer
    NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage.
  • HY-103435
    Vialinin A

    Terrestrin A

    Deubiquitinase Cancer Inflammation/Immunology
    Vialinin A (Terrestrin A) is a p-terphenyl compound with antioxidant properties. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A (Terrestrin A) can be used for autoimmune diseases and cancer research.
  • HY-19359
    ZED-1227

    Glutaminase Inflammation/Immunology
    ZED-1227 is a specific and orally active transglutaminase 2 (TG2) inhibitor, with an IC50 of 45 nM. ZED-1227 can block inflammation-induced TG2 expression and activity. ZED-1227 can be used for the research of celiac disease (CeD).
  • HY-130648
    Thalidomide-NH-PEG7

    Drug-Linker Conjugates for ADC E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide-NH-PEG7 is a synthesized E3 ligase ligand-linker conjugate for ADC. Thalidomide-NH-PEG7 can be connected to the ligand for protein by a linker to form PROTAC iRucaparib-AP6, a highly specific PARP1 degrader.
  • HY-101445B
    (S)-Trolox

    Others Neurological Disease
    (S)-Trolox is an analogue of vitamin E, in which the phytyl chain is replaced with a carboxyl group. (S)-Trolox is frequently used as a model compound for studies of structural features, as well as a standard for evaluation of antioxidant activity. (S)-Trolox has potent and specific neuroprotective and antioxidant effects.
  • HY-15164
    Icotinib Hydrochloride

    BPI-2009H

    EGFR Cancer
    Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q.
  • HY-10444
    R-1479

    4'-Azidocytidine

    HCV DNA/RNA Synthesis Infection
    R-1479 (4'-Azidocytidine), a nucleoside analogue, is a specific inhibitor of RNA-dependent RNA polymerase (RdRp) of HCV. R-1479 inhibits HCV replication in the HCV subgenomic replicon system (IC50=1.28 μM).
  • HY-122243
    IU1-47

    Deubiquitinase Neurological Disease
    IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 inhibits IsoT/USP5 with an IC50 of 20 μM. IU1-47 induces tau elimination in cultured neurons.
  • HY-13297
    PYZD-4409

    E1/E2/E3 Enzyme Cancer
    PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
  • HY-100781A
    L-AP4

    L-APB

    mGluR Neurological Disease
    L-AP4 (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-111350
    FT827

    Deubiquitinase Cancer
    FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor (Ki=4.2 µM). FT827 binds to the USP7 catalytic domain (USP7CD; residues 208-560) with an apparent Kd value of 7.8 µM.
  • HY-15480
    NSC 42834

    JAK2 Inhibitor V; Z3

    JAK Cancer
    NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
  • HY-100540
    Golgicide A

    GCA

    Enterovirus Cancer Infection
    Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1. Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species.
  • HY-N2360
    Hinokiflavone

    E1/E2/E3 Enzyme Cancer
    Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
  • HY-101667
    LTURM34

    DNA-PK Cancer
    LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.
  • HY-A0082
    Diphenidol hydrochloride

    Difenidol hydrochloride

    mAChR Sodium Channel Neurological Disease
    Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells.
  • HY-101908
    BMS CCR2 22

    CCR Inflammation/Immunology Endocrinology
    BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM).
  • HY-15358
    ALK inhibitor 2

    ALK FAK Cancer
    ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).
  • HY-17402S1
    Nisoldipine-d4

    Calcium Channel Reactive Oxygen Species Cardiovascular Disease
    Nisoldipine-d4 (BAY-k 5552-d4) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.
  • HY-16767
    Doravirine

    MK-1439

    HIV Reverse Transcriptase Infection
    Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively.
  • HY-P2282
    APTSTAT3-9R

    STAT Cancer
    APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity.
  • HY-P0023
    Cyclo(-RGDfK)

    Integrin Cancer
    Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • HY-129944
    MJ33-OH

    Phospholipase Inflammation/Immunology
    MJ33-OH is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.
  • HY-15357
    ALK inhibitor 1

    ALK FAK Cancer
    ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
  • HY-17402S2
    Nisoldipine-d7

    Calcium Channel Reactive Oxygen Species Cardiovascular Disease
    Nisoldipine-d7 (BAY-k 5552-d7) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.
  • HY-B0372A
    Bromhexine hydrochloride

    SARS-CoV Autophagy HIV Metabolic Disease
    Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions.
  • HY-136406
    Bongkrekic acid

    ATP Synthase Cancer Infection
    Bongkrekic acid is a mitochondrial toxin secreted by the bacteria Pseudomonas cocovenenans. Bongkrekic acid specific ligand for mitochondrial adenine nucleotide translocase (ANT) rather than the electron transport chain. Bongkrekic acid has to cross the mitochondrial inner membrane to produce its inhibitory effect on ADP/ATP transport.
  • HY-14566S
    Donepezil-d7 hydrochloride

    E2020-d7

    AChE Neurological Disease
    Donepezil-d7 (hydrochloride) (E2020-d7) is the deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively.
  • HY-15838
    ID-8

    DYRK Cancer
    ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs.
  • HY-112038
    GSK2983559 free acid

    RIP kinase Inflammation/Immunology
    GSK2983559 free acid (compound 3) is a potent, specific and oral active receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid has excellent activity in blocking many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
  • HY-100859
    LSD1-IN-5

    Histone Demethylase Cancer
    LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-111623
    USP30 inhibitor 11

    Deubiquitinase Cancer
    USP30 inhibitor 11 is a selective and potent ubiquitin specific peptidase 30 (USP30) inhibitor with an IC50 of 0.01 µΜ, the example 83 extracted from patent WO2017009650A1. USP30 inhibitor 11 is used for the study of cancer and conditions involving mitochondrial dysfunction.
  • HY-100954
    2,4-Diamino-6-hydroxypyrimidine

    NO Synthase Inflammation/Immunology
    2,4-Diamino-6-hydroxypyrimidine is a specific GTP cyclohydrolase I inhibitor (the rate-limiting enzyme in de novo pterin synthesis). 2,4-Diamino-6-hydroxypyrimidine blocks Tetrahydrobiopterin (BH4) synthesis and suppresses NO production.
  • HY-139147
    iHCK-37

    ASN05260065

    Src Cancer Infection
    iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM. iHCK-37 blocks HIV-1 viral replication with an EC50 value of 12.9 μM. iHCK-37 is used for chronic myeloid leukemia (CML) research.
  • HY-129944A
    MJ33-OH lithium

    Phospholipase Inflammation/Immunology
    MJ33-OH lithium is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.
  • HY-111895A
    Macropa-NH2 hydrochloride

    Others Cancer
    Macropa-NH2 hydrochloride is the precursor of Macropa-NCS. Macropa-NCS is conjugated to Anti-Human HER2 (HY-P9907) as well as to the prostate-specific membrane antigen-targeting compound RPS-070 and is a promising therapeutic radionuclide applied in the treatment of soft-tissue metastases.
  • HY-100860
    LSD1-IN-6

    Histone Demethylase Cancer
    LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-101246
    RPI-1

    RET Cancer
    RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity.
  • HY-P0018
    Pepstatin

    Pepstatin A

    Proteasome HIV Protease Autophagy Infection Cancer
    Pepstatin (Pepstatin A) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
  • HY-120075
    TJ191

