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Targets Recommended: IKK

Results for "productlist/I" in MCE Product Catalog:

357

Inhibitors & Agonists

5

Screening Libraries

6

Dye Reagents

3

Biochemical Assay Reagents

45

Peptides

2

MCE Kits

1

Inhibitory Antibodies

100

Natural
Products

12

Recombinant Proteins

Cat. No. Product Name Target Research Area
  • HY-117793
    I-191

    Protease-Activated Receptor (PAR) Cancer
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
  • HY-P1768
    Urechistachykinin I

    Uru-TK I

    Bacterial Infection
    Urechistachykinin I (Uru-TK I), an invertebrate tachykinin-related peptides (TRPs) isolated from echiuroid worms, shows antimicrobial activities without a hemolytic effect.
  • HY-N2013
    Aristolactam I

    Aristololactam; Aristolactam

    Caspase Inflammation/Immunology
    Aristololactam I (AL-I), is the main metabolite of aristolochic acid I (AA-I), participates in the processes that lead to renal damage. Aristololactam I (AL-I) directly injures renal proximal tubule cells, the cytotoxic potency of AL-I is higher than that of AA-I and that the cytotoxic effects of these molecules are mediated through the induction of apoptosis in a caspase-3-dependent pathway.
  • HY-15167
    Glyoxalase I inhibitor

    Others Cancer
    Glyoxalase I inhibitor is a potent Glyoxalase I inhibitor, candidate for anticancer agents.
  • HY-N1939
    Icariside I

    Icarisid I

    Others Others
    Icariside I is a metabolite of Icarlin, which could regulate bone remodeling and is recognized as an effective agent for the treatment of osteoporosis.
  • HY-N0887
    Isoastragaloside I

    Isoastragaloside-I

    Others Metabolic Disease
    Isoastragaloside I is a natural compound from the medicinal herb Radix Astragali; possesses the activity of elevating adiponectin production.
  • HY-112134A
    (R)-CSN5i-3

    Others Others
    (R)-CSN5i-3 is the (R)-enantiomer of CSN5i-3. CSN5i-3 is a potent, selective and orally available inhibitor of CSN5.
  • HY-N0407
    Picroside I

    6'-Cinnamoylcatalpol

    STAT Inflammation/Immunology
    Picroside I is the major ingredient of Picrorhiza kurroa. Picrorhiza kurroa is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II. Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ.
  • HY-N0331
    Ziyuglycoside I

    MDM-2/p53 Apoptosis Cancer
    Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics. Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential drug candidate for treating triple-negative breast cancer (TNBC).
  • HY-B0175
    Toltrazuril

    BAY-i 9142

    Parasite Infection
    Toltrazuril (BAY-i 9142) is an antiprotozoal agent that acts upon Coccidia parasites.
  • HY-N7022
    Eclalbasaponin I

    Others Cancer
    Eclalbasaponin I is isolated from Eclipta prostrata L with antitumor activity. Eclalbasaponin I inhibits the proliferation of hepatoma cell smmc-7721 with an IC50 value of 111.1703 μg/ml.
  • HY-N5157
    Licorisoflavan I

    Others Others
    Licorisoflavan I, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch..
  • HY-N2286
    Kushenol I

    Others Others
    Kushenol I is a natural compound isolated from the roots of Sophora flavescens.
  • HY-107284
    Officinalisinin I

    Others Others
    Officinalisinin I is a steroidal saponin, isolated from Anemarrhena asphodeloides.
  • HY-N4213
    Anemarrhenasaponin I

    Others Others
    Anemarrhenasaponin I, a traditional Chinese medicine, is isolated from Anemarrhena asphodeloides Bunge.
  • HY-N0612
    Siamenoside I

    Others Others
    Siamenoside I is one of the mogrosides that has several kinds of bioactivities.
  • HY-N3030
    Sylvestroside I

