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Targets Recommended: PD-1/PD-L1
Results for "

PD

" in MCE Product Catalog:

168

Inhibitors & Agonists

8

Screening Libraries

1

Dye Reagents

19

Peptides

6

Inhibitory Antibodies

9

Natural
Products

25

Recombinant Proteins

5

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-103407A
    PD 168568 dihydrochloride

    Dopamine Receptor Neurological Disease
    PD 168568 dihydrochloride is an orally active and selective D4 dopamine receptor antagonist, with a Ki of 8.8 nM.
  • HY-103048
    PD-1/PD-L1-IN 3

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN 3, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC50s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 can be used for the research of various diseases, including cancer and infectious diseases.
  • HY-103048A
    PD-1/PD-L1-IN 3 TFA

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN 3 TFA, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 TFA interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC50s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 TFA can be used for the research of various diseases, including cancer and infectious diseases.
  • HY-129172A
    PD-1/PD-L1-IN 5

    PD-1/PD-L1 Cancer Infection Inflammation/Immunology
    PD-1/PD-L1-IN 5 is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM.
  • HY-138407
    Evixapodlin

    PD-1/PD-L1-IN 7

    PD-1/PD-L1 HBV Cancer Infection
    Evixapodlin (PD-1/PD-L1-IN 7) is a human PD-1/PD-L1 protein/protein interaction inhibitor with an IC50 of 0.213 nM. Evixapodlin has anticancer and antiviral functions.
  • HY-132192
    PD-1/PD-L1-IN-9

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model.
  • HY-134884
    PD-1/PD-L1-IN-8

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-8 (example 24) is a PD-1/PD-L1 inhibitor, with an IC50 <= 10 nM.
  • HY-131347
    PD-1/PD-L1-IN-NP19

    PD-1/PD-L1 Cancer Inflammation/Immunology
    PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.
  • HY-129172
    PD-1/PD-L1-IN 5 TFA

    PD-1/PD-L1 Cancer Infection Inflammation/Immunology
    PD-1/PD-L1-IN 5 TFA is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM.
  • HY-132202
    PD-1/PD-L1-IN-10

    PD-1/PD-L1 Apoptosis Cancer
    PD-1/PD-L1-IN-10 (compound B2) is an orally active PD-1/PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy.
  • HY-10578
    PD 169316

    p38 MAPK Autophagy Enterovirus Cancer
    PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC50 of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.
  • HY-112345
    PD-089828

    FGFR PDGFR EGFR Src Cancer
    PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.
  • HY-100434
    PD-161570

    FGFR PDGFR EGFR Src TGF-β Receptor Cancer Cardiovascular Disease
    PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
  • HY-21098A
    PD-168077 maleate

    Dopamine Receptor Neurological Disease
    PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.
  • HY-101093B
    PD-1-IN-20

    PD-1/PD-L1 Cancer
    PD-1-IN-20 is the less active enantiomer of PD-1-IN-1. PD-1-IN-1 is an inhibitor of programmed cell dealth-1 (PD-1) extracted from patent WO 2015033299 A1, compound example 4.
  • HY-134886
    PD-1-IN-24

    PD-1/PD-L1 Cancer
    PD-1-IN-24 (compound 1) is an orally active PD-1 inhibitor.
  • HY-16958
    PD 404182

    Others Inflammation/Immunology
    PD 404182 is a potent and competitive inhibitor of human dimethylarginine dimethylaminohydrolase 1 (DDAH1), with an IC50 of 9 μM. PD 404182 exhibits antiangiogenic and antiviral activity in vitro.
  • HY-108512
    PD 144418

    Sigma Receptor Neurological Disease
    PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity.
  • HY-12062
    PD318088

    MEK Cancer
    PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research.
  • HY-101093
    PD-1-IN-1

    PD-1/PD-L1 Inflammation/Immunology
    PD-1-IN-1 is an inhibitor of programmed cell dealth-1 (PD-1) extracted from patent WO2015033299A1, compound example 4. PD-1-IN-1 can be used as immune modulator.
  • HY-118402
    PD 119819

    Dopamine Receptor Neurological Disease
    PD 119819 is a highly selective benzopyran-4-one brain dopamine autoreceptor agonist. PD 119819, a heterocyclic piperazine, inhibits spontaneous locomotor activity and brain dopamine synthesis.
  • HY-101098
    PD-1-IN-18