    Apoptosis Cancer
    TJ191 is a potent and specific anti-cancer agent that targets low TβRIII-expressing malignant T-cell leukemia/lymphoma cells. TJ191 has no affects on the proliferation of other cancer cells or normal fibroblasts or immune cells. TJ191 can be used for cancer research.
  • HY-30008
    Cycloleucine

    iGluR Cancer Infection Metabolic Disease Neurological Disease
    Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects.
  • HY-13682C
    Mifamurtide TFA

    MTP-PE TFA; L-MTP-PE TFA; CGP 19835 TFA

    Others Cancer Inflammation/Immunology
    Mifamurtide TFA (MTP-PE TFA), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide TFA, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide TFA has the potential for osteosarcoma research.
  • HY-125263
    OP-1074

    Estrogen Receptor/ERR Cancer
    OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
  • HY-16590
    X-376

    ALK c-Met/HGFR Cancer
    X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
  • HY-19231
    DPI-3290

    Org 41793

    Opioid Receptor Neurological Disease
    DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively。DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity.
  • HY-107600
    IQ-3

    JNK Inflammation/Immunology
    IQ-3 is a specific inhibitor of the c-Jun N-terminal kinase (JNK) family, with preference for JNK3. IQ-3 exhibits Kd values of 0.24 μM, 0.29 μM and 0.066 μM for JNK1, JNK2 and JNK3, respectively.
  • HY-P0018A
    Pepstatin Trifluoroacetate

    Pepstatin A Trifluoroacetate

    Proteasome HIV Protease Infection
    Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
  • HY-P0018B
    Pepstatin Ammonium

    Pepstatin A Ammonium

    Proteasome HIV Protease Cancer Infection
    Pepstatin Ammonium is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
  • HY-13434
    Ionomycin

    SQ23377

    Calcium Channel PKC Bacterial Apoptosis Antibiotic Cancer Infection
    Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin (SQ23377) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin also induces the activation of protein kinase C (PKC).
  • HY-P0023A
    Cyclo(-RGDfK) TFA

    Integrin Cancer
    Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • HY-100202
    TPEN

    TPEDA

    Reactive Oxygen Species Apoptosis Autophagy Cancer
    TPEN (TPEDA) is a specific cell-permeable heavy metal chelator. TPEN has a higher affinity for Zn 2+, but a lower affinity for Mg 2+ and Ca 2+. TPEN induces DNA damage and increases intracellular ROS production. TPEN also inhibits cell proliferation and induces apoptosis.
  • HY-133118
    6RK73

    Deubiquitinase Cancer
    6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer.
  • HY-15027S
    5-Aminosalicylic Acid-D3 hydrochloride

    Mesalamine-D3 hydrochloride; 5-ASA-D3 hydrochloride; Mesalazine-D3 hydrochloride

    PPAR PAK NF-κB Endogenous Metabolite Inflammation/Immunology Cancer
    5-Aminosalicylic Acid-D3 (Mesalamine-D3) hydrochloride is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) hydrochloride acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-111848A
    PROTAC AR Degrader-4 TFA

    SNIPER PROTACs Androgen Receptor Cancer
    PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
  • HY-17042AS
    Cetirizine D4 dihydrochloride

    Histamine Receptor Inflammation/Immunology
    Cetirizine D4 dihydrochloride is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-N8022
    Lucidin primeveroside

    Lucidin 3-O-β-primeveroside

    Others Cancer
    Lucidin primeveroside (Lucidin 3-O-β-primeveroside) is an anthraquinone derivative present in madder root, which has been used as a coloring agent and food additive. Lucidin primeveroside can be metabolically converted to genotoxic compound Lucidin, which subsequently forms lucidin-specific DNA adducts.
  • HY-126390
    (E/Z)-BCI

    NSC 150117

    Phosphatase Apoptosis Cancer Inflammation/Immunology
    (E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.
  • HY-17042S
    Cetirizine D4

    Histamine Receptor Inflammation/Immunology
    Cetirizine D4 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-135425
    10,12-Tricosadiynoic acid

    Acyltransferase Metabolic Disease
    10,12-Tricosadiynoic acid is a highly specific, selective, high affinity and orally active acyl-CoA oxidase-1 (ACOX1) inhibitor. 10,12-Tricosadiynoic acid can treat high fat diet- or obesity-induced metabolic diseases by improving mitochondrial lipid and ROS metabolism.
  • HY-141800
    MurA-IN-1

    Others Others
    MurA-IN-1 (compound 1a) is a PTPRR inhibitor, with IC50 values of 0.23 μM, 0.8 μM, 0.75 μM and 0.09 μM for PTP1B, PTPN5, PTPN7 and PTPRR, respectively. (A family of human MAPK-specific protein tyrosine phosphatases)
  • HY-17042S1
    Cetirizine D8

    Histamine Receptor Inflammation/Immunology
    Cetirizine D8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-12728
    Tautomycin

    Phosphatase Inflammation/Immunology
    Tautomycin, an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus, is a potent and specific inhibitor of protein phosphatases 1 and 2A and induces contraction of smooth muscle under Ca 2+-free conditions, with Kiapp values of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively.
  • HY-12185
    BRD7389

    Ribosomal S6 Kinase (RSK) Cancer Metabolic Disease
    BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells.
  • HY-130592
    Compound 48/80 trihydrochloride

    C48/80 trihydrochloride

    Phospholipase Neurological Disease
    Compound 48/80 trihydrochloride (C48/80 trihydrochloride) is a mixture of condensation products of N-methyl-p-methoxyphenethylamine with formaldehyde. Compound 48/80 trihydrochloride is also a histamine releaser and a mast cell degranulator. Compound 48/80 inhibits phosphatidylinositol-specific phospholipase C activity from human platelets .
  • HY-15777S
    Ribociclib D6

    LEE011 D6

    CDK Cancer
    Ribociclib D6 (LEE011 D6) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-101122
    LX2761

    SGLT Metabolic Disease
    LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract.
  • HY-133807
    Benpyrine

    TNF Receptor Inflammation/Immunology
    Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
  • HY-16012
    Domatinostat tosylate

    4SC-202

    HDAC Apoptosis Cancer
    Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
  • HY-117656
    ESI-05

    NSC 116966

    Others Others
    ESI-05 (NSC 116966) is a specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 µM. ESI-05 (NSC 116966) inhibits cAMP-mediated activation of EPAC2 as well as EAPC2 mediated Rap1 activation.
  • HY-W011094
    Win 18446

    Aldehyde Dehydrogenase (ALDH) Endocrinology
    Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC50 of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes.
  • HY-15777AS
    Ribociclib D6 hydrochloride

    LEE011 D6 hydrochloride

    CDK Cancer
    Ribociclib D6 (LEE011 D6) hydrochloride is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-17042AS1
    Cetirizine D8 dihydrochloride

    Histamine Receptor Inflammation/Immunology
    Cetirizine D8 dihydrochloride is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-136175
    SNDX-5613

    Epigenetic Reader Domain Cancer
    SNDX-5613 is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).
  • HY-111848
    PROTAC AR Degrader-4

    SNIPER PROTACs Androgen Receptor Cancer
    PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
  • HY-N7119
    Cimicifugoside