    Others Others
    Sylvestroside I is an iridoid isolated from Acicarpha tribuloides.
  • HY-76293
    I2906

    Bacterial Infection
    I2906 showed antimycobacterial and cytotoxic activity against mycobacterium tuberculosis.
  • HY-N2541
    Gymnemic acid I

    Others Metabolic Disease
    Gymnemic acid I is a bioactive triterpene saponin found in Gymnema sylvestre. Gymnemic acid I decreases the apoptosis under the high glucose stress.
  • HY-15167A
    Glyoxalase I inhibitor free base

    Others Cancer
    Glyoxalase I inhibitor (free base) is a potent Glyoxalase I (GLO1) inhibitor, candidate for anticancer agents.
  • HY-110199
    TC-I 2014

    TRP Channel Neurological Disease
    TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.
  • HY-N0047
    Polyphyllin I

    JNK mTOR Akt PDK-1 Autophagy Apoptosis Cancer
    Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.
  • HY-100383
    BH3I-1

    BHI1; BH 3I1

    Bcl-2 Family MDM-2/p53 E1/E2/E3 Enzyme Cancer
    BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
  • HY-N7026
    Celosin I

    Others Metabolic Disease
    Celosin I, an oleanane-type triterpenoid saponin isolated from the seeds of Celosia argentea L, could be used as chemical markers for the quality control of C. argentea seeds. Celosin I exhibits significant hepatoprotective effect on carbon tetrachloride-induced and N,N-dimethylformamide-induced hepatotoxicity in mice.
  • HY-N0201
    Atractylenolide I

    Toll-like Receptor (TLR) JAK STAT Cancer
    Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
  • HY-N0745
    Senkyunolide I

    Caspase Inflammation/Immunology
    Senkyunolide I, isolated from Ligusticum chuanxiong Hort, is an anti-migraine compound. Senkyunolide I protects rat brain against focal cerebral ischemia-reperfusion injury by up-regulating p-Erk1/2, Nrf2/HO-1 and inhibiting caspase 3.
  • HY-N0360
    Dihydrotanshinone I

    Others Cardiovascular Disease
    Dihydrotanshinone I is a natural compound extracted from Salvia miltiorrhiza Bunge which has been widely used for treating cardiovascular diseases.
  • HY-N6889
    Rebaudioside I

    Others Others
    Rebaudioside I is a natural non-claoric sweetener isolated from S. rebaudiana Morita.
  • HY-N7141
    Spiramycin I

    Parasite Infection
    Spiramycin I, isolated from Streptomyces ambofaciens, is a macrolide antibiotic and antiparasitic.
  • HY-N5095
    Eupteleasaponin I

    Others Others
    Eupteleasaponin I is a component of Euptelea polyandra, may has gastroprotective activity.
  • HY-B1919
    Dihydroisotanshinone I

    STAT Cancer
    Dihydroisotanshinone I is a bioactive compound present in a widely used traditional Chinese medicine named danshen.
  • HY-112134
    CSN5i-3

    Others Cancer
    CSN5i-3 is a potent, selective and orally available inhibitor of CSN5, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM.
  • HY-100341
    M2I-1

    Others Others
    M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC).
  • HY-18771
    O4I1

    Oct3/4 Others
    O4I1 is as a potent Oct3/4 inducer.
  • HY-107400
    B I09

    IRE1 Cancer
    B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
  • HY-135680
    I-OMe-Tyrphostin AG 538

    I-OMe-AG 538

    IGF-1R Cancer Metabolic Disease
    I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
  • HY-N5042
    Forsythoside I

    Others Inflammation/Immunology
    Forsythoside I, a caffeoyl phenylethanoid glycoside (CPG) isolated from the fruits of Forsythia suspense (Thunb.) Vahl, may possesses anti-inflammatory activities.
  • HY-P0324
    Parasin I

    Bacterial Infection
    Parasin I is a 19-amino acid histone H2A-derived peptide isolated from the skin of the catfish, and shows antimicrobial activity.
  • HY-N4246
    Bacopaside I

