1. Search Result

Search Result

Results for "29 nexentury slc24a5 Inhibitors" in MCE Product Catalog:

185

Inhibitors & Agonists

2

Biochemical Assay Reagents

23

Peptides

16

Natural
Products

1

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • 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-19931
    COH29

    RNR Inhibitor COH29

    DNA/RNA Synthesis Cancer
    COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
  • HY-122054
    BPK-29

    Others Cancer
    BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
  • HY-122054A
    BPK-29 hydrochloride

    Others Cancer
    BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
  • HY-136266
    HCV-IN-29

    HCV Cancer
    HCV-IN-29 is a hepatitis C virus (HCV) inhibitor exacted from patent US8329159B2, compound 1e.
  • HY-100461
    C29

    Toll-like Receptor (TLR) Inflammation/Immunology
    C29 is a Toll-like receptor 2 (TLR2) inhibitor. C29 blocks hTLR2/1 and hTLR2/6 signaling with IC50s of 19.7 and 37.6 μM, respectively.
  • HY-17537
    APY29

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-141027
    Bis-PEG29-acid

    PROTAC Linker Cancer
    Bis-PEG29-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-18977
    KML29

    MAGL Metabolic Disease
    KML29 is a potent and selective MAGL inhibitor with IC50 = 5.9, 15, and 43 nM in human, mouse, and rat brain proteomes, respectively.
  • HY-P1522
    β-Amyloid 29-40

    Amyloid beta-protein(29-40)

    Amyloid-β Neurological Disease
    β-Amyloid (29-40) is a fragment of Amyloid-β peptide.
  • HY-N1713
    29-Nor-20-oxolupeol

    Others Neurological Disease
    29-Nor-20-oxolupeol, extracted from Impatiens basamina, reduces NO levels in LPS-activated murine microglial cells with an IC50 of 44.21 µM.
  • HY-128592
    TAB29

    Others Cancer
    TAB29 is a potent inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) with an IC50 of 874 nM, possesses therapeutic potential for human cancers.
  • HY-P1601
    Neuropeptide Y(29-64)

    Neuropeptide Y Receptor Neurological Disease Endocrinology
    Neuropeptide Y(29-64) is a 36 amino acid peptide, a fragment of Neuropeptide Y.
  • HY-P0198
    Neuropeptide Y (29-64), amide, human

    Human neuropeptide Y (29-64)

    Neuropeptide Y Receptor Neurological Disease Endocrinology
    Neuropeptide Y (29-64), amide, human is a biologically active 36-amino acid peptide.
  • HY-P1490
    Bradykinin (2-9)

    Des-Arg1-bradykinin

    Bradykinin Receptor Cardiovascular Disease Endocrinology
    Bradykinin (2-9) is an amino-truncated Bradykinin peptide. Bradykinin (2-9) is a metabolite of Bradykinin, cleaved by Aminopeptidase P.
  • 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-N0357
    3,29-Dibenzoyl rarounitriol

    Others Others
    3,29-Dibenzoyl rarounitriol is one major bioactive compound of multiflorane triterpene esters Trichosanthes kirilowii, can be chosen as the marker for quantitation of Trichosanthes kirilowii.
  • 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-P1132
    Galanin (1-29)(rat, mouse)

    Neuropeptide Y Receptor Neurological Disease
    Galanin (1-29)(rat, mouse) is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3 respectively. Anticonvulsant effect.
  • HY-P0198A
    Neuropeptide Y (29-64), amide, human TFA

    Neuropeptide Y Receptor Neurological Disease Endocrinology
    Neuropeptide Y (29-64), amide, human (TFA) is involved in Alzheimer's disease (AD) and protects rat cortical neurons against β-Amyloid toxicity.
  • HY-126313
    BnOH-NH-bis-(C2-S)-propane-O-isoprene ester

    PROTAC Linker 29

    PROTAC Linker Cancer
    BnOH-NH-bis-(C2-S)-propane-O-isoprene ester (PROTAC Linker 29) is an alkyl ether-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-P1132A
    Galanin (1-29)(rat, mouse) TFA

