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Targets Recommended: IGF-1R c-Fms IRAK PERK

Results for "A2A/2B R Inhibitors" in MCE Product Catalog:

9687

Inhibitors & Agonists

38

Screening Libraries

23

Dye Reagents

15

Biochemical Assay Reagents

360

Peptides

6

MCE Kits

12

Inhibitory Antibodies

1472

Natural
Products

22

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-P1114
    2B-(SP)

    GSK-3 Neurological Disease
    2B-(SP) is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) is readily phosphorylated by both the α and β isoforms of GSK-3.
  • HY-P1114A
    2B-(SP) (TFA)

    GSK-3 Cancer
    2B-(SP) TFA is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) TFA is readily phosphorylated by both the α and β isoforms of GSK-3.
  • HY-102024
    A2A receptor antagonist 1

    CPI-444 analog

    Adenosine Receptor Cancer Neurological Disease
    A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Ki values of 4 and 264 nM, respectively.
  • HY-116463C
    (2R,3R)-E1R

    Sigma Receptor Neurological Disease
    (2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-U00321
    A2B receptor antagonist 1

    Adenosine Receptor Inflammation/Immunology Cancer
    A2B receptor antagonist 1 is a potent A2B adenosine receptor antagonist extracted from patent WO 2009157938 A1 EXAMPLE 9B.
  • HY-P0117
    Tat-NR2B9c

    Tat-NR2Bct; NA-1

    iGluR NO Synthase Neurological Disease
    Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.
  • HY-P0117A
    Tat-NR2B9c TFA

    Tat-NR2Bct TFA; NA-1 TFA

    iGluR NO Synthase Neurological Disease
    Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c TFA disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.
  • HY-B1915
    Micronomicin

    Gentamicin C2B; Antibiotic XK-62-2; Sagamicin

    Bacterial Infection
    Micronomicin (Gentamicin C2b) is an aminoglycoside antibiotic, with antibacterial and bactericidal activities.
  • HY-126057S
    (R)-Praziquantel D11

    Parasite 5-HT Receptor Infection
    (R)-Praziquantel D11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer.
  • HY-103186
    MRS-1706

    Adenosine Receptor Inflammation/Immunology
    MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively.
  • HY-111767
    BAY-545

    Adenosine Receptor Inflammation/Immunology
    BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. BAY-545 also exhibits IC50s of 66, 400, 280 nM for human, mouse, rat A2B adenosine receptor in cells, respectively, and a Ki of 97 nM for human A2B adenosine receptor, with more selectivity over A1, A2A, and A3 adenosine receptor.
  • HY-110279
    Ogerin

    Others Neurological Disease
    Ogerin is a selective GPR68 positive allosteric modulator, with a pEC50 of 6.83. Ogerin shows inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptoor and weak antagonist activity (Ki, 736 nM) at 5-HT2B receptor. Ogerin blocks recall in fear conditioning in mice.
  • HY-103169
    SCH442416

    Adenosine Receptor Neurological Disease
    SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain.
  • HY-19533
    SCH 58261

    Adenosine Receptor Cancer
    SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively.
  • HY-B2006
    Fenvalerate

    Phosphatase Bacterial Infection
    Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide.
  • HY-100678
    CGS 15943

    Adenosine Receptor PI3K Cancer Inflammation/Immunology
    CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. [1].
  • HY-10238
    Danoprevir

    ITMN-191; R7227; RO5190591; RG7227

    HCV Protease HCV Infection
    Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC50 of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC50 higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC50s=0.2-0.4 nM) as well as 2b and 3a (IC50s=1.6, 3.5 nM).
  • HY-106441A
    Rislenemdaz

    MK-0657; CERC-301

    iGluR Neurological Disease
    Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
  • HY-108307
    Micronomicin sulfate

    Gentamicin C2B sulfate; Antibiotic XK-62-2 sulfate; Sagamicin sulfate

    Antibiotic Bacterial Infection
    Micronomicin sulfate (Gentamicin C2b sulfate) is an aminoglycoside antibiotic isolated from Micromonospora. Micronomicin sulfate is a broad-spectrum antibiotic close to the gentamicin-type antibiotics, exhibits a high activity against Pseudomonas, Proteus, Klebsiella pneumoniae, Serratia, etc (MIC=0.001-8.3 μg/ml).
  • HY-B0228
    Adenosine

    Adenine riboside; D-Adenosine

    Nucleoside Antimetabolite/Analog Autophagy Apoptosis Endogenous Metabolite Cancer Metabolic Disease
    Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
  • HY-12294
    PEAQX

    NVP-AAM077

    iGluR Neurological Disease
    PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).
  • HY-135785
    OSMI-3

    Acyltransferase Metabolic Disease
    OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells.
  • HY-15472
    PRX-08066

    5-HT Receptor Cardiovascular Disease
    PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
  • HY-11100
    Asenapine maleate

    Org 5222 maleate

    5-HT Receptor Neurological Disease
    Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.
  • HY-A0168
    Regadenoson

    CVT-3146

    Adenosine Receptor Cardiovascular Disease Cancer
    Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents.
  • HY-103154
    SB228357

    5-HT Receptor Neurological Disease
    SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects.
  • HY-103171
    BAY 60-6583

    Adenosine Receptor Inflammation/Immunology Cardiovascular Disease
    BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50 = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model.
  • HY-14873
    Tonapofylline

    BG 9928

    Adenosine Receptor Metabolic Disease Cardiovascular Disease
    Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure.
  • HY-16567
    Asenapine hydrochloride

    5-HT Receptor Dopamine Receptor Neurological Disease
    Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
  • HY-114204
    GSK8814

    Epigenetic Reader Domain Cancer
    GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1.
  • HY-N3513
    Mulberrin

    Kuwanon C

    Others Cardiovascular Disease
    Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
  • HY-100014
    KDM5A-IN-1

    Histone Demethylase Cancer
    KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
  • HY-P2307
    Tat-NR2Baa

    iGluR NO Synthase Neurological Disease
    Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
  • HY-P2307A
    Tat-NR2Baa TFA

    iGluR NO Synthase Neurological Disease
    Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
  • HY-19778
    (R)-BPO-27

    CFTR Autophagy Inflammation/Immunology
    (R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitive CFTR inhibitor with an IC50 of 4 nM.
  • HY-18596
    SB-215505

    5-HT Receptor Neurological Disease
    SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively. SB-215505 increases wakefulness and motor activity in rats.
  • HY-136233
    PSB 0777 ammonium

    Adenosine Receptor Inflammation/Immunology
    PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research.
  • HY-106638
    Voclosporin

    ISAtx-247

    Phosphatase Inflammation/Immunology
    Voclosporin (ISAtx-247) is a calcineurin (PP2B) (CN) inhibitor.
  • HY-13993
    Ro 25-6981

    iGluR Neurological Disease
    Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.
  • HY-136165
    (S,R,S)-AHPC-PEG3-propionic acid

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG3-propionic acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
  • HY-103129A
    SB-200646

    5-HT Receptor Neurological Disease
    SB-200646 is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo.
  • HY-B0531
    Triflusal

    COX Inflammation/Immunology
    Triflusal irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1.
  • HY-103129
    SB-200646A

    5-HT Receptor Neurological Disease
    SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.
  • HY-136299A
    Sepimostat dimethanesulfonate

    FUT-187

    iGluR Neurological Disease
    Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 µM.
  • HY-136299
    Sepimostat

    FUT-187 free base

    iGluR Neurological Disease
    Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7 µM.
  • HY-108539
    CE3F4

    Others Cardiovascular Disease
    CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
  • HY-N0859
    Schisanhenol

    Schizanhenol; Gomisin-K3

    Others Cancer
    Schisanhenol is a natural compound solated from Schisandra rubriflora; UGT2B7 UDP-glucuronosyltransferases inhibitor.
  • HY-N5132
    (-)-Fenchone

    Others Others
    (-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Thuja occidentalis. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6.
  • HY-14153A
    Tegaserod maleate

    SDZ-HTF-919; HTF-919

    5-HT Receptor Metabolic Disease Neurological Disease
    Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract.
  • HY-14390
    LAS101057

    Adenosine Receptor Inflammation/Immunology
    LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
  • HY-15296
    Cabergoline

    FCE-21336

    Dopamine Receptor Autophagy Endocrinology
    Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
  • HY-13409A
    SB 242084 hydrochloride

    5-HT Receptor Neurological Disease
    SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.
  • HY-13409
    SB 242084

    5-HT Receptor Neurological Disease
    SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.
  • HY-131032
    KI-7

    Adenosine Receptor Others
    KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively.
  • HY-15419
    RS-127445 hydrochloride

    5-HT Receptor Neurological Disease
    RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
  • HY-N7136
    α-​Terpinyl acetate

    Cytochrome P450 Metabolic Disease
    α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM.
  • HY-15419A
    RS-127445

    5-HT Receptor Neurological Disease
    RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
  • HY-B1184
    Mephenytoin

    Cytochrome P450 Neurological Disease
    Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate.
  • HY-12451
    FICZ

    6-Formylindolo[3,2-b]carbazole

    Aryl Hydrocarbon Receptor Others
    FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a Kd of 70 pM.
  • HY-12962
    NMDA-IN-1

    iGluR Neurological Disease
    NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
  • HY-N0092
    Inosine

    Adenosine Receptor Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-13993A
    Ro 25-6981 Maleate

    iGluR Neurological Disease
    Ro 25-6981 Maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit.
  • HY-10559
    Nelotanserin

    APD125

    5-HT Receptor Cancer Neurological Disease
    Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
  • HY-111500A
    NMDAR antagonist 1

    iGluR Neurological Disease
    NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist.
  • HY-N6937
    (R,R)-Secoisolariciresinol diglucoside

    (R,R)-SDG; (R,R)-LGM2605

    Others Inflammation/Immunology
    (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) is the minor isomer of Secoisolariciresinol diglucoside in flaxseed. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) possesses antioxidant and free radical scavenging activities and DNA-radioprotective properties. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) inhibits myeloperoxidase (MPO) activity by suppressing both the peroxidase and chlorination cyclesin inflammatory cells.
  • HY-10564
    Sarpogrelate hydrochloride

    MCI-9042

    5-HT Receptor Cardiovascular Disease
    Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
  • HY-15543A
    CP-809101 hydrochloride

    5-HT Receptor Neurological Disease
    CP-809101 hydrochloride is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively.
  • HY-15543
    CP-809101

    5-HT Receptor Neurological Disease
    CP-809101 is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively.
  • HY-B0365A
    Memantine hydrochloride

    D-145 hydrochloride

    Cytochrome P450 iGluR Autophagy Neurological Disease
    Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively.
  • HY-B0761
    (R,R)-Glycopyrrolate

    (R,R)-Glycopyrronium bromide; (R,R)-Glycopyrrolate bromide

    mAChR Neurological Disease
    (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) is an anticholinergic agent. (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) has the ability to reduce the frequency of drooling in vivo with developmental disabilities.
  • HY-103110A
    ST1936 oxalate

    5-HT Receptor Neurological Disease
    ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human α2 adrenergic receptor.
  • HY-13457
    TCN 201

    iGluR Neurological Disease
    TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDA receptor, with a pIC50 of 6.8. TCN 201 is selective for GluN1/GluN2A NMDA receptor over GluN1/GluN2B NMDA receptor (pIC50<4.3).
  • HY-10995
    Tozadenant

    SYN115

    Adenosine Receptor Neurological Disease
    Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A.
  • HY-78131B
    (R)-(-)-Ibuprofen

    (R)-Ibuprofen

    NF-κB Inflammation/Immunology Cancer
    (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
  • HY-100615A
    R 80123

    Phosphodiesterase (PDE) Cardiovascular Disease
    R 80123 is the Z-isomer of R 79595, is also a highly selective phosphodiesterase inhibitor.
  • HY-13728A
    (R)-Plevitrexed

    (R)-ZD 9331; (R)-BGC9331

    Others Cancer
    (R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.
  • HY-B0822
    Fipronil

    GABA Receptor Cytochrome P450 Neurological Disease
    Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC500s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
  • HY-13079
    Cobimetinib (R-enantiomer)

    GDC-0973 R-enantiomer; XL-518 R-enantiomer

    MEK Cancer
    Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
  • HY-N1992
    Theaflavin 3,3'-digallate

    TF-3; ZP10

    Virus Protease HSV HIV Cancer Infection
    Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 µM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent.
  • HY-101474B
    (R)-Zanubrutinib

    (R)-BGB-3111

    Others Others
    (R)-Zanubrutinib is the R enantiomer of Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
  • HY-131452
    1-Ethynylpyrene

    Cytochrome P450 Cancer
    1-Ethynylpyrene is an aryl acetylenic inhibitor of cytochromes P450 1A1, 1A2, and 2B1 with IC50s of 0.18, 0.32, and 0.04 μM, respectively.
  • HY-109854A
    (R)-Lisofylline

    (R)-Lisophylline

    STAT Metabolic Disease Inflammation/Immunology
    (R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC50 of 0.6 µM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research.
  • HY-U00341
    ST4206

    Adenosine Receptor Neurological Disease
    ST4206 is a potent adenosine A2A antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively.
  • HY-10809A
    Bitopertin (R enantiomer)

    RG1678 (R enantiomer); RO4917838 (R enantiomer)

    GlyT Neurological Disease
    Bitopertin R enantiomer (RG1678 R enantiomer; RO4917838 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
  • HY-14121
    MRS 1754

    Adenosine Receptor Metabolic Disease Inflammation/Immunology
    MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats.
  • HY-111500
    (Rac)-NMDAR antagonist 1

    iGluR Neurological Disease
    (Rac)-NMDAR antagonist 1 is the racemate of NMDAR antagonist 1. NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist.
  • HY-15187A
    (R)-Filanesib

    (R)-ARRY-520

    Kinesin Cancer
    (R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of Filanesib (HY-15187). Filanesib is a synthetic kinesin spindle protein (KSP) inhibitor with an IC50 of 6 nM.
  • HY-112840
    ST3932

    Adenosine Receptor Neurological Disease
    ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.
  • HY-135336
    (R)-Verapamil hydrochloride

    (R)-(+)-Verapamil hydrochloride

    P-glycoprotein Apoptosis Cancer
    (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs.
  • HY-106841
    Draflazine

    R-75231; R88021

    Others Inflammation/Immunology
    Draflazine (R-75231) is a ENT1 inhibitor. Draflazine (R-75231) completely reverses the hypersensitivity in the complete Freund’s adjuvant (CFA) model of mechanical hyperalgesia and the carrageenan inflammation model of thermal and mechanical hyperalgesia.
  • HY-10895
    SB-334867

    SB 334867A

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
  • HY-B1033
    Metergoline

    5-HT Receptor Dopamine Receptor Sodium Channel Neurological Disease
    Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline also is a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.
  • HY-12882A
    Ifenprodil tartrate

    iGluR Potassium Channel Neurological Disease
    Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator.
  • HY-U00180
    KF21213

    Adenosine Receptor Neurological Disease
    KF21213 is a highly selective ligand for mapping CNS adenosine A2A receptors. KF21213 shows a high affinity for the adenosine A2A receptors (Ki=3.0 nM).
  • HY-103138A
    (Rac)-WAY-161503

    5-HT Receptor Metabolic Disease Neurological Disease
    (Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects.
  • HY-19939S2
    (R)-VX-984

    (R)-M9831

    Others Others
    (R)-VX-984 ((R)-M9831) is the (R)-enantiomer of VX-984. VX-984 is a potent DNA-PK inhibitor.
  • HY-12953
    R-268712

    TGF-β Receptor Cancer
    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  • HY-16420
    R112

    Syk Inflammation/Immunology
    R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.
  • HY-A0021C
    (R,R)-Palonosetron Hydrochloride

    5-HT Receptor Inflammation/Immunology
    (R,R)-Palonosetron Hydrochloride is the active enantiomer of Palonosetron.
  • HY-12279F
    Umbralisib R-enantiomer

    TGR-1202 R-enantiomer; RP5264 R-enantiomer

    PI3K Cancer
    Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
  • HY-14777
    Radiprodil

    RGH-896

    iGluR Neurological Disease
    Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions.
  • HY-14658B
    (R)-Thalidomide

    (R)-(+)-Thalidomide

    Others Metabolic Disease
    (R)-Thalidomide ((R)-(+)-Thalidomide) is the R-enantiomer of Thalidomide. (R)-Thalidomide has sedative properties.
  • HY-15996A
    Seviteronel R enantiomer

    VT-464 (R enantiomer)

    Others Cancer
    Seviteronel R enantiomer (VT-464 R enantiomer) is the R enantiomer of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM); Seviteronel (VT-464) R enantiomer's activity is unknown.
  • HY-13201
    CGS 21680

    Adenosine Receptor Neurological Disease
    CGS 21680 is a selective adenosine A2A receptor agonist, with a Ki of 27 nM.
  • HY-13201A
    CGS 21680 Hydrochloride

    Adenosine Receptor Neurological Disease
    CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.
  • HY-59125
    (R,R)-(+)-Hydrobenzoin

    Endogenous Metabolite Others
    (R,R)-(+)-Hydrobenzoin is a organocatalysts.
  • HY-112254
    ZINC03129319

    Virus Protease Infection
    ZINC03129319 is a dengue virus (DENV) NS2B-NS3 protease inhibitor extracted from patent US20150141521A1, has inhibition constants (Ki1) of 92 μM and Ki3 of 20 μM.
  • HY-10895A
    SB-334867 free base

    SB334867A free base

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
  • HY-100888A
    (R)-Simurosertib

    (R)-TAK-931

    Others Others
    (R)-Simurosertib ((R)-TAK-931) is the (R)-enantiomer of Simurosertib. Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM .
  • HY-112172
    Tenalisib R Enantiomer

    RP6530 R Enantiomer

    Others Cancer
    Tenalisib R Enantiomer (RP6530 R Enantiomer) is an R enantiomer of Tenalisib. Tenalisib is a potent and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.
  • HY-B0105
    Ketoconazole

    Ketoconazol; R 41400

    Fungal Cytochrome P450 Ras Infection Cancer
    Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
  • HY-108263B
    (R)-3-Hydroxy Midostaurin

    (R)-CGP52421

    FLT3 Drug Metabolite Cancer
    (R)-3-Hydroxy Midostaurin ((R)-CGP52421) is a potent kinases inhibitor. (R)-3-Hydroxy Midostaurin is a major metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (R)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML).
  • HY-17416
    Guanfacine hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors.
  • HY-10081
    GS-6201

    CVT-6883

    Adenosine Receptor Inflammation/Immunology
    GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.
  • HY-106136
    TIK-301

    PD-6735; LY-156735

    Melatonin Receptor 5-HT Receptor Neurological Disease
    TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.
  • HY-100637
    Hydroxybupropion

    Adrenergic Receptor nAChR Neurological Disease
    Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6. Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC50 value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonist .
  • HY-10619D
    Niraparib (R-enantiomer)

    MK 4827 (R-enantiomer)

    PARP Cancer
    Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM.
  • 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-12693
    R(+)-IAA-94

    R(+)-Methylindazone

    Chloride Channel Others
    R(+)-IAA-94 (R(+)-Methylindazone) is a potent indanyloxyacetic acid blocker of epithelial chloride channels. R(+)-IAA-94 inhibits Nef-sdAb19 (single-domain antibody) interaction and binds to negative factor (Nef).
  • HY-122219
    R243

    CCR Inflammation/Immunology
    R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects.
  • HY-W010195
    2,6-Dimethylquinoline

    Cytochrome P450 Others
    2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM.
  • HY-12993B
    RSV604 (R enantiomer)

    A-60444 (R enantiomer)

    RSV Infection
    RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is an inhibitor of respiratory syncytial virus (RSV) replication. R-enantiomer is less active against RSV.
  • HY-104075
    R916562

    TAM Receptor VEGFR Cancer
    R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.
  • HY-135336S
    (R)-Verapamil D7 hydrochloride

    (R)-(+)-Verapamil D7 hydrochloride

    P-glycoprotein Apoptosis Cancer
    (R)-Verapamil D7 hydrochloride ((R)-(+)-Verapamil D7 hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs.
  • HY-102091
    (2R,4R)-APDC

    mGluR Neurological Disease
    (2R,4R)-APDC is a selective group II metabotropic glutamate receptors (mGluRs) agonist. (2R,4R)-APDC has anticonvulsant and neuroprotective effects.
  • HY-13038A
    Fostamatinib

    R788

    Syk FLT3 Inflammation/Immunology Cancer
    Fostamatinib (R788) is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-16900A
    (R)-(-)-Rolipram

    (R)-Rolipram; (-)-Rolipram

    Phosphodiesterase (PDE) Neurological Disease
    (R)-(-)-Rolipram is the R-enantiomer of Rolipram. Rolipram is a selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.
  • HY-13737
    R1530

    VEGFR FGFR Apoptosis Cancer
    R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kds of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50s of 10 nM and 28 nM, respectively.
  • HY-118152
    Org-12962

    5-HT Receptor Neurological Disease
    Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.
  • HY-108900A
    Leu-AMS R enantiomer

    Aminoacyl-tRNA Synthetase Others
    Leu-AMS R enantiomer is the R enatiomer of Leu-AMS. Leu-AMS is a potent inhibitor of leucyl-tRNA synthetase (LRS) and inhibits the growth of bacteria.
  • HY-17504C
    (3R,5R)-Rosuvastatin

    HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Metabolic Disease Cardiovascular Disease
    (3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
  • HY-W015851
    (R)-3-Hydroxybutanoic acid sodium

    (R)-(-)-3-Hydroxybutanoic acid sodium; (R)-3-Hydroxybutyric acid sodium

    Endogenous Metabolite Neurological Disease
    (R)-3-Hydroxybutanoic acid sodium ((R)-3-Hydroxybutyric acid) is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid sodium has applications as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones.
  • HY-B0352B
    (R)-Mirtazapine