    Others Neurological Disease
    Bacopaside I, a saponin isolated from Bacopa monniera, exbibits antioxidant properties and free radical scavenging capacity and exerts antidepressant-like effect.
  • HY-N2102
    Tenacissoside I

    Others Others
    Tenacissoside I is a C21 steroid from the Marsdenia tenacissima, which is detected at relatively high level in M. tenacissima.
  • HY-W008452
    H-Tyr(3-I)-OH

    Endogenous Metabolite Others
    H-Tyr(3-I)-OH is an effective tyrosine hydroxylase inhibitor.
  • HY-50713
    Calcium-Sensing Receptor Antagonists I

    CaSR Others
    Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
  • HY-P1593
    Mini Gastrin I, human

    Cholecystokinin Receptor Cancer Endocrinology
    Mini Gastrin I, human is a shorter version of human gastrin, consists of amino acids 5-17 of the parent peptide.
  • HY-18772
    O4I2

    Oct3/4 Others
    O4I2 is a potent Oct3/4 inducer in various human cell lines including human fibroblasts.
  • HY-18975
    I-BRD9

    Epigenetic Reader Domain Cancer
    I-BRD9 is the first selective cellular chemical probe for BRD9 (pIC50=7.3).
  • HY-N7052
    Tubulysin I

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin I is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin I is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-125733
    Thiocillin I

    Bacterial Infection
    Thiocillin I is a thiopeptide antibiotic and has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Thiocillin I against S. aureus 1974149, E. faecalis 1674621, B. subtilis ATCC 6633 and S. pyogenes 1744264 are 2 μg/mL, 0.5 μg/mL, 4 μg/mL and 0.5 μg/mL, respectively.
  • HY-P1542
    Urotensin I

    Catostomus urotensin I

    CRFR Cardiovascular Disease Endocrinology
    Urotensin I is, 41-aa neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF and mCRF receptors, respectively.
  • HY-N6649
    Isotanshinone I

    Glucosidase Infection
    Isotanshinone I has inhibitory activity against α-glucosidase and formation of AGE, with IC50s of 1.13, 0.432 μM for α-glucosidase and AGE, respectively.
  • HY-N0432
    Astragaloside I

    Astrasieversianin IV; Cyclosieversioside B

    Others Others
    Astragaloside I is a natural product isolated from Astragalus.
  • HY-N5004
    Guanfu base I

    Acorine

    Others Cardiovascular Disease
    Guanfu base I (Acorine) is an active metabolite of Guanfu base A, isolated from Aconitum coreanum, and has a potent anti-arrhythmic effect.
  • HY-N6724
    Altertoxin I

    Dihydroalterperylenol

    Others Metabolic Disease
    Altertoxin I (Dihydroalterperylenol) is a quinone-type mycotoxin produced by Alternaria alternata fungi, which is mutagenic and cytotoxic, and can weakly disrupts metabolic communication.
  • HY-N0134
    Tanshinone I

    Tanshinone A

    Phospholipase Cardiovascular Disease Cancer
    Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC50=11 μM) and rabbit recombinant cPLA2 (IC50=82 μM).
  • HY-124691
    D-I03

    DNA/RNA Synthesis Cancer
    D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 µM and 8 µM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin.
  • HY-13418A
    Dorsomorphin

    BML-275; Compound C

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin (BML-275; Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.
  • HY-P1593A
    Mini Gastrin I, human TFA

    Cholecystokinin Receptor Cancer Endocrinology
    Mini Gastrin I, human (TFA) is a shorter version of human gastrin, consists of amino acids 5-17 of the parent peptide.
  • HY-13329
    IRAK-1-4 Inhibitor I

    IRAK-1/4 Inhibitor I

    IRAK Inflammation/Immunology
    IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.
  • HY-P0324A
    Parasin I (TFA)