    Others Inflammation/Immunology
    Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity. Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function.
  • HY-P1105
    GaTx2

    Others Neurological Disease
    GaTx2 is a seletive and a high affinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types.
  • HY-110130
    RN-1 dihydrochloride

    Histone Demethylase Cancer Cardiovascular Disease
    RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC50 values of 0.51 μM and 2.785 μM respectively.
  • HY-16661
    Skp2 Inhibitor C1

    SKPin C1

    E1/E2/E3 Enzyme Cancer
    Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.
  • HY-N0742
    Absinthin

    Others Others
    Absinthin is a structurally unique triterpene, and is responsible for the high bitter value of wormwood. Absinthin is an agonist of the bitter taste receptor hTAS2R46, which reduces cytosolic Ca 2+-rises induced by histamine by a receptor-specific mechanism mediated by hTAS2R46.
  • HY-P1136B
    TAT-Gap19

    Gap Junction Protein Inflammation/Immunology Cardiovascular Disease
    TAT-Gap19, a Cx mimetic peptide, is a specific connexin43 hemichannel (Cx43 HC) inhibitor. TAT-Gap19 does not inhibits the corresponding Cx43 GJCs. TAT-Gap19 traverses the blood-brain barrier and alleviate liver fibrosis in mice.
  • HY-100933
    MY-5445

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology Cardiovascular Disease
    MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a Ki of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect.
  • HY-10219S
    Rapamycin-d3

    Sirolimus-d3; AY-22989-d3

    mTOR FKBP Autophagy Cancer
    Rapamycin-d3 (Sirolimus-d3) is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-N8537
    Enfumafungin

    Fungal Infection
    Enfumafungin, a triterpene glycoside, is isolated from extracts derived from an endophytic species of Hormonema. Enfumafungin is an antifungal compound that is acting on the fungal cell wall, as the (1,3)-beta-D-glucan synthase inhibitor. Enfumafungin is specific for yeasts and fungi (excluding Cryptococcus) and does not inhibit the growth of Bacillus subtilis.
  • HY-B1811
    Vasopressin

    Endogenous Metabolite Neurological Disease
    Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors.
  • HY-W008610
    GBR 12783

    Dopamine Receptor Neurological Disease
    GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats.
  • HY-N2306A
    Aclacinomycin A hydrochloride

    Aclarubicin hydrochloride

    Proteasome Topoisomerase Cancer
    Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors.
  • HY-N7648
    Atherosperminine

    Atherospermine

    Parasite Infection
    Atherosperminine(Atherospermine)is a nature occurring alkaloid, has antiplasmodial activities in vitro, with an IC50 of 5.80 μM. Atherosperminine is a good reductant with the ability to chelate metals. Atherosperminine has scavenging activity towards the free radical DPPH, with an IC50 of 29.56 µg/mL. Atherosperminine exerts a non-specific relaxant effect on the trachealis.
  • HY-N2345
    Procyanidin B3

    Histone Acetyltransferase Cancer
    Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgen receptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase).
  • HY-P1380A
    Difopein TFA

    Apoptosis Cancer
    Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to induction of apoptosis and enhances the ability of cisplatin to kill cells.
  • HY-103710
    IBR2

    RAD51 Apoptosis Cancer
    IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis.
  • HY-103661
    BI-6C9

    Mitochondrial Metabolism Apoptosis Neurological Disease
    BI-6C9 is a highly specific BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from mitochondrial apoptosis inducing factor (AIF) release and caspase-independent cell death in neurons.
  • HY-103489
    PI-273

    PI4K Apoptosis Cancer
    PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.
  • 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-128923
    SKF-34288 hydrochloride

    3-Mercaptopicolinic acid hydrochloride

    Others Metabolic Disease
    SKF-34288 hydrochloride (3-Mercaptopicolinic acid) is a phosphoenolpyruvate carboxykinase (PEPCK) inhibitor. SKF-34288 hydrochloride is a potent hypoglycemic agent via inhibition of glucose synthesis through the specific inhibition of PEPCK in the gluconeogenesis pathway. SKF-34288 hydrochloride inhibits Asn metabolism and results in an increase in amino acids and amides.
  • HY-W058849
    MT 63-78

    AMPK mTOR Apoptosis Cancer
    MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.
  • HY-15888
    PTC-209

    Autophagy Cancer
    PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment.
  • HY-10044
    WYE-132

    WYE-125132

    mTOR Apoptosis Cancer
    WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC50: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibits mTORC1 and mTORC2.
  • HY-125835
    CP-10

    PROTACs CDK Cancer
    CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6.
  • HY-124838
    EG1

    Others Cancer
    EG1, a specific Pax2 inhibitor, directly binds the paired domain of Pax2 (Kd=1.35-1.5 μM) and inhibits Pax2-DNA interactions. EG1 can inhibit embryonic kidney development, a process directly dependent on Pax2 activity.
  • HY-100968
    GBR 12783 dihydrochloride

    Dopamine Receptor Neurological Disease
    GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats.
  • HY-112210
    Shield-1

    FKBP Others
    Shield-1 is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize the entire fusion protein.
  • HY-B0240
    Disulfiram

    Tetraethylthiuram disulfide; TETD

    Aldehyde Dehydrogenase (ALDH) Interleukin Related Pyroptosis Metabolic Disease Cancer
    Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1-4].
  • HY-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-16012A
    Domatinostat

    4SC-202 free base

    HDAC Apoptosis Cancer
    Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
  • HY-B1496
    Tranylcypromine hemisulfate

    dl-Tranylcypromine hemisulfate; trans-2-Phenylcyclopropylamine hemisulfate salt

    Monoamine Oxidase Histone Demethylase Neurological Disease
    Tranylcypromine hemisulfate (dl-Tranylcypromine hemisulfate) is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects.
  • HY-122051
    AC1903

    TRP Channel Metabolic Disease
    AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.
  • HY-B0682A
    Mitiglinide calcium hydrate

    KAD-1229; S-21403

    Potassium Channel Metabolic Disease
    Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K + (KATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes.
  • HY-129039
    Butyrolactone 3

    Histone Acetyltransferase Cancer
    Butyrolactone 3 is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM)
  • HY-114268
    BRD-K98645985

    HIV Infection
    BRD-K98645985 is a BAF (mammalian SWI/SNF) transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, without T cell activation or toxicity.
  • 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-13103
    NS 11021

    Potassium Channel Others
    NS 11021 is a potent and specific Ca 2+-activated big-conductance K + Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials.
  • HY-13771
    Ursodeoxycholic acid

    Ursodiol; UDCA

    Endogenous Metabolite Metabolic Disease Cancer
    Ursodeoxycholic acid (Ursodiol) is a potent liver-specific fatty acid transport protein 5 (FATP5) inhibitor. Ursodeoxycholic acid inhibit LCFA uptake by primary hepatocytes in a FATP5-dependent manner. Ursodeoxycholic acid reduces cholesterol absorption and is used to dissolve gallstones and has the potential for obesity-associated fatty liver disease research.
  • HY-111139
    MS417

    GTPL7512

    Epigenetic Reader Domain HIV Infection Inflammation/Immunology
    MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).
  • HY-136363
    MDR-652