    Neuropeptide Y Receptor Neurological Disease
    Galanin (1-29)(rat, mouse) TFA is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3, respectively. Anticonvulsant effect.
  • HY-N6049
    Lup-20(29)-en-28-oic acid

    Others Cancer Inflammation/Immunology
    Lup-20(29)-en-28-oic acid, a triterpenoid saponins of Pulsatilla koreana Root, possesses anti-inflammatory and anti-tumor effect.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-P1581
    Ceratotoxin A

    Bacterial Infection
    Ceratotoxin A, a 29-residue peptide isolated from the accessory gland secretion fluid, with strong anti-bacterial activity.
  • HY-101524
    TC13172

    Mixed Lineage Kinase Cancer
    TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells.
  • HY-13734
    PX-12

    IV-2

    Others Cancer
    PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • 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-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-12494
    LDC1267

    TAM Receptor Inflammation/Immunology Cancer
    LDC1267 is a highly selective TAM (Tyro3, Axl and Mer) kinase inhibitor with IC50s of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively.
  • HY-19406
    AE-3763

    Elastase Inflammation/Immunology Cardiovascular Disease
    AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC50 of 29 nM.
  • HY-12855A
    Lys05

    Lys01 trihydrochloride

    Autophagy Cancer
    Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.
  • HY-P1215
    HS024

    Melanocortin Receptor Metabolic Disease
    HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake.
  • HY-P1215A
    HS024 TFA

    Melanocortin Receptor Metabolic Disease
    HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake.
  • HY-130981
    FN-1501-propionic acid

    CDK Ligand for Target Protein for PROTAC Cancer
    FN-1501-propionic acid is a CDK2/9 ligand for PROTAC. FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader (HY-130709).
  • HY-12308
    TCS 2314

    Integrin Inflammation/Immunology
    TCS 2314 (compound 3) is orally active and selective very late antigen-4 (VLA-4, α4β1, CD49d/CD29) antagonist with an IC50 of 4.4 nM.
  • HY-N0532
    Morroniside

    MMP Metabolic Disease Neurological Disease
    Morroniside has neuroprotective effect by inhibiting neuron apoptosis and MMP2/9 expression.
  • 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-100333
    PF-02575799

    Others Metabolic Disease
    PF-02575799 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.77±0.29 nM.
  • 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-10389
    Alvespimycin

    17-DMAG; NSC 707545

    HSP Cancer
    Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50 of 62 ± 29 nM.
  • HY-100269
    Chymase-IN-1

    Others Inflammation/Immunology
    Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM.
  • HY-14444
    Plinabulin

    NPI-2358

    Microtubule/Tubulin Cancer
    Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC50 of 9.8 nM against HT-29 cells. Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells.
  • HY-100006
    MRT68921

    ULK Cancer
    MRT68921 is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
  • HY-100130
    N-[(4-Aminophenyl)methyl]adenosine

    Adenosine Receptor Neurological Disease
    N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5′-Nucleotidase.
  • HY-18988
    ETC-159

    ETC-1922159

    Wnt Cancer
    ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
  • HY-13413
    Tofogliflozin (hydrate)

    CSG-452 hydrate

    SGLT Reactive Oxygen Species Metabolic Disease
    Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells.
  • HY-N1962
    Ophiopojaponin C

    Others Others
    Ophiopojaponin C is a naturally occurring C29 steroidal glycoside isolated from the tubers of O. japonicas.
  • HY-126142
    Top1 inhibitor 1

    Topoisomerase ADC Cytotoxin Cancer
    Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM.
  • HY-128569
    ALK-IN-5

    ALK Neurological Disease
    ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK), with an IC50 of 2.9 nM.
  • HY-12432A
    Gilteritinib hemifumarate

    ASP2215 hemifumarate

    FLT3 TAM Receptor Cancer
    Gilteritinib hemifumarate is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
  • HY-100006A
    MRT68921 dihydrochloride

    ULK Cancer
    MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-105189
    Meclinertant

    SR 48692

    Neurotensin Receptor Neurological Disease
    Meclinertant (SR 48692) is a potent, selective, nonpeptide and orally active neurotensin receptor 1 (NTS1) antagonist. In human colon carcinoma (HT-29) cells, Meclinertant competitively antagonizes neurotensin-induced intracellular Ca 2+ mobilization with a pA2 values of 8.13. Meclinertant has anxiolytic, anti-addictive and memory-impairing effects.
  • HY-130709
    PROTAC CDK2/9 Degrader-1