    Bacterial Infection
    Parasin I (TFA) is a 19-amino acid histone H2A-derived peptide isolated from the skin of the catfish, and shows antimicrobial activity.
  • HY-I0512
    Sofosbuvir impurity I

    HCV Infection
    Sofosbuvir impurity I, an diastereoisomer of sofosbuvir, is the impurity of sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.
  • HY-N6854
    Mogroside I A1

    Others Cancer Metabolic Disease
    Mogroside I A1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
  • HY-N6853
    Mogroside I E1

    Others Cancer Metabolic Disease
    Mogroside I E1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
  • HY-19541
    I-CBP112

    Histone Acetyltransferase Epigenetic Reader Domain Cancer
    I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.
  • HY-13032B
    Molibresib besylate

    GSK 525762C; I-BET 762 besylate

    Epigenetic Reader Domain Cancer
    Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
  • HY-N0890
    Tubeimoside I

    Tubeimoside-1; Lobatoside-H

    Apoptosis Cancer
    Tubeimoside I(Lobatoside-H) is an extract from Chinese herbal medicine Bolbostemma paniculatum (MAXIM.
  • HY-103002
    SU5408

    VEGFR2 Kinase Inhibitor I

    VEGFR Cardiovascular Disease
    SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
  • HY-B1411
    i-Inositol

    myo-Inositol; meso-Inositol

    Endogenous Metabolite Others
    i-Inositol is a chemical compound, associated lipids are found in many foods, in particular fruit, especially cantaloupe and oranges.
  • HY-135748
    Polyinosinic-polycytidylic acid sodium

    Poly(I:C) sodium

    Toll-like Receptor (TLR) Apoptosis Cancer Inflammation/Immunology
    Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis.
  • HY-13418
    Dorsomorphin dihydrochloride

    BML-275 dihydrochloride; Compound C dihydrochloride

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy.
  • HY-P1336
    Deltorphin I

    Deltorphin 1; Deltorphin C

    Opioid Receptor Neurological Disease
    Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.
  • HY-107613
    R 59-022

    DKGI-I; Diacylglycerol kinase inhibitor I

    PKC 5-HT Receptor Inflammation/Immunology
    R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
  • HY-13032
    Molibresib

    I-BET762; GSK525762; GSK525762A

    Epigenetic Reader Domain Cancer
    Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
  • HY-13867
    Bisindolylmaleimide I

    GF109203X; Go 6850

    PKC Metabolic Disease Cancer
    Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
  • HY-N1405
    Cucurbitacin I

    Elatericin B; JSI-124; NSC-521777

    STAT JAK Cancer
    Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
  • HY-N0011
    Baohuoside I

    Icariin-II; Icariside-II

    CXCR Apoptosis Cancer Inflammation/Immunology Endocrinology
    Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
  • HY-13235
    I-BET151

    GSK1210151A

    Epigenetic Reader Domain Cancer
    I-BET151 is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
  • HY-18964
    MG-101

    Calpain inhibitor I; Ac-LLnL-CHO; ALLN

    Proteasome Cancer
    MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively.
  • HY-16721
    Cyclopropavir

    Filociclovir; ZSM-I-62; MBX-400

    CMV HSV Infection
    Cyclopropavir (Filociclovir; ZSM-I-62; MBX-400) is a broad-spectrum anti-herpesvirus compound, has good antiviral activity against cytomegalovirus (CMV), herpes simplex virus (HHV)-6 and HHV-8 with EC50s of 0.7 μM to 8 μM.
  • HY-N0170
    Indole-3-carbinol

    I3C; 3-Indolemethanol

    NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Cancer
    Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).
  • HY-A0126A
    Epoprostenol sodium

    Prostaglandin I2 sodium salt; Prostacyclin sodium salt; Flolan

    Others Cardiovascular Disease
    Epoprostenol sodium (Prostaglandin I2 (sodium salt)), the synthetic form of the natural prostaglandin derivative prostacyclin (prostaglandin I2), is registered worldwide for the treatment of Pulmonary arterial hypertension (PAH). Epoprostenol sodium is used in pulmonary hypertension and transplantation as a potent inhibitor of platelet aggregation.
  • HY-107443
    I-BET762 carboxylic acid