    (R)-Org3770; (R)-6-Azamianserin

    5-HT Receptor Neurological Disease
    (R)-Mirtazapine ((R)-Org3770) is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4.
  • HY-10888
    Istradefylline

    KW-6002

    Adenosine Receptor Neurological Disease
    Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
  • HY-B0006C
    (R)-Carvedilol

    (R)-BM 14190

    Adrenergic Receptor Cardiovascular Disease
    (R)-Carvedilol ((R)-BM 14190), the R-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (R)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).
  • HY-107774
    BMS-986163

    iGluR Neurological Disease
    BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
  • 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-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-10013B
    Taranabant ((1R,2R)stereoisomer)

    MK0364 (1R,2R)stereoisomer

    Cannabinoid Receptor Others
    Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.
  • HY-N2071
    Cedrol

    (+)-Cedrol; α-Cedrol

    Cytochrome P450 Fungal Infection Inflammation/Immunology Cancer
    Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities.
  • HY-15452B
    Selisistat R-enantiomer

    EX-527 (R-enantiomer)

    Sirtuin Cancer
    Selisistat R-enantiomer (EX-527 R-enantiomer) is much less active R-enantiomer of Selisistat, with an IC50 of > 100 μM for SIRT1.
  • HY-15781A
    Morinidazole (R enantiomer)

    R-Morinidazole

    Bacterial Infection
    Morinidazole R enantiomer is the R-enantiomer of Morinidazole. Morinidazole is a new 5-nitroimidazole class antimicrobial agent. Morinidazole R enantiomer is the less active enantiomer.
  • HY-116463A
    (2R,3S)-E1R

    Sigma Receptor Neurological Disease
    (2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-10857
    Vipadenant

    BIIB-014; CEB-4520

    Adenosine Receptor Neurological Disease
    Vipadenant (BIIB-014; CEB-4520) is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively.
  • HY-B0526
    Flumequine

    R-802

    Bacterial Topoisomerase Antibiotic Infection Cancer
    Flumequine (R-802) is a quinolone antibiotic, and acts as a topoisomerase II inhibitor, with an IC50 of 15 μM (3.92 μg/mL).
  • HY-17044A
    Duvelisib (R enantiomer)

    IPI-145 R enantiomer; INK1197 R enantiomer

    PI3K Cancer
    Duvelisib R enantiomer is a PI3K inhibitor, which is the less active enantiomer of Duvelisib.
  • HY-108355
    R59949

    PKC Cancer
    R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.
  • HY-135406
    (3R,5R)-Rosuvastatin Lactone

    Others Cardiovascular Disease Metabolic Disease
    (3R,5R)-Rosuvastatin Lactone is an isomer of Rosuvastatin Lactone.
  • HY-B0612D
    (R)-Lercanidipine hydrochloride

    Calcium Channel Cardiovascular Disease
    (R)-Lercanidipine hydrochloride is the R-enantiomer of Lercanidipine. (R)-lercanidipine hydrochloride is a calcium channel blocker.
  • HY-16106A
    (8R,9S)-Talazoparib

    (8R,9S)-BMN-673; (8R,9S)-LT-673

    PARP Cancer
    (8R,9S)-Talazoparib ((8R,9S)-BMN-673) is an enantiomer of Talazoparib (HY-16106). (8R,9S)-Talazoparib is an PARP1 inhibitor, with an IC50 of 144 nM.
  • HY-100032
    PD 117519

    CI947

    Adenosine Receptor Neurological Disease
    PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.
  • HY-100300
    AGN 192836

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.
  • 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-I0636
    (R)-Apremilast

    (R)-CC-10004

    Others Inflammation/Immunology
    (R)-Apremilast ((R)-CC-10004) is a enantiomer of Apremilast.
  • HY-17554
    (R)-Oxiracetam

    (R)-(+)-Oxiracetam

    Others Neurological Disease
    (R)-Oxiracetam is the (R)-enantiomer of the nootropic drug oxiracetam. Oxiracetam (ISF 2522) is a nootropic drug of the racetam family and stimulant.
  • HY-15355
    Loviride

    R 89439

    Reverse Transcriptase HIV Infection
    Loviride (R 89439) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), with an IC50 of 0.3 µM for reverse transcriptase from HIV-1. Loviride (R 89439) inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells.
  • HY-10889
    Preladenant

    SCH-420814

    Adenosine Receptor Neurological Disease
    Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.
  • HY-W051723
    (R)-3-Hydroxybutanoic acid

    (R)-(-)-3-Hydroxybutanoic acid; (R)-3-Hydroxybutyric acid

    Endogenous Metabolite Others
    (R)-3-Hydroxybutanoic acid is a metabolite, and converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid has applications as a nutrition source and as a precursor for vitamins, antibiotics and pheromones.
  • HY-19532
    ZM241385

    Adenosine Receptor Neurological Disease Cancer
    ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM.
  • HY-12067
    R406

    Syk FLT3 Apoptosis Cancer Inflammation/Immunology
    R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-78846
    2R,4R-Sacubitril

    Others Cardiovascular Disease
    2R,4R-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
  • HY-B0105A
    (+)-Ketoconazole

    (+)-Ketoconazol; (+)-R 41400

    Fungal Cytochrome P450 Infection
    (+)-Ketoconazole ((+)-R 41400) is an imidazole anti-fungal agent, a CYP3A4 inhibitor.
  • HY-124257
    (R)-Citronellol

    D-Citronellol; (R)-(+)-β-Citronellol

    Endogenous Metabolite Inflammation/Immunology
    (R)-Citronellol (D-Citronellol) is an alcoholic monoterpene found in geranium essential oil. (R)-Citronellol inhibits degranulation of mast cells and does not affect caffeine bitterness perception. (R)-Citronellol can be used in decorative cosmetics, toiletries as well as in non-cosmetic products.
  • HY-19488B
    Ribocil-C (R enantiomer)

    Bacterial Infection
    Ribocil-C R enantiomer is the R enantiomer of Ribocil-C. Ribocil-C is a highly selective inhibitor of bacterial riboflavin riboswitches.
  • HY-101978
    CPI-444

    V81444; ciforadenant

    Adenosine Receptor Cancer
    CPI-444 (V81444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.
  • 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-112164A
    IACS-8968 R-enantiomer

    IDO/TDO Inhibitor (R-enantiomer)

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IACS-8968 (R-enantiomer) is the R-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
  • HY-108250
    (R)-Bicalutamide

    Androgen Receptor Cancer
    (R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
  • HY-B0105B
    (-)-Ketoconazole

    (-)-Ketoconazol; (-)-R 41400

    Fungal Infection Inflammation/Immunology
    (-)-Ketoconazole ((-)-R 41400) is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
  • HY-U00189
    Sch412348

    Adenosine Receptor Neurological Disease
    Sch412348 is a potent competitive antagonist of the human adenosine A2A receptor (Ki=0.6 nM) and has >1000-fold selectivity over all other adenosine receptors.
  • HY-14365
    TC-G 1004

    Adenosine Receptor Neurological Disease
    TC-G 1004 (compound 16j) is an orally active A2A adenosine receptor antagonist, with Ki values of 0.44 nM and 80 nM for hA2A and hA1, respectively.
  • HY-120097
    R-10015

    LIM Kinase (LIMK) Reverse Transcriptase Infection
    R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1.
  • HY-N2049
    20(R)-Notoginsenoside R2

    Others Neurological Disease
    20(R)-Notoginsenoside R2 is an isolated notoginsenoside from Panax notoginseng.
  • HY-15658
    GSK2801

    Epigenetic Reader Domain Apoptosis Cancer
    GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4.
  • HY-B2111
    (R)-(+)-Atenolol

    Adrenergic Receptor Others
    (R)-(+)-Atenolol is the less active enantiomer of the (R,S)-atenolol. (R,S)-atenolol is a β-adrenergic receptor antagonist.
  • HY-P3061
    [Hyp3]-Bradykinin

    Bradykinin Receptor Endocrinology Cardiovascular Disease
    [Hyp3]-Bradykinin, naturally occurring peptide hormone, is a bradykinin receptor agonist. [Hyp3]-Bradykinin interacts with B2-bradykinin receptors and stimulates inositol phosphate production in cultured human fibroblasts.
  • HY-U00244
    Benzquinamide

    P2647; BZQ; Benzoquinamide

    Adrenergic Receptor Metabolic Disease Endocrinology
    Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively.
  • HY-101610
    OPC-28326

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    OPC-28326 is a selective peripheral vasodilator and an angatonist of α2-adrenergic receptor, with Ki of 2040, 285, and 55 nM for α2A-, α2B- and α2C-adrenoceptors, respectively.
  • HY-N2040
    (20R)-Protopanaxadiol

    Others Cancer Infection
    (20R)-Protopanaxadiol is a triterpenoid saponin metabolite of 20(R)-ginsenoside Rg3 in black ginseng. (20R)-Protopanaxadiol exhibits anti-tumor activity and cytotoxicity, and potently inhibits the growth of Helicobacter pylori.
  • HY-105285
    Piromelatine

    Neu-P11

    Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel Neurological Disease
    Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
  • HY-B1101
    Pimethixene

    Pimetixene

    5-HT Receptor Histamine Receptor Neurological Disease Endocrinology
    Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
  • HY-B1101A
    Pimethixene maleate

    Pimetixene maleate

    5-HT Receptor Histamine Receptor Neurological Disease Endocrinology
    Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
  • HY-13662B
    (R)-Lansoprazole

    Dexlansoprazole

    Proton Pump Inflammation/Immunology
    (R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
  • HY-11017AS
    (R)-Rivastigmine D6 tartrate

    AChE Others
    (R)-Rivastigmine D6 tartrate is the deuterium labeled (R)-Rivastigmine, which is an cholinesterase inhibitor.
  • HY-101405
    Gestrinone

    R 2323

    Estrogen Receptor/ERR Inflammation/Immunology
    Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
  • HY-N0615
    Notoginsenoside R1

    Sanchinoside R1; Sanqi glucoside R1

    Amyloid-β Apoptosis Others
    Notoginsenoside R1 (Sanchinoside R1), a saponin, is isolated from P. notoginseng. Notoginsenoside R1 exhibits anti-oxidation, anti-inflammatory, anti-angiogenic, and anti-apoptosis activities. Notoginsenoside R1 provides cardioprotection against ischemia/reperfusion (I/R) injury. Notoginsenoside R1 also provides neuroprotection in H2O2-induced oxidative damage in PC12 cells.
  • HY-15125
    (R)-(+)-Bay-K-8644

    Calcium Channel Cardiovascular Disease
    (R)-(+)-Bay-K-8644 is a calcium channel inhibitor. (R)-(+)-Bay-K-8644 inhibits Ba 2+ currents (IBa) (IC50=975 nM).
  • HY-P9803
    Anti-SARS-80R mAb

    SARS-80R; SARS Antibody-80R

    SARS-CoV Infection
    Anti-SARS-80R mAb (SARS-80R) is a human monoclonal IgG1 antibody produced in CHO cells. Anti-SARS-80R mAb can specifically bind to Spike (S1) protein to prevent SARS virus infection of susceptible cells.
  • HY-13038
    Fostamatinib Disodium

    R788(Disodium)

    Syk FLT3 Inflammation/Immunology Cancer
    Fostamatinib Disodium (R788 Disodium) is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • 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-135387
    4-Desmethyl Istradefylline

    Drug Metabolite Neurological Disease
    4-Desmethyl Istradefylline is a metabolite of Istradefylline. 4-Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
  • HY-12881
    Eliprodil

    SL-820715

    iGluR Neurological Disease
    Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
  • HY-136459
    NMDA receptor antagonist 2

    iGluR Neurological Disease
    NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
  • 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-B0590B
    (+)-Tetrabenazine

    (+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine

    Monoamine Transporter Cancer
    (+)-Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.
  • HY-15193A
    EMD638683 R-Form

    SGK Metabolic Disease
    EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
  • HY-19322C
    (1S,3R,5R)-PIM447 dihydrochloride

    (1S,3R,5R)-LGH447 dihydrochloride

    Pim Cancer
    (1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor extracted from patent US 20100056576 A1, compound example 72, has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3.
  • HY-101774
    CSF1R-IN-1

    c-Fms Cancer
    CSF1R-IN-1 is a CSF1R inhibitor with an with an IC50 of 0.5 nM.
  • HY-12422C
    (2S,3R)-Voruciclib

    CDK Cancer
    (2S,3R)-Voruciclib is the (2S,3R)-enantiomer of Voruciclib. (2S,3R)-Voruciclib is an orally active CDK inhibitor.
  • HY-B0352BS
    (R)-Mirtazapine D3

    (R)-Org3770 D3; (R)-6-Azamianserin D3

    5-HT Receptor Neurological Disease
    (R)-Mirtazapine D3 ((R)-Org3770 D3) is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4.
  • HY-100754B
    (2R,5S)-Ritlecitinib

    (2R,5S)-PF-06651600

    JAK Inflammation/Immunology
    (2R,5S)-Ritlecitinib ((2R,5S)-PF-06651600) is a potent and selective JAK3 inhibitor (IC50=144.8 nM) extracted from patent US20150158864A1, example 68.
  • HY-103181
    N6-Cyclopentyladenosine

    CPA; UK-80882

    Adenosine Receptor Neurological Disease
    N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively.
  • HY-W015954
    (2R,3R)-Butane-2,3-diol

    Endogenous Metabolite Metabolic Disease
    (2R,3R)-Butane-2,3-diol is an endogenous metabolite.
  • HY-109785A
    (R)-Gyramide A hydrochloride

    Infection
    (R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
  • HY-13259C
    (R)-MG-132

    (S,R,S)-(-)-MG-132; Z-Leu-D-Leu-Leu-al

    Proteasome Cancer
    (R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132.
  • HY-B0418A
    Loperamide hydrochloride

    R-18553 hydrochloride

    Opioid Receptor Autophagy Metabolic Disease Neurological Disease
    Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist. Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect.
  • HY-10291
    Tarenflurbil

    (R)-Flurbiprofen; MPC7869

    RAR/RXR Autophagy Inflammation/Immunology Neurological Disease
    Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [ 3H]9-cis-RA to RXRα LBD with IC50 of 75 μM.
  • HY-14802
    Talarozole (R enantiomer)

    (R)-Talarozole

    Cytochrome P450 Cancer
    Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.
  • HY-14149
    Cisapride

    R 51619; (±)-Cisaprid

    5-HT Receptor Neurological Disease
    Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
  • HY-136588
    trans-R-138727MP

    Prasugrel metabolite R-138727MP

    P2Y Receptor Cardiovascular Disease
    trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel (HY-15284). Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
  • HY-101445A
    (R)-Trolox

    Tyrosinase Cancer
    (R)-Trolox is a water soluble vitamin E analogue and a competitive tyrosinase inhibitor with a Ki value of 0.83 mM and a ID50 value of 1.88 mM. The (R)-Trolox has stronger tyrosinase affinity than the (S) enantiomer (Ki value of 0.61 mM).
  • HY-W087952
    (R)-(-)-2-Butanol

    Others Metabolic Disease
    (R)-(-)-2-Butanol is released by the females of the white grub beetle, Dasylepida ishigakiensis, to attract males. (R)-(-)-2-Butanol is an intermediate of pharmaceutical synthesis by coupling.
  • HY-75087
    (R)-pyrrolidine-2-carboxylic acid

    (+)-(R)-Proline; (R)-(+)-Proline; (R)-2-Carboxypyrrolidine; (R)-Proline

    Endogenous Metabolite Metabolic Disease
    (R)-pyrrolidine-2-carboxylic acid is an endogenous metabolite.
  • HY-B0580B
    (R)-Ketorolac

    (+)-Ketorolac

    Others Neurological Disease
    (R)-Ketorolac is the R-enantiomer of Ketorolac, shows potent analgesic activity, reduces ulcerogenic potential. (R)-Ketorolac is inactive on COX.
  • HY-15481
    KU14R

    Insulin Receptor Metabolic Disease Endocrinology
    KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.
  • HY-B1675
    Levalbuterol

    (R)-Albuterol; (R)-Salbutamol; Levosalbutamol

    Adrenergic Receptor Inflammation/Immunology
    Levalbuterol ((R)-Albuterol; (R)-Salbutamol) is a short-acting β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. Levalbuterol is a more potent bronchodilator than Salbutamol and has the potential for the treatment of COPD.
  • HY-19988
    THZ1-R

    CDK Cancer
    THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.
  • HY-100742A
    (R)-GNE-140

    Lactate Dehydrogenase Cancer
    (R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.
  • HY-107985A
    (R)-FT671

    Others Others
    (R)-FT671 is the R-isomer of FT671. FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.
  • HY-40354D
    (3R,4S)-Tofacitinib

    JAK Inflammation/Immunology
    (3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
  • HY-106408A
    Salfaprodil

    Neu2000 potassium

    iGluR Neurological Disease
    Salfaprodil (Neu2000 potassium) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Salfaprodil is also a free radical scavenger. Salfaprodil has excellent neuroprotection against NMDA- and free radical-induced cell death.
  • HY-15609
    AZD-3463

    ALK/IGF1R inhibitor

    ALK IGF-1R Autophagy Apoptosis Cancer Endocrinology
    AZD-3463 (ALK/IGF1R inhibitor) is an orally active ALK/IGF1R inhibitor, with a Ki of 0.75 nM for ALK. AZD3463 induces apoptosis and autophagy in neuroblastoma cells.
  • HY-U00213
    Furaprofen

    R803

    HCV Infection
    Furaprofen (R803) is an effective HCV replication inhibitor. Furaprofen (R803) is substantially more potent against genotype 1a and 1b replicons (EC50, ~30 nM) than against the genotype 2a replicon (EC50, ~1,000 nM).
  • HY-76948
    5-R-Rivaroxaban

    Factor Xa Cardiovascular Disease
    5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
  • HY-103096
    R162

    Others Cancer
    R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.
  • HY-13636B
    Fulvestrant (R enantiomer)

    ICI 182780 (R enantiomer); ZD 9238 (R enantiomer); ZM 182780 (R enantiomer)

    Others Cancer
    Fulvestrant R enantiomer (ICI 182780 R enantiomer) is the R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
  • HY-B0612DS
    (R)-Lercanidipine D3 hydrochloride

    Calcium Channel Cardiovascular Disease
    (R)-lercanidipine D3 (hydrochloride) is a deuterium labeled (R)-Lercanidipine hydrochloride. (R)-Lercanidipine D3 (hydrochloride), the R-enantiomer of Lercanidipine, is a calcium channel blocker.
  • HY-12365
    Namodenoson

    CF-102; 2-Cl-IB-MECA

    Adenosine Receptor Cancer
    Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
  • HY-108235C
    (R)-Lanicemine

    (R)-AZD6765

    iGluR Neurological Disease
    (R)-Lanicemine ((R)-AZD6765) is the less active R-enantiomer of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects.
  • HY-10216
    Refametinib (R enantiomer)

    BAY 869766 R enantiomer; RDEA119 R enantiomer

    MEK Cancer
    Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM.
  • HY-18733
    Lipoic acid

    (R)-(+)-α-Lipoic acid; R-(+)-Thioctic acid

    Mitochondrial Metabolism Endogenous Metabolite Reactive Oxygen Species Inflammation/Immunology Cancer
    Lipoic acid ((R)-(+)-α-Lipoic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. (R)-(+)-α-Lipoic acid is more effective than racemic Lipoic acid.
  • HY-18767A
    (R,S)-Ivosidenib

    (R,S)-AG-120

    Isocitrate Dehydrogenase (IDH) Cancer
    (R,S)-Ivosidenib ((R,S)-AG-120) is the less active enantiomer of Ivosidenib (AG-120).
  • HY-116463D
    (Rac)-E1R

    Sigma Receptor Neurological Disease
    (Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders.
  • HY-15677A
    INT-777 R-enantiomer

    S-EMCA R enantiomer

    GPCR19 Others
    INT-777 (R-enantiomer) is the R-enantiomer of INT-777, with EC50 of 4.79 μM for TGR5, and less potent than INT-777.
  • HY-101281B
    (R)-VU 6008667

    Others Neurological Disease
    (R)-VU 6008667, the less active (R)-enantiomer to VU 6008667, is devoid of M5 NAM activity (IC50>10 μM).
  • HY-15298C
    Grazoprevir sodium salt

    MK-5172 (sodium salt)

    HCV HCV Protease Infection
    Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
  • HY-15298B
    Grazoprevir hydrate

    MK-5172 hydrate

    HCV HCV Protease Infection
    Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
  • HY-15298
    Grazoprevir

    MK-5172

    HCV Protease HCV Infection
    Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
  • HY-15298A
    Grazoprevir potassium salt

    MK-5172 (potassium salt)

    HCV HCV Protease Infection
    Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
  • HY-135397
    (R)-​Linezolid

    (R)-PNU-100766

    Others Infection
    (R)-Linezolid is an impurity of Linezolid (PNU-100766). Linezolid, the first member of the class of oxazolidinone synthetic antibiotic, acts by inhibiting the initiation of bacterial protein synthesis.
  • HY-13038B
    Fostamatinib disodium hexahydrate

    R788 disodium hexahydrate

    Syk FLT3 Cancer Inflammation/Immunology
    Fostamatinib (R788) disodium hexahydrate is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-124151
    Adenosine-2'-monophosphate

    2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate

    Adenosine Receptor Endogenous Metabolite Neurological Disease
    Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
  • HY-101980
    AZD4635

    HTL1071

    Adenosine Receptor Cancer
    AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors.
  • HY-15793A
    Trans (2,3)-Dihydrotetrabenazine

    (2R,3R,11bR)-rel-Dihydrotetrabenazine; (2R,3R,11bR)-rel-DHTBZ

    Drug Metabolite Monoamine Transporter Neurological Disease
    Trans (2,3)-Dihydrotetrabenazine ((2R,3R,11bR)-rel-Dihydrotetrabenazine), a metabolite of Tetrabenazine, shows remarkable inhibition activity on vesicular monoamine transporter (VMAT2).
  • HY-34516
    (R)-Ornithine hydrochloride