    PROTAC CDK Cancer
    PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand.
  • HY-18564
    HCV-IN-3

    HCV Infection
    HCV-IN-3 is a hepatitis C virus (HCV) NS3/4a protein inhibitor, with an IC50 of 20 μM, a Kd of 29 μM.
  • HY-12432
    Gilteritinib

    ASP2215

    FLT3 TAM Receptor Cancer
    Gilteritinib is a potent FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
  • HY-10448
    Capsaicin

    (E)-Capsaicin

    TRP Channel Autophagy Cancer
    Capsaicin ((E)-Capsaicin) is a mixture of Capsaicin and Dihydrocapsaicin. Capsaici is a TRPV1 agonist with an EC50 of 0.29 μM in HEK293 cells.
  • HY-100443B
    (-)-PX20606 trans isomer

    (-)-PX-102 trans isomer; (-)-PX-104

    FXR Autophagy Metabolic Disease
    (-)-PX20606 trans isomer is a FXR agonist with EC50s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.
  • HY-B0162AS1
    Ivabradine D3 Hydrochloride

    Adrenergic Receptor Endocrinology
    Ivabradine D3 Hydrochloride is the deuterium labeled Ivabradine hydrochloride. Ivabradine hydrochloride is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.
  • HY-B0162AS
    Ivabradine D6 hydrochloride

    Adrenergic Receptor Endocrinology
    Ivabradine D6 hydrochloride is the deuterium labeled Ivabradine hydrochloride. Ivabradine hydrochloride is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.
  • HY-12024
    Alvespimycin hydrochloride

    17-DMAG hydrochloride; KOS-1022; BMS 826476

    HSP Apoptosis Cancer
    Alvespimycin hydrochloride (17-DMAG hydrochloride; KOS-1022; BMS 826476) is a potent inhibitor of Hsp90, binding to Hsp90 with EC50 of 62±29 nM.
  • HY-18957
    Lifirafenib

    BGB-283

    EGFR Raf Cancer
    Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRaf V600E and EGFR, respectively.
  • HY-10129
    Veliparib

    ABT-888

    PARP Autophagy Cancer
    Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
  • HY-111655
    SKA-31

    Potassium Channel Cardiovascular Disease
    SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure.
  • HY-12648A
    FASN-IN-4 tosylate

    Fatty Acid Synthase (FASN) Cancer
    FASN-IN-4 tosylate is a potent inhibitor of fatty acid synthase (FASN) extracted from patent WO 2012064642 A1, compound 29; has an IC50 of 10 nM.
  • HY-10130
    Veliparib dihydrochloride

    ABT-888 dihydrochloride

    PARP Autophagy Cancer
    Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.
  • HY-110263
    EML 425

    Histone Acetyltransferase Epigenetic Reader Domain Metabolic Disease Neurological Disease Cardiovascular Disease
    EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.
  • HY-128352
    SMYD3-IN-1

    Histone Methyltransferase Cancer
    SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM.
  • HY-103028A
    GSK963

    RIP kinase Others
    GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro.
  • HY-16667
    HLM006474

    Others Cancer
    HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
  • HY-12032
    AG14361

    PARP Cancer
    AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively.
  • HY-N3516
    Oxyresveratrol 2-O-β-D-glucopyranoside

    Tyrosinase Metabolic Disease
    Oxyresveratrol 2-O-β-D-glucopyranoside is a phenolic compound isolated from Morus nigra root and is an effective tyrosinase inhibitor with an IC50 of 29.75 μM.
  • HY-12648
    FASN-IN-4

    Fatty Acid Synthase (FASN) Metabolic Disease
    FASN-IN-4 is a potent inhibitor of fatty acid synthase (FASN) extracted from patent WO 2012064642 A1, compound 29; has an IC50 of 10 nM.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-18175
    CCT244747

    Checkpoint Kinase (Chk) Cancer
    CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
  • HY-U00427
    PDE2/PDE10-IN-1