    Molibresib carboxylic acid; GSK525762A carboxylic acid; PROTAC BRD4-binding moiety 2

    Ligand for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.
  • HY-P0054A
    Glucagon-Like Peptide (GLP) I (7-36), amide, human

    Human GLP-1-(7-36)-amide

    Glucagon Receptor Metabolic Disease
    Glucagon-Like Peptide (GLP) I (7-36), amide, human (Human GLP-1-(7-36)-amide) is a physiological incretin hormone that stimulates insulin secretion.
  • HY-100738
    Ubiquitin Isopeptidase Inhibitor I, G5

    NSC144303

    Apoptosis Cancer
    Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
  • HY-N0510
    Aristolochic acid A

    Aristolochic acid I; TR 1736

    NF-κB Cancer
    Aristolochic acid A (Aristolochic acid I; TR 1736) is the main component of plant extract Aristolochic acids, which are found in various herbal plants of genus Aristolochia and Asarum. Aristolochic acid A significantly reduces both activator protein 1 (AP-1) and NF-κB activities. Aristolochic acid A reduces BLCAP gene expression in human cell lines.
  • HY-18600A
    Azimilide Dihydrochloride

    NE-10064 Dihydrochloride

    Potassium Channel Cardiovascular Disease
    Azimilide Dihydrochloride (NE-10064 Dihydrochloride) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
  • HY-18600
    Azimilide

    NE-10064

    Potassium Channel Cardiovascular Disease
    Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
  • HY-112275
    TNF-α-IN-1

    TNF Receptor Cancer Inflammation/Immunology
    TNF-α-IN-1 is a TNF-α inhibitor extracted from patent US20030096841A1, compound example I-7.
  • HY-16562
    Irinotecan

    (+)-Irinotecan; CPT-11

    Topoisomerase Autophagy Cancer
    Irinotecan is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
  • HY-103660
    18:0 LYSO-PE

    Stearoyl lysophosphatidylethanolamine

    Others Neurological Disease
    18:0 LYSO-PE is an agent that can induce [Ca 2+]i increase.
  • HY-116448
    Metaflumizone

    BAS-320I

    Parasite Sodium Channel Infection
    Metaflumizone is a semicarbazone insecticide, acts as a potent sodium channel blocker.
  • HY-N6675
    Gardenia yellow

    Crocin I

    Sirtuin Neurological Disease Cancer
    Gardenia yellow is an active member of crocin, increases mRNA expression of SIRT3, and acts as an orally active antidepressant agent.
  • HY-N1166
    Tephrosin

    Deguelinol I; Hydroxydeguelin

    EGFR Cancer
    Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors.
  • HY-N0864
    Macranthoidin B

    Macranthoiside I

    Others Cancer
    Macranthoidin B is a major bioactive saponin in rat plasma after oral administration of extraction of saponins from Flos Lonicerae.
  • HY-N6790
    Nonactin

    Ammonium ionophore I

    Potassium Channel Mitochondrial Metabolism Apoptosis Cancer Infection
    Nonactin is a naturally occurring macrotetrolide antibiotic from Streptomyces griseus. Nonactin acts as an ionophore for monovalent cations, including K +, and NH4 +. Nonactin is able to uncouple the oxidative phosphorylation of mitochondria. Nonactin selectively induces apoptosis in cell lines harboring active mutant β-catenin. Nonactin inhibits the surface expression of endogenous HSP60.
  • HY-101647
    Intoplicine

    Topoisomerase Cancer
    Intoplicine is a DNA topoisomerase I and II inhibitor.
  • HY-N7089
    Benzoyleneurea

    Bacterial Infection
    Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors.
  • HY-15481
    KU14R