    PD-1/PD-L1 Inflammation/Immunology
    PD-1-IN-18 is a PD1 signaling pathway inhibitor, which acts as an immunomodulator.
  • HY-101058
    PD1-PDL1-IN 1

    PD-1/PD-L1 Inflammation/Immunology
    PD1-PDL1-IN 1 is a potent programmed cell death 1 (PD-1) inhibitor. PD1-PDL1-IN 1 is useful as immune modulator.
  • HY-128605
    PD-1-IN-22

    PD-1/PD-L1 Cancer
    PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor with an IC50 of 92.3 nM.
  • HY-101598
    PD-159020

    Endothelin Receptor Cardiovascular Disease Endocrinology
    PD-159020 is a non-selective ETA/ETB antagonist, with IC50s of 30 and 50 nM for hETA and hETB, respectively.
  • HY-18961
    PD 407824

    Checkpoint Kinase (Chk) Wee1 Cancer Inflammation/Immunology
    PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4.
  • HY-108594
    PD-118057

    Potassium Channel Metabolic Disease
    PD-118057 is a human ether-a-go-go-related gene (hERG) channel activator that does not cause hERG blockade.
  • HY-108512A
    PD 144418 oxalate

    Sigma Receptor Neurological Disease
    PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity.
  • HY-12028
    PD98059

    MEK ERK Aryl Hydrocarbon Receptor Autophagy Cancer
    PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits autophagy.
  • HY-13896
    PD168393

    EGFR Autophagy Apoptosis Cancer
    PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC.
  • HY-10259
    PD 123319

    (S)-(+)-PD 123319

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.
  • HY-101097
    PD-1-IN-17

    PD-1/PD-L1 Cancer
    PD-1-IN-17 is a programmed cell death-1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM.
  • HY-10259A
    PD 123319 ditrifluoroacetate

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.
  • HY-19991
    BMS-1

    PD-1/PD-L1 inhibitor 1

    PD-1/PD-L1 Apoptosis Cancer Inflammation/Immunology
    BMS-1 is an inhibitor of the PD-1/PD-L1 protein/protein interaction (IC50 between 6 and 100 nM).
  • HY-101097A
    PD-1-IN-17 TFA

    PD-1/PD-L1 Cancer
    PD-1-IN-17 TFA is a programmed cell death-1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM.
  • HY-107428
    PD-166793

    MMP Cardiovascular Disease
    PD-166793 is a potent, selective, orally active and wide‐broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure.
  • HY-13925
    PD0166285

    Wee1 Apoptosis Cancer
    PD0166285, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 exhibits an IC50 of 3.433 μM for Chk1.
  • HY-13925A
    PD0166285 dihydrochloride

    Wee1 Apoptosis Cancer
    PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC50 of 3.433 μM for Chk1.
  • HY-U00236
    PD0176078

    Calcium Channel Cardiovascular Disease
    PD0176078 is a newly found N-type Calcium channel blocker.
  • HY-103274
    PD180970

    Bcr-Abl Src c-Kit Apoptosis Cancer Neurological Disease
    PD180970 is a highly potent and ATP-competitive p210 Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210 Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research.
  • HY-131295
    PD0325901-O-C2-dioxolane

    MEK Ligand for Target Protein for PROTAC Cancer
    PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader.
  • HY-101296
    PD-166866

    FGFR Autophagy Cancer
    PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM.
  • HY-19749
    PD 151746

    Proteasome Cardiovascular Disease
    PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM).
  • HY-50295
    CI-1040

    PD 184352

    MEK Apoptosis Cancer
    CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
  • HY-U00250
    β-Amino Acid Imagabalin Hydrochloride

    PD-0332334

    Calcium Channel Neurological Disease
    β-Amino Acid Imagabalin Hydrochloride (PD-0332334) is a ligand for the α2δ subunit of the voltage-dependent calcium channel.
  • 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-103318
    PD173212

    Calcium Channel Neurological Disease
    PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.
  • HY-10367
    Canertinib

    CI-1033; PD-183805

    EGFR Cancer
    Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
  • HY-109567
    Gemcabene

    PD-72953

    Others Metabolic Disease Inflammation/Immunology
    Gemcabene (PD-72953), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity.
  • HY-10395
    PD173955