    Phosphodiesterase (PDE) Neurological Disease
    PDE2/PDE10-IN-1 is a phosphodiesterase 2 (PDE2) and PDE10 inhibitor with IC50s of 29 and 480 nM, respectively.
  • HY-111413
    c(phg-isoDGR-(NMe)k)

    Integrin Cancer
    c(phg-isoDGR-(NMe)k) is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.
  • HY-111824
    VH032-thiol-C6-NH2

    VHL Ligand-Linker Conjugates 14; E3 ligase Ligand-Linker Conjugates 29

    E3 Ligase Ligand-Linker Conjugate Cancer
    VH032-thiol-C6-NH2 (VHL Ligand-Linker Conjugates 14) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
  • HY-111413A
    c(phg-isoDGR-(NMe)k) TFA

    Integrin Cancer
    c(phg-isoDGR-(NMe)k) TFA is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.
  • HY-135516
    Wnt pathway activator 1

    Wnt Cancer
    Wnt pathway activator 1 is a potent Wnt activator extracted from patent WO2012024404A1, compound 1, has an IC50s of 28-29 nM.
  • HY-130233
    S516

    Microtubule/Tubulin Cancer
    S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM. S516 has marked antitumor activity.
  • HY-11004
    AZ 628

    Raf Apoptosis Cancer
    AZ 628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
  • HY-N6957
    8-Keto-berberine

    Others Metabolic Disease
    8-Keto-berberine (compound 29) is a non-naturally occurring 11, 12-oxygenated protoberberine derived from naturally occurring 9, 10-oxygenated protoberberine.
  • HY-B1714A
    NSC 601980

    Others Cancer
    NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
  • HY-14902
    Tofogliflozin

    CSG452

    SGLT Metabolic Disease
    Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.
  • HY-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-P1435
    NoxA1ds

    NADPH Oxidase
    NoxA1ds is a potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. NoxA1ds inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. NoxA1ds attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro.
  • HY-130845
    AR antagonist 1

    Ligand for E3 Ligase Cancer
    AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
  • HY-10991
    MGCD-265 analog

    c-Met/HGFR VEGFR Apoptosis Cancer
    MGCD-265-analog (structurally related to MGCD-265) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively.
  • HY-15815
    Bromosporine

    Epigenetic Reader Domain Cancer
    Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.
  • HY-P1435A
    NoxA1ds TFA

    NADPH Oxidase
    NoxA1ds TFA is a potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds TFA exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. NoxA1ds TFA inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro.
  • HY-15874A
    Fiboflapon sodium

    GSK2190915 sodium salt; AM-803 sodium

    FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
  • HY-114173
    DDR1-IN-4

    Discoidin Domain Receptor Inflammation/Immunology
    DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.
  • HY-15874
    Fiboflapon

    GSK2190915; AM-803

    FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
  • HY-100763
    Mcl1-IN-12

    Bcl-2 Family Cancer
    Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity.
  • HY-119366
    S18-000003

    ROR Inflammation/Immunology
    S18-000003 is a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor with an IC50 of 29 nM. S18-000003 inhibits IL-17 production.
  • 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-110392
    CMP8

    Estrogen Receptor/ERR Cancer
    CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively.
  • HY-100781A
    L-APB

    L-AP 4

    mGluR Neurological Disease
    L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
  • HY-125839
    OP-3633

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism.
  • HY-119377
    UPGL00004

    Glutaminase Cancer
    UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
  • HY-P1872
    OV-1, sheep

    Bacterial Infection
    OV-1, sheep is an alpha-helical antimicrobial ovispirin peptide derived from SMAP29 peptide (sheep), which inhibits several antibiotic-resistant bacterial strains including mucoid and nonmucoid Pseudomonas aeruginosa.
  • HY-107658
    SN 6

    Na+/Ca2+ Exchanger Cardiovascular Disease
    SN 6 is a selective Na +/Ca 2+ exchanger (NCX) inhibitor, and inhibits 45Ca 2+ uptake by NCX1, NCX2, and NCX3, with IC50s of 2.9, 16, and 8.6 μM, respectively.
  • HY-N6002
    3'-Hydroxypterostilbene