    Endogenous Metabolite Metabolic Disease
    (R)-Ornithine hydrochloride is an endogenous metabolite.
  • HY-101183A
    THK5351 (R enantiomer)

    Others Neurological Disease
    THK5351 R enantiomer is an R enantiomer of THK5351.
  • HY-50949A
    Bay 65-1942 (R form)

    IKK Inflammation/Immunology
    Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is an ATP-competitive and selective IKKβ inhibitor.
  • HY-12422B
    (2S,3R)-Voruciclib hydrochloride

    CDK Cancer
    (2S,3R)-Voruciclib hydrochloride is the enantiomer of Voruciclib hydrochloride. (2S,3R)-Voruciclib is an orally active CDK inhibitor.
  • HY-14858
    Derenofylline

    SLV 320

    Adenosine Receptor Cardiovascular Disease
    Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.
  • HY-B1370B
    (R)-Hydroxychloroquine

    (R)-HCQ

    Parasite Toll-like Receptor (TLR) SARS-CoV Autophagy Infection
    (R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
  • HY-B0371B
    (R)-Terazosin

    Adrenergic Receptor Endocrinology
    (R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.
  • HY-13953
    JIB-04

    Histone Demethylase Apoptosis Cancer
    JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
  • HY-109112
    Brilaroxazine

    RP5063

    Dopamine Receptor 5-HT Receptor Inflammation/Immunology Neurological Disease
    Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
  • HY-N0049
    Nuciferine

    5-HT Receptor Dopamine Receptor Neurological Disease
    Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
  • HY-N1400
    (20R)-Ginsenoside Rh1

    Others Cancer
    (20R)-Ginsenoside Rh1, the R isomer of Ginsenoside Rh1 isolated from Panax Ginseng, inhibits the thrombin-induced conversion of fibrinogen to fibrin.
  • HY-P0162
    HCV-IN-4

    HCV Infection
    HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC90s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively.
  • HY-15415
    KB-R7943 mesylate

    Na+/Ca2+ Exchanger Autophagy Cancer
    KB-R7943 mesylate is a widely used inhibitor of the reverse Na +/Ca 2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.
  • HY-N2207
    rel-(8R,8'R)-Dimethyl-(7S,7'R)-bis(3,4-methylenedioxyphenyl)tetrahydro-furan

    Others Others
    rel-(8R,8'R)-Dimethyl-(7S,7'R)-bis(3,4-methylenedioxyphenyl)tetrahydro-furan is a chemical constituent of the fruit of Myristica fragrans.
  • HY-11108
    R406 free base

    Syk FLT3 Apoptosis Inflammation/Immunology Cancer
    R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-14975
    R1487 Hydrochloride

    p38 MAPK Autophagy Cancer
    R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with Kd values of 0.2 nM and 29 nM for p38α and p38β, respectively.
  • HY-12515C
    (R)-Nicardipine

    (R)-YC-93 free base

    Others Neurological Disease Cardiovascular Disease
    (R)-Nicardipine ((R)-YC-93 free base) is the less active R enantiomer of Nicardipine. Nicardipine (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
  • HY-111095B
    (2R)-2-Hydroxypropanoate sodium

    Endogenous Metabolite Metabolic Disease
    (2R)-2-Hydroxypropanoate sodium is an endogenous metabolite.
  • HY-B0843A
    Metalaxyl-M

    (R)-Metalaxyl

    Fungal Infection
    Metalaxyl-M ((R)-Metalaxyl) is the active (R)-enantiomer of Metalaxyl. Metalaxyl-M is a broad-spectrum fungicide that inhibits protein and ribosomal RNA synthesis in fungi. Metalaxyl is used for research of plant diseases caused by pathogens of the Oomycota division.
  • HY-136573
    5-Hydroxytoluene-2,4-disulphonic acid diammonium

    Virus Protease Infection
    5-Hydroxytoluene-2,4-disulphonic acid diammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
  • HY-136575
    4-Hydroxy-2-methylbenzenesulfonic acid ammonium

    Virus Protease Infection
    4-Hydroxy-2-methylbenzenesulfonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
  • HY-136574
    2-Hydroxy-4-methylbenzenesulphonic acid ammonium

    Virus Protease Infection
    2-Hydroxy-4-methylbenzenesulphonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
  • HY-P1115
    AKTide-2T

    Akt Others
    AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
  • HY-126047B
    (R)-(+)-Anatabine

    NF-κB Amyloid-β nAChR Inflammation/Immunology Neurological Disease
    (R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
  • HY-77490
    (R)-(-)-1,3-Butanediol

    Endogenous Metabolite Metabolic Disease
    (R)-(-)-1,3-Butanediol is used to regulate the metabolism of carbohydrate and lipid.
  • HY-112218A
    (R)-MIK665

    Bcl-2 Family Cancer
    (R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special Mcl-1 inhibitor with an IC50 of 1.81 nM.
  • HY-113038
    D-α-Hydroxyglutaric acid

    (R)-2-Hydroxyglutarate; (R)-2-Hydroxyglutaric acid; (R)-2-Hydroxypentanedioic acid

    Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    D-α-Hydroxyglutaric acid ((R)-2-Hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling.
  • HY-N6679
    (R)-10,11-Dehydrocurvularin

    Others Cancer
    (R)-10,11-Dehydrocurvularin is a secondary metabolite isolated from Curvularia sp.. (R)-10,11-Dehydrocurvularin displays concentration-dependent cytotoxicity towards human tumor cell lines with a mean IC50 value of 1.25 µM.
  • HY-15703
    QNZ46

    iGluR Neurological Disease
    QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively).
  • HY-106408
    Salfaprodil free base

    Neu2000

    iGluR Neurological Disease
    Salfaprodil free base (Neu2000) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Salfaprodil free base is also a free radical scavenger. Salfaprodil free base has excellent neuroprotection against NMDA- and free radical-induced cell death.
  • HY-P1115A
    AKTide-2T TFA

    Akt Others
    AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
  • HY-P1404
    R8-T198wt

    Pim Cancer
    R8-T198wt is a cell-permeable carboxyl-terminal p27 Kip1 peptide exhibits anti-tumor activity by inhibiting Pim-1 kinase.
  • HY-Z0031
    (R)-(-)-1,2-Propanediol

    Others Metabolic Disease
    (R)-(-)-1,2-Propanediol is a (R)-enantiomer of 1,2-Propanediol that produced from glucose in Escherichia coli expressing NADH-linked glycerol dehydrogenase genes.
  • HY-N1376
    20(R)-Ginsenoside Rg3

    20(R)-Propanaxadiol; R-ginsenoside Rg3

    Others Cancer
    20(R)-ginsenoside Rg3 (20(R)-Propanaxadiol), one of the active compounds present in ginseng root, has a potent angiosuppressive and antitumor activities.
  • HY-14664B
    (3R,5S)-Fluvastatin

    (3R,5S)-XU 62-320 free acid

    HMG-CoA Reductase (HMGCR) Autophagy Cancer Cardiovascular Disease
    (3R,5S)-Fluvastatin is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
  • HY-18102A
    GLPG0492 (R enantiomer)

    Androgen Receptor Neurological Disease
    GLPG0492 R enantiomer is the R enantiomer of GLPG-0492, which is a novel selective androgen receptor modulator.
  • HY-112316A
    (R)-BAY1238097

    Epigenetic Reader Domain Cancer
    (R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome.
  • HY-101682B
    (R)-SCH 42495

    Others Others
    (R)-SCH 42495 is the less active enantiomer of SCH 42495. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
  • HY-126050
    (R)-Pantetheine

    Pantetheine

    Others Metabolic Disease
    (R)-Pantetheine is the biosynthetic precursor to CoA. (R)-Pantetheine and its corresponding disulfide pantethine, play a key role in metabolism as a building block of coenzyme A (CoA).
  • HY-116463
    E1R

    Sigma Receptor Neurological Disease
    E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.
  • HY-15150
    Bemcentinib

    R428; BGB324

    TAM Receptor Cancer
    Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM.
  • HY-135483A
    AR-R17779 hydrochloride

    nAChR Neurological Disease
    AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways.
  • HY-P2247
    JTP10-△-R9 TFA

    JNK Cancer
    JTP10-△-R9 TFA is a selective JNK2 peptide inhibitor, with an IC50 of 89 nM, exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3.
  • HY-129079
    TFMB-(R)-2-HG

    Others Cancer
    TFMB-(R)-2-HG, a cell membrane-permeable version of (R)-2-HG, is a carcinogenic factor in Acute myeloid leukemia (AML). TFMB-(R)-2-HG impairs SCF ER-Hoxb8 cells differentiation in response to estrogen withdrawal.
  • HY-18340
    (R)​-​CR8

    CR8, (R)-Isomer

    CDK Apoptosis Cancer Neurological Disease
    (R)​-​CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)​-​CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)​-​CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.
  • HY-18340A
    (R)-CR8 trihydrochloride

    CR8, (R)-Isomer trihydrochloride

    CDK Apoptosis Cancer Neurological Disease
    (R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.
  • HY-12481A
    SAR405 R enantiomer

    Others Cancer
    SAR405 R enantiomer is the less active enantiomer of SAR405. SAR405 is a PIK3C3/Vps34 inhibitor.
  • HY-17356
    Fenofibrate

    PPAR Cytochrome P450 Autophagy Cardiovascular Disease Cancer
    Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
  • HY-50202
    Etomoxir

    (R)-(+)-Etomoxir

    Apoptosis Cancer Metabolic Disease
    Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
  • HY-50202A
    Etomoxir sodium salt

    (R)-(+)-Etomoxir sodium salt

    Apoptosis Metabolic Disease Cancer
    Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
  • HY-103016
    WZ4141R

    Others Others
    WZ4141R is an intermediate in the synthesis of compounds.
  • HY-13030A
    (R)-(-)-JQ1 Enantiomer

    Epigenetic Reader Domain Cancer
    (R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (R)-(-)-JQ1 Enantiomer has no effect.
  • HY-W002304
    (R)-5-Oxopyrrolidine-2-carboxylic acid

    Endogenous Metabolite Metabolic Disease
    (R)-5-Oxopyrrolidine-2-carboxylic acid is an endogenous metabolite.
  • HY-112134A
    (R)-CSN5i-3

    Others Cancer
    (R)-CSN5i-3 is the (R)-enantiomer of CSN5i-3. CSN5i-3 is a potent, selective and orally available inhibitor of CSN5.
  • HY-100207
    CP21R7

    CP21

    GSK-3 Cancer
    CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.
  • HY-18675
    IQ-R

    Others Others
    IQ-R is a novel hypoxia-sensitive fluorescent probe, consisting of an indolequinone unit and a rhodol fluorophore.
  • HY-17355A
    Dexpramipexole dihydrochloride

    (R)-Pramipexole dihydrochloride; R-(+)-Pramipexole dihydrochloride; KNS-760704 dihydrochloride

    Dopamine Receptor Neurological Disease
    Dexpramipexole dihydrochloride ((R)-Pramipexole dihydrochloride) is a neuroprotective agent and weak non-ergoline dopamine agonist.
  • HY-10167A
    Tecalcet Hydrochloride

    R-568 hydrochloride

    CaSR Others
    Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+.
  • HY-17429
    Flecainide acetate

    R-818

    Sodium Channel Cardiovascular Disease
    Flecainide acetate (R-818) is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.
  • HY-B1470
    Azaperone

    R-1929

    Dopamine Receptor Neurological Disease
    Azaperone (R-1929) acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
  • HY-113108
    (R)-3-Hydroxyisobutyric acid

    Endogenous Metabolite Metabolic Disease
    (R)-3-Hydroxyisobutyric acid is an intermediate in the pathways of l-valine and thymine and plays an important role in the diagnosis of the very rare inherited metabolic diseases 3-hydroxyisobutyric aciduria and methylmalonic semialdehyde dehydrogenase deficiency.
  • HY-135374
    (3R,5S)-Atorvastatin sodium

    Others Metabolic Disease Inflammation/Immunology
    (3R,5S)-Atorvastatin sodium is an impurity of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
  • HY-106019C
    Liarozole dihydrochloride

    R75251 dihydrochloride

    Cytochrome P450 Cancer Inflammation/Immunology
    Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase). Liarozole dihydrochloride prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.
  • HY-111501
    H4R antagonist 1

    Histamine Receptor Inflammation/Immunology Endocrinology
    H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.
  • HY-P9917
    Tocilizumab

    Anti-Human IL6R, Humanized Antibody

    Interleukin Related Cancer Inflammation/Immunology
    Tocilizumab (Anti-Human IL6R, Humanized Antibody) is an anti-human interleukin-6 receptor (IL-6R) neutralizing antibody, prevents binding of IL-6 to the IL-6R, thereby inhibiting both classic and trans-signaling. Tocilizumab (Anti-Human IL6R, Humanized Antibody) can be used for the treatment of rheumatoid arthritis. Tocilizumab is remarkablely effective for the study of severe COVID-19 (coronavirus disease).
  • HY-103641
    (2R)-Octyl-α-hydroxyglutarate

    (2R)-Octyl-2-HG

    Others Cancer
    (2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a modified form of D-isomer 2-Hydroxyglutarate.
  • HY-15267A
    (24R)-MC 976

    VD/VDR Metabolic Disease
    (24R)-MC 976 is a Vitamin D3 derivative.
  • HY-N1401
    20(R)-Ginsenoside Rh2

    MMP Apoptosis HSV Cancer Infection Inflammation/Immunology
    20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity. 20(R)-Ginsenoside Rh2 inhibits the replication and proliferation of mouse and human gammaherpesvirus 68 (MHV-68) with an IC50 of 2.77 μM for murine MHV-68.
  • HY-100808
    (R)-Serine

    iGluR Endogenous Metabolite Others
    (R)-Serine, an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. (R)-Serine has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration.
  • HY-W021425
    (2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal hydrochloride

    Endogenous Metabolite Metabolic Disease
    (2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal hydrochloride is an endogenous metabolite.
  • HY-13856
    (R)-PS210

    PDK-1 Cancer
    (R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.
  • HY-U00396
    MC-4R Agonist 1

    Melanocortin Receptor Metabolic Disease Endocrinology
    MC-4R Agonist 1 is an agonist of human melanocortin-4 receptor (MC-4R), used in the research of obesity, diabetes, and sexual dysfunction.
  • HY-135383A
    (3S,5R)-Pitavastatin calcium

    Others Metabolic Disease
    (3S,5R)-Pitavastatin cacium is the enantiomer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.
  • HY-N4266
    Vinaginsenoside R8

    Others Cardiovascular Disease
    Vinaginsenoside R8, a triterpenoid glycoside isolated from the rhizomes of Panacis majoris. Vinaginsenoside R8 displays activities against adenosine diphosphate (ADP)-induced platelet aggregation (IC50=25.18 μM).
  • HY-14664C
    (3S,5R)-Fluvastatin sodium

    (3S,5R)-XU 62-320

    HMG-CoA Reductase (HMGCR) Cancer Cardiovascular Disease
    (3S,5R)-Fluvastatin sodium ((3S,5R)-XU 62-320) is the (3S,5R)-enantiomer of Fluvastatin. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
  • HY-40354B
    (3S,4R)-Tofacitinib

    JAK Inflammation/Immunology
    (3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
  • HY-121119
    MRS 1523

    Adenosine Receptor Calcium Channel Inflammation/Immunology Neurological Disease Cardiovascular Disease
    MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons.
  • HY-B0100
    Etomidate

    R 16659

    GABA Receptor Neurological Disease
    Etomidate (R 16659) is a potent GABAA receptor agonist. Etomidate is a neurological drug and effective parenteral medication and has the potential for management of endogenous hypercortisolaemia.
  • HY-B0357
    Diclazuril

    R-64433

    Parasite Antibiotic Infection
    Diclazuril (R-64433), a benzeneacetonitrile derivative, is a potent and orally active anticoccidial agent. Diclazuril can be used for the research of certain infectious and parasitic diseases, including coccidiosis, acute toxoplasmosis, equine protozoal pyoencephalitis (EPM) et.al.
  • HY-133872
    [(3R)-3-Hydroxydodecanoyl]-L-carnitine

    Endogenous Metabolite Others
    [(3R)-3-Hydroxydodecanoyl]-L-carnitine is an endogenous metabolite.
  • HY-116463B
    (2S,3S)-E1R

    Sigma Receptor Neurological Disease
    (2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-A0007
    Rotigotine Hydrochloride

    N-0923 Hydrochloride

    Dopamine Receptor Adrenergic Receptor 5-HT Receptor Neurological Disease
    Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
  • HY-106376
    DL-Buthionine-(S,R)-sulfoximine

    Buthionine sulfoximine; BSO

    Ferroptosis Cancer
    DL-Buthionine-(S,R)-sulfoximine is a potent inhibitor of glutamylcysteine synthetase biosynthesis.
  • HY-B0602S
    (R)-(-)-O-Desmethyl Venlafaxine D6

    Drug Metabolite Neurological Disease
    (R)-(-)-O-Desmethyl Venlafaxine D6 is the deuterium labeled (R)-(-)-O-Desmethyl Venlafaxine. O-Desmethyl Venlafaxine is an active metabolite of Venlafaxine. Venlafaxine (HY-B0196) is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class.
  • HY-N4131
    25R-Inokosterone

    Others Others
    25R-Inokosterone is a phytoecdysone isolated from Achyranthis Radix.
  • HY-104028
    BAY 73-6691

    (R)-BAY 73-6691

    Phosphodiesterase (PDE) Neurological Disease
    BAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor.
  • HY-17355B
    Dexpramipexole

    (R)-Pramipexole; R-(+)-Pramipexole; KNS-760704

    Dopamine Receptor Neurological Disease
    Dexpramipexole(KNS-760704), also known as R-(+)-Pramipexole, is a neuroprotective agent and weak non-ergoline dopamine agonist.
  • HY-107613
    R 59-022

    DKGI-I; Diacylglycerol kinase inhibitor I

    PKC 5-HT Receptor Inflammation/Immunology
    R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
  • HY-101116
    GLP-1R Antagonist 1

    Glucagon Receptor Metabolic Disease
    GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM.
  • HY-N6924
    Zingibroside R1

    HIV Infection Metabolic Disease
    Zingibroside R1 is dammaranae-type triterpenoid saponin, isolated from rhizomes, taproots, and lateral roots of Panax japonicas C. A. Meyer, shows excellent anti-tumor effects as well as anti-angiogenic activity. Zingibroside R1 possesses some anti-HIV-1 activity. Zingibroside R1 has inhibitory effects on the 2-deoxy-D-glucose (2-DG) uptake by EAT cells (IC50=91.3 μM).
  • HY-107479
    (R)-JNJ-31020028

    Neuropeptide Y Receptor Neurological Disease
    (R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects.
  • HY-10443A
    Balapiravir hydrochloride

    Ro 4588161 hydrochloride; R1626 hydrochloride

    HCV DNA/RNA Synthesis Infection
    Balapiravir hydrochloride (Ro 4588161 hydrochloride; R1626 hydrochloride) is an orally active prodrug of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir hydrochloride has anti-HCV activity.
  • HY-10443
    Balapiravir

    Ro 4588161; R1626

    HCV DNA/RNA Synthesis Infection
    Balapiravir (Ro 4588161; R1626) is an orally active prodrug of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir has anti-HCV activity.
  • HY-117026
    LKY-047

    Cytochrome P450 Metabolic Disease Inflammation/Immunology
    LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A.
  • HY-13058B
    (R)-ADX-47273

    mGluR Neurological Disease
    (R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
  • HY-B0454
    Miconazole

    R18134

    Fungal Bacterial Antibiotic Infection
    Miconazole (R18134) is an imidazole antifungal agent. Miconazole also has antibacterial effects.
  • HY-114395A
    (R)-NVS-ZP7-4

    Others Inflammation/Immunology
    (R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-78847
    2R,4S-Sacubitril

    Others Cardiovascular Disease
    2R,4S-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
  • HY-106376B
    DL-Buthionine-(S,R)-sulfoximine hydrochloride

    Buthionine sulfoximine hydrochloride; BSO hydrochloride

    Ferroptosis Cancer
    DL-Buthionine-(S,R)-sulfoximine hydrochloride (Buthionine sulfoximine hydrochloride) is a potent inhibitor of glutamylcysteine synthetase biosynthesis.
  • HY-10014
    R547

    CDK GSK-3 Apoptosis Cancer
    R547 is a potent, selective and oral orally bioavailable ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.
  • HY-N2550
    (+)-Coclaurine

    (+)-(R)-Coclaurine; (R)-Coclaurine; d-Coclaurine

    Others Neurological Disease
    (+)-Coclaurine ((+)-(R)-Coclaurine), benzyltetrahydroisoquinoline alkaloid isolated from a variety of plant sources. (+)-Coclaurine has anti-aging activity.
  • HY-141186A
    (R)-TCO-OH

    PROTAC Linker Cancer
    (R)-TCO-OH is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-108414
    (R)-Equol

    (+)-Equol

    Estrogen Receptor/ERR Cancer
    (R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
  • HY-W010841
    Levocetirizine dihydrochloride

    (R)-Cetirizine dihydrochloride

    Histamine Receptor Endocrinology Inflammation/Immunology
    Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.
  • HY-B0814
    Levocetirizine

    (R)-Cetirizine

    Histamine Receptor Inflammation/Immunology Endocrinology
    Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.
  • HY-P1039
    R18

    PHCVPRDLSWLDLEANMCLP

    Others Cancer
    R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1.
  • HY-110203
    R-7050

    TNF-α Antagonist III

    TNF Receptor Cancer
    R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
  • HY-30216
    (R)-Leucic acid

    D-α-Hydroxyisocaproic acid

    Endogenous Metabolite Others
    (R)-Leucic acid is an amino acid metabolite.
  • HY-112219A
    H3R-IN-1 Hydrochloride