    Insulin Receptor Metabolic Disease Endocrinology
    KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.
  • HY-10432A
    A 83-01 sodium salt

    TGF-β Receptor Cancer
    A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-10432
    A 83-01

    TGF-β Receptor Cancer
    A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-16568
    Irinotecan hydrochloride trihydrate

    Topoisomerase Autophagy Cancer
    Irinotecan hydrochloride trihydrate is a topoisomerase I inhibitor with antitumor activity.
  • HY-14821
    Namitecan

    ST-1968

    Topoisomerase Cancer
    Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
  • HY-U00232
    Bidisomide

    SC40230

    Others Cardiovascular Disease
    Bidisomide (SC40230) is a class I antiarrhythmic agent.
  • HY-13217
    Vanoxerine dihydrochloride

    GBR-12909 dihydrochloride; I893 dihydrochloride

    Dopamine Transporter Neurological Disease
    Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).
  • HY-130518
    Cdc7-IN-6

    CDK Cancer
    Cdc7-IN-6 (compound I-D) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity.
  • HY-100876
    GGTI298

    Ras Apoptosis Cancer
    GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
  • HY-15871
    GGTI298 Trifluoroacetate

    Apoptosis Ras Cancer
    GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.
  • HY-15466
    CH5132799

    PI3K Cancer
    CH5132799 is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
  • HY-125817
    BI-3406

    Others Others
    BI-3406 (compound I-6) is a Son of Sevenless 1 (SOS1) inhibitor with an IC50 of 6 nM. BI-3406 has anticancer activity.
  • HY-12484
    BMH-21

    DNA/RNA Synthesis Cancer
    BMH-21 is a small molecule DNA intercalator that binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription; does not cause phosphorylation of H2AX.
  • HY-120350
    BI-1347

    CDK Cancer
    BI-1347 is a potent CDK8 inhibitor extracted from patent WO2017202719A1, product I-003, has an IC50 of 1.1 nM.
  • HY-101692
    AZ-1355

    Prostaglandin Receptor Metabolic Disease Endocrinology
    AZ-1355 is an effctive lipid-lowering compound, which also inhibits platelet aggregation in vivo and elevates the prostaglandin I2/thromboxane A2 ratio in vitro.
  • HY-113970A
    Nebracetam hydrochloride

    WEB 1881 FU hydrochloride

    mAChR Neurological Disease
    Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca 2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca 2+]i.
  • HY-128829
    Kv3 modulator 2

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 2 (formula (I)) is a potent Kv3 channels modulator extracted from patent WO2018109484A1, compound formula (I) , has analgesic activity and is used in the prophylaxis or treatment of related disorders.
  • HY-16562A
    Irinotecan hydrochloride

    CPT-11 hydrochloride; Camptothecin 11 hydrochloride

    Topoisomerase Autophagy Cancer
    Irinotecan hydrochloride is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.
  • HY-17020A
    Miglustat hydrochloride

    N-Butyldeoxynojirimycin, Hydrochloride; NB-DNJ hydrochloride; OGT918 hydrochloride

    Others Neurological Disease
    Miglustat hydrochloride is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1).
  • HY-U00159
    McN3716

    Methyl palmoxirate; NSC359682

    Others Metabolic Disease
    McN3716 is a carnitine palmitoyltransferase I (CPT-1) inhibitor.
  • HY-16228
    Genz-644282

    Topoisomerase Cancer
    Genz-644282 is a non-camptothecin topoisomerase I inhibitor, used for cancer research.
  • HY-13768A
    Topotecan Hydrochloride

    SKF 104864A Hydrochloride; NSC 609669 Hydrochloride

    Topoisomerase Apoptosis Autophagy Cancer
    Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.
  • HY-112037A
    IACS-10759 Hydrochloride

    Apoptosis Cancer
    IACS-10759 Hydrochloride is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).
  • HY-18712
    BG45