    Bcr-Abl Src Apoptosis Cancer
    PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.
  • HY-18609
    PD158780

    EGFR Cancer
    PD158780 is a potent EGFR family inhibitor with IC50s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.
  • HY-50767
    Palbociclib

    PD 0332991

    CDK Cancer
    Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research.
  • HY-100937
    DPCPX

    PD 116948

    Adenosine Receptor Cardiovascular Disease
    DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes.
  • HY-100529
    PD150606

    Proteasome Cancer
    PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor with Ki values of 0.21 μM and 0.37 μM for μ- and m-calpains respectively, which is neuroprotective.
  • HY-110166
    PD 90780

    Others Neurological Disease
    PD 90780 is a non peptide antagonist of nerve growth factor (NGF) binding to the P75 NGF receptor, inhibits NGF-p75 NTR interaction with IC50s values of 23.1 µM and 1.8 µM in PC12 cells and PC12 nnr5 cells, respectively .
  • HY-103286
    PD176252

    Bombesin Receptor Cancer
    PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
  • HY-10321
    PD173074

    FGFR VEGFR Apoptosis Cancer
    PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.
  • HY-100399
    Nevanimibe

    PD-132301; ATR-101

    Acyltransferase Apoptosis Cancer
    Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer.
  • HY-100399A
    Nevanimibe hydrochloride

    PD-132301 hydrochloride; ATR101 hydrochloride

    Acyltransferase Apoptosis Cancer
    Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.
  • HY-103157
    PD146176

    NSC168807

    Autophagy Ferroptosis Cardiovascular Disease
    PD146176 (NSC168807), a 15-Lipoxygenase (15-LO) inhibitor, inhibits rabbit reticulocyte 15-LO (Ki=197 nM, IC50=0.54 μM). PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.
  • HY-13215
    Avasimibe

    CI-1011; PD-148515

    Acyltransferase Cancer
    Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.
  • HY-50767A
    Palbociclib monohydrochloride

    PD 0332991 monohydrochloride

    CDK Cancer
    Palbociclib (PD 0332991) monohydrochloride is a highly selective CDK4/6 inhibitor with IC50s of 11 nM and 16 nM, respectively. Palbociclib monohydrochloride has the potential for ER-positive and HER2-negative breast cancer research.
  • HY-109567A
    Gemcabene calcium

    PD-72953 calcium

    Others Metabolic Disease Inflammation/Immunology
    Gemcabene calcium (PD-72953 calcium), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity.
  • HY-10254
    Mirdametinib

    PD0325901; PD325901

    MEK Autophagy Apoptosis Cancer
    Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts.
  • HY-50767S
    Palbociclib D8

    PD 0332991 D8

    CDK Cancer
    Palbociclib D8 (PD 0332991 D8) is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research.
  • HY-12013
    PD153035 Hydrochloride

    SU-5271 Hydrochloride; AG1517 Hydrochloride; ZM 252868 Hydrochloride

    EGFR Cancer
    PD153035 Hydrochloride (SU-5271 Hydrochloride) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.
  • 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-14346
    PD153035

    SU-5271; AG1517; ZM 252868

    EGFR Cancer
    PD153035 (SU-5271; AG1517; ZM 252868) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.
  • HY-105226
    CI-988

    PD134308

    Cholecystokinin Receptor Cancer Neurological Disease
    CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects.
  • HY-10581A
    Gatifloxacin hydrochloride

    AM-1155 hydrochloride; BMS-206584 hydrochloride; PD135432 hydrochloride

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
  • HY-10581B
    Gatifloxacin mesylate

    AM-1155 mesylate; BMS-206584 mesylate; PD135432 mesylate

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin mesylate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin mesylate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin mesylate can be used to treat bacterial conjunctivitis in vivo.
  • HY-10581
    Gatifloxacin

    AM-1155; BMS-206584; PD135432

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50=0.109 μg/ml). Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
  • HY-10581C
    Gatifloxacin sesquihydrate

    AM-1155 sesquihydrate; BMS-206584 sesquihydrate; PD135432 sesquihydrate

    Bacterial Topoisomerase Antibiotic Infection Inflammation/Immunology
    Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis in vivo.
  • HY-A0065
    Palbociclib isethionate

    PD 0332991 isethionate

    CDK Cancer
    Palbociclib isethionate is a highly selective inhibitor of CDK4/6 with IC50s of 11 nM/16 nM, respectively.
  • HY-B0536
    Clinafloxacin