    Histamine Receptor Inflammation/Immunology Endocrinology
    H3R-IN-1 Hydrochloride is a histamine receptor 3 (H3R) inverse agonist extracted from patent WO2013107336A1, compound example 2.
  • HY-B0330D
    (R)-Ofloxacin

    Dextrofloxacin

    Bacterial Infection
    (R)-Ofloxacin (Dextrofloxacin) is an antibiotic useful for the treatment of a number of bacterial infections. Antibacterial activity.
  • HY-U00181
    Fludazonium chloride

    R23633

    Fungal Infection
    Fludazonium chloride (R23633) is an anti-fungal agent, which can be used in the treatment and prevention of superficial and systemic fungal infections.
  • HY-101354
    R-IMPP

    PF-00932239

    Ser/Thr Protease Cancer Cardiovascular Disease
    R-IMPP (PF-00932239) is an anti-secretagogue of PCSK9 (IC50=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation.
  • HY-19908B
    (R)-BAY-85-8501

    Others Metabolic Disease
    (R)-BAY-85-8501 is the less active Enantiomer of BAY-85-8501. BAY-85-8501 is a selective and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM.
  • HY-131004
    CB2R PAM

    Cannabinoid Receptor Neurological Disease
    CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain.
  • HY-124607
    (R)-BRD3731

    GSK-3 Neurological Disease
    (R)-BRD3731 is a GSK3 inhibitor extracted from patent US20160375006A1, compound example 273, has IC50s of 1.05 and 6.7 μM for GSK3β and GSK3α, respectively.
  • HY-17514
    Itraconazole

    R51211

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects.
  • HY-17354
    (R)-Baclofen

    STX209

    GABA Receptor Neurological Disease
    (R)-Baclofen(STX209) is a selective GABAB receptor agonist.
  • HY-11018A
    Risperidone hydrochloride

    R 64 766 hydrochloride

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone hydrochloride (R 64 766 hydrochloride) 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-N6696
    Aflatoxin B2

    Bacterial Antibiotic Cancer Infection
    Aflatoxin B2 is a major naturally produced aflatoxin. Aflatoxin B2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-75502
    Rotigotine

    N-0437; N-0923

    Dopamine Receptor Adrenergic Receptor 5-HT Receptor Neurological Disease Endocrinology
    Rotigotine (N-0437; N-0923) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
  • HY-15394
    (Rac)-Rotigotine hydrochloride

    Dopamine Receptor Adrenergic Receptor 5-HT Receptor Endocrinology Neurological Disease
    (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
  • HY-N6698
    Aflatoxin G2

    Bacterial Antibiotic Cancer Infection
    Aflatoxin G2 is a major naturally produced aflatoxin. Aflatoxin G2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-N0909
    Notoginsenoside R2

    20(S)-Notoginsenoside R2; Ginsenoside Ng-R2

    Others Neurological Disease
    Notoginsenoside R2 is a newly isolated notoginsenoside from Panax notoginseng, showed neuroprotective effects against 6-OHDA-induced oxidative stress and apoptosis.
  • HY-13755A
    (R)-Sulforaphane

    L-Sulforaphane

    Others Cancer
    (R)-Sulforaphane (L-Sulforaphane) is a highly potent inducer of the Keap1/Nrf2/ARE pathway. (R)-Sulforaphane is a far more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer.
  • HY-U00249
    Saperconazole

    R66905

    Fungal Infection
    Saperconazole (R66905) is a broad-spectrum antifungal triazole and has potent activity against Aspergillus with an MIC90 of 0.19 mg/L.
  • HY-14818
    Laninamivir

    R 125489

    Influenza Virus Infection
    Laninamivir (R 125489) is a potent influenza neuraminidase (NA) inhibitor with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively.
  • HY-100822
    (R)-(+)-HA-966

    (+)-HA-966

    iGluR Neurological Disease
    (R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine. (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain.
  • HY-14417A
    (1R,2S)-VU0155041

    mGluR Neurological Disease
    (1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
  • HY-11018B
    Risperidone mesylate

    R 64 766 mesylate

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-100999
    (R)-(-)-α-Methylhistamine dihydrobromide

    Histamine Receptor Neurological Disease
    (R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective H3 histamine receptor agonist with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrobromide can cross the blood-brain barrier, and can enhance memory retention, attenuates memory impairment in rats.
  • 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-N8096
    Raddeanoside R17

    Pulchinenoside E3

    Others Inflammation/Immunology
    Raddeanoside R17 (Pulchinenoside E3) is a saponins compound that can be isolated from the root of Pulsatilla koreana. Raddeanoside R17 shows anti-inflammatory effects.
  • HY-B0180
    Imiquimod

    R 837

    Toll-like Receptor (TLR) Autophagy SARS-CoV HSV Cancer Infection Inflammation/Immunology
    Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19.
  • HY-B0180A
    Imiquimod hydrochloride

    R 837 hydrochloride

    Toll-like Receptor (TLR) Autophagy SARS-CoV HSV Cancer Infection Inflammation/Immunology
    Imiquimod hydrochloride (R 837 hydrochloride), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod hydrochloride exhibits antiviral and antitumor effects in vivo. Imiquimod hydrochloride can be used for the research of external genital, perianal warts, cancer and COVID-19.
  • HY-B0180B
    Imiquimod maleate

    R 837 maleate

    Toll-like Receptor (TLR) Autophagy SARS-CoV HSV Cancer Infection Inflammation/Immunology
    Imiquimod maleate (R 837 maleate), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod maleate exhibits antiviral and antitumor effects in vivo. Imiquimod maleate can be used for the research of external genital, perianal warts, cancer and COVID-19.
  • HY-B0418AS
    Loperamide D6 hydrochloride

    R-18553 D6 hydrochloride

    Opioid Receptor Autophagy Metabolic Disease Neurological Disease
    Loperamide D6 hydrochloride (R-18553 D6 hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea.
  • HY-N6700
    Aflatoxin M2

    Others Cancer
    Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-N6699
    Aflatoxin M1

    Bacterial Cancer Infection
    Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-13534A
    Abarelix Acetate

    PPI 149 Acetate; R 3827 Acetate

    GnRH Receptor Cancer Endocrinology
    Abarelix Acetate (PPI 149 Acetate; R 3827 Acetate) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer research.
  • HY-14531
    Talarozole

    R115866

    RAR/RXR Cytochrome P450 Autophagy Inflammation/Immunology
    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
  • HY-U00214
    Ibafloxacine

    R835; S25930

    Bacterial Infection
    Ibafloxacine (R835) is a fluoroquinolone antibiotic agent that is developed exclusively for veterinary use.
  • HY-112895A
    (R)-UT-155

    Androgen Receptor Cancer
    (R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer.
  • HY-128732
    rel-(2R,3S)-2,3-Dihydroxysuccinic acid hydrate

    Endogenous Metabolite Metabolic Disease
    rel-(2R,3S)-2,3-Dihydroxysuccinic acid (hydrate) is an endogenous metabolite.
  • HY-14277A
    Levocabastine hydrochloride

    R 50547 hydrochloride

    Histamine Receptor Neurotensin Receptor Inflammation/Immunology
    Levocabastine (R 50547) hydrochloride is a long acting, highly potent and selective histamine H1-receptor antagonist with anti-allergic activity. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2.
  • HY-10240
    Mericitabine

    RG 7128; R-7128; PSI 6130 diisobutyrate

    HCV Infection
    Mericitabine (RG 7128; R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication.
  • HY-50674A
    INCB3344 R-isomer

    Others Inflammation/Immunology
    INCB3344 R-isomer is the R-isomer of INCB3344. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
  • HY-N7025
    Suavissimoside R1

    Others Neurological Disease
    Suavissimoside R1, isolated from the roots of Rubus parvifollus, possesses potent neuroprotective activity and has the potential to treat anti-Parkinson's disease drug.
  • HY-12772
    Hydroxy Itraconazole

    Itraconazole metabolite Hydroxy Itraconazole; R-63373

    Fungal Drug Metabolite Others
    Hydroxy Itraconazole (Itraconazole metabolite Hydroxy Itraconazole; R-63373) is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.
  • HY-124909
    (6R)-FR054

    Apoptosis Cancer
    (6R)-FR054 is an active isomer of FR054. FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect. FR054induces endoplasmic reticulum (ER) stress and a ROS-dependent apoptosis.
  • HY-101930B
    (R)-BMS-816336

    Others Metabolic Disease
    (R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .
  • HY-W050145
    (1R,2S,3S,4R,5S)-6,8-Dioxabicyclo[3.2.1]octane-2,3,4-triol

    Endogenous Metabolite Metabolic Disease
    (1R,2S,3S,4R,5S)-6,8-Dioxabicyclo[3.2.1]octane-2,3,4-triol is an endogenous metabolite.
  • HY-B0100A
    Etomidate hydrochloride

    R16659 hydrochloride

    GABA Receptor Neurological Disease
    Etomidate hydrochloride (R 16659 hydrochloride) is a potent GABAA receptor agonist. Etomidate hydrochlorideis a neurological drug and effective parenteral medication and has the potential for management of endogenous hypercortisolaemia.
  • HY-U00117
    Lusaperidone

    R107474

    Adrenergic Receptor Neurological Disease Endocrinology
    Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.
  • HY-N2296
    (2R,3R)-3,7-Dihydroxy-2-(4-hydroxyphenyl)-5-methoxy-8-(3-methylbut-2-en-1-yl)chroman-4-one

    Others Others
    (2R,3R)-3,7,4'-Trihydroxy-5-methoxy-8-prenylflavanone can be used in a flame retardant for transparent polycarbonate products or in elevator illumination devices research.
  • HY-135331
    N-Desmethyl-Apalutamide

    Androgen Receptor Cytochrome P450 Cancer
    N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration.
  • HY-A0124A
    Sapropterin dihydrochloride

    (6R)-BH4 dihydrochloride; (6R)-Tetrahydro-L-biopterin dihydrochloride

    Others Cardiovascular Disease
    Sapropterin ((6R)-BH4) dihydrochloride is a synthetic form of BH4 that is approved for the treatment of BH4 responsive PKU.
  • HY-131082
    (R)-8-Azido-2-(Fmoc-amino)octanoic acid

    ADC Linker Cancer
    (R)-8-Azido-2-(Fmoc-amino)octanoic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-32337
    Tacalcitol

    1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3

    VD/VDR Metabolic Disease
    Tacalcitol (1,24(R)-Dihydroxyvitamin D3; 1.
  • HY-P1175
    L-R4W2

    TRP Channel Neurological Disease
    L-R4W2 is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 may act as a potent analgesic.
  • HY-10256A
    SB 203580 hydrochloride

    RWJ 64809 hydrochloride

    p38 MAPK Autophagy Mitophagy Inflammation/Immunology Cancer
    SB 203580 hydrochloride (RWJ 64809 hydrochloride) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy and mitophagy activator.
  • HY-108539A
    (R)-CE3F4

    Others Metabolic Disease
    (R)-CE3F4 is a potent and selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1), with an IC50 of 4.2 μM, with 10-fold selectivity for Epac1 over Epac2 (IC50, 44 μM). (R)-CE3F4 is more potent than racemic CE3F4 and (S)-CE3F4.
  • HY-12532
    Astemizole

    R 43512

    Histamine Receptor Potassium Channel Inflammation/Immunology Endocrinology
    Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K + channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects.
  • HY-103319
    Calmidazolium chloride

    R 24571

    CaMK Autophagy Cancer Neurological Disease
    Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to CaMK with a Kd of 3 nM.
  • HY-10791
    Ritanserin

    R 55667

    5-HT Receptor Histamine Receptor Dopamine Receptor Adrenergic Receptor Neurological Disease
    Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
  • HY-32338
    Tacalcitol monohydrate

    1,24(R)-Dihydroxyvitamin D3 monohydrate

    VD/VDR Metabolic Disease
    Tacalcitol monohydrate (1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3) promotes normal bone development by regulating calcium.
  • HY-B0769
    Phenylephrine

    (R)-(-)-Phenylephrine; L-Phenylephrine

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    (R)-(-)-Phenylephrine is a selective α1-adrenoceptor agonist primarily used as a decongestant.
  • HY-17039S
    Alcaftadine-D3

    R89674-D3

    Histamine Receptor Endocrinology Inflammation/Immunology
    Alcaftadine-D3 (R89674-D3) is a deuterium labeled Alcaftadine. Alcaftadine (HY-17039) is a H1 histamine receptor antagonist.
  • HY-14190
    Valategrast

    R-411 free base

    Integrin Inflammation/Immunology
    Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.
  • HY-111787
    CSF1R-IN-2

    Src c-Met/HGFR c-Fms Cancer
    CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
  • HY-50081
    CCR2-RA-[R]

    CCR Inflammation/Immunology Endocrinology
    CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC50 of 103 nM.
  • HY-N4265
    Vinaginsenoside R4

    Others Inflammation/Immunology
    Vinaginsenoside R4, isolated from the leaves of hydroponic Panax ginseng. It has an inhibitory effect on melanin biosynthesis without any cytotoxic effects on the melan-a cells, and enhances the depigmentation on the zebrafish.
  • HY-19282A
    (5R)-BW-4030W92

    Others Neurological Disease
    (5R)-BW-4030W92 is the R enantiomer of BW-4030W92. BW-4030W92 is a non-selective, voltage-, and use-dependent sodium channel antagonist.
  • HY-N6262
    20(S),24(R)-Ocotillol

    Others Others
    20(S),24(R)-Ocotillol is isolated from Panax ginseng.
  • HY-108573
    P-1075

    Potassium Channel Cardiovascular Disease
    P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.
  • HY-N6695
    Aflatoxicol

    Aflatoxin R0

    Others Cancer
    Aflatoxin (Aflatoxin R0) is a metabolite of aflatoxin B1 produced from Rhizopus spp, and is mutagenic and carcinogenic mycotoxin.
  • HY-130642
    (S,R,S)-AHPC-Me-C10-Br

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-Me-C10-Br is a synthesized E3 ligase ligand-linker conjugate. (S,R,S)-AHPC-Me-C10-Br incorporates a VHL E3 ligase linker and MS432 based on the MEK1/2 inhibitor PD0325901.
  • HY-111664
    (R)-(+)-Citronellal

    (+)-Citronellal

    Endogenous Metabolite Metabolic Disease
    (R)-(+)-Citronellal, isolated from citrus, lavender and eucalyptus oils, is a monoterpenoid and main component of citronellal oil with a distinct lemon scent. A flavouring agent. Used for insect repellent and antifungal properties.
  • HY-15464
    (R)-(-)-Gossypol

    AT-101; R-(-)-gossypol acetic acid

    Bcl-2 Family Autophagy Cancer
    (R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
  • HY-B0661A
    Tamsulosin hydrochloride

    (R)-(-)-YM12617; LY253351

    Adrenergic Receptor Neurological Disease Endocrinology
    Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models.
  • HY-14605
    Rasagiline mesylate

    (R)-AGN1135 mesylate; TVP1012 mesylate

    Monoamine Oxidase Autophagy Apoptosis Neurological Disease
    Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively.
  • HY-14605A
    Rasagiline

    (R)-AGN1135; TVP1012

    Monoamine Oxidase Neurological Disease
    Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively.
  • HY-17354A
    (R)-Baclofen hydrochloride

    STX 209 hydrochloride

    GABA Receptor Neurological Disease
    (R)-Baclofen hydrochloride (STX 209 hydrochloride) is a selective GABAB receptor agonist.
  • HY-14664CS
    (3S,5R)-Fluvastatin D6 sodium

    (3S,5R)-XU 62-320 D6

    HMG-CoA Reductase (HMGCR) Cancer Cardiovascular Disease
    (3S,5R)-Fluvastatin D6 sodium is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
  • HY-B0411
    Domperidone

    R33812

    Dopamine Receptor Neurological Disease
    Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine.
  • HY-15015A
    OT-R antagonist 2

    Oxytocin receptor antagonist 2

    Oxytocin Receptor Endocrinology
    OT-R antagonist 2 is a nonpeptide low molecular weight OT-R antagonist.
  • HY-100328
    CB2R-IN-1

    Cannabinoid Receptor Neurological Disease
    CB2R-IN-1 is a potent cannabinoid CB2 receptor inverse agonist with a Ki of 0.9 nM.
  • HY-B0454A
    Miconazole nitrate

    R18134 nitrate

    Fungal Bacterial Antibiotic Infection
    Miconazole nitrate (R18134 nitrate) is an imidazole antifungal agent. Miconazole nitrate also has antibacterial effects.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-10256
    SB 203580

    RWJ 64809

    p38 MAPK Autophagy Mitophagy Inflammation/Immunology Cancer
    SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.
  • HY-W010396
    (R)-3-Hydroxy-4,4-dimethyldihydrofuran-2(3H)-one

    Endogenous Metabolite Metabolic Disease
    (R)-3-Hydroxy-4,4-dimethyldihydrofuran-2(3H)-one is an endogenous metabolite.
  • HY-14664DS
    (3S,5R)-Fluvastatin D6

    (3S,5R)-XU 62-320 free acid D6

    Autophagy Cancer Cardiovascular Disease
    (3S,5R)-Fluvastatin D6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
  • HY-A0295
    (R)-Propranolol hydrochloride

    Adrenergic Receptor Endocrinology Neurological Disease Cardiovascular Disease
    (R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol (HY-B0573). Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively.
  • HY-113025A
    L-hydroxylysine dihydrochloride

    (2S,5R)-5-Hydroxylysine dihydrochloride

    Endogenous Metabolite Others
    L-hydroxylysine dihydrochloride ((2S,5R)-5-Hydroxylysine dihydrochloride), an amino acid, is exclusive to collagen protein, which is formed by posttranslational hydroxylation of some lysine residues.
  • HY-106376A
    L-Buthionine-(S,R)-sulfoximine

    L-Buthionine sulfoximine; L-BSO

    Ferroptosis Cancer
    L-Buthionine-(S,R)-sulfoximine is a cell-permeable, potent, fast acting and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively.
  • HY-P1175A
    L-R4W2 TFA

    TRP Channel Neurological Disease
    L-R4W2 TFA is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 TFA may act as a potent analgesic.
  • HY-17504D
    (3S,5R)-Rosuvastatin

    HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Metabolic Disease Cardiovascular Disease
    (3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
  • HY-N2380
    N-Benzoyl-(2R,3S)-3-phenylisoserine

    Others Cancer
    N-Benzoyl-(2R,3S)-3-phenylisoserine is a Taxol C-13 Side Chain and crucial for the strong antitumor activity of Taxol.
  • HY-15015
    OT-R antagonist 1

    Oxytocin receptor antagonist 1

    Oxytocin Receptor Endocrinology
    OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist.
  • HY-123109
    (S,R,S)-AHPC-Boc

    VH032-Boc

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Boc is used in PROTAC technology.
  • HY-100542
    D-α-Hydroxyglutaric acid disodium

    Disodium (R)-2-hydroxyglutarate

    Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling.
  • HY-131959
    (S,R,S)-AHPC-PEG5-Boc

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG5-Boc is a E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for Cdc20 degrader CP5V.
  • HY-N4264
    Vinaginsenoside R3

    Others Inflammation/Immunology
    Vinaginsenoside R3 is a saponin composition of roots of Panax ginseng. Ginsengs have been not only used as therapeutic agents with tonic, sedative, anti-fatigue, and anti-gastric ulcer effect but also marketed as dietary supplements and raw materials of health food.
  • HY-W011241
    Cinchonine hydrochloride

    (8R,9S)-Cinchonine hydrochloride; LA40221 hydrochloride

    Apoptosis Parasite Cancer
    Cinchonine hydrochloride ((8R,9S)-Cinchonine hydrochloride) is a natural alkaloid present in Cinchona bark, with antimalarial activity. Cinchonine hydrochloride activates endoplasmic reticulum (ER) stress-induced apoptosis in human liver cancer cells.
  • HY-W010271
    (2S,3R,4S)-4-Hydroxyisoleucine

    (2S,3R,4S)-4-Hydroxy-L-isoleucine

    Others Metabolic Disease
    (2S,3R,4S)-4-Hydroxyisoleucine is an orally active compound isolated from Trigonella foenum-graecum, with anti-diabetes and anti-diabetic nephropathy activity.
  • HY-13716
    Noscapine

    (S,R)-Noscapine

    Opioid Receptor Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier.
  • HY-13716A
    Noscapine hydrochloride

    (S,R)-Noscapine hydrochloride

    Opioid Receptor Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Noscapine hydrochloride ((S,R)-Noscapine hydrochloride) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
  • HY-136163
    (S,R,S)-AHPC-C2-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C2-NH2 dihydrochloride incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-OH can be used in the synthesis of a series of PROTACs.
  • HY-15956A
    CPI-169

    CPI 169 R-enantiomer

    Histone Methyltransferase Cancer
    CPI-169 (CPI 169 R-enantiomer) is a novel and potent EZH2 inhibitor, with IC50s of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
  • HY-115681
    (2R/S)-6-PNG

    6-Prenylnaringenin

    Calcium Channel Neurological Disease
    (2R/S)-6-PNG (6-Prenylnaringenin) is a Cav3.2 (T-type) Ca 2+ channel blocker (IC50=991 nM). (2R/S)-6-PNG suppresses neuropathic allodynia in mouse pain models.
  • HY-Z0081
    2S,4R-Sacubitril

    Others Cardiovascular Disease
    2S,4R-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
  • HY-13534
    Abarelix

    R3827; PPI 149

    GnRH Receptor Cancer Endocrinology
    Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
  • HY-B0371D
    (S)-Terazosin

    Adrenergic Receptor Endocrinology
    (S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

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

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-I1070
    D-Isoleucine

    (R)-Isoleucine

    Others Neurological Disease
    D-Isoleucine ((R)-Isoleucine), an isoleucine stereoisomer, is a selective activator of Asc-1 antiporter, which enhances long-term potentiation at the hippocampal CA1-CA3 via release of endogenous D-serine.
  • HY-N2039
    20(R)-Ginsenoside Rg2