    TRP Channel Neurological Disease
    MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.
  • HY-120118
    Metarrestin

    ML246

    DNA/RNA Synthesis Cancer
    Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models.
  • HY-10293
    Aderbasib

    INCB007839; INCB7839

    MMP Cancer
    Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 + breast cancer, gliomas, et al.
  • HY-100540A
    (Rac)-Golgicide A

    (Rac)-GCA

    Enterovirus Infection
    (Rac)-Golgicide A ((Rac)-GCA) is a racemate of Golgicide A. Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1.Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species.
  • HY-14951
    Firategrast

    SB 683699

    Integrin Neurological Disease
    Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.
  • HY-15508
    JANEX-1

    WHI-P131; Jak3 inhibitor I

    JAK Cancer
    JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
  • HY-115579
    MALAT1-IN-1

    Others Cancer
    MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
  • HY-114153
    PLX5622

    c-Fms Neurological Disease
    PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals.
  • HY-103000
    HSF1A

    HSP Cancer Cardiovascular Disease
    HSF1A is a cell-permeable activator of heat shock transcription factor 1 (HSF1). HSF1A also acts as a specific inhibitor of TRiC/CCT. Chaperonin TCP-1 ring complex (TRiC)/chaperonin containing TCP-1 (CCT) plays a pivotal role in toxin translocation and/or refolding.
  • HY-13838
    PLX647

    c-Fms c-Kit Cancer
    PLX647 is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, respectively. PLX647 shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively).
  • HY-B0352S
    Mirtazapine D3

    Org3770 D3; 6-Azamianserin D3

    5-HT Receptor Neurological Disease
    Mirtazapine D3 (Org3770 D3; 6-Azamianserin D3) is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors.
  • HY-124701
    Filastatin

    Fungal Infection
    Filastatin is a long-lasting inhibitor of Candida albicans filamentation. Filastatin inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 μM in the GFP-based adhesion assay. Filastatin inhibits fungal adhesion to polystyrene and human cells, the yeast-to-hyphal morphological transition, induction of the hyphal-specific HWP1 promoter. Filastatin has potent antifungal effect.
  • HY-17398
    Mitiglinide calcium

    KAD-1229 anhydrous; S21403 anhydrous

    Potassium Channel Metabolic Disease
    Mitiglinide Calcium (KAD-1229 anhydrous), an insulinotropic agent, is an ATP-sensitive K + (KATP) channel antagonist. Mitiglinide Calcium is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium can be used for the research of type 2 diabetes.
  • HY-111675
    Ac-FLTD-CMK

    Caspase Pyroptosis Inflammation/Immunology
    Ac-FLTD-CMK, a gasdermin D (GSDMD)-derived inhibitor, is a specific inflammatory caspases inhibitor. Ac-FLTD-CMK is effective against caspases-1 (IC50 of 46.7 nM), caspases-4 (IC50 of 1.49 μM), caspases-5 (IC50 of 329 nM), and caspases-11 , but not the apoptotic caspases such as caspase-3.
  • HY-18754
    FR 167653 free base

    p38 MAPK Autophagy Endocrinology
    FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
  • HY-105028
    Tenidap

    CP-66248

    COX Inflammation/Immunology
    Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 µM and 1.2 µM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties. Tenidap is also a specific SLC26A3 inhibitor.
  • HY-100789
    ON1231320

    Polo-like Kinase (PLK) Apoptosis Cancer
    ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 µM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity.
  • HY-122054
    BPK-29

    Others Cancer
    BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
  • HY-P1136C
    TAT-Gap19 TFA

    Gap Junction Protein Inflammation/Immunology Cardiovascular Disease
    TAT-Gap19 TFA, a Cx mimetic peptide, is a specific connexin43 hemichannel (Cx43 HC) inhibitor. TAT-Gap19 TFA does not inhibits the corresponding Cx43 GJCs. TAT-Gap19 TFA traverses the blood-brain barrier and alleviate liver fibrosis in mice.
  • HY-13838A
    PLX647 dihydrochloride

    c-Fms c-Kit Cancer Inflammation/Immunology
    PLX647 dihydrochloride is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively).
  • HY-15888A
    PTC-209 hydrobromide

    Autophagy Cancer
    PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment.
  • HY-139466
    PF-03622905

    PKC Metabolic Disease
    PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases.
  • HY-122054A
    BPK-29 hydrochloride

    Others Cancer
    BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
  • HY-133146
    DJ001

    Phosphatase Apoptosis Inflammation/Immunology
    DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration.
  • HY-P1119
    WRW4

    Others Neurological Disease
    WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.
  • HY-15785
    Pimitespib

    TAS-116

    HSP Cancer
    Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. Pimitespib demonstrates less ocular toxicity.
  • HY-122578
    P53R3

    MDM-2/p53 Cancer
    P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53 R175H, p53 R248W and p53 R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53 M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research.
  • HY-117370
    USP25/28 inhibitor AZ1

    AZ1

    Deubiquitinase Cancer
    USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model.
  • HY-134817
    USP7-IN-8

    Deubiquitinase Cancer
    USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects.
  • HY-19121A
    TCV-309 chloride

    Others Cancer
    TCV-309 chloride is a potent and specific platelet activating factor (PAF) antagonist. TCV-309 chloride specifically inhibits PAF-induced aggregation of rabbit and human platelets, and [3H]PAF binding to rabbit platelet microsomes with IC50 values of 33 nM, 58 nM and 27 nM, respectively. TCV-309 chloride has beneficial effects in anaphylactic shock.
  • HY-13434A
    Ionomycin calcium

    SQ23377 calcium

    Calcium Channel PKC Bacterial Apoptosis Antibiotic Cancer Infection
    Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin calcium (SQ23377 calcium) also induces the activation of protein kinase C (PKC).
  • HY-14340
    WAY-181187

    SAX-187

    5-HT Receptor Neurological Disease
    WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
  • HY-108645
    AL 8697

    p38 MAPK Autophagy Inflammation/Immunology
    AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity.
  • HY-122903
    TK216

    DNA/RNA Synthesis Cancer
    TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity.
  • HY-13413
    Tofogliflozin (hydrate)

    CSG-452 hydrate

    SGLT Reactive Oxygen Species Metabolic Disease
    Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells.
  • HY-P3138
    (Sar1)-Angiotensin II

    Angiotensin Receptor Cardiovascular Disease
    (Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. (Sar1)-Angiotensin II binds to brain membrane-rich particles, with a Kd of 2.7 nM. (Sar1)-Angiotensin II can stimulate protein synthesis and cell growth in embryonic chick myocytes.
  • HY-10574
    Rilpivirine

    R278474; TMC278; DB08864

    HIV Reverse Transcriptase Infection
    Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV.
  • 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-139297
    SCR130

    DNA/RNA Synthesis Apoptosis Cancer
    SCR130 is a SCR7-based DNA nonhomologous end-joining (NHEJ) inhibitor. SCR130 inhibits the end-joining of DNA in a Ligase IV-dependent manner. SCR130 is specific to Ligase IV, and shows minimal or no effect on Ligase III and Ligase I mediated joining. SCR130 induces cell apoptosis and has anticancer activity.
  • HY-14452
    Fatostatin

    125B11

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-10974
    MK-0752

    γ-secretase Neurological Disease Cancer
    MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo.
  • HY-10220
    SF1126