    AM-1091; CI-960; PD 127391

    Bacterial Antibiotic Infection
    Clinafloxacin (AM 1091) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitory activity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro. Clinafloxacin is against DNA gyrase and topoisomerase IV of S. aureus with IC50 values of 0.92 µg/ml and 1.62 µg/ml, respectively.
  • HY-108969
    Pyrazoloacridine

    NSC 366140; PD 115934

    Topoisomerase Apoptosis Cancer
    Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment.
  • 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-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-10367A
    Canertinib dihydrochloride

    CI-1033 dihydrochloride; PD-183805 dihydrochloride

    EGFR Cancer
    Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
  • HY-B0502
    Enrofloxacin

    BAY Vp 2674; PD160788

    Bacterial Antibiotic Infection
    Enrofloxacin (BAY Vp 2674) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
  • HY-B0502A
    Enrofloxacin monohydrochloride

    BAY Vp 2674 monohydrochloride; PD160788 monohydrochloride

    Bacterial Antibiotic Infection
    Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
  • HY-B0536A
    Clinafloxacin hydrochloride

    AM 1091 hydrochloride; CI 960 hydrochloride; PD127391 hydrochloride

    Bacterial Antibiotic Infection
    Clinafloxacin hydrochloride (AM 1091 hydrochloride) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitory activity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro. Clinafloxacin hydrochloride is against DNA gyrase and topoisomerase IV of S. aureus with IC50 values of 0.92 µg/ml and 1.62 µg/ml, respectively.
  • HY-131183
    PROTAC PD-1/PD-L1 degrader-1

    PROTACs PD-1/PD-L1 Inflammation/Immunology
    PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 degrader, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
  • HY-P2478
    Human PD-L1 inhibitor V

    PD-1/PD-L1 Inflammation/Immunology
    Human PD-L1 inhibitor V, a human PD-1 protein binding peptide with a Kd value of 3.32 μM. Human PD-L1 inhibitor V inhibit the interaction of hPD-1/hPD-L1.
  • HY-P2477
    Human PD-L1 inhibitor IV

    PD-1/PD-L1 Inflammation/Immunology
    Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a Kd value of 1.38 μM. Human PD-L1 inhibitor IV inhibits the interaction of hPD-1/hPD-L1.
  • HY-P2564
    Human PD-L1 inhibitor III

    PD-1/PD-L1 Cancer Inflammation/Immunology
    Human PD-L1 inhibitor III is a human PD-L1 inhibitor.
  • HY-P2478A
    Human PD-L1 inhibitor V TFA

    PD-1/PD-L1 Inflammation/Immunology
    Human PD-L1 inhibitor V TFA, a human PD-1 protein binding peptide with a Kd value of 3.32 μM. Human PD-L1 inhibitor V TFA inhibit the interaction of hPD-1/hPD-L1.
  • HY-P2470
    Human PD-L1 inhibitor II

    PD-1/PD-L1 Cancer
    Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.
  • HY-123962
    G6PD activator AG1

    Others Metabolic Disease
    G6PD activator AG1 is a potent and selective glucose-6-phosphate dehydrogenase (G6PD) activator with an EC50 of 3 µΜ. G6PD activator AG1 reduces hemolysis of human erythrocytes.
  • HY-110000
    (+)-PD 128907 hydrochloride

    Dopamine Receptor Neurological Disease
    (+)-PD 128907 hydrochloride is a selective dopamine D2/D3 receptor agonist, with Kis of 1.7, 0.84 nM for human and rat D3 receptors, 179, 770 n M for human and rat D3 receptors, respectively.
  • HY-121246
    Fluorofenidone

    AKF-PD

    Others Inflammation/Immunology
    Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway.
  • HY-132296
    GSK215

    FAK PROTACs Cancer
    GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.
  • HY-108730
    Avelumab

    Anti-Human PD-L1, Human Antibody; MSB 0010718C; MSB0010718C

    PD-1/PD-L1 Cancer Inflammation/Immunology
    Avelumab is a fully human IgG1 anti-PD-L1 monoclonal antibody with potential antibody-dependent cell-mediated cytotoxicity.
  • HY-110125
    ML-193

    CID 1261822

    GPR55 Neurological Disease
    ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC50 of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats.
  • HY-131386
    BMS-1166-N-piperidine-CO-N-piperazine