    Others Cancer
    20(R)-Ginsenoside Rg2, isolated from Ginseng stems and leaves, shows inhibitory effects on lung cancer NCI-H1650 cells. Anti-cancer activities.
  • HY-W013078
    (2R)-3-(((2-Aminoethoxy)(hydroxy)phosphoryl)oxy)propane-1,2-diyl ditetradecanoate

    Endogenous Metabolite Metabolic Disease
    (2R)-3-(((2-Aminoethoxy)(hydroxy)phosphoryl)oxy)propane-1,2-diyl ditetradecanoate is an endogenous metabolite.
  • HY-130849
    (S,R,S)-AHPC-Me-C5-COOH

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-Me-C5-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-C5-COOH can be used in PROTAC DT2216 (HY-130604).
  • HY-N1372
    (R)-Fangchinoline

    Thalrugosine; Thaligine

    Bacterial Antibiotic Cancer Infection Inflammation/Immunology Cardiovascular Disease
    (R)-Fangchinoline (Thalrugosine), a alkaloids from genus Stephania,exhibits antimicrobial and hypotensive activity. The roots and stems of several plants from genus Stephania are all used as traditional Chinese medicine and have been used for treatment of fever, diarrhea, dyspepsia and urinary disease.
  • HY-14127
    R121919

    NBI30775

    CRFR Neurological Disease Endocrinology
    R121919 (NBI30775) is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-10562A
    Ketanserin tartrate

    R41468 tartrate

    5-HT Receptor Potassium Channel Autophagy Neurological Disease
    Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
  • HY-13987
    (R)-1,2,3,4-Tetrahydro-3-isoquinolinecarboxylic acid

    D-phenylalanine analogue

    Others Others
    (R)-1,2,3,4-Tetrahydro-3-isoquinolinecarboxylic acid is a constrained Phe analogue which can fold into a beta-bend and a helical structure, and to adopt a preferred side-chain disposition in the peptide.
  • HY-14728
    Aleglitazar

    R1439; RO0728804

    PPAR Metabolic Disease
    Aleglitazar (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.
  • HY-Z0075
    (Z)2S,4R-Sacubitril

    Others Cardiovascular Disease
    (Z)2S,4R-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
  • HY-17039
    Alcaftadine

    R89674

    Histamine Receptor Inflammation/Immunology Endocrinology
    Alcaftadine (R89674) is a histamine H1 receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects.
  • HY-B0471
    Phenylephrine hydrochloride

    (R)-(-)-Phenylephrine hydrochloride; L-Phenylephrine hydrochloride

    Adrenergic Receptor Endogenous Metabolite Cardiovascular Disease Endocrinology
    (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
  • HY-128836
    (4R,5S)-Nutlin carboxylic acid

    MDM2 ligand 2; E3 ligase Ligand 15

    Ligand for E3 Ligase Cancer
    (4R,5S)-Nutlin carboxylic acid (MDM2 ligand 2) is the Nutlin 3-based MDM2 ligand. (4R,5S)-Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTACs.
  • HY-116830B
    BRD5648

    (R)-BRD0705

    GSK-3 Cancer
    BRD5648 ((R)-BRD0705) is a negative control of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).
  • HY-B0661
    Tamsulosin

    (R)-(-)-YM12617 free base; LY253351 free base

    Adrenergic Receptor Cancer Endocrinology Neurological Disease
    Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models.
  • HY-130640
    (S,R,S)-AHPC-Me-C7 ester

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-Me-C7 ester is a E3 ligase ligand-linker conjugate used to synthesise BCL-XL PROTAC degraders.
  • HY-15464A
    (R)-(-)-Gossypol acetic acid

    AT-101 (acetic acid); (-)-Gossypol acetic acid; (R)-Gossypol acetic acid

    Bcl-2 Family Autophagy Cancer
    (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
  • HY-W040240
    (3S,4R,5S)-1,3,4,5,6-Pentahydroxyhexan-2-one

    Endogenous Metabolite Metabolic Disease
    (3S,4R,5S)-1,3,4,5,6-Pentahydroxyhexan-2-one is an endogenous metabolite.
  • HY-130847
    (S,R,S)-AHPC-Me-C10-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-Me-C10-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-C10-NH2 can be used in PROTAC MS432 (HY-130602).
  • HY-P0133
    (Arg)9

    Nona-L-arginine; Peptide R9

    Others Neurological Disease
    (Arg)9 (Nona-L-arginine;Peptide R9) is a cell-penetrating peptide; exhibits neuroprotective activity with an IC50 of 0.78 μM in the glutamic acid model.
  • 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-B2246
    L-Carnitine hydrochloride

    (R)-Carnitine hydrochloride

    Endogenous Metabolite Metabolic Disease
    L-Carnitine hydrochloride ((R)-Carnitine hydrochloride), a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine hydrochloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine hydrochloride is an antioxidant. L-Carnitine hydrochloride can ameliorate metabolic imbalances in many inborn errors of metabolism.
  • HY-100703
    Pipamperone

    Floropipamide; McN-JR 3345; R 3345

    5-HT Receptor Dopamine Receptor Neurological Disease
    Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7).
  • HY-108059
    β-Cryptoxanthin

    (3R)-β-Cryptoxanthin

    Endogenous Metabolite Neurological Disease
    β-Cryptoxanthin ((3R)-β-Cryptoxanthin), isolated from Satsuma mandarin orange, is an oxygenated carotenoid and a potent antioxidant. β-Cryptoxanthin has an anti-stress effect.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-N2185
    (5R,6E)-5-Hydroxy-1,7-diphenyl-6-hepten-3-one

    Others Inflammation/Immunology
    (5R,6E)-5-Hydroxy-1,7-diphenyl-6-hepten-3-one is the methylene chloride extract of Alpinia nutans, has antioxidant activity.
  • HY-50730
    Asparagusic acid

    Parasite Infection
    Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
  • HY-12987S
    Pimozide D4

    R6238 D4

    Dopamine Receptor Adrenergic Receptor STAT Cancer Endocrinology Neurological Disease
    Pimozide D4 (R6238 D4) is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-115292
    Simvastatin hydroxy acid sodium

    Tenivastatin sodium; Simvastatin Impurity A sodium

    HMG-CoA Reductase (HMGCR) Cancer
    Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
  • HY-15266
    24R-Calcipotriol

    PRI 2202; Impurity D of Calcipotriol

    VD/VDR Cancer
    24R-Calcipotriol(PRI 2202) is an impurity of Calcipotriol; Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors.
  • HY-114176B
    (S,R,S)-AHPC-C4-NH2 dihydrochloride

    VH032-C4-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C4-NH2 dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.
  • HY-114176A
    (S,R,S)-AHPC-C4-NH2

    VH032-C4-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.
  • HY-N0221
    Daurisoline

    (R,R)-Daurisoline

    Autophagy Potassium Channel Cancer
    Daurisoline is a hERG inhibitor and also an autophagy blocker.
  • HY-42680
    (3S,4S,5R)-1,3,4,5,6-Pentahydroxyhexan-2-one

    Tagatose, D- (8CI)

    Endogenous Metabolite Metabolic Disease
    (3S,4S,5R)-1,3,4,5,6-Pentahydroxyhexan-2-one is an endogenous metabolite.
  • HY-14645A
    (+)-DHMEQ

    (1R,2R,6R)-Dehydroxymethylepoxyquinomicin; (1R,2R,6R)-DHMEQ

    Keap1-Nrf2 Inflammation/Immunology
    (+)-DHMEQ is an activator of antioxidant transcription factor Nrf2. (+)-DHMEQ is the enantiomer of (-)-DHMEQ. (-)-DHMEQ inhibits NF-kB than its enantiomer (+)-DHMEQ.
  • HY-100218A
    RSL3

    (1S,3R)-RSL3

    Glutathione Peroxidase Ferroptosis Cancer
    RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.
  • HY-103187
    HEMADO

    Adenosine Receptor Cancer Inflammation/Immunology
    HEMADO is a potent and selective adenosine A3 receptor agonist with a Ki of 1.1 nM at the human A3 subtype.
  • HY-136183
    (S,R,S)-AHPC-phenol-alkylC6-amine dihydrochloride

    VH032 phenol-alkylC6-amine dihydrochloride

    E3 Ligase Ligand-Linker Conjugate
    (S,R,S)-AHPC-phenol-alkylC6-amine (dihydrochloride) is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC. (S,R,S)-AHPC-phenol-alkylC6-amine incorporates an E3 ligase ligand plus an alkyl linker ready for conjugation to a target protein ligand.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-108400
    SCH-23390 maleate

    R-(+)-SCH-23390 maleate

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-19545A
    SCH-23390 hydrochloride

    R-(+)-SCH-23390 hydrochloride

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-128941
    CCK2R Ligand-Linker Conjugates 1

    Drug-Linker Conjugates for ADC Cancer
    CCK2R Ligand-Linker Conjugates 1 is a ligand-linker conjugate, which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker.
  • HY-129941
    (S,R,S)-AHPC-C10-NH2

    VH032-C10-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC.
  • HY-129941A
    (S,R,S)-AHPC-C10-NH2 dihydrochloride

    VH032-C10-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-C10-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC.
  • HY-B0203A
    Nebivolol hydrochloride

    R 065824 hydrochloride

    Adrenergic Receptor Apoptosis Cardiovascular Disease Endocrinology
    Nebivolol hydrochloride selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.
  • HY-B0203
    Nebivolol

    R 065824

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.
  • HY-112078
    (S,R,S)-AHPC-Me

    VHL ligand 2; E3 ligase Ligand 1A

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-14788
    Drinabant

    AVE1625

    Cannabinoid Receptor Metabolic Disease
    Drinabant (AVE1625) is an orally active CB1 receptor antagonist. Drinabant (AVE1625) inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-107836
    Methiothepin mesylate

    Metitepine mesylate; Ro 8-6837 mesylate

    5-HT Receptor Neurological Disease
    Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
  • HY-126456
    (S,R,S)-AHPC-propargyl

    VH032-propargyl; VHL ligand 7

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-propargyl (VH032-propargyl) is a VHL ligand which is used in “click reaction” for PROTACs.
  • HY-103603B
    (S,R,S)-AHPC-PEG2-NH2 dihydrochloride

    VH032-PEG2-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG2-NH2 dihydrochloride (VH032-PEG2-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.
  • HY-42424
    (S,R,S)-AHPC-Me hydrochloride

    VHL ligand 2 hydrochloride; E3 ligase Ligand 1

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-42424A
    (S,R,S)-AHPC-Me dihydrochloride

    VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-117244
    AZD7507

    c-Fms Cancer
    AZD7507 is a potent and orally active CSF-1R inhibitor, with antitumor activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-112929B
    (1S,2S,3R)-DT-061

    Others Cancer
    (1S,2S,3R)-DT-061 is an enantiomer of DT-061. DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
  • HY-12475
    Mutant IDH1-IN-1

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-136184
    (S,R,S)-AHPC-phenol-C4-NH2 dihydrochloride

    VH032-phenol-C4-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate
    (S,R,S)-AHPC-phenol-C4-NH2 dihydrochloride is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC. (S,R,S)-AHPC-phenol-C4-NH2 dihydrochloride incorporates an E3 ligase ligand plus an alkyl linker ready for conjugation to a target protein ligand.
  • HY-19540
    GSK864

    Isocitrate Dehydrogenase (IDH) Cancer
    GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-101763A
    (S,R,S)-AHPC hydrochloride

    VH032-NH2 hydrochloride; VHL ligand 1 hydrochloride

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC hydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
  • HY-10165
    PSI-6130

    R 1656

    HCV Infection
    PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM. 
  • HY-N0095
    (S)-10-Hydroxycamptothecin

    10-HCPT; 10-Hydroxycamptothecin

    Topoisomerase Apoptosis Cancer
    (S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.
  • HY-50866
    NVP-AEW541

    AEW541

    IGF-1R Insulin Receptor Autophagy Cancer Endocrinology
    NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 0.15 μM, also inhibits InsR, with IC50 of 0.14 μM.
  • HY-41094
    cis-Isolimonenol

    (1S,4R)-p-Mentha-2,8-dien-1-ol

    Others Others
    cis-Isolimonenol ((1S,4R)-p-Mentha-2,8-dien-1-ol) is a chemical composition of essential oil.
  • HY-125845
    (S,R,S)-AHPC

    VH032-NH2; VHL ligand 1

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
  • HY-131387
    (S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 can be used in PROTAC BRD4 Degrader-5 (HY-133737) and PROTAC BRD4 Degrader-5-CO-PEG3-N3 (HY-133736).
  • HY-15494
    Picropodophyllin

    AXL1717; Picropodophyllin; PPP

    IGF-1R Apoptosis Cancer Endocrinology
    Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
  • 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-107977
    IDH1 Inhibitor 3

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1 R132H.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-123960
    Raphin1

    Phosphatase Neurological Disease
    Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
  • HY-123960A
    Raphin1 acetate

    Phosphatase Neurological Disease
    Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
  • HY-128523
    Kgp-IN-1

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

    Others Inflammation/Immunology
    Kgp-IN-1 hydrochloride is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.
  • HY-136055
    (S,R,S)-AHPC-C5-COOH

    VH032-C5-COOH

    E3 Ligase Ligand-Linker Conjugate HIF/HIF Prolyl-Hydroxylase Cancer
    (S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases.
  • HY-119424
    SP4206

    Interleukin Related Inflammation/Immunology
    SP4206 is an IL-2/IL-2Rα interaction inhibitor. SP4206 binds with high affinity (Kd=70 nM) to IL-2 and blocks binding to its natural receptor IL-2Rα (Kd=10 nM).
  • HY-136006
    (S,R,S)-AHPC-C6-NH2 dihydrochloride

    VH032-C6-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C6-NH2 dihydrochloride (VH032-C6-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 dihydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1.
  • HY-133487B
    (S,R,S)-AHPC-C8-NH2

    VH032-C8-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1.
  • HY-136006A
    (S,R,S)-AHPC-C6-NH2 hydrochloride

    VH032-C6-NH2 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C6-NH2 hydrochloride (VH032-C6-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 hydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1.
  • HY-133487
    (S,R,S)-AHPC-C8-NH2 dihydrochloride

    VH032-C8-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C8-NH2 dihydrochloride (VH032-C8-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1.
  • HY-130711
    (S,R,S)-AHPC-C3-NH2

    VH032-C3-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-101335
    DCG-IV

    mGluR Neurological Disease
    DCG-IV is a potent agonist of group II mGluRs with EC50s of 0.35 and 0.09 μM for mGlu2R and mGlu3R, reapectively. DCG-IV is also a competitive antagonist at group I (IC50: mGlu1R/5R=389/630 μM) and III receptors (IC50: mGlu4R/6R/7R/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects.
  • HY-103608
    (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl

    VHL Ligand-Linker Conjugates 11; E3 ligase Ligand-Linker Conjugates 11

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
  • HY-114176
    (S,R,S)-AHPC-C4-NH2 hydrochloride

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

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.
  • HY-103599
    (S,R,S)-AHPC-PEG2-N3

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

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in PROTAC technology.
  • HY-103604
    (S,R,S)-AHPC-PEG4-NH2 hydrochloride

    VH032-PEG4-NH2 hydrochloride; VHL Ligand-Linker Conjugates 4 hydrochloride; E3 ligase Ligand-Linker Conjugates 7

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
  • HY-103601
    (S,R,S)-AHPC-PEG4-N3

    VH032-PEG4-N3; VHL Ligand-Linker Conjugates 5; E3 ligase Ligand-Linker Conjugates 4

    E3 Ligase Ligand-Linker Conjugate Others
    (S,R,S)-AHPC-PEG4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
  • HY-103600
    (S,R,S)-AHPC-PEG1-N3

    VH032-PEG1-N3; VHL Ligand-Linker Conjugates 9; E3 ligase Ligand-Linker Conjugates 3

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG1-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology.
  • HY-103598
    (S,R,S)-AHPC-PEG3-N3

    VH032-PEG3-N3; VHL Ligand-Linker Conjugates 8; E3 ligase Ligand-Linker Conjugates 12

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG3-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
  • HY-103602
    (S,R,S)-AHPC-PEG3-NH2 hydrochloride

    VH032-PEG3-NH2 hydrochloride; VHL Ligand-Linker Conjugates 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 5

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
  • HY-103606
    (S,R,S)-AHPC-PEG6-C4-Cl

    VH032-PEG6-C4-Cl; VHL Ligand-Linker Conjugates 10; E3 ligase Ligand-Linker Conjugates 9

    PROTAC Cancer
    (S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
  • HY-103607
    (S,R,S)-AHPC-PEG2-C4-Cl

    VH032-PEG2-C4-Cl; VHL Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 10

    PROTAC Cancer
    (S,R,S)-AHPC-PEG2-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
  • HY-101526
    GENZ-882706

    RA03546849

    c-Fms Inflammation/Immunology
    GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1.
  • HY-18785
    Indirubin Derivative E804

    IGF-1R Cancer Endocrinology
    Indirubin Derivative E804 is a potent inhibitor of Insulin-like Growth Factor 1 Receptor (IGF1R), with an IC50 of 0.65 μM for IGF1R.
  • HY-90009C
    ent-Tadalafil

    ent-IC-351

    Phosphodiesterase (PDE) Cancer
    ent-Tadalafil (ent-IC-351), compound (6S,12aS), is a inactive cis-enantiomer of compound (6R,12aS). compound (6R,12aS) is a potent PDE5 inhibitor with an IC50 of 0.090 μM, while ent-Tadalafil is inactive at concentrations up to 10 µM.
  • HY-100615
    Revizinone

    R80122

    Phosphodiesterase (PDE) Cardiovascular Disease
    Revizinone is a novel selective phosphodiesterase (PDE) inhibitor with IC50 values on this enzyme to 0.036 microM.
  • HY-103602A
    (S,R,S)-AHPC-PEG3-NH2

    VH032-PEG3-NH2; VHL Ligand-Linker Conjugates 1; E3 ligase Ligand-Linker Conjugates 5 Free Base

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
  • HY-103604A
    (S,R,S)-AHPC-PEG4-NH2

    VH032-PEG4-NH2; VHL Ligand-Linker Conjugates 4 ; E3 ligase Ligand-Linker Conjugates 7 Free Base

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
  • HY-108494
    CYM50260

    LPL Receptor Cardiovascular Disease
    CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R.
  • HY-136238
    PM226

    Cannabinoid Receptor Neurological Disease
    PM226 is a selective cannabinoid CB2R agonist (Ki (CB2R)=13 nM; EC50 (CB2R)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo.
  • HY-130654
    (S,R,S)-AHPC-C2-PEG4-N3

    VH032-C2-PEG4-N3

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM.
  • HY-110402
    (S,R,S)-AHPC TFA

    VH032-NH2 TFA; VHL ligand 1 TFA

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC TFA (VH032-NH2 TFA) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-108495
    CYM50308

    ML248

    LPL Receptor Cardiovascular Disease
    CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.
  • HY-19320
    Orexin 2 Receptor Agonist

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Orexin 2 Receptor Agonist is a potent (EC50 on OX2R is 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio is 70) agonist.
  • HY-P0227
    SHU 9119

    Melanocortin Receptor Metabolic Disease
    SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
  • HY-104042
    Vorasidenib

    AG-881

    Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.
  • HY-130271
    (S,R,S)-AHPC-PEG5-COOH

    VH032-PEG5-COOH; VHL Ligand-Linker Conjugates 16; E3 Ligase Ligand-Linker Conjugates 58

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 5-unit PEG linker used in PROTAC technology.
  • HY-136186
    (S,R,S)-AHPC-C7-amine

    VH032-C7-amine

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader.
  • HY-12872
    Nazartinib

    EGF816

    EGFR Cancer
    Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min −1 on EGFR(L858R/790M) mutant, respectively.
  • HY-131312
    Mutant IDH1-IN-6

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.
  • HY-P1205A
    MCH(human, mouse, rat) TFA

    MCHR1 (GPR24) Neurological Disease
    MCH (human, mouse, rat) TFA is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively.
  • HY-P1205
    MCH(human, mouse, rat)

    MCHR1 (GPR24) Neurological Disease
    MCH (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively.
  • HY-13972
    Mutant IDH1 inhibitor

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
  • HY-103605
    (S,R,S)-AHPC-C6-PEG3-C4-Cl

    VH032-C6-PEG3-C4-Cl; VHL Ligand-Linker Conjugates 12; E3 ligase Ligand-Linker Conjugates 8

    PROTAC Cancer
    (S,R,S)-AHPC-C6-PEG3-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
  • HY-13784
    Pirodavir

    R77975

    Enterovirus Infection
    Pirodavir is a potent, broad-spectrum picornavirus inhibitor, and is highly active against both group A and group B rhinovirus serotypes. Pirodavir is very potent in a virus yield reduction assay (IC90=2.3 nM).
  • HY-18690
    Enasidenib

    AG-221

    Isocitrate Dehydrogenase (IDH) Cancer
    Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively.
  • HY-12872A
    Nazartinib mesylate

    EGF816 mesylate

    EGFR Cancer
    Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min −1 on EGFR(L858R/790M) mutant, respectively.
  • HY-112608
    CHMFL-PI3KD-317

    PI3K Cancer
    CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.
  • HY-11018
    Risperidone

    R 64 766

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-19974
    TAK-220

    CCR HIV Infection Endocrinology
    TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
  • HY-111950
    (-)-Ibuprofenamide

    (R)-Ibuprofenamide

    Others Inflammation/Immunology
    (-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-119942
    c-Fms-IN-8

    c-Fms Cancer
    c-Fms-IN-8 (compound 4a) is a colony stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor, with an IC50 of 9.1 nM.
  • HY-18634
    NSC319726