    PI3K Apoptosis Cancer
    SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis.
  • HY-114153A
    PLX5622 hemifumarate

    c-Fms Neurological Disease
    PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals.
  • HY-18754A
    FR 167653

    FR 167653 sulfate

    p38 MAPK Autophagy Endocrinology
    FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
  • 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-12649
    Y16

    Ras Cancer
    Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP.
  • HY-117147A
    GSK2945 hydrochloride

    Cytochrome P450 Metabolic Disease
    GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
  • HY-106225
    Rotigaptide

    ZP123

    Gap Junction Protein Cardiovascular Disease
    Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation.
  • HY-117147
    GSK2945

    Cytochrome P450 Metabolic Disease
    GSK2945 is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
  • HY-109016
    Valnivudine

    FV-100 free base

    Antibiotic Bacterial Infection
    Valnivudine (FV-100 free base), a prodrug of CF-1743, is an orally active anti-herpes zoster (HZ) nucleoside analogue. CF-1743, a bicyclic nucleoside analog (BCNA), has highly specific antiviral activity against varicella-zoster virus (VZV). Valnivudine is rapidly and extensively converted to CF-1743 in vivo.
  • HY-111844
    PROTAC RAR Degrader-1

    SNIPER PROTACs RAR/RXR Cancer
    PROTAC RAR Degrader-1 comprises a IAP ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
  • HY-122607
    DPA-714

    Others Cancer Inflammation/Immunology
    DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model.
  • HY-131970
    LSD1/HDAC6-IN-1

    Histone Demethylase Cancer
    LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM).
  • HY-102078
    ZINC69391

    Ras Apoptosis Cancer
    ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects.
  • HY-139659
    ARD-61

    PROTACs Androgen Receptor Progesterone Receptor Apoptosis Cancer
    ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice.
  • HY-112041
    Unesbulin

    PTC596

    Apoptosis Cancer
    Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity.
  • HY-124290
    Carotegrast methyl

    AJM300

    Integrin Inflammation/Immunology
    Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
  • HY-130173
    Bafilomycin C1

    Bacterial Fungal Na+/K+ ATPase Apoptosis Cancer Infection
    Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H +-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi. Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC).
  • HY-17447SA
    (rel)-Tranylcypromine D5 hydrochloride

    2-Phenylcyclopropylamine D5 hydrochloride

    Monoamine Oxidase Histone Demethylase Neurological Disease
    (rel)-Tranylcypromine D5 hydrochloride (2-Phenylcyclopropylamine D5 hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. (rel)-Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. (rel)-Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis.
  • HY-101451
    PBIT

    Histone Demethylase Cancer
    PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively.
  • HY-129707
    AMG 837 hemicalcium

    GPR40 Metabolic Disease
    AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium 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-W011391
    GPNA hydrochloride

    Apoptosis Cancer
    GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na +-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na +-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells.
  • HY-17372
    Rofecoxib

    MK 966

    COX Inflammation/Immunology Cancer
    Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).
  • HY-116788
    Lipofermata

    Bacterial Infection
    Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata, an analog of spiro-indoline-thadiazole, shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM.
  • HY-16592
    Brefeldin A

    BFA; Cyanein; Decumbin

    Autophagy CRISPR/Cas9 Mitophagy HSV Antibiotic Cancer Infection
    Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
  • HY-114170
    ML604440

    Proteasome Inflammation/Immunology
    ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
  • HY-138559
    GW604714X

    Mitochondrial Metabolism Neurological Disease
    GW604714X is a potent inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X is a highly specific mitochondrial pyruvate carrier (MPC) inhibitor with a Ki <0.1 nM. GW604714X also inhibits L-lactate transport by the plasma membrane monocarboxylate transporter (MCT1), but at concentrations more than 4 orders of magnitude greater than the MPC.
  • HY-128729
    DNA2 inhibitor C5

    Others Cancer
    DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
  • HY-18756A
    NSC-87877 disodium

    Phosphatase Apoptosis Cancer
    NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
  • HY-108542
    Tautomycetin

    Phosphatase Inflammation/Immunology
    Tautomycetin is a potent and specifical PP1 inhibitor with the potential apoptosis-inducing activity. Tautomycetin inhibits purified PP1 and PP2A enzymes with IC50s of 1.6 nM and 62 nM, respectively. Tautomycetin is an antifungal antibiotic and has immunosuppressive effects in vivo. Tautomycetin can be used as a novel powerful tool to elucidate the physiological roles of PP1 in various biological events.
  • HY-129388A
    Pulrodemstat

    CC-90011; LSD1-IN-7

    Histone Demethylase Cancer
    Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-100421
    CPI-455

    Histone Demethylase Cancer
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
  • HY-13967B
    AMG 837 calcium hydrate

    GPR40 Metabolic Disease
    AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents.
  • HY-128204
    AN3661

    Parasite Infection
    AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections.
  • HY-18756
    NSC-87877

    Phosphatase Apoptosis Others
    NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
  • HY-21997
    Dmt-2'fluoro-da(bz) amidite

    DNA/RNA Synthesis Others
    Dmt-2'fluoro-da(bz) amidite, an uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotide, is a nuclease-resistant antisense compound with high affinity and specificity for RNA targets. Dmt-2'fluoro-da(bz) amidite is also an intermediate for 5’-DMT-3’-phosphoramidite synthesis.
  • HY-P1439A
    RS 09 TFA

    Toll-like Receptor (TLR) Inflammation/Immunology
    RS 09 TFA is a TLR4 agonist. RS 09 TFA promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 TFA acts as an adjuvant in vivo; RS 09 TFA enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
  • HY-B0352
    Mirtazapine

    Org3770; 6-Azamianserin

    5-HT Receptor Histamine Receptor Adrenergic Receptor Inflammation/Immunology Neurological Disease
    Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
  • HY-P1597
    Malantide

    PKA PKC Cancer
    Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
  • HY-136261
    DM1-PEG4-DBCO

    Drug-Linker Conjugates for ADC Cancer
    DM1-(PEG)4-DBCO is a drug-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody drug conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.
  • HY-W014622
    CRT0044876

    DNA/RNA Synthesis Cancer
    CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds.
  • HY-15648A
    GSK-J2

    Histone Demethylase Cancer
    GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.
  • HY-126154
    L48H37

    Toll-like Receptor (TLR) Inflammation/Immunology
    L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is used for the research of sepsis or lung injury treatment.
  • HY-17387
    (-)-Huperzine A

    Huperzine A

    AChE Apoptosis iGluR Neurological Disease
    (-)-Huperzine A (Huperzine A) is an alkaloid isolated from a Chinese club moss, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
  • HY-128872
    EHP-101

    VCE-​004.8

    PPAR Cannabinoid Receptor HIF/HIF Prolyl-Hydroxylase Metabolic Disease Inflammation/Immunology
    EHP-101 (VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. EHP-101 inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. EHP-101, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. EHP-101 attenuates adipogenesis and prevents diet-induced obesity.
  • HY-15039
    SSR240612

    Bradykinin Receptor Metabolic Disease Inflammation/Immunology Endocrinology
    SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
  • HY-111532B
    (3S,4S)-A2-32-01