    Target Protein Ligand-Linker Conjugate Cancer
    BMS-1166-N-piperidine-CO-N-piperazine incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM.
  • HY-102011
    BMS-1166

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-102011A
    BMS-1166 hydrochloride

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-116274
    BMS-8

    PD-1/PD-L1 Cancer
    BMS-8 inhibits the PD-1/PD-L1 interaction with IC50 of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1.
  • HY-131187
    BMS-1166-N-piperidine-COOH

    Ligand for Target Protein for PROTAC Cancer
    BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-19745
    BMS-202

    PD-1/PD-L1 Apoptosis Cancer
    BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity.
  • HY-P9971
    Camrelizumab

    SHR-1210

    PD-1/PD-L1 Cancer
    Camrelizumab (SHR-1210) is a potent humanied high-affinity IgG4-κ monoclonal antibody (mAb) to PD-1. Camrelizumab binds PD-1 at a high affinity of 3 nM and inhibits the binding interaction of PD-1 and PD-L1 with an IC50 of 0.70 nM. Camrelizumab acts as anti-PD-1/PD-L1 agent and can be used for cancer research, including NSCLC, ESCC, Hodgkin lymphoma, and advanced HCC et,al.
  • HY-120635
    BMS-1001 hydrochloride

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1001 hydrochloride is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 hydrochloride exhibits low-toxicity in cells.
  • HY-P9919
    Durvalumab

    MEDI 4736

    PD-1/PD-L1 Cancer
    Durvalumab (MEDI 4736) is an humanized anti-PD-L1 monoclonal antibody. Durvalumab (MEDI4736) completely blocks the binding of PD-L1 to both PD-1 and CD80, with IC50s of 0.1 and 0.04 nM, respectively.
  • HY-30105
    N-Boc-piperazine

    PROTAC Linker Cancer
    N-Boc-piperazine is a Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183).
  • HY-B0410A
    Pramipexole dihydrochloride hydrate

    Dopamine Receptor Neurological Disease
    Pramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
  • HY-B0410
    Pramipexole

    Dopamine Receptor Neurological Disease
    Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
  • HY-17355
    Pramipexole dihydrochloride

    Dopamine Receptor Neurological Disease
    Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
  • HY-P9902
    Pembrolizumab

    MK-3475; Lambrolizumab

    PD-1/PD-L1 Cancer
    Pembrolizumab is a humanized antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.
  • HY-W004701
    Br-C3-methyl ester

    PROTAC Linker Cancer
    Br-C3-methyl ester is a Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183).
  • HY-P1812
    AUNP-12

    NP-12

    PD-1/PD-L1 Cancer
    AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs).
  • HY-P3143A
    BMSpep-57 hydrochloride

    PD-1/PD-L1 Cancer
    BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs.
  • HY-P9903
    Nivolumab

    BMS-936558; ONO-4538; MDX-1106

    PD-1/PD-L1 Cancer
    Nivolumab is a programmed death receptor-1 (PD-1) blocking antibody to treat advanced (metastatic) non-small cell lung cancer.
  • HY-P1812A
    AUNP-12 TFA

    NP-12 TFA

    PD-1/PD-L1 Cancer
    AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs).
  • HY-P3143
    BMSpep-57

    PD-1/PD-L1 Cancer
    BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 facilitates T cell function by in creasing IL-2 production in PBMCs.
  • HY-19745A
    N-deacetylated BMS-202

    PD-1/PD-L1 Cancer
    N-deacetylated BMS-202 is the deacetylated of BMS-202. BMS-202 is an inhibitor of the PD-l/PD-Ll interaction, mainly used for cancer treatment.
  • HY-109150
    Mesdopetam

    IRL790

    Dopamine Receptor Neurological Disease
    Mesdopetam (IRL790) is an orally active and low toxicity dopamine D3 receptor antagonist. Mesdopetam can be used for the research of Parkinson's disease (PD).
  • HY-131186
    Pomalidomide-amido-C3-piperazine-N-Boc

    E3 Ligase Ligand-Linker Conjugate Cancer
    Pomalidomide-amido-C3-piperazine-N-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183).
  • HY-101454
    SR0987

    ROR Cancer Inflammation/Immunology
    SR0987, a SR1078 analog, is a RORγt agonist, with an EC50 of 800 nM. SR0987 increases IL17 expression while repressing the expression of PD-1.
  • HY-131184
    N-Boc-piperazine-C3-COOH