    ZMC1

    MDM-2/p53 Cancer
    NSC319726 (ZMC1) is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.
  • HY-112451
    cFMS Receptor Inhibitor II

    c-Fms Inflammation/Immunology
    cFMS Receptor Inhibitor II is a CSF1R kinase inhibitor. CSF-1 is a cytokine.
  • HY-13520
    Nocodazole

    Oncodazole; R17934

    Microtubule/Tubulin Bcr-Abl CRISPR/Cas9 Autophagy Apoptosis Cancer
    Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
  • HY-B0363
    Nimesulide

    R805

    COX Inflammation/Immunology
    Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
  • HY-12987
    Pimozide

    R6238

    Dopamine Receptor Adrenergic Receptor STAT Cancer Neurological Disease Endocrinology
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-130816
    (S,R,S)-AHPC-O-Ph-PEG1-NH2

    VH032-O-Ph-PEG1-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02.
  • HY-128597
    BRD-IN-3

    Epigenetic Reader Domain Cancer
    BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ.
  • HY-15749
    XL228

    Aurora Kinase Bcr-Abl IGF-1R Src Cancer Endocrinology
    XL228 is a multi-targeted tyrosine kinase inhibitor with IC50s of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.
  • 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-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-100013A1
    (1R,2R)-2-PCCA(hydrochloride)

    Others Neurological Disease
    (1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay.
  • HY-122906
    JTE-952

    c-Fms Inflammation/Immunology
    JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis.
  • HY-103603
    (S,R,S)-AHPC-PEG2-NH2 hydrochloride

    VH032-PEG2-NH2 hydrochloride; VHL Ligand-Linker Conjugates 3 hydrochloride; E3 ligase Ligand-Linker Conjugates 6

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG2-NH2 hydrochloride (VH032-PEG2-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.
  • 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-P1453A
    CMD178 TFA

    STAT Inflammation/Immunology
    CMD178 (TFA) is a lead peptide that consistently reduces the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 (TFA) also is an inhibitor of STAT5 and inhibits Tregcells development.
  • HY-116819
    VU0453379

    Glucagon Receptor Metabolic Disease
    VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM.
  • HY-103603A
    (S,R,S)-AHPC-PEG2-NH2

    VH032-PEG2-NH2 ; VHL Ligand-Linker Conjugates 3 ; E3 ligase Ligand-Linker Conjugates 6 Free Base

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG2-NH2 (VH032-PEG2-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.
  • HY-10253
    AG1024

    Tyrphostin AG 1024

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.
  • HY-N0898A
    (-)-Catechin

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

    COX Cancer
    (-)-Catechin, isolated from green tea, is an isomer of Catechin having a trans 2S,3R configuration at the chiral center. Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
  • HY-15772A
    Osimertinib mesylate

    AZD-9291 mesylate; Mereletinib mesylate

    EGFR Cancer
    Osimertinib mesylate (AZD-9291 mesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
  • HY-10896
    JNJ-10397049

    Orexin Receptor (OX Receptor) Neurological Disease
    JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold selective for the OX2R over the OX1R.
  • HY-10624
    THIQ

    Melanocortin Receptor Metabolic Disease
    THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants.
  • HY-111415
    EGFR-IN-5

    EGFR Cancer
    EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFR L858R, EGFR L858R/T790M, and EGFR L858R/T790M/C797S, respectively.
  • HY-12085S2
    (Rac)-Apremilast D5

    (Rac)-CC-10004 D5

    Others Inflammation/Immunology
    (Rac)-Apremilast D5 ((Rac)-CC-10004 D5) is a deuterium labeled (R)-Apremilast. (R)-Apremilast ((R)-CC-10004) is a enantiomer of Apremilast.
  • HY-101708
    N-(2-Chloro-6-methylphenyl)-N'-4-pyridinylurea

    Others Neurological Disease
    N-[(1R)-4-[(Aminoiminomethyl)amino]-1-[[[(1R)-1-(4-hydroxyphenyl)ethyl]amino]carbonyl]butyl]-α-phenylbenzeneacetamide is an anticonvulsant agent with potential for the treatment of generalized tonic-clonic and partial seizures.
  • HY-105272A
    Loreclezole hydrochloride

    R 72063 hydrochloride

    GABA Receptor Neurological Disease
    Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
  • HY-105272
    Loreclezole

    R 72063

    GABA Receptor Neurological Disease
    Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
  • HY-136187
    (S,R,S)-AHPC-C5-NH2

    VH032-C5-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader.
  • HY-12768
    BLZ945

    c-Fms Cancer
    BLZ945 is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.
  • HY-15772
    Osimertinib

    AZD-9291; Mereletinib

    EGFR Cancer
    Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
  • HY-79077
    Osimertinib dimesylate

    AZD-9291 dimesylate; Mereletinib dimesylate

    EGFR Cancer
    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
  • HY-12790
    CB1-IN-1

    BPRCB1184

    Cannabinoid Receptor Neurological Disease
    CB1-IN-1 (BPRCB1184) is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively.
  • HY-B0794A
    AZ7550 hydrochloride

    EGFR IGF-1R Drug Metabolite Cancer Endocrinology
    AZ7550 hydrochloride is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
  • HY-B0794
    AZ7550

    EGFR IGF-1R Drug Metabolite Cancer Endocrinology
    AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
  • HY-B0794B
    AZ7550 Mesylate

    AZ7550 trimesylate salt

    EGFR IGF-1R Drug Metabolite Cancer Endocrinology
    AZ7550 Mesylate is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
  • HY-90005
    Etravirine

    R165335; TMC125

    Reverse Transcriptase HIV Infection
    Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
  • HY-10261A
    Afatinib dimaleate

    BIBW 2992MA2

    EGFR Autophagy Cancer
    Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
  • HY-P9926
    Dupilumab

    REGN-668; SAR-231893

    Interleukin Related Inflammation/Immunology
    Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis.
  • HY-130638
    (S,R,S)-AHPC-O-Ph-PEG1-NH-Boc

    VH032-O-Ph-PEG1-NH-Boc

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-O-Ph-PEG1-NH-Boc (VH032-O-Ph-PEG1-NH-Boc) is a synthesized E3 ligase ligand-linker conjugate which is used for the EED-targeted PROTAC.
  • HY-P2242A
    RO27-3225 TFA

    Melanocortin Receptor Inflammation/Immunology Neurological Disease
    RO27-3225 TFA is potent and selective melanocortin 4 receptor (MC4R) agonist with an EC50 of 1 nM and 8 nM for MC4R and MC1R, respectively. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R. RO27-3225 TFA has neuroprotective and anti-inflammatory effects.
  • HY-15656A
    Ceritinib dihydrochloride

    LDK378 dihydrochloride

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency.
  • HY-15656
    Ceritinib

    LDK378

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency.
  • HY-114459
    Mutant IDH1-IN-4

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells.
  • HY-N0328
    alpha-Mangostin

    α-Mangostin

    Reactive Oxygen Species Apoptosis Bacterial Fungal Virus Protease Cancer
    alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
  • HY-10261
    Afatinib

    BIBW 2992

    EGFR Autophagy Cancer
    Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
  • HY-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-104036
    IDH-305

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)).
  • HY-12972
    Mavelertinib

    PF-06747775

    EGFR Cancer
    Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).
  • HY-107623
    TC-MCH 7c

    MCHR1 (GPR24) Metabolic Disease
    TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.
  • HY-111539
    BAY-1316957

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC50 of 15.3 nM for human EP4-R. BAY-1316957 has excellent drug metabolism and pharmacokinetics properties, and can be used for endometriosis research.
  • HY-P1540
    Angiotensin III, human, mouse

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    Angiotensin III, human, mouse is a heptapeptide, acts as an endogenous angiotensin type 2 receptor (AT2R) agonist, with IC50s of 0.648 nM and 21.1 nM for AT2R and AT1R, respectively.
  • HY-126297
    c-Fms-IN-10

    c-Fms Cancer Inflammation/Immunology
    c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, an kinase inhibitor of FMS (Colony stimulating factor-1 receptor, CSF-1R) with IC50 of 2 nM. c-Fms-IN-10 has anti-tumor activity.
  • HY-111095
    D-(-)-Lactic acid

    (R)-2-Hydroxypropionic acid

    Endogenous Metabolite Metabolic Disease
    D-(-)-Lactic acid is a normal intermediate in the fermentation (oxidation, metabolism) of sugar. D-(-)-Lactic acid is identified to be a competitive inhibitor of ProDH (proline dehydrogenase) in plants.
  • HY-101601
    Bamirastine

    TAK-427

    Histamine Receptor Inflammation/Immunology Endocrinology
    Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.
  • HY-13203
    NVP-TAE 226

    TAE226

    FAK Pyk2 IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively.
  • HY-112601
    IDH1 Inhibitor 1

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively. Anticancer activity.
  • HY-B1655
    Fluspirilene

    R 6218; Redeptin

    Calcium Channel Neurological Disease
    Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic drug used for schizophrenia.
  • HY-10262
    BMS-536924

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity.
  • HY-P0242
    Neurokinin B

    Neurokinin Receptor Neurological Disease Endocrinology
    Neurokinin B belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect.
  • HY-13072
    Cenisertib

    AS-703569; R-763

    Aurora Kinase Bcr-Abl Akt STAT FLT3 Cancer
    Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
  • HY-B1194
    Tetramisole hydrochloride

    (±)-Tetramisole hydrochloride; DL-Tetramisole hydrochloride; R-829

    Parasite Phosphatase Antibiotic Infection
    Tetramisole hydrochloride is an inhibitor of alkaline phosphatases, is a high purity antiparasitic.
  • HY-P0242A
    Neurokinin B TFA

    Neurokinin Receptor Neurological Disease Endocrinology
    Neurokinin B TFA belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect.
  • HY-13820
    GSK2656157

    PERK Autophagy Apoptosis Cancer
    GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.
  • HY-10252
    NVP-ADW742

    ADW742; GSK 552602A; ADW

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
  • HY-112679
    GLP-1 receptor agonist 2

    Glucagon Receptor Others
    GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.
  • HY-18099A
    S1RA hydrochloride

    E-52862 hydrochloride

    Sigma Receptor Neurological Disease
    S1RA hydrochloride (E-52862 hydrochloride) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).
  • HY-18627A
    PFI-2 hydrochloride

    (R)-PFI-2 hydrochloride

    Histone Methyltransferase Cancer
    PFI-2 hydrochloride is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.
  • HY-18627
    PFI-2

    (R)-PFI-2

    Histone Methyltransferase Cancer
    PFI-2 is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.
  • HY-101768
    PRN1371

    FGFR c-Fms Cancer
    PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively.
  • HY-15772S
    Osimertinib D6

    AZD-9291 D6; Mereletinib D6

    EGFR Cancer
    Osimertinib D6 (AZD-9291 D6) is a deuterium labeled Osimertinib. Osimertinib is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
  • HY-133780
    Afatinib impurity 11

    EGFR Autophagy Cancer
    Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
  • HY-100742
    GNE-140 racemate

    Lactate Dehydrogenase Cancer
    GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is a potent lactate dehydrogenase A (LDHA) inhibitor.
  • HY-18072
    GSK2606414

    PERK Autophagy Apoptosis Cancer
    GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.
  • HY-18099
    S1RA

    E-52862

    Sigma Receptor Neurological Disease
    S1RA(E-52862) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).
  • HY-10346
    AV-412

    MP412

    EGFR Cancer
    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
  • HY-15811
    XMD8-87

    ACK1-B19

    Tyrosinase Cancer
    XMD8-87 is a potent TNK2 inhibitor with IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively.
  • HY-18082
    AGI-5198

    IDH-C35

    Isocitrate Dehydrogenase (IDH) Cancer
    AGI-5198 (IDH-C35) is a potent and selective mutant IDH1 R132H inhibitor with an IC50 of 0.07 μM.
  • HY-101243
    XMD16-5

    Tyrosinase Cancer
    XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively.
  • 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-107382
    RF9

    Neuropeptide Y Receptor Endocrinology Neurological Disease Cardiovascular Disease
    RF9 is a potent and selective Neuropeptide FF receptor antagonist, with Ki values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively.
  • HY-112484
    RS-246204

    Others Cancer
    RS-246204 is a R-spondin-1 substitute compound that is able initiate small intestinal organoids without the use of the R-spondin-1 protein.
  • HY-107382A
    RF9 hydrochloride

    Neuropeptide Y Receptor Endocrinology Neurological Disease Cardiovascular Disease
    RF9 hydrochloride is a potent and selective Neuropeptide FF receptor antagonist, with Ki values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively.
  • HY-10204
    OSI-930

    c-Kit VEGFR c-Fms Apoptosis Cancer
    OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity.
  • HY-128656
    LML134

    Histamine Receptor Neurological Disease Endocrinology
    LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders.
  • HY-14881A
    Bedaquiline fumarate

    R403323; TMC207 fumarate; R207910 fumarate

    Bacterial Antibiotic Infection
    Bedaquiline fumarate, a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections.
  • HY-13984
    Mutant EGFR inhibitor

    EGFR Cancer
    Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
  • HY-14881
    Bedaquiline

    TMC207; R207910

    Bacterial Antibiotic Infection
    Bedaquiline (TMC207) is a diarylquinoline drug and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-drug resistant tuberculosis.
  • HY-14266
    Dapivirine

    TMC120; R147681

    HIV Reverse Transcriptase Apoptosis Autophagy Infection
    Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.
  • HY-125108
    PHPS1 sodium

    Phosphatase Cancer Cardiovascular Disease
    PHPS1 sodium is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively.
  • HY-B0793
    AZ-5104

    EGFR Cancer
    AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFR L858R/T790M, EGFR L858R, EGFR L861Q, EGFR and ErbB4, respectively.
  • HY-100213
    EAI045

    EGFR Cancer
    EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.
  • HY-109012A
    Seltorexant hydrochloride

    JNJ-42847922 hydrochloride

    Orexin Receptor (OX Receptor) Endocrinology Neurological Disease
    Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
  • HY-10684
    Pridopidine

    ACR16; ASP2314; FR310826

    Dopamine Receptor Neurological Disease
    Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.
  • HY-133080
    BAY-784

    GnRH Receptor Cancer
    BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively.
  • HY-10405
    Pamapimod

    Ro4402257; R1503

    p38 MAPK Autophagy Inflammation/Immunology
    Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.
  • HY-104066
    Theliatinib

    HMPL-309

    EGFR Cancer
    Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity.
  • HY-10346A
    AV-412 free base

    MP-412 free base

    EGFR Cancer
    AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
  • HY-12170
    Prinomastat

    AG3340; KB-R9896

    MMP Apoptosis Cancer
    Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
  • HY-12170A
    Prinomastat hydrochloride

    AG3340 hydrochloride; KB-R9896 hydrochloride

    MMP Apoptosis Cancer
    Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
  • HY-12190A
    JNJ-5207852 dihydrochloride

    Histamine Receptor Neurological Disease
    JNJ-5207852 dihydrochloride is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
  • HY-12190
    JNJ-5207852

    Histamine Receptor Neurological Disease Endocrinology
    JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
  • HY-P1852
    TIP 39, Tuberoinfundibular Neuropeptide

    Adenylate Cyclase Neurological Disease
    TIP 39, Tuberoinfundibular Neuropeptide is a neuropeptide and parathyroid hormone 2 receptor (PTH2R) agonist. TIP 39 is highly conserved among species. TIP39 from all species activates adenylyl cyclase and elevates intracellular calcium levels through parathyroid hormone 2 receptor (PTH2R).
  • HY-30237
    Seliciclib

    Roscovitine; CYC202; R-roscovitine

    CDK Cancer
    Seliciclib (Roscovitine) is an orally bioavailable and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
  • HY-P1504
    β-Melanocyte Stimulating Hormone (MSH), human

    Beta-MSH (1-22) (human)

    Melanocortin Receptor Metabolic Disease Neurological Disease Endocrinology
    β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.
  • HY-N5056
    DL-Goitrin

    Others Infection
    DL-Goitrin, also called (R, S)- report by the spring, consists of the epigoitrin (reported by the R- Spring) and the spring (-S- reported by spring), and the two mutually isomers, and the mixture is the ingredient of Radix.
  • HY-18678A
    Bremelanotide Acetate

    PT-141 Acetate

    Melanocortin Receptor Endocrinology
    Bremelanotide Acetate (PT-141 Acetate), a synthetic peptide analogue of α-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R for the treatment of sexual dysfunction.
  • HY-136429
    Ethylhydrocupreine

    Optochin

    Bacterial Parasite Infection
    Ethylhydrocupreine (Optochin) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.
  • HY-136429A
    Ethylhydrocupreine hydrochloride

    Optochin hydrochloride

    Bacterial Parasite Infection
    Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine hydrochloride also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine hydrochloride is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.
  • HY-130608
    Mutated EGFR-IN-3

    EGFR Cancer
    Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
  • HY-128862
    EGFR-IN-7

    EGFR Cancer
    EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.
  • HY-12026
    WZ4002

    EGFR Cancer
    WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750 and EGFR E746_A750/T790M, respectively.
  • HY-A0024
    Tolterodine

    (R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583

    mAChR Neurological Disease
    Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo.
  • HY-10502
    Tipifarnib

    IND 58359; R115777

    Farnesyl Transferase Cancer
    Tipifarnib (IND 58359) binds to and inhibits farnesyltransferase (FTase) with an IC50 of 0.86 nM. Antineoplastic activity.
  • HY-P1504A
    β-Melanocyte Stimulating Hormone (MSH), human TFA

    Beta-MSH (1-22) (human) TFA

    Melanocortin Receptor Metabolic Disease Neurological Disease Endocrinology
    β-Melanocyte Stimulating Hormone (MSH), human TFA, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.
  • HY-N2000
    Bellidifolin

    HIV Cancer Infection Inflammation/Immunology
    Bellidifolin is a xanthone isolated from the stems of Swertia punicea, with hepatoprotective, hypoglycemic, anti-oxidation, anti-inflammatory and antitumor activities. Bellidifolin also acts as a viral protein R (Vpr) inhibitor.
  • HY-109012
    Seltorexant

    JNJ-42847922

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
  • HY-100139
    Diflumidone

    R807

    Others Inflammation/Immunology
    Diflumidone is a non-steroidal antiinflammatory drug.
  • HY-B1077
    Penfluridol

    R-16341

    Calcium Channel Autophagy Neurological Disease Cancer
    Penfluridol is a highly potent, first generation diphenylbutylpiperidine antipsychotic.
  • HY-B1547A
    Benzetimide hydrochloride

    R4929

    mAChR Neurological Disease
    Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist.
  • HY-101094
    Ocaperidone

    R79598

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
  • HY-101589
    Sotirimod

    R850

    Others Inflammation/Immunology
    Sotirimod is an immunostimulant, and can potentially treat for actinic keratosis.
  • HY-B0901
    Bromperidol

    R-11333

    5-HT Receptor Neurological Disease
    Bromperidol is a butyrophenone derivative, is a potent and long-acting neuroleptic, used as an antipsychotic in the treatment of schizophrenia.
  • HY-10562
    Ketanserin

    R41468

    5-HT Receptor Potassium Channel Autophagy Neurological Disease
    Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
  • HY-100265
    Cinperene

    R5046

    Others Neurological Disease
    Cinperene is an atropine-like drug which can block pilocarpine-induced lacrimation and salivation.
  • HY-B1790
    Terconazole

    R42470

    Fungal Infection
    Terconazole is a broad-spectrum antifungal medication for the treatment of vaginal yeast infection.
  • HY-135270
    ADRA1D receptor agonist 1

    Adrenergic Receptor Endocrinology
    ADRA1D receptor agonist 1 (compound (R)-9S) is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM.
  • HY-12001
    WZ-3146

    EGFR Cancer
    WZ3146 is a mutant selective EGFR inhibitor with IC50s of 2, 2, 5, 14 and 66 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750, EGFR E746_A750/T790M and EGFR, respectively.
  • HY-114226
    Olutasidenib

    FT-2102

    Isocitrate Dehydrogenase (IDH) Cancer Inflammation/Immunology
    Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) [1].
  • HY-19617A
    EGFR-IN-1 hydrochloride

    EGFR Cancer
    EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • 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-100349
    SU4312

    PDGFR VEGFR Cancer
    SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively.
  • HY-116624
    MAZ51

    VEGFR Apoptosis Cancer
    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.
  • HY-114410
    CCI-006

    Mitochondrial Metabolism Cancer
    CCI-006 is a selective inhibitor and chemosensitizer of MLL-rearranged leukemia cells, by inhibits mitochondrial respiration resulting in insurmountable mitochondrial depolarization and a pro-apoptotic unfolded protein response (UPR) in a subset of MLL-r leukemia cells.
  • HY-103032
    Multi-kinase inhibitor 1

    PDGFR c-Kit Bcr-Abl Cancer
    Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
  • HY-10013
    Taranabant

    MK-0364

    Cannabinoid Receptor Metabolic Disease
    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
  • HY-N4267
    Yangambin

    Calcium Channel Infection Cardiovascular Disease
    Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+ influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM.
  • HY-12324
    SB269652

    Dopamine Receptor Neurological Disease
    SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
  • HY-122190
    TAK-071

    mAChR Neurological Disease
    TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
  • HY-P0201A
    Substance P TFA

    Neurokinin P TFA

    Neurokinin Receptor Endocrinology Neurological Disease
    Substance P TFA (Neurokinin P TFA) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
  • HY-14799
    Palovarotene

    R 667; Ro 3300074

    RAR/RXR Autophagy Others
    Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.
  • HY-13493
    AC710

    PDGFR c-Kit FLT3 Cancer
    AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
  • HY-B0751
    Fumagillin

    Amebacilin; NSC9168

    Parasite HIV Antibiotic Infection
    Fumagillin(NSC9168) is a complex biomolecule and used as an antimicrobial agent. Fumagillin can inhibits HIV‐1 infection through the inhibition of HIV-1 viral protein R (Vpr) activity.
  • HY-78869
    Mutated EGFR-IN-1