    Others Infection
    (3S,4S)-A2-32-01 is a less active S-enantiomer of (3R,4R)-A2-32-01. (3R,4R)-A2-32-01 is an anti-virulence agent and a specific caseinolytic protein proteases (ClpP) inhibitor.
  • HY-136260
    DBCO-PEG4-Ahx-DM1

    Drug-Linker Conjugates for ADC Cancer
    DBCO-PEG4-Ahx-DM1 is a drug-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody drug conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.
  • HY-P1036
    Compstatin

    Complement System Others
    Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
  • HY-134901
    WM-3835

    Histone Acetyltransferase Apoptosis Cancer
    WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1 33. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.
  • HY-107139
    JNJ-10229570

    Melanocortin Receptor Endocrinology
    JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
  • HY-14452A
    Fatostatin hydrobromide

    125B11 hydrobromide

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-112163A
    rel-Zotatifin

    rel-eFT226

    Eukaryotic Initiation Factor (eIF) SARS-CoV Apoptosis Cancer Infection
    rel-Zotatifin is the racemic isomer of Zotatifin, acts as an eIF4A inhibitor with activity less than Zotatifin. Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex.
  • HY-12646A
    Rhosin

    Ras Apoptosis Cancer
    Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
  • HY-12646
    Rhosin hydrochloride

    Ras Apoptosis Cancer
    Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
  • HY-131043
    NVS-PAK1-C

    PAK Cancer
    NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC50 values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC50=270 nM) and phosphorylated PAK2 (IC50=720 nM).
  • HY-P1597A
    Malantide TFA

    PKA PKC Cancer
    Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM.
  • HY-100558
    Bafilomycin A1

    Proton Pump Autophagy Antibiotic Bacterial Apoptosis Cancer Infection
    Bafilomycin A1 is a specific and reversible inhibitor of vacuolar H +-ATPase (V-ATPase) with IC50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis.
  • HY-12072
    Lck Inhibitor

    Src Inflammation/Immunology
    Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
  • HY-136431
    BC-DXI-843

    Others Cancer
    BC-DXI-843 is a potent and specific AIMP2-DX2 inhibitor with an IC50 of 0.92 μM, more than 100-fold selectivity over AIMP2 (IC50 >100 μM) in a luciferase assay. BC-DXI-843 acts as a promising lead targeting AIMP2-DX2 in lung cancer.
  • HY-117800
    BJE6-106

    B106

    PKC Apoptosis Cancer Inflammation/Immunology
    BJE6-106 (B106) is a potent, selective 3 rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM). BJE6-106 (B106) induces caspase-dependent apoptosis. BJE6-106 (B106) possesses tumor-specific effect.
  • HY-131031
    KCC-07

    DNA Alkylator/Crosslinker Cancer
    KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
  • HY-10037
    Quiflapon

    MK-591

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.
  • HY-100900
    ML364

    Deubiquitinase Cancer
    ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP.
  • HY-109520
    Glatiramer acetate

    Others Inflammation/Immunology
    Glatiramer acetate, a synthetic analogue of myelin basic protein and an immunomodulating agent, can be used for the research of multiple sclerosis. Glatiramer acetate exhibits strong and promiscuous binding to MHC molecules and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression.
  • HY-15486
    Salubrinal

    Phosphatase HSV Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.
  • HY-B0965
    Thioridazine hydrochloride

    Dopamine Receptor Apoptosis 5-HT Receptor Autophagy Bacterial Cancer Infection Neurological Disease
    Thioridazine hydrochloride, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
  • HY-13863
    Hydroxy-Dynasore

    Dyngo-4a

    Dynamin Neurological Disease
    Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.
  • HY-114141
    BI-671800

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has potential for the treatment of poorly controlled asthma.
  • HY-129388B
    Pulrodemstat benzenesulfonate

    CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate

    Histone Demethylase Cancer
    CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-106224
    Orexin A (human, rat, mouse)

    Orexin Receptor (OX Receptor) Neurological Disease
    Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
  • HY-12404
    Diminazene aceturate

    Diminazene diaceturate

    Parasite Angiotensin-converting Enzyme (ACE) Infection Inflammation/Immunology
    Diminazene aceturate (Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties.
  • HY-W010983
    SC-236

    COX PPAR Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model.
  • HY-P1318
    Ac-RYYRIK-NH2

    Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
  • HY-114407
    TD-428

    PROTACs Epigenetic Reader Domain Cancer
    TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.
  • HY-100237
    SZL P1-41

    E1/E2/E3 Enzyme Apoptosis Cancer
    SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities.
  • HY-134539
    IMT1

    Mitochondrial Metabolism DNA/RNA Synthesis Cancer Metabolic Disease
    IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases.
  • HY-105066
    Davunetide

    Microtubule/Tubulin Amyloid-β Neurological Disease
    Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity.
  • HY-19569
    Upadacitinib

    ABT-494

    JAK Inflammation/Immunology
    Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) is used in development for the treatment of several autoimmune disorders.
  • HY-125039
    N-Acetyl lysyltyrosylcysteine amide

    Glutathione Peroxidase Neurological Disease Cardiovascular Disease
    N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation.
  • HY-12688
    Succinyl phosphonate

    Endogenous Metabolite Reactive Oxygen Species Neurological Disease
    Succinyl phosphonate is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
  • HY-123275A
    H-D-Phe-Pip-Arg-pNA hydrochloride

    S-2238 hydrochloride

    Others Others
    H-D-Phe-Pip-Arg-pNA (S-2238) hydrochloride, a chromogenic substrate, is patterned after the N-terminal portion of the A alpha chain of fibrinogen, which is the natural substrate of thrombin. H-D-Phe-Pip-Arg-pNA hydrochloride is specific for thrombin and is used to measure antithrombin-heparin cofactor (AT-III). The AT-III assay using H-D-Phe-Pip-Arg-pNA hydrochloride is sensitive, accurate, and easy to perform.
  • HY-129388
    Pulrodemstat Methylbenzenesulfonate

    CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate

    Histone Demethylase Cancer
    CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-P1036A
    Compstatin TFA

    Complement System Others
    Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
  • HY-128570
    FD-IN-1

    Complement System Inflammation/Immunology
    FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5 µM, respectively.
  • HY-123275C
    H-D-Phe-Pip-Arg-pNA dihydrochloride

    S-2238 dihydrochloride

    Others Others
    H-D-Phe-Pip-Arg-pNA (S-2238) dihydrochloride, a chromogenic substrate, is patterned after the N-terminal portion of the A alpha chain of fibrinogen, which is the natural substrate of thrombin. H-D-Phe-Pip-Arg-pNA dihydrochloride is specific for thrombin and is used to measure antithrombin-heparin cofactor (AT-III). The AT-III assay using H-D-Phe-Pip-Arg-pNA dihydrochloride is sensitive, accurate, and easy to perform.
  • HY-130426
    Maleimido-tri(ethylene glycol)-propionic acid

    Mal-PEG3-acid

    ADC Linkers PROTAC Linkers Cancer
    Maleimido-tri(ethylene glycol)-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Maleimido-tri(ethylene glycol)-propionic acid is used for the preparation of neolymphostin-based ADC precursors for site-specific cysteine mutant trastuzumab-A114C conjugation. Maleimido-tri(ethylene glycol)-propionic acid also can be used as a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-P1318A
    Ac-RYYRIK-NH2 TFA

    Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
  • HY-17624
    Framycetin

    Neomycin B; Fradiomycin B

    Antibiotic 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-10571A
    Delavirdine mesylate

    U 90152 mesylate; BHAP-U 90152 mesylate

    HIV Reverse Transcriptase Infection
    Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
  • HY-114962
    S-22153

    Melatonin Receptor Neurological Disease
    S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes.
  • HY-100671
    L002

    Histone Acetyltransferase STAT Cancer Inflammation/Immunology
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.
  • HY-N2425
    Rhodiosin

    AChE Metabolic Disease
    Rhodiosin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.420 μM and a Ki of 0.535 μM. Rhodiosin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL. Rhodiosin exhibits potent DPPH free radical scavenging activities, with an IC50 of 27.77 μM.
  • HY-135318
    NBDHEX

    Glutathione Peroxidase Apoptosis Autophagy Cancer
    NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
  • HY-108944
    LYP-IN-1

    Phosphatase Inflammation/Immunology
    LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki and an IC50 of 110 nM and 0.259 μM, respectively. LYP-IN-1 also has selectivity for a large panel of PTPs, such as SHP1 (IC50=5 μM) and SHP2 (IC50=2.5 μM). LYP-IN-1 exhibits highly efficacious cellular activity in T- and mast cells. LYP-IN-1 can be used for the study of autoimmune disorders.
  • HY-N0241
    Rhodionin

    AChE Metabolic Disease
    Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM. Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL. Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM.
  • HY-10514
    BX795

    PDK-1 IKK Autophagy Cancer
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
  • HY-111846
    PROTAC ERα Degrader-2

    SNIPER PROTACs Estrogen Receptor/ERR Cancer
    PROTAC ERα Degrader-2 comprises a IAP ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
  • HY-119016A
    SK1-​I hydrochloride

    BML-258 hydrochloride

    SphK Cancer
    SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity.
  • HY-106224A
    Orexin A (human, rat, mouse) (TFA)

    Orexin Receptor (OX Receptor) Neurological Disease
    Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
  • HY-17624A
    Framycetin sulfate

    Neomycin B sulfate; Fradiomycin B sulfate

    Antibiotic 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-N0822
    Shikonin

    C.I. 75535; Isoarnebin 4

    Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV Cancer
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
  • HY-126350
    CL2-SN-38

    Drug-Linker Conjugates for ADC Cancer
    CL2-SN-38 is a part of the antibody drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is a DNA topoisomerase I inhibitor. The anti-Trop-2 hRS7-CL2A-SN-38 ADC provides significant and specific antitumor effects against a range of human solid tumor types.
  • HY-10571
    Delavirdine

    U 90152; BHAP-U 90152

    HIV Reverse Transcriptase Infection
    Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
  • HY-B0682S
    Mitiglinide-d8 calcium hydrate

    Potassium Channel Metabolic Disease
    Mitiglinide-d8 calcium hydrate (KAD-1229-d8) is the deuterium labeled Mitiglinide calcium hydrate. Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K + (KATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes.
  • HY-12688A
    Succinyl phosphonate trisodium salt

    Endogenous Metabolite Reactive Oxygen Species Cancer Metabolic Disease Neurological Disease
    Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
  • HY-115570
    GW406108X

    GW108X

    Kinesin ULK Autophagy Cancer
    GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK.
  • HY-119016
    SK1-I

    BML-258

    SphK Cancer
    SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity.
  • HY-136092
    Androsta-1,4,6-triene-3,17-dione

    Aromatase Endocrinology Neurological Disease
    Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor with a Ki of 0.18 μM. Androsta-1,4,6-triene-3,17-dione inhibits estrogen biosynthesis and shows antifertility effects. Androsta-1,4,6-triene-3,17-dione induces impairment of spatial memory.
  • HY-100277
    Mifobate

    SR-202

    PPAR Metabolic Disease
    Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects.
  • HY-N0005
    Curcumin

    Diferuloylmethane; Natural Yellow 3; Turmeric yellow

    Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis Cancer
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
  • HY-122214
    AC-73

    Autophagy Cancer
    AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells. AC-73 is also an anti-proliferative drug and an inducer of autophagy in leukemic cells.
  • HY-107146
    PZ-128

    P1pal-7

    Protease-Activated Receptor (PAR) Cancer Cardiovascular Disease
    PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects.
  • HY-P1323
    [Leu31,Pro34]-Neuropeptide Y(human,rat)

    Neuropeptide Y Receptor Neurological Disease Cardiovascular Disease
    [Leu31,Pro34]-Neuropeptide Y(human,rat) is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) can increase blood pressure in anesthetized rats and increases food intake.
  • HY-126675A
    AS2863619

    CDK STAT Inflammation/Immunology
    AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.
  • HY-32329
    Setiptiline

    Org-8282

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
  • HY-17372S
    Rofecoxib (D5)

    COX Inflammation/Immunology Cancer
    Rofecoxib D5 (MK 966 D5) is the deuterium labeled Rofecoxib. Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).
  • HY-N0142
    Phloretin

    NSC 407292; RJC 02792

    SGLT Endogenous Metabolite GLUT Metabolic Disease Cancer
    Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Prunus mandshurica, has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively.Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation.
  • HY-125751
    UCSF924

    Dopamine Receptor Neurological Disease
    UCSF924 is a potent and specific dopamine D4 receptor (DRD4) partial agonist with a EC50 of 4.2 nM. UCSF924 has a high-affinity with a Ki value of 3 nM for DRD4 and shows no measurable affinity for D2, D3 or the F261V/L328F D4 mutant. UCSF924 is a 7.4-fold bias toward arrestin over Gαi/o signaling, referenced to quinpirole.
  • HY-P0262
    Galantide

    Neuropeptide Y Receptor Metabolic Disease Inflammation/Immunology Neurological Disease Endocrinology
    Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM).
  • HY-101676
    RG-12525

    NID 525

    Leukotriene Receptor PPAR Cytochrome P450 Metabolic Disease
    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
  • HY-16729A
    Relenopride hydrochloride

    YKP10811 hydrochloride

    5-HT Receptor Inflammation/Immunology
    Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility.
  • HY-119271
    CMLD010509

    SDS-1-021

    c-Myc Apoptosis Cancer
    CMLD010509 (SDS-1-021) is a highly specific inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. CMLD010509 (SDS-1-021) shows an IC50 below 10 nM for most MM cell lines and induces apoptosis. CMLD010509 (SDS-1-021) is a potent and selective translation inhibitor through an eIF4E phosphorylation-independent mechanism.
  • HY-128850
    N-Acetyl-D-mannosamine

    N-Acetylmannosamine; ManNAc

    Bacterial Neurological Disease
    N-Acetyl-D-mannosamine (ManNAc) is an essential precursor of N-acetylneuraminic acid (NeuAc), the specific monomer of bacterial capsular polysialic acid (PA). N-Acetyl-D-mannosamine (ManNAc) can be metabolized by GNE and GlcNAc 2-epimerase (Renin binding protein, RnBP), into ManNAc-6-phosphate and GlcNAc, respectively.  N-Acetyl-d-mannosamine (ManNAc) and its derivatives activates hypocretin (HCRT) gene expression in the orexin neurons, providing a potential model for the testing of a therapy for neural disorders.
  • HY-113846
    CMP-5 hydrochloride