    Apoptosis Autophagy Cancer
    3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.
  • HY-12832
    JNJ-42041935

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    JNJ-42041935 is a potent, competitive and selective inhibitor of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.
  • HY-75564
    Cyclo(Ala-Gly)

    Endogenous Metabolite Cancer
    Cyclo(Ala-Gly), a metabolite of a mangrove endophytic fungus, Penicillium thomi, exhibits cytotoxicity against A549, HepG2 and HT29 cells. The IC50 values range from 9.5 to 18.1 μM.
  • HY-122856
    AZ12601011

    TGF-β Receptor Cancer
    AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
  • HY-B1714
    NSC 601980 (analog)

    Others Cancer
    NSC 601980 analog is the analog of the NSC601980, NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
  • 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-106101
    Echinomycin

    Quinomycin A; NSC-13502

    HIF/HIF Prolyl-Hydroxylase Cancer
    Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.
  • HY-111756
    BLM-IN-1

    Apoptosis Cancer
    BLM-IN-1 (compound 29) is an effective Bloom syndrome protein (BLM) inhibitor, with a strong BLM binding KD of 1.81 μM and an IC50 of 0.95 μM for BLM. Induces DNA damage response, as well as apoptosis and proliferation arrest in cancer cells.
  • HY-101024
    PF-06263276

    JAK Inflammation/Immunology
    PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively.
  • 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-W062835
    CGP77675

    Src Cancer
    CGP77675 is a potent inhibitor of Src family kinases. CGP77675 inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity.
  • 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-N0907
    Ginsenoside Rg6

    NF-κB Apoptosis Cancer Inflammation/Immunology
    Ginsenoside Rg6 is the component isolated from notoginseng. Ginsenoside Rg6 inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 29.34±2.22 μM in HepG2 cells. Ginsenoside Rg6 also exhibits apoptosis-inducing effect.
  • HY-13636
    Fulvestrant

    ICI 182780; ZD 9238; ZM 182780

    Estrogen Receptor/ERR Autophagy Apoptosis Cancer
    Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
  • HY-110318
    VUF11207 fumarate

    CXCR Cancer
    VUF11207 fumarate (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7.
  • HY-14903
    Ulimorelin

    TZP-101

    GHSR Adrenergic Receptor Metabolic Disease
    Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.
  • HY-12294A
    PEAQX tetrasodium hydrate

    NVP-AAM077 tetrasodium hydrate

    iGluR Apoptosis Neurological Disease
    PEAQX tetrasodium hydrate (NVP-AAM077 tetrasodium hydrate) 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-114308
    SGL5213

    SGLT Metabolic Disease
    SGL5213 is a potent, oral active and low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor, with IC50 values of 29 nM and 20 nM for hSGLT1 and hSGLT2, respectively. SGL5213 has potential to treat type 2 diabetes treatment.
  • HY-120528A
    GB-110 hydrochloride

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-P1341
    OXA(17-33)

    Orexin Receptor (OX Receptor) Neurological Disease
    OXA(17-33) is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM).
  • HY-N6775
    Sonolisib

    PX-866

    PI3K Cancer
    Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.
  • HY-17623
    Tegoprazan

    Proton Pump Metabolic Disease
    Tegoprazan, a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H +/K +-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro.
  • HY-100246
    CI-1044

    PD-189659

    Phosphodiesterase (PDE) Inflammation/Immunology
    CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively.
  • HY-120528
    GB-110

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-13898
    Taselisib

    GDC-0032; RG-7604

    PI3K Cancer
    Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
  • HY-100430
    CCF642

    Others Cancer
    CCF642 is a potent protein disulfide isomerases (PDI) inhibitor with an IC50 of 2.9 μM. CCF642 causes acute endoplasmic reticulum (ER) stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release. CCF642 has broad anti-multiple myeloma activity.
  • HY-103392
    Stiripentol

    BCX2600

    Cytochrome P450 Neurological Disease
    Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively.
  • HY-P1341A
    OXA(17-33) TFA

    Orexin Receptor (OX Receptor) Neurological Disease
    OXA(17-33) TFA is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) TFA shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM).
  • HY-103647
    K00546