    Osimertinib analog

    EGFR Cancer
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
  • HY-13493A
    AC710 Mesylate

    PDGFR Cancer
    AC710 Mesylate is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
  • HY-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-135805
    JBJ-04-125-02

    EGFR Cancer
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
  • HY-19617B
    EGFR-IN-1 TFA

    EGFR Cancer
    EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-19617
    EGFR-IN-1

    EGFR Cancer
    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-10524
    GSK1904529A

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.
  • HY-16749A
    Pexidartinib hydrochloride

    PLX-3397 hydrochloride

    c-Fms c-Kit Apoptosis Cancer
    Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity.
  • HY-19668A
    SGS518 oxalate

    5-HT Receptor Neurological Disease
    SGS518 oxalate is a selective 5-HT6R antagonist. SGS518 oxalate can be used for the research of cognitive impairments such as amnesia, anxiety and depression, and it is effective in protecting mouse retina at high doses[1]
  • HY-110066
    (Z)-Guggulsterone

    Apoptosis VEGFR Akt Cancer
    Z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis.
  • HY-12297
    Sulfatinib

    HMPL-012

    FGFR VEGFR Cancer
    Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.
  • HY-10408
    Ki20227

    c-Fms VEGFR c-Kit PDGFR Inflammation/Immunology
    Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.
  • HY-17385
    Atomoxetine hydrochloride

    Tomoxetine hydrochloride; LY 139603; (R)-Tomoxetine hydrochloride

    Others Neurological Disease
    Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).
  • HY-103178
    MRE3008F20

    Adenosine Receptor Cancer
    MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibiting agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM.
  • HY-136362
    ARRY-382

    c-Fms Cancer Inflammation/Immunology
    ARRY-382 is a potent, oral and highly selective inhibitor of CSF1R/c-Fms with an IC50 of 9 nM. ARRY-382 can be used for the research of advanced or metastatic cancers.
  • HY-18697
    JD-5037

    Cannabinoid Receptor Metabolic Disease Cancer
    JD-5037 is a potent CB1R antagonist with an IC50 of 1.5 nM.
  • HY-107734
    L 152804

    Neuropeptide Y Receptor Metabolic Disease Endocrinology
    L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.
  • HY-P3137
    TRV056

    Angiotensin Receptor Cardiovascular Disease
    TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists.
  • HY-P3136
    TRV055

    Angiotensin Receptor Cardiovascular Disease
    TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.
  • HY-13291
    WIN 55,212-2 Mesylate

    (R)-(+)-WIN 55212

    Cannabinoid Receptor Neurological Disease
    WIN 55,212-2 Mesylate is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.
  • HY-P2546
    Biotin-Substance P

    Neurokinin Receptor Neurological Disease
    Biotin-Substance P is the biotin tagged Substance P. Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
  • HY-N2566
    Euscaphic acid

    DNA/RNA Synthesis PI3K Apoptosis Cancer
    Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.
  • HY-100274
    Adenosine antagonist-1

    Adenosine Receptor Neurological Disease
    Adenosine antagonist-1 is an adenosine A3 receptor (AA3R) antagonist.
  • HY-N6629
    3'-Methoxyflavonol

    Others Neurological Disease
    3'-Methoxyflavonol is a selective agonist of neuromedin U 2 receptor (NMU2R).
  • HY-19670
    Befetupitant

    Ro67-5930

    Neurokinin Receptor Neurological Disease Endocrinology
    Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.
  • HY-13796
    IPSU

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
  • HY-14432
    Pavinetant

    MLE-4901; AZD2624; AZD4901

    Neurokinin Receptor Neurological Disease Endocrinology
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
  • HY-115682
    (S)-ZINC-3573

    Others Others
    (S)-ZINC-3573, an inactive enantiomer of ZINC-3573, is a negative control for (R)-ZINC-3573. (R)-ZINC-3573 is a selective MRGPRX2 agonist. (S)-ZINC-3573 displays no activity at MRGPRX2 at concentrations below 100 μM.
  • HY-135279
    CFTR corrector 4

    CFTR Inflammation/Immunology
    CFTR corrector 4 (Compound 13), an active (R,R)-form enantiomer, is a highly potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 4 can increase CFTR levels at the cell surface and have the potential for treatment of cystic fibrosis.
  • HY-116790A
    (+)-Penbutolol

    (R)-Penbutolol; (+)-Isopenbutolol

    Adrenergic Receptor Metabolic Disease Endocrinology
    (+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM. (+)-Penbutolol is an optical isomer of l-penbutolol with Na + channel-blocking action.
  • HY-Y0378
    D-Leucine

    (R)-Leucine

    Endogenous Metabolite Neurological Disease
    D-Leucine is a more potent anti-seizure agent than L-leucine. D-leucine potently terminates seizures even after the onset of seizure activity. D-leucine, but not L-leucine, reduces long-term potentiation but had no effect on basal synaptic transmission in vitro.
  • HY-N0596
    Panaxadiol

    20(R)-Panaxadiol

    Others Cancer
    Panaxadiol is a novel antitumor agent extracted from the Chinese medical herb Panax ginseng.
  • HY-12694
    Prucalopride succinate

    R-108512

    5-HT Receptor Others
    Prucalopride succinate is a selective, high affinity 5-HT4 receptor agonist with pKi of 8.6/8.1 for 5-HT4a/4b.
  • HY-100805
    D-Glutamic acid

    (R)-Glutamic acid

    Endogenous Metabolite Neurological Disease
    D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods.
  • HY-14789
    (R)-Elagolix

    NBI-56418

    GnRH Receptor Cancer Endocrinology
    Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
  • HY-16749
    Pexidartinib

    PLX-3397

    c-Fms c-Kit Apoptosis Cancer
    Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity.
  • HY-B1658A
    Frovatriptan succinate hydrate

    (R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate

    5-HT Receptor Neurological Disease
    Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research.
  • HY-B1658B
    Frovatriptan succinate

    (R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate

    5-HT Receptor Neurological Disease
    Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research.
  • 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-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-19632
    Fezolinetant

    ESN-364

    Neurokinin Receptor Endocrinology
    Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
  • HY-130798
    (S,R,S)-AHPC-amido-C5-acid

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-amido-C5-acid incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design XY028-133 (HY-129180).
  • HY-119104
    AZD1940

    Cannabinoid Receptor Neurological Disease
    AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action.
  • HY-109043A
    Solriamfetol hydrochloride

    JZP-110 hydrochloride; ADX-N05 hydrochloride; R228060 hydrochloride

    Dopamine Receptor Neurological Disease
    Solriamfetol hydrochloride (JZP-110 hydrochloride) is an orally active and selective dopamine and norepinephrine reuptake inhibitor with IC50s of 2.9 μM and 4.4 μM for dopamine and norepinephrine transporters, respectively. Solriamfetol hydrochloride has robust wake-promoting effects.
  • HY-109043
    Solriamfetol

    JZP-110; ADX-N05; R228060

    Dopamine Receptor Neurological Disease
    Solriamfetol (JZP-110) is an orally active and selective dopamine and norepinephrine reuptake inhibitor with IC50s of 2.9 μM and 4.4 μM for dopamine and norepinephrine transporters, respectively. Solriamfetol has robust wake-promoting effects.
  • HY-129997
    Luteolinidin chloride

    Others Inflammation/Immunology
    Luteolinidin is a natural deoxyanthocyanidin, isolated from mosses and ferns. Luteolinidin is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.
  • HY-112140
    JH-VIII-157-02

    ALK Cancer
    JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.
  • HY-15734
    AGI-6780

    Isocitrate Dehydrogenase (IDH) Cancer
    AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2 R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2 WT with IC50 of 190±8.1 nM.
  • HY-12686
    5Z-7-Oxozeaenol

    FR148083; L783279; LL-Z 1640-2

    MAP3K VEGFR Antibiotic Infection Inflammation/Immunology
    5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
  • HY-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase MicroRNA Infection Inflammation/Immunology Neurological Disease
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway.Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM .
  • HY-13106
    Olodanrigan

    EMA401; PD-126055

    Angiotensin Receptor Neurological Disease Endocrinology
    Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
  • HY-W009724
    2-Aminoethyl diphenylborinate

    2-APB

    Calcium Channel TRP Channel Infection
    2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca 2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
  • HY-100308
    SB-568849

    MCHR1 (GPR24) Metabolic Disease Endocrinology
    SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.
  • HY-128860
    Mutated EGFR-IN-2

    EGFR Cancer
    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=<1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
  • HY-P1531
    γ-1-Melanocyte Stimulating Hormone (MSH), amide

    Melanocortin Receptor Metabolic Disease Endocrinology
    γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. γ-1-Melanocyte Stimulating Hormone (MSH) regulates sodium (Na +) balance and blood pressure through activation of the melanocortin receptor 3 (MC3-R).
  • HY-14813
    Cutamesine

    SA4503; AGY 94806

    Sigma Receptor Neurological Disease
    Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
  • HY-114153
    PLX5622

    c-Fms Neurological Disease
    PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals.
  • HY-17457
    Levalbuterol tartrate

    Levosalbutamol tartrate

    Adrenergic Receptor Neurological Disease Endocrinology
    Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol.
  • HY-16756
    Toreforant

    JNJ-38518168

    Histamine Receptor Neurological Disease Endocrinology
    Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM.
  • HY-125845A
    (S,S,S)-AHPC hydrochloride

    (S,S,S)-VH032-NH2 hydrochloride

    Ligand for E3 Ligase Cancer
    (S,S,S)-AHPC hydrochloride is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC (Compound 27) is a ligand used as a negative control for (S,R,S)-AHPC. (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein.
  • HY-P9923
    Benralizumab

    MEDI-563; BIW-8405

    Interleukin Related Inflammation/Immunology
    Benralizumab (MEDI-563) is an interleukin-5 receptor α (IL-5Rα)-directed cytolytic monoclonal antibody that induces direct, rapid and nearly complete depletion of eosinophils via enhanced antibody-dependent cell-mediated cytotoxicity. Benralizumab can be used for severe eosinophilic asthma.
  • HY-134189A
    EST73502 hydrochloride

    Sigma Receptor Opioid Receptor Neurological Disease
    EST73502 hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity.
  • HY-129657
    GLP-1 receptor agonist 4

    Glucagon Receptor Metabolic Disease
    GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist extracted from patent WO2009111700A2, compound 87, has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.
  • HY-P1858
    Urocortin III, mouse

    CRFR Neurological Disease Cardiovascular Disease Endocrinology
    Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2. Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics.
  • HY-134189
    EST73502

    Opioid Receptor Sigma Receptor Neurological Disease
    EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.
  • HY-15729
    Rociletinib

    CO-1686; AVL-301; CNX-419

    EGFR Cancer
    Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
  • HY-112950
    RET-IN-1

    RET Cancer
    RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .
  • HY-15295
    Vonoprazan Fumarate

    TAK-438

    Proton Pump Metabolic Disease
    Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
  • HY-U00433
    JMV 2959

    GHSR Neurological Disease Endocrinology
    JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
  • HY-100007
    Vonoprazan

    TAK-438 free base

    Proton Pump Endocrinology
    Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
  • HY-133552
    RORγt Inverse agonist 10

    ROR Inflammation/Immunology
    RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
  • HY-P1858A
    Urocortin III, mouse TFA

    CRFR Neurological Disease Cardiovascular Disease Endocrinology
    Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2. Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics.
  • HY-114153A
    PLX5622 hemifumarate

    c-Fms Neurological Disease
    PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals.
  • HY-103061
    Dehydro-ZINC39395747

    Others Cardiovascular Disease
    Dehydro-ZINC39395747 is a derivative of ZINC39395747. ZINC39395747 is a potent cytochrome b5 reductase 3 (CYB5R3) inhibitor with an IC50 of 9.14 μM and a Kd of 1.11 μM. ZINC39395747 can increase NO bioavailability in vascular cells.
  • HY-42068
    (-)-Aspartic acid

    (R)-Aspartic acid; D-(-)-Aspartic acid

    Endogenous Metabolite iGluR Neurological Disease
    (-)-Aspartic acid is an endogenous NMDA receptor agonist.
  • HY-13740
    Resiquimod

    R848; S28463

    Toll-like Receptor (TLR) HCV Inflammation/Immunology Cancer
    Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α.
  • HY-N0507
    Rosavin

    Others Neurological Disease
    Rosavin is isolated from R. rosea, Rosavin shows antidepressant-like, adaptogenic, anxiolytic-like effects in mice model.
  • HY-15243
    Capromorelin Tartrate

    CP 424391-18

    GHSR Neurological Disease Endocrinology
    Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
  • HY-131945
    CU-115

    Toll-like Receptor (TLR) Inflammation/Immunology
    CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.
  • HY-15729A
    Rociletinib hydrobromide

    CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide

    EGFR Cancer
    Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
  • HY-13406
    TAK-779

    Takeda 779

    CCR HIV CXCR Infection Inflammation/Immunology Endocrinology
    TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
  • HY-112823
    Almonertinib

    HS-10296

    EGFR Cancer
    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
  • HY-112823B
    Almonertinib hydrochloride

    HS-10296 hydrochloride

    EGFR Cancer
    Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer.
  • HY-128579
    DW14800

    Histone Methyltransferase Cancer
    DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
  • HY-18750
    Zorifertinib

    AZD3759

    EGFR Cancer
    Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively.
  • HY-B0244
    Praziquantel

    Parasite Antibiotic Infection
    Praziquantel is a racemic mixture, which is composed of (R)-Praziquantel and (S)- Praziquantel. Praziquantel is safe and has been used for the research of schistosomiasis.
  • HY-114194
    CCR1 antagonist 7

    CCR Inflammation/Immunology Endocrinology
    CCR1 antagonist 7 (compound 16r) is a chemokine receptor 1 (CCR1) antagonist, with an IC50 of 4 nM.
  • HY-141016
    (S,R,S)-AHPC-PEG2-acid

    PROTAC Linker Cancer
    (S,R,S)-AHPC-PEG2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-N2084
    Perillartine

    DL-Perillartine

    Endogenous Metabolite Others
    Perillartine is a sweetener, which activates the taste receptor type 1 member 2 (Tas1r2) subunit in a species-dependent manner.
  • HY-135884
    PKR activator 2

    Pyruvate Kinase Cardiovascular Disease
    PKR activator 2 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035863A1, compound 385.
  • HY-13011
    Alectinib

    CH5424802; RO5424802; AF802

    ALK Cancer
    Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.
  • HY-90005S
    Etravirine D4

    TMC-125 D4; R-165335 D4

    Reverse Transcriptase HIV Infection
    Etravirine D4 (TMC-125 D4) is the deuterium labeled Etravirine. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
  • HY-119944
    JND3229

    EGFR Cancer
    JND3229 is a highly potent and fourth-generation EGFR C797S reversible inhibitor with IC50 value of 5.8 nM, and also potently suppressed EGFR L858R/T790M and EGFR WT with IC50 values of 30.5 and 6.8 nM.
  • HY-15748
    JNJ-40411813

    ADX-71149

    mGluR Neurological Disease
    JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM.
  • HY-17004
    Olmesartan

    RNH-6270

    Angiotensin Receptor Cardiovascular Disease
    Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
  • HY-14887
    Fedovapagon

    Vasopressin Receptor Metabolic Disease
    Fedovapagon is a selective vasopressin V2 receptor (V2R) agonist with an EC50 of 24 nM, which is being developed for the treatment of nocturia.
  • HY-13508
    JNJ-7777120

    Histamine Receptor Inflammation/Immunology Endocrinology
    JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits >1000-fold selectivity over the other histamin receptors.
  • 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-12405
    CGP-42112

    CGP42112A

    Angiotensin Receptor Neurological Disease Endocrinology
    CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.
  • HY-15452A
    Selisistat S-enantiomer

    EX-527 (S-enantiomer)

    Sirtuin Cancer
    Selisistat S-enantiomer (EX-527 S-enantiomer) is the S-enantiomer of Selisistat, with an IC50 of 123 nM for SIRT1. Selisistat S-enantiomer is much more potent than Selisistat R-enantiomer.
  • HY-136390
    ML417

    Dopamine Receptor Neurological Disease
    ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.
  • HY-125821
    Sigma-1 receptor antagonist 1

    Sigma Receptor Neurological Disease
    Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain.
  • HY-135805A
    (Rac)-JBJ-04-125-02

    EGFR Cancer
    (Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M.
  • HY-114370
    Selpercatinib

    LOXO-292

    RET Cancer
    Selpercatinib (LOXO-292) is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 163, has an IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively. Antineoplastic activity.
  • HY-130613
    MAC-545496

    Bacterial Infection
    MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA).
  • HY-18213
    EGFR-IN-9

    EGFR Cancer
    EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.
  • HY-14258
    Escitalopram

    (S)-Citalopram; (S)-(+)-Citalopram

    Serotonin Transporter Neurological Disease
    Escitalopram ((S)-Citalopram), the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram is an antidepressant for the research of major depression.
  • HY-16900
    Rolipram

    (R,S)-Rolipram; SB 95952; ZK 62711

    Phosphodiesterase (PDE) Bacterial HIV Neurological Disease Cancer
    Rolipram is a selective phosphodiesterases PDE4 inhibitor with IC50s of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.
  • HY-135883
    PKR activator 1

    Pyruvate Kinase Cardiovascular Disease
    PKR activator 1 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035865A1, compound E7-93.
  • HY-118930
    MK-0493

    Melanocortin Receptor Endocrinology Metabolic Disease
    MK-0493 is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake.
  • HY-128934
    Antitumor agent-2

    Others Cancer Inflammation/Immunology
    Antitumor agent-2 is sourced from patent CN102250203, compound 6a-r, has antitumor action and anti-inflammatory action.
  • HY-131277
    Dehydro Olmesartan

    Angiotensin Receptor Cardiovascular Disease
    Dehydro Olmesartan is a derivative of Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist and has the potential for high blood pressure study.
  • HY-P1208
    PG-931

    Melanocortin Receptor Inflammation/Immunology
    PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
  • HY-13011A
    Alectinib Hydrochloride

    CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride

    ALK Cancer
    Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.
  • HY-117273
    AZ304

    Raf Autophagy Cancer
    AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity.
  • HY-107661
    Arundic Acid

    ONO-2506; (R)-2-Propyloctanoic acid

    Others Neurological Disease
    Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid has the potential for stroke and Alzheimer’s disease research.
  • HY-B1173
    (+)-Camphor

    D-(+)-Camphor; (1R)-(+)-Camphor

    Bacterial Others
    (+)-Camphor is an ingredient in cooking, and as an embalming fluid for medicinal purposes,
  • HY-101042
    AG-494

    Tyrphostin AG 494

    EGFR CDK Cancer
    AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis.
  • HY-131003
    Taletrectinib

    DS-6051b; AB-106

    ROS Cancer
    Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
  • HY-10847B
    SB-277011 hydrochloride

    SB-277011A hydrochloride

    Dopamine Receptor 5-HT Receptor Neurological Disease
    SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
  • HY-128778
    DBPR112

    EGFR Cancer
    DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy.
  • HY-129946
    Dopamine D2 receptor antagonist-1

    Dopamine Receptor Neurological Disease
    Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity.
  • HY-U00433A
    JMV 2959 hydrochloride

    GHSR Neurological Disease Endocrinology
    JMV 2959 hydrochloride is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32±3 nM in LLC-PK1 cells.
  • HY-131274
    Fexofenadine Impurity F

    Others Others
    Fexofenadine Impurity F is the impurity of Fexofenadine. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial.
  • HY-12195
    ABT-239

    Histamine Receptor TRP Channel Neurological Disease Endocrinology
    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist. 
  • HY-P1208A
    PG-931 TFA

    Melanocortin Receptor Inflammation/Immunology
    PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R(IC50=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
  • HY-15971A
    AMD 3465

    GENZ-644494

    CXCR HIV Infection Endocrinology
    AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-110123
    ML-00253764 hydrochloride

    Melanocortin Receptor Cancer Endocrinology
    ML-00253764 is a nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki and IC50 of 0.16 µM and 0.103 µM, respectively. Brain penetrant.
  • HY-131276
    Olmesartan lactone impurity

    Angiotensin Receptor Cardiovascular Disease
    Olmesartan lactone impurity is a cyclic ester impurity of Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist and has the potential for high blood pressure study.
  • HY-112801
    F-1

    ALK ROS Cancer
    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively.
  • HY-129492
    GNF4877

    DYRK GSK-3 Metabolic Disease
    GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells).
  • HY-14258A
    Escitalopram oxalate

    (S)-Citalopram oxalate; (S)-(+)-Citalopram oxalate

    Serotonin Transporter Neurological Disease
    Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression.
  • HY-B0847
    Propiconazole

    Fungal Reactive Oxygen Species Infection
    Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS).
  • HY-131003A
    Taletrectinib free base

    DS-6051b free base; AB-106 free base

    ROS Cancer
    Taletrectinib (DS-6051b) free base is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
  • HY-15971
    AMD 3465 hexahydrobromide

    GENZ-644494 hexahydrobromide

    CXCR HIV Infection Endocrinology
    AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-B0801A
    Fexofenadine hydrochloride

    MDL-16455 hydrochloride; Terfenadine carboxylate hydrochloride

    Histamine Receptor Inflammation/Immunology Endocrinology
    Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years).
  • HY-U00333
    α1 adrenoceptor-MO-1

    Adrenergic Receptor Neurological Disease Endocrinology
    α1 adrenoceptor-MO-1, an S enantiomer, has affinity at alpha 1 adrenergic receptor, shows alphalytic activity, and possesses analgesic action; more active than R enantiomer.
  • HY-P0201
    Substance P

    Neurokinin P

    Neurokinin Receptor Endogenous Metabolite Neurological Disease Endocrinology
    Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
  • HY-17004S
    Olmesartan D4

    RNH-6270 D4

    Angiotensin Receptor Others
    Olmesartan D4 (RNH-6270 D4) is the deuterium labeled Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
  • HY-133775
    Olmesartan impurity