    Histone Methyltransferase Cancer
    CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
  • HY-111329
    JGB1741

    ILS-JGB-1741

    Sirtuin Apoptosis Cancer
    JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research.
  • HY-B0268A
    Enoxacin hydrate

    Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate

    Bacterial DNA/RNA Synthesis MicroRNA Antibiotic Infection Cancer
    Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
  • HY-111310
    ML351

    Lipoxygenase Metabolic Disease Neurological Disease
    ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC50 of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2. ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D.
  • HY-120137
    CMP-5

    Histone Methyltransferase Cancer
    CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
  • HY-141512
    JB170

    PROTACs Aurora Kinase Cancer
    JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase.
  • HY-15701
    Leukadherin-1

    Integrin Complement System Inflammation/Immunology
    Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling.
  • HY-122156
    IMB-301

    HIV Infection
    IMB-301 is a specific HIV-1 replication inhibitor that binds to hA3G (human APOBEC3G), interrupts the hA3G-Vif interaction and inhibits Vif-mediated degradation of hA3G. IMB-301 inhibits the replication of HIV-1 in H9 cells (IC50=8.63 uM). Human APOBEC3G is a restriction factor that inhibits human immunodeficiency 1 virus (HIV-1) replication.
  • HY-112163
    Zotatifin

    eFT226

    Eukaryotic Initiation Factor (eIF) SARS-CoV Apoptosis Cancer Infection
    Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM). Zotatifin induces cell apoptosis.
  • HY-B0151
    Pregnenolone

    3β-Hydroxy-5-pregnen-20-one

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-B0268
    Enoxacin

    AT 2266; CI 919

    Bacterial DNA/RNA Synthesis MicroRNA Antibiotic Cancer Infection
    Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
  • HY-N6257
    Cafestol

    ERK PGE synthase COX NF-κB Cancer Inflammation/Immunology
    Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects.
  • HY-N2187
    Deoxyshikonin

    Bacterial HIF/HIF Prolyl-Hydroxylase Cancer Infection Cardiovascular Disease
    Deoxyshikonin is isolated from Lithospermum erythrorhizon Sieb with antitumor activity. Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF, indicates a prolymphangiogenesis as well as a proangiogenesis effect in vitro. Deoxyshikonin shows significant synergic antimicrobial activity against S. pneumonia (MIC=17 μg/mL), also shows significantly inhibitory activities against MRSA.
  • HY-126675
    AS2863619 free base

    CDK STAT Inflammation/Immunology
    AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
  • HY-50751
    Linifanib

    ABT-869; AL-39324

    PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis Cancer
    Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
  • HY-N1584
    Halofuginone

    RU-19110

    DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Cancer Infection Inflammation/Immunology Cardiovascular Disease
    Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
  • HY-32329A
    Setiptiline maleate

    MO-8282

    5-HT Receptor Neurological Disease
    Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
  • HY-P1323A
    [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA

    Neuropeptide Y Receptor Neurological Disease Cardiovascular Disease
    [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA can increase blood pressure in anesthetized rats and increases food intake.
  • HY-136522
    S2116

    Histone Demethylase Apoptosis Cancer
    S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
  • HY-122815
    Fusicoccin

    Fusicoccin A

    Apoptosis Cancer
    Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.
  • HY-14604
    Xaliproden hydrochloride

    SR57746A; SR57746 hydrochloride

    5-HT Receptor Dopamine Receptor Neurological Disease
    Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases.
  • 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-110133
    JTE-607

    Others Inflammation/Immunology
    JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively. Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607.
  • HY-17038A
    Agomelatine hydrochloride

    S-20098 hydrochloride

    Melatonin Receptor 5-HT Receptor Neurological Disease
    Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
  • HY-14850
    Sograzepide

    Netazepide; YF 476; YM-220

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively.
  • HY-B1739
    Pregnenolone monosulfate

    3β-Hydroxy-5-pregnen-20-one monosulfate

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-111673
    8-CPT-Cyclic AMP sodium

    8-CPT-cAMP sodium; 8-(p-Chlorophenylthio)-cAMP sodium

    PKA Phosphodiesterase (PDE) Inflammation/Immunology
    8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epac activator.
  • HY-17038
    Agomelatine

    S-20098

    Melatonin Receptor 5-HT Receptor Neurological Disease
    Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
  • HY-18980
    Rottlerin

    Mallotoxin; NSC 56346; NSC 94525

    PKC Autophagy Apoptosis HIV Infection Cancer
    Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.
  • HY-N1584A
    Halofuginone hydrobromide

    RU-19110 hydrobromide

    DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Cancer Infection Inflammation/Immunology Cardiovascular Disease
    Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
  • HY-100034
    NSC 663284

    DA-3003-1

    Phosphatase Histone Methyltransferase Cancer
    NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM).
  • HY-110189
    Pregnenolone monosulfate sodium salt

    3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-114041
    Resolvin E1

    RvE1

    Endogenous Metabolite Inflammation/Immunology
    Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production.
  • HY-112289
    IDH889

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM.
  • HY-136523
    S2157

    Histone Demethylase Apoptosis Cancer
    S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
  • HY-135680
    I-OMe-Tyrphostin AG 538

    I-OMe-AG 538

    IGF-1R Cancer Metabolic Disease
    I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
  • HY-12398A
    TEI-9648

    VD/VDR Metabolic Disease Inflammation/Immunology
    TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research.
  • HY-12398
    TEI-9647

    VD/VDR Metabolic Disease Inflammation/Immunology
    TEI-9647, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9647 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9647 inhibits bone resorption and HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9647 has the potential for suppressing the excessive bone resorption and osteoclast formation in Paget's disease.
  • HY-13453
    BAY 11-7082

    BAY 11-7821

    IKK Deubiquitinase Autophagy Apoptosis Cancer Inflammation/Immunology
    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
  • HY-128946
    CL2A-SN-38

    Drug-Linker Conjugates for ADC Cancer Inflammation/Immunology
    CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.
  • HY-108543
    NSC 95397

    Phosphatase Apoptosis Cancer
    NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)). NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.
  • HY-17038B
    Agomelatine (L(+)-Tartaric acid)

    S-20098 L(+)-Tartaric acid

    Melatonin Receptor 5-HT Receptor Neurological Disease
    Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
  • HY-32329S
    Setiptiline-d3

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Setiptiline-d3 (Org-8282-d3) is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
  • HY-101508
    GNA002

    Histone Methyltransferase Cancer
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
  • HY-16561
    Resveratrol

    trans-Resveratrol; SRT501

    IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Cancer Infection Inflammation/Immunology
    Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
  • HY-B0268S
    Enoxacin-d8

    Bacterial DNA/RNA Synthesis MicroRNA Antibiotic Cancer Infection
    Enoxacin-d8 (AT 2266-d8) is the deuterium labeled Enoxacin. Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
  • HY-116716
    PIN1 inhibitor API-1

    MicroRNA Cancer
    PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development.
  • HY-P1110
    AF12198

    Interleukin Related Inflammation/Immunology
    AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo.
  • HY-15310
    Ivermectin

    MK-933

    Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.