    Apoptosis HDAC Cancer
    BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM).
  • HY-U00432
    S-MTC

    NO Synthase Neurological Disease
    S-MTC is a selective type I nitric oxide synthase (NOS) inhibitor.
  • HY-14812
    Karenitecin

    Cositecan; BNP 1350

    Topoisomerase Cancer
    Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.
  • HY-112037
    IACS-10759

    Apoptosis Cancer
    IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).
  • HY-N5028
    Enmein

    Others Inflammation/Immunology
    Enmein is isolated from I. serra with immunosuppressive effect.
  • HY-B0483
    Tioxolone

    Carbonic Anhydrase Metabolic Disease
    Tioxolone, a metalloenzyme carbonic anhydrase I inhibitor, is an anti-acne preparation.
  • HY-100309
    9-amino-CPT

    9-amino-20(S)-camptothecin

    Topoisomerase Cancer
    9-Aminocamptothecin is a topoisomerase I inhibitor with potent anticancer activity.
  • HY-16560
    Camptothecin

    Campathecin; (S)-(+)-Camptothecin; CPT

    Topoisomerase Apoptosis ADC Cytotoxin Cancer
    Camptothecin (Campathecin) is a potent DNA enzyme topoisomerase I inhibitor, with an IC50 of 679 nM.
  • HY-118916A
    FTI-2148 diTFA

    Farnesyl Transferase Cancer
    FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
  • HY-N0822
    Shikonin

    C.I. 75535; Isoarnebin 4

    Chloride Channel Pyruvate Kinase NF-κB HIV TNF Receptor Cancer
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway.
  • HY-13686
    PQ401

    Apoptosis IGF-1R Cancer
    PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis.
  • HY-16231
    GGTI-2418

    Others Cancer
    GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors.
  • HY-N0925
    Tetrahydroberberine

    Canadine

    Dopamine Receptor Neurological Disease
    Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00).
  • HY-100110
    KNK437

    Heat Shock Protein Inhibitor I

    HSP Cancer
    KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
  • HY-13748
    Silibinin

    Silybin; Silibinin A; Silymarin I

    Autophagy Reactive Oxygen Species Cancer
    Silibinin (Silybin), an effective anti-cancer and chemopreventive agent, has been shown to exert multiple effects on cancer cells, including inhibition of both cell proliferation and migration.
  • HY-N0099
    Astragaloside A

    Astramembrannin I; Astragalin A

    Apoptosis Cancer
    Astragaloside A is one of the major active constituents of Astragalus membranaceus in Traditional Chinese Medicine; has been widely used to treat ischemic diseases.
  • HY-10324
    D4476

    Casein Kinase I Inhibitor

    Casein Kinase Apoptosis Autophagy Cancer
    D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC50 value of 0.3 μM in vitro.
  • HY-13217A
    Vanoxerine

    GBR 12909; I893

    Dopamine Transporter Neurological Disease
    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT).
  • HY-13960
    GSK1324726A

    I-BET726

    Apoptosis Epigenetic Reader Domain Cancer
    GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
  • HY-130516
    Cdc7-IN-4

    CDK Cancer
    Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-10071
    Y-27632

    ROCK Apoptosis Cancer
    Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively, which primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
  • HY-130517
    Cdc7-IN-5

    CDK Cancer
    Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-130515
    Cdc7-IN-3

    CDK Cancer
    Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-75161
    (-)-Menthol

    TRP Channel Cancer
    (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca 2+-permeable nonselective cation channel, to increase [Ca 2+]i. Antitumor activity.
  • HY-130519
    Cdc7-IN-7

    CDK Cancer
    Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-15320
    NBI-74330

    CXCR Inflammation/Immunology Endocrinology
    NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of ( 125I)CXCL10 and ( 125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
  • HY-10431
    SB-431542

    TGF-β Receptor Cancer
    SB-431542 is a potent and selective inhibitor of ALK5/TGF-β type I Receptor with an IC50 value of 94 nM.
  • HY-P1533
    CRF, bovine