    Angiotensin Receptor Metabolic Disease
    Olmesartan impurity is an Olmesartan impurity. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist has the potential for high blood pressure study.
  • HY-131279
    Olmesartan ethyl ester

    Others Others
    Olmesartan ethyl ester (compound 11) is an Olmesartan impurity. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to in the high blood pressure study.
  • 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-P2141
    TRV-120027

    Angiotensin Receptor Cardiovascular Disease
    TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-P2141A
    TRV-120027 TFA

    Angiotensin Receptor Cardiovascular Disease
    TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-100360
    MS049

    Histone Methyltransferase Cancer
    MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and do not affect the growth of HEK293 cells.
  • HY-100360A
    MS049 dihydrochloride

    Histone Methyltransferase Cancer
    MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and do not affect the growth of HEK293 cells.
  • HY-108618
    BC11-38

    Phosphodiesterase (PDE) Endocrinology
    BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells.
  • HY-B0596
    Taltirelin

    TA-0910

    Thyroid Hormone Receptor Neurological Disease Endocrinology
    Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
  • HY-15393
    VU 0357121

    mGluR Neurological Disease
    VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.
  • HY-125789
    PF-04753299

    Bacterial Infection
    PF-04753299 is a potent and selective UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) inhibitor. PF-04753299 is bactericidal for the gonococcal isolates. PF-04753299 inhibits E. coli, P. aeruginosa and K. pneumoniae strains with MIC90 values of 2 μg/ml, 4 μg/ml and 16 μg/ml, respectively. PF-04753299 is used for the study of gram-negative bacteria infection.
  • HY-P0165
    Taspoglutide

    ITM077; R1583; BIM51077

    Glucagon Receptor Metabolic Disease
    Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC50 value of 0.06 nM.
  • HY-B0596A
    Taltirelin acetate

    TA-0910 acetate

    Thyroid Hormone Receptor Neurological Disease Endocrinology
    Taltirelin acetate (TA-0910 acetate) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
  • HY-10622
    PF-00446687

    Melanocortin Receptor Endocrinology
    PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. Pf-446687 is brain penetrant.
  • HY-12461
    WS6

    Others Inflammation/Immunology
    WS6 is a novel small molecule that promotes β cell proliferation in rodent and human primary islets with EC50 of 0.28 uM(R7T1 cell viability).
  • HY-135953
    CDDO-3P-Im

    Apoptosis Cancer
    CDDO-3P-Im is an analogue of CDDO-Imidazolide with chemopreventive effect. CDDO-3P-Im can reduce the size and the severity of the lung tumors in mouse lung cancer model. CDDO-3P-Im is a orally active necroptosis inhibitor that can be used for the research of ischemia/reperfusion (I/R).
  • HY-10200
    BMS-754807

    IGF-1R Insulin Receptor Cancer Endocrinology
    BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively.
  • HY-128720
    Diethyl oxalpropionate

    Endogenous Metabolite Metabolic Disease
    Diethyl oxalpropionate is an intermediate for poly((R,S)-3,3-dimethylmalic acid) (PDMMLA) derivative synthesis. PDMMLA derivative can be used in synthesis of nanoparticles and study of warfarin encapsulation and controlled release.
  • HY-100657
    meta-Fexofenadine

    meta-MDL-16455; meta-Terfenadine carboxylate

    Others Inflammation/Immunology
    meta-Fexofenadine (meta-MDL-16455) is an impurity of Fexofenadine. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial.
  • HY-12707
    Piribedil

    Adrenergic Receptor Dopamine Receptor Neurological Disease Endocrinology
    Piribedil is a dopamine D2 receptor (D2R) agonist which also displays antagonist property at 1A-adrenoceptor (1A-AR).
  • HY-124733A
    LIT-001

    Oxytocin Receptor Neurological Disease
    LIT-001 is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 improves social interaction in a mouse model of autism.
  • HY-P0049
    Argipressin

    Vasopressin; Arg8-vasopressin; AVP

    Vasopressin Receptor Neurological Disease
    Argipressin binds to the V1, V2, V3-vascular arginine vasopressin receptor, with a Kd value of 1.31 nM in A7r5 rat aortic smooth muscle cells for V1.
  • HY-N3199
    Neorauflavene

    Bacterial Infection
    Neorauflavene is a phenolic neorautanenia isoflavanoid isolated from Neorautanenia edulis. Neorauflavene shows antibacterial activities against E. faecalis, S. suis, S. agalactiae, P. aeruginosa, B. subtilis, and R. anatipestifer.
  • HY-19834
    Fenebrutinib

    GDC-0853

    Btk Cancer
    Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.
  • HY-130616
    EGFR-IN-11

    EGFR Apoptosis Cancer
    EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.
  • HY-P2161
    TAK-683

    Others Cancer
    TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
  • HY-116474
    Viridicatol

    Fungal Infection
    Viridicatol, a quinolinone alkaloid, is isolated from the fermentation of an endophytic fungus Penicillium sp. R22 in Nerium indicum. Viridicatol has strong antifungal activity against Staphylococcus aureus with MIC value of 15.6 μg/mL.
  • HY-50760
    L-692585

    GHSR Endocrinology
    L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release.
  • HY-W016087
    Monoethyl pimelate

    PROTAC Linker 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-138072
    EMI1

    EGFR Cancer
    EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC).
  • HY-N1353
    Rhamnocitrin

    Others Inflammation/Immunology Cardiovascular Disease
    Rhamnocitrin is a flavonoid isolated from astragalus complanatus R. Br. (Sha-yuan-zi). Rhamnocitrin is a scavenger of DPPH with an IC50 of 28.38 mM. Rhamnocitrin has anti-oxidant, anti-inflammatory and an-tiatherosclerosis activity.
  • HY-17499
    EGFR-IN-12

    EGFR Apoptosis Cancer
    EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.
  • HY-19654B
    (-)-GSK598809

    1S,5R-GSK598809

    Dopamine Receptor Others
    (-)-GSK598809 is an isomer of GSK598809. GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist.
  • HY-B1950
    Quizalofop-p-ethyl

    (R)-Quizalofop ethyl; Quinofop-ethyl

    Others Others
    Quizalofop-P-ethyl is a slightly toxic, selective, postemergence phenoxy herbicide, used to control annual and perennial grass weeds in potatoes, soybeans, sugar beets, peanuts vegetables, cotton and flax.
  • HY-N1459
    Campesterol

    (24R)-5-Ergosten-3β-ol

    Endogenous Metabolite Cancer
    Campesterol is a plant sterol with cholesterol lowering and anticarcinogenic effects.
  • HY-Y0152
    Cinchonine

    (8R,9S)-Cinchonine; LA40221

    Apoptosis Parasite Cancer
    Cinchonine is a natural compound present in Cinchona bark. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
  • HY-12772S
    Hydroxy Itraconazole D8

    R-63373 D8

    Fungal Others
    Hydroxy Itraconazole D8 is the deuterium labeled Hydroxy Itraconazole. Hydroxy Itraconazole is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.
  • HY-32343
    Secalciferol

    (24R)-24,25-Dihydroxyvitamin D3

    VD/VDR Endogenous Metabolite Inflammation/Immunology
    Secalciferol is a metabolite of Vitamin D, a possibly anti-inflammatory steroid which is involved in bone ossification.
  • HY-12597
    Quisqualic acid

    L-Quisqualic acid

    iGluR mGluR Neurological Disease
    Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and mGluR) of excitatory amino acid (EAA) agonist with an EC50 of 45 nM and a Ki of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis chinensis.
  • HY-11083
    GW-803430

    GW-3430

    MCHR1 (GPR24) Metabolic Disease
    GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3. GW-803430 is orally active in an animal model of obesity.
  • HY-P0122
    iRGD peptide

    c(CRGDKGPDC)

    Integrin Cancer
    iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
  • HY-N6972
    Cepharanthine

    HIV Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Cepharanthine is an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities. Cepharanthine attenuates muscle and kidney injuries induced by limb ischemia/reperfusion (I/R). Cepharanthine induces autophagy, apoptosis and cell cycle arrest in breast cancer cells. Cepharanthine inhibits the HIV-1 entry process by reducing plasma membrane fluidity.
  • HY-124733
    LIT-001 free base

    Oxytocin Receptor Neurological Disease
    LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 free base improves social interaction in a mouse model of autism.
  • HY-125819
    Sigma-1 receptor antagonist 2

    Sigma Receptor Neurological Disease
    Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (σ1 R) antagonist with Kis of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively.
  • HY-14886
    Fasitibant chloride

    MEN16132 free base

    Bradykinin Receptor Neurological Disease Cardiovascular Disease
    Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model.
  • HY-44234A
    Fmoc-Gly-Gly-D-Phe-OtBu

    ADC Linker Cancer
    Fmoc-Gly-Gly-D-Phe-OtBu is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Gly-Gly-D-Phe-OtBu is the R-isomer of Fmoc-Gly-Gly-Phe-OtBu (HY-44234).
  • HY-B2078A
    Eprazinone dihydrochloride

    Neurokinin Receptor Inflammation/Immunology
    Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen.
  • HY-135887
    ZX-29

    ALK Apoptosis Autophagy Cancer
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
  • HY-136057
    iFSP1

    Ferroptosis Cancer
    iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A).
  • HY-124828
    CMLD-2

    Apoptosis Cancer
    CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation.
  • HY-B0850
    Difenoconazole

    Fungal Infection
    Difenoconazole is a broad-spectrum triazole fungicide that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Difenoconazole inhibits the growth of F. graminearum isolates in vitro (EC50s=1.69-19.6 mg/L for mycelial growth). Difenoconazole also inhibits growth of A. sonali, F. fulva, B. cinerea, and R. solani (EC50s=0.131, 0.069, 0.297, and 0.252 mg/L, respectively).
  • HY-103693
    NAZ2329

    Phosphatase Cancer
    NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.
  • HY-P0252
    α-Melanocyte-Stimulating Hormone (MSH), amide

    Melanocortin Receptor Metabolic Disease
    α-Melanocyte-Stimulating Hormone (MSH), amide is an endogenous neuropeptide, with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC), acts as an endogenous melanocortin receptor 4 (MC4R) agonist.
  • HY-130248
    BAY-899

    Others Endocrinology
    BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels.
  • HY-112653A
    (±)8-HETE

    Endogenous Metabolite Metabolic Disease
    (±)8-HETE is one of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of Arachidonic acid (HY-109590). The biological activity of (±)8-HETE is likely to resemble that of its constituent enantiomers (8(R)-HETE and 8(S)-HETE).
  • HY-P1074
    SNX-482

    Calcium Channel Neurological Disease
    SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, high affinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect.
  • HY-I1060
    L-Alloisoleucine

    (3R)-LS-Isoleucine; L-Allo-isoleucine

    Endogenous Metabolite Others
    L-Alloisoleucine is a branched chain amino acid and is a stereo-isomer of L-isoleucine. L-Alloisoleucine is a common constituent of human plasma (albeit at low levels).
  • HY-19815
    Olafertinib

    EGFR Cancer
    Olafertinib is a third-generation EGFR TKI, with GI50 values of 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19) and 689 nM (EGFR WT), respectively. Olafertinib has the potential for NSCLC research.
  • HY-131905S
    BMS-986144

    HCV Protease HCV Cancer Infection Inflammation/Immunology
    BMS-986144 is a third-generation, pan-genotype (GT) NS3/4A protease inhibitor. BMS-986144 inhibits HCV replicon with EC50s of 2.3, 0.7, 1.0, 12, 8.0, and 5.8 nM for GT-1a, GT-1b, GT-2a, GT-3a, 1a R155X, and 1b D168V, respectively. BMS-986144 has the potential for the research of HCV infection.
  • HY-109086
    Edicotinib

    JNJ-40346527; JNJ-527

    c-Fms Inflammation/Immunology Neurological Disease
    Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research.
  • HY-128856
    P7C3-OMe

    Others Neurological Disease
    P7C3-OMe is a pro-neurogenic compound, has therapeutic benefits in neuropsychiatric and/or neurodegenerative disease. The R-enantiomer of P7C3-OMe is far more active than the S-enantiomer.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
  • HY-W033577
    Tricarbonyldichlororuthenium(II) dimer

    CORM-2

    Others Inflammation/Immunology
    Tricarbonyldichlororuthenium(II) dimer is a pharmacological donor of CO releasing. CO releases from Tricarbonyldichlororuthenium(II) dimer prevents gastric mucosal oxidative damage induced by ischemia/reperfusion (I/R) improving gastric blood flow (GBF), decreasing DNA oxidation and inflammatory response on systemic level.
  • HY-12752
    Alimemazine

    Trimeprazine

    Others Inflammation/Immunology Neurological Disease
    Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays sedative, antiserotonin, antispasmodic, and antiemetic properties.
  • HY-15730
    Poziotinib

    HM781-36B; NOV120101

    EGFR Apoptosis Cancer
    Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR wt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR T790M and EGFR L858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity.
  • HY-13238
    Dolutegravir

    S/GSK1349572

    HIV Integrase HIV Infection
    Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
  • HY-130249
    BAY-298

    Others Endocrinology
    BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels.
  • HY-123921
    Gefitinib-based PROTAC 3

    PROTAC EGFR Cancer
    Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.
  • HY-125773
    β-cyano-L-Alanine

    Beta-cyano-l-alanine

    Others Neurological Disease
    β-cyano-L-Alanine (Beta-cyano-l-alanine), a nitrile of widespread occurrence in higher plants, is enzymatically produced by cyanoalanine synthase from cyanide and cysteine as substrates. β-cyano-L-Alanine abolishes the protective effect of ethanol on cerebral ischemia/reperfusion (I/R) injury.
  • HY-B0927
    Hydrastine

    (-)-β-Hydrastine; (1R,9S)-β-Hydrastine

    Others Others
    Hydrastine is a natural alkaloid which is present in Hydrastis canadensis and other plants of the ranunculaceae family.
  • HY-107608
    Leukotriene B4

    LTB4; 5(S),12(R)-DiHETE

    PROTAC Linker Endogenous Metabolite Leukotriene Receptor Cancer Inflammation/Immunology
    Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-101588
    Gefapixant

    MK-7264; AF-219

    P2X Receptor Inflammation/Immunology
    Gefapixant (MK-7264) is an orally active P2X3 receptor (P2X3R) antagonist with IC 50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
  • HY-108669
    AZ10606120 dihydrochloride

    P2X Receptor Cancer Neurological Disease
    AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth.
  • HY-100452
    TCS-OX2-29

    Orexin Receptor (OX Receptor) Cancer Endocrinology
    TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1.
  • HY-13238A
    Dolutegravir sodium

    S/GSK1349572 sodium

    HIV Integrase HIV Infection
    Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
  • HY-14151
    Prucalopride

    5-HT Receptor Neurological Disease
    Prucalopride (R093877) is a drug acting as a selective, high affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); >150-fold higher affinity for 5-HT4 receptors than for other receptors.
  • HY-N7539
    Cognac oil

    Others Metabolic Disease
    Cognac oil, mainly found in wine lees, has unique fatty acid profiles, including Palmitic acid (59.26%), Linoleic acid (11.92%), Myristic acid (8.97%), Oleic acid (8.3%) and other fatty acids. Cognac oil leads to a general increase in the permeation of R6G (Rhodamine 6G) across all the membranes.
  • HY-N2273
    Gymnestrogenin

    LXR Metabolic Disease
    Gymnestrogenin is a pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br. Gymnestrogenin is a LXR antagonist with IC50s of 2.5 and 1.4 μM for LXRα and LXRβ transactivation, respectively. Gymnestrogenin reduces the transcriptional activity of LXR even on its own promoter, thus reducing the mRNA expression.
  • HY-111759
    Jaspamycin

    7-CN-7-C-Ino

    PKA Parasite Infection
    Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity.
  • HY-18137
    PF-04995274

    5-HT Receptor Neurological Disease
    PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
  • HY-12545
    Brevetoxin-3

    PbTx-3

    Sodium Channel Inflammation/Immunology
    Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
  • HY-N0408
    Picroside II

    NF-κB Reactive Oxygen Species Apoptosis Influenza Virus Cancer Infection Inflammation/Immunology Neurological Disease
    Picroside II, an iridoid compound extracted from Picrorhiza, exhibits anti-inflammatory and anti-apoptotic activities. picroside II alleviates the inflammatory response in sepsis and enhances immune function by inhibiting the activation of NLRP3 inflammasome and NF-κB pathways. Picroside II is an antioxidant, exhibits a significant neuroprotective effect through reducing ROS production and protects the blood-brain barrier (BBB) after cerebral ischemia-reperfusion (CI/R) injury. Picroside II has antioxidant, anti-inflammatory, immune regulatory, anti-virus and other pharmacological activities.
  • HY-125959
    Ucf-101

    Apoptosis Neurological Disease Cardiovascular Disease
    Ucf-101 is a selctive and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC50>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect.
  • HY-41700
    D-Alanine

    (R)-Alanine; Ba 2776; D-α-Alanine

    Endogenous Metabolite Others
    D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
  • HY-15514A
    Merestinib dihydrochloride

    LY2801653 dihydrochloride

    c-Met/HGFR FLT3 ROS Discoidin Domain Receptor Cancer
    Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).
  • HY-15514
    Merestinib

    LY2801653

    c-Met/HGFR FLT3 ROS Discoidin Domain Receptor Cancer
    Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).
  • 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-101522
    CHMFL-EGFR-202

    EGFR BMX Kinase Btk MEK Cancer
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
  • 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-101034
    CHMFL-ABL/KIT-155

    CHMFL-ABL-KIT-155

    Bcr-Abl c-Kit Apoptosis Cancer
    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.
  • HY-103369
    PG01

    CFTR Endocrinology
    PG01 is a potent CFTR Cl - channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl - current after adding Forskolin.
  • HY-101198
    Clobenpropit dihydrobromide

    Histamine Receptor Apoptosis Cancer Neurological Disease
    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
  • HY-137471
    RBPJ Inhibitor-1

    RIN1

    Notch Cancer
    RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
  • HY-131344
    mTOR inhibitor-8

    mTOR Autophagy Cancer
    mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.
  • HY-136123
    Tubulin inhibitor 8

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
  • HY-136122
    Tubulin inhibitor 7

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
  • HY-136121
    Tubulin inhibitor 6

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
  • HY-112851
    Diacylglycerol acyltransferase inhibitor-1

    Acyltransferase Metabolic Disease
    Diacylglycerol acyltransferase inhibitor-1 is a diacylglycerol acyltransferase (DGAT1) inhibitor.
  • HY-112812
    SCD1 inhibitor-1

    Stearoyl-CoA Desaturase (SCD) Cancer Metabolic Disease
    SCD1 inhibitor-1 is a potent and liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitor.
  • HY-18353
    mTOR inhibitor-3

    mTOR Cancer
    mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
  • HY-B0552A
    Dibucaine hydrochloride

    Cinchocaine hydrochloride

    Sodium Channel Neurological Disease
    Dibucaine hydrochloride (Cinchocaine hydrochloride) is a sodium channel inhibitor. Dibucaine hydrochloride is a potent SChE inhibitor.
  • HY-112911
    Endothelial lipase inhibitor-1

    Others Cardiovascular Disease
    Endothelial lipase inhibitor-1 is a potent endothelial lipase inhibitor with an IC50 of 49 nM.
  • HY-B0552
    Dibucaine

    Cinchocaine

    Sodium Channel Neurological Disease
    Dibucaine (Cinchocaine) is a sodium channel inhibitor. Dibucaine is a potent SChE inhibitor.
  • HY-112722
    Neurotoxin Inhibitor

    Others Neurological Disease
    Neurotoxin Inhibitor is a neurotoxin inhibitor.
  • HY-137497
    KRAS inhibitor-9

    Ras Apoptosis Cancer
    KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
  • 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-101275
    EMT inhibitor-1

    Hippo (MST) TGF-beta/Smad Wnt Cancer
    EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
  • HY-13278A
    IRAK inhibitor 4 trans

    IRAK Inflammation/Immunology
    IRAK inhibitor 4 (trans) is the trans form of IRAK inhibitor 4. IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor.
  • HY-111370
    mTOR inhibitor-2

    mTOR Cancer
    mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.
  • HY-119369
    FadD32 Inhibitor-1

    Bacterial Infection
    FadD32 Inhibitor-1 is a potent FadD32 inhibitor with anti-tubercular activity.
  • HY-111412
    DAAO inhibitor-1

    Others Neurological Disease
    DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor with an IC50 of 0.12 μM.
  • HY-21141
    Cysteine protease inhibitor-2

    Cathepsin Cancer
    Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
  • HY-17541A
    Cysteine Protease inhibitor hydrochloride

    Cathepsin Others
    Cysteine Protease inhibitor hydrochloride is an inhibitor of cysteine protease.
  • HY-17541
    Cysteine Protease inhibitor

    Cathepsin Others
    Cysteine Protease inhibitor is an inhibitor of cysteine protease.
  • HY-112914
    mTOR inhibitor-1

    mTOR Autophagy Cancer
    mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.
  • HY-70005
    CPA inhibitor

    Carboxypeptidase inhibitor

    Carboxypeptidase Metabolic Disease
    CPA inhibitor (Carboxypeptidase inhibitor; compound 5) is a potent carboxypeptidase A (CPA) inhibitor with a Ki of 0.32 μM.
  • HY-130260
    KRAS inhibitor-4

    Ras Cancer
    KRAS inhibitor-4 (compound F12) is a potent KRAS inhibitor and developed as anticancer agents.
  • HY-128703
    Bromodomain inhibitor-8

    Epigenetic Reader Domain Inflammation/Immunology
    Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases.
  • HY-10442
    3-Deazaneplanocin A

    DZNep; 3-Deazaneplanocin

    Histone Methyltransferase Cancer
    3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.
  • HY-138295
    KRAS inhibitor-10

    Ras Cancer
    KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.