    CDK Cancer
    K00546 is a potent CDK1 and CDK2 inhibitor and is a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively. K00546 is also a triazole-1-carbothioamide inhibitor.
  • HY-106376A
    L-Buthionine-(S,R)-sulfoximine

    L-Buthionine sulfoximine

    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-P1428
    RFRP-1(human)

    Neuropeptide Y Receptor
    RFRP-1(human) is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
  • HY-P1428A
    RFRP-1(human) TFA

    Neuropeptide Y Receptor
    RFRP-1(human) TFA is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
  • HY-P7061A
    ALX 40-4C Trifluoroacetate

    CXCR Infection Endocrinology
    ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
  • HY-N6061
    Ophiopogonin C

    Others Cancer
    Ophiopogonin C, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin C shows cytotoxic activity against two human tumor cell lines MG-63 and SNU387 with IC50s of 19.76 μM and 15.51 μM, respectively.
  • HY-P7061
    ALX 40-4C

    CXCR Infection Endocrinology
    ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
  • HY-100753
    STAT3-IN-1

    STAT Apoptosis Cancer
    STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis.
  • HY-16531A
    YF-2 hydrochloride

    Histone Acetyltransferase Cancer Neurological Disease
    YF-2 hydrochloride is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
  • HY-15670
    BMS-906024

    γ-secretase Notch Cancer
    BMS-906024 is an oral and selective gamma secretase inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.
  • HY-124037
    SRT 1460

    Sirtuin Cancer
    SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues.
  • HY-16531
    YF-2

    Histone Acetyltransferase Cancer Neurological Disease
    YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
  • HY-N6883
    6-Methoxytricin

    Aldose Reductase Metabolic Disease
    6-Methoxytricin (Compound 6) is an flavonoid isolated from Artemisia iwayomogi. 6-Methoxytricin (Compound 6) is an inhibitor on aldose reductase (AR) and advanced glycation endproduct (AGE) formation activities with IC50 values of 30.29 μM and 134.88 μM, respectively. 6-Methoxytricin (Compound 6) has potential as an anti-diabetic complications agent.
  • HY-130602
    MS432

    PROTAC MEK Cancer
    MS432 is a first-in-class and highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
  • HY-U00278
    Deloxolone

    (3β,20β)-3-(3-Carboxy-1-oxopropoxy)olean-9(11)-en-29-oic acid

    Others Inflammation/Immunology
    Deloxolone has the potential for inflammatory, ischemic and proliferative diseases treatment.
  • HY-B0623A
    Ropinirole hydrochloride

    SKF 101468 hydrochloride

    Dopamine Receptor Neurological Disease
    Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.
  • HY-130713
    Thalidomide-C2-amido-C2-COOH

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-C2-amido-C2-COOH incorporates a CRBN ligand for the E3 ubiquitin ligase, and a linker. Thalidomide-C2-amido-C2-COOH can be used to design PROTAC CDK2/9 Degrader-1 (HY-130709).
  • HY-122942
    Moracin M

    Phosphodiesterase (PDE) Endogenous Metabolite Inflammation/Immunology
    Moracin M, a phenolic component in the skin of Morus alba L., is a potent phosphodiesterase-4 (PDE4) inhibitor with IC50 values of 2.9, 4.5, >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. Moracin M has anti-inflammatory activity.
  • HY-19801
    CVT-10216

    Aldehyde Dehydrogenase (ALDH) Neurological Disease
    CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.
  • HY-125209A
    TH5427 hydrochloride

    DNA/RNA Synthesis Cancer
    TH5427 hydrochloride is a potent, selective NUDT5 inhibitor (IC50=29 nM). TH5427 hydrochloride shows an apparent 690-fold selectivity for NUDT5 over MTH1. TH5427 hydrochloride blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells.
  • HY-18285
    Longdaysin

    Casein Kinase ERK CDK Cancer
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
  • HY-108628
    SU16f

    PDGFR Cancer
    SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration.
  • HY-12164
    Mocetinostat

    MGCD0103

    HDAC Autophagy Apoptosis Cancer
    Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.
  • HY-130712
    NH2-C2-amido-C2-Boc