    PROTAC Linker Inflammation/Immunology
    N-Boc-piperazine-C3-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-N-piperazine-C3-COOH can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183).
  • HY-P3139
    TPP-1

    PD-1/PD-L1 Cancer
    TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function.
  • HY-P3139A
    TPP-1 TFA

    PD-1/PD-L1 Cancer
    TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function.
  • HY-N0460
    1-Caffeoylquinic acid

    NF-κB Cancer
    1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with Ki of 0.002 μM and binding energy of 1.50 Kcal/mol. 1-Caffeoylquinic acid has anti-oxidative stress ability. 1-Caffeoylquinic acid inhibits PD-1/PD-L1 interact.
  • HY-14417
    VU0155041

    mGluR Neurological Disease
    VU0155041 is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
  • HY-14417B
    VU0155041 sodium

    mGluR Neurological Disease
    VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
  • HY-130602
    MS432

    PROTACs MEK Cancer
    MS432 is a first-in-class and highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
  • HY-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-N0242
    Fraxinellone

    PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT Cancer Inflammation/Immunology
    Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.
  • HY-U00341
    ST4206

    Adenosine Receptor Neurological Disease
    ST4206 is a potent and orally active adenosine A2A receptor antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively. ST4206 has the potential for Parkinson׳s disease research.
  • HY-P1314
    2-Furoyl-LIGRLO-amide

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0..
  • HY-P9904
    Atezolizumab

    MPDL3280A

    PD-1/PD-L1 Apoptosis Autophagy Cancer
    Atezolizumab (MPDL3280A) is a selective humanized monoclonal IgG1 antibody against programmed death ligand 1 (PD-L1), used for cancer research.
  • HY-14347
    EBE-A22

    Others Cancer
    EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
  • HY-P1314A
    2-Furoyl-LIGRLO-amide TFA

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    2-Furoyl-LIGRLO-amide TFA is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0..
  • HY-135902
    Synucleozid

    NSC 377363

    DNA/RNA Synthesis Neurological Disease
    Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
  • HY-135902A
    Synucleozid hydrochloride

    NSC 377363 hydrochloride

    DNA/RNA Synthesis Neurological Disease
    Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
  • HY-N0079
    Praeruptorin C

    Calcium Channel Cardiovascular Disease
    Praeruptorin C is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin C is a calcium antagonist with pD2 ′ value of 5.7.
  • HY-N6066
    Praeruptorin E

    Calcium Channel Cardiovascular Disease
    Praeruptorin E is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin C is a calcium antagonist with pD2 ′ value of 5.2.
  • 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-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-N0596
    Panaxadiol

    20(R)-Panaxadiol

    Others Cancer
    Panaxadiol is found in the roots of Panax ginseng, activities neuroprotective and anti-tumour functions. Panaxadiol inhibits programmed cell death-ligand 1(PD-L1) expression and tumour proliferation.
  • HY-15378
    Talibegron hydrochloride

    ZD2079 hydrochloride

    Adrenergic Receptor Cardiovascular Disease
    Talibegron hydrochloride (ZD2079 hydrochloride) is a potent β3-adrenoceptor agonist with a pD2 of 3.72 on phenylephrine-preconstricted rat mesenteric artery. Talibegron hydrochloride has potent vasorelaxant effect.
  • HY-P1335
    CTAP

    Opioid Receptor Neurological Disease
    CTAP is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID).
  • HY-P1335A
    CTAP TFA

    Opioid Receptor Neurological Disease
    CTAP TFA is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID).
  • 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-16743
    Ibiglustat

    Venglustat; SAR402671; GZ402671

    Others Metabolic Disease
    Ibiglustat (Venglustat), a potential therapy for PD Parkinson’s disease, SRT in Fabry’s and Gaucher’s, is a selective, allosteric inhibitor of glucosylceramide synthase (GCS) with ability to cross the blood-brain barrier.
  • HY-129600
    MYCi361

    NUCC-0196361

    c-Myc Cancer
    MYCi361 (NUCC-0196361) is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 (NUCC-0196361) suppresses tumor growth and enhances anti-PD1 immunotherapy.
  • HY-123637
    Autotaxin-IN-1