    PROTAC Linker Cancer
    NH2-C2-amido-C2-Boc is a PROTAC linker, which refers to the alkyl/ether composition. NH2-C5-NH-Boc can be used in the synthesis of a series of PROTACs, such as the PROTAC CDK2/9 Degrader-1 (HY-130709).
  • HY-108938
    SDZ285428

    Cytochrome P450 Fungal Parasite Infection
    SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h).
  • HY-135123
    DC4SMe

    ADC Cytotoxin Cancer
    DC4SMe, a phosphate prodrug of cytotoxic DNA alkylator DC4, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4SMe exhibits IC50s of 1.9 nM, 2.9 nM, and 1.8 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC4SMe can be used for the targeted treatment of cancer.
  • HY-107429
    Abrocitinib

    PF-04965842

    JAK Inflammation/Immunology
    Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.
  • HY-B0731A
    Perospirone

    SM-9018 free base

    5-HT Receptor Dopamine Receptor Neurological Disease
    Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic drug and has the potential for schizophrenic disease.
  • HY-N3504
    Ophiopogonin D'

    Sirtuin Cancer
    Ophiopogonin D', isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D' shows cytotoxic activity against two human tumor cell lines MG-63 and SNU387 with IC50s of 3.09 μM and 3.63 μM, respectively. Ophiopogonin D' activates SIRT1 in a dose-dependent manner.
  • HY-120214
    TAS05567

    Syk Inflammation/Immunology
    TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases.
  • HY-133012
    GFB-8438

    TRP Channel Neurological Disease
    GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.
  • 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-19306
    SB-267268

    Integrin Cancer
    SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
  • HY-103387
    DuP-697

    COX Apoptosis Cancer Inflammation/Immunology
    DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects.
  • HY-124295
    MPT0E028

    HDAC Akt Apoptosis Cancer
    MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity.
  • HY-16961
    Sitravatinib

    MGCD516; MG-516

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-100034
    NSC 663284

    DA-3003-1

    Phosphatase Histone Methyltransferase Cancer
    NSC 663284 is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM).
  • HY-16961A
    Sitravatinib malate

    MGCD516 malate; MG-516 malate

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-19744
    T6167923

    MyD88 Inflammation/Immunology
    T6167923 is a potent and selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with an 50 of 2.7  μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.
  • HY-124131
    DS-437

    Histone Methyltransferase Cancer Inflammation/Immunology
    DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.
  • HY-104040
    MKC8866

    IRE1 Cancer
    MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.
  • HY-130814
    Thalidomide-NH-C4-NH2 TFA

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader.
  • HY-135858
    SARS-CoV-IN-3

    SARS-CoV Parasite HIV Infection
    SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-3 shows anti-Coronavirus activity with an EC50 of 3.6 μM in Vero cells. SARS-CoV-IN-3 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 11.7 and 20.4 nM; and IC90s of 29.19 and 56 nM; respectively. SARS-CoV-IN-3 reduces HIV-1-induced cytopathic effect with an EC50 of 10 μM in MT-4 cells.
  • HY-108648
    2-Methylthioadenosine diphosphate trisodium

    2-Methylthio-ADP trisodium

    P2Y Receptor Neurological Disease
    2-Methylthioadenosine diphosphate trisodium is a potent purinergic P2Y receptors agonist, with EC50s of 19, 6.2, and 5 nM for human P2Y13, mouse P2Y13 and human P2Y12, respectively. 2-Methylthioadenosine diphosphate trisodium has pEC50s of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. 2-Methylthioadenosine diphosphate trisodium induces platelet aggregation and shape change, and inhibits cyclic AMP accumulation in platelets exposed to prostaglandin E1.
  • HY-N0515
    Ophiopogonin D

    PPAR NF-κB Calcium Channel Inflammation/Immunology Cardiovascular Disease
    Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
  • HY-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-120874
    PF-06372865

    GABA Receptor Neurological Disease
    PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 has the potential for epilepsy.
  • HY-135856
    SARS-CoV-IN-2

    SARS-CoV Parasite HIV Infection
    SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC50 of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 21.5 and 30 nM; and IC90s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC50 of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities.
  • 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.