    Phosphodiesterase (PDE) Inflammation/Immunology
    Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain.
  • HY-N0120A
    Polydatin

    Piceid

    Autophagy Apoptosis Mitophagy Inflammation/Immunology Cancer
    Polydatin (Piceid), extracted from the roots of Polygonum cuspidatum Sieb, a widely used traditional Chinese remedies, possesses anti-inflammatory activity in several experimental models. Polydatin (Piceid) inhibits G6PD and induces oxidative and ER stresses.
  • HY-135303
    GLPG1205

    GPR84 Inflammation/Immunology
    GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
  • HY-16743A
    Ibiglustat (L-Malic acid)

    Venglustat (L-Malic acid); SAR402671 (L-Malic acid); GZ402671 (L-Malic acid)

    Others Metabolic Disease
    Ibiglustat L-Malic acid (Venglustat L-Malic acid), a potential therapy for PD Parkinson’s disease, SRT in Fabry’s and Gaucher’s, is a selective, allosteric inhibitor of glucosylceramide synthase (GCS) with ability to cross the blood-brain barrier.
  • HY-138559
    GW604714X

    Mitochondrial Metabolism Neurological Disease
    GW604714X is a potent inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X is a highly specific mitochondrial pyruvate carrier (MPC) inhibitor with a Ki <0.1 nM. GW604714X also inhibits L-lactate transport by the plasma membrane monocarboxylate transporter (MCT1), but at concentrations more than 4 orders of magnitude greater than the MPC.
  • HY-116016
    Etilevodopa

    L-DOPA ethyl ester; Levodopa ethyl ester

    Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester), an ethyl-ester prodrug of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable prodrug as it facilitates CNS penetration and delivers dopamine.
  • HY-116016A
    Etilevodopa hydrochloride

    L-DOPA ethyl ester hydrochloride; Levodopa ethyl ester hydrochloride

    Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester) hydrochloride, an ethyl-ester prodrug of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa hydrochloride is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable prodrug as it facilitates CNS penetration and delivers dopamine.
  • HY-136220A
    AHR antagonist 5 hemimaleate

    Aryl Hydrocarbon Receptor Cancer
    AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39).
  • HY-136220
    AHR antagonist 5

    Aryl Hydrocarbon Receptor Cancer
    AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
  • HY-124729
    BL-918

    ULK Autophagy Neurological Disease
    BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.
  • HY-117290
    BMS-962212

    Factor Xa Cardiovascular Disease
    BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity.
  • HY-126147
    J22352

    HDAC Cancer
    J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1.
  • HY-W010342
    6-Aminonicotinamide

    Others Cancer
    6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP +-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM). 6-Aminonicotinamide interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, such as Cisplatin, in killing cancer cells.
  • HY-109052
    Atabecestat

    JNJ-54861911

    Beta-secretase Neurological Disease
    Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat (JNJ-54861911) is tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment.
  • HY-129601
    MYCi975

    NUCC-0200975

    c-Myc Cancer Inflammation/Immunology
    MYCi975 (NUCC-0200975) is an orally active MYC inhibitor, which disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 (NUCC-0200975) exhibits potent anti-tumor efficacy with good tolerability, increases tumor immune cell infiltration, and sensitizes tumors to anti-PD1 immunotherapy.
  • HY-138139A
    AXC-715 hydrochloride

    Toll-like Receptor (TLR) Inflammation/Immunology
    AXC-715 hydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1. AXC-715, compound D from WO2020190734A1, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants.
  • HY-16438
    RRx-001

    Apoptosis Parasite Cancer Infection Inflammation/Immunology
    RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.
  • HY-100022
    Tomivosertib

    eFT508

    MNK PD-1/PD-L1 Cancer
    Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines. Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance.
  • HY-136927
    MSA-2

    STING Cancer Inflammation/Immunology
    MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models.
  • HY-138742
    HPK1-IN-7

    MAP4K Cancer
    HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.
  • HY-117482
    BPN-15606

    γ-secretase Neurological Disease
    BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-117482A
    BPN-15606 besylate

    γ-secretase Neurological Disease
    BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-B0410S
    Pramipexole (N-Propyl-3,3,3-d3) (dihydrochloride)

    Dopamine Receptor Neurological Disease
    Pramipexole (N-Propyl-3,3,3-d3) dihydrochloride is the deuterium labeled Pramipexole. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).