    Corticotropin Releasing Factor bovine

    CRFR Inflammation/Immunology Endocrinology
    CRF, bovine is a potent agonist of CRF receptor, and displaces [ 125I-Tyr]ovine CRF with a Ki of 3.52 nM.
  • HY-N5038
    Mauritianin

    Topoisomerase Others
    Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor.
  • HY-U00248
    LMP744

    MJ-III65; NSC706744

    Topoisomerase Cancer
    LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
  • HY-100486
    BTTAA

    Others Others
    BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.
  • HY-13566A
    Belotecan hydrochloride

    CKD-602

    Topoisomerase Cancer
    Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic and water-soluble camptothecin derivative.
  • HY-15144
    Trichostatin A

    TSA

    HDAC Cancer
    Trichostatin A (TSA) is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.
  • HY-100495
    FT011

    Others Inflammation/Immunology
    FT011 is an anti-fibrotic agent, reduces mRNA expression of collagens I and III and inhibits collagen synthesis.
  • HY-16273A
    L-778123 hydrochloride

    L-778,123 hydrochloride

    Farnesyl Transferase Cancer
    L-778123 hydrochloride is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.
  • HY-U00314
    Anti-neurodegeneration agent 1

    Others Neurological Disease
    Anti-neurodegeneration agent 1 a neurodegeneration-targeting compound extracted from patent WO2008039514A1, Compound I.
  • HY-13631
    Exatecan

    DX-8951

    Topoisomerase Cancer
    Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
  • HY-N2331
    Proscillaridin A

    Topoisomerase Cancer
    Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively.
  • HY-10943
    GNF-7

    Bcr-Abl Cancer
    GNF-7 inhibits Bcr-Abl WT and Bcr-Abl T315I with IC50 of 133 nM and 61 nM, respectively.
  • HY-13631A
    Exatecan Mesylate

    DX8951f

    Topoisomerase Cancer
    Exatecan Mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
  • HY-13783
    BIBF0775

    TGF-β Receptor Cancer
    BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
  • 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-12075
    LY2109761

    TGF-β Receptor Autophagy Cancer
    LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
  • HY-Y0801
    2,6-Dihydroxybenzoic acid

    Endogenous Metabolite Others
    2,6-Dihydroxybenzoic acid is a secondary metabolite of salicylic acid which has been hydrolyzed by liver enzymes during phase I metabolism.
  • HY-17020
    Miglustat

    N-Butyldeoxynojirimycin; NB-DNJ; OGT918

    Others Neurological Disease
    Miglustat(OGT918) is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1).
  • HY-U00248A
    LMP744 hydrochloride

    MJ-III65 hydrochloride; NSC706744 hydrochloride

    Topoisomerase Cancer
    LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
  • HY-W015346
    Desaminotyrosine

    3-(4-Hydroxyphenyl)propionic acid

    Influenza Virus Endogenous Metabolite Infection
    Desaminotyrosine is a microbially associated metabolite protecting from influenza through augmentation of type I interferon signaling.
  • HY-13758
    TAS-103

    BMS-247615

    Topoisomerase Cancer
    TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
  • HY-100372
    E4CPG

    mGluR Neurological Disease
    E4CPG is a novel group I/group II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG .
  • HY-100052
    6-Hydroxybentazon

    6-Hydroxybentazone

    Others Others
    6-Hydroxybentazon is a phase I metabolite of bentazone, and bentazone is a chemical for use in herbicides.
  • HY-13226
    Galunisertib

    LY2157299

    TGF-β Receptor Cancer
    Galunisertib (LY2157299) is a oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
  • HY-13618
    Edotecarin

    J 107088; PF 804950

    Topoisomerase Cancer
    Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM.
  • HY-15775
    Arginase inhibitor 1

    Arginase Cancer
    Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.
  • HY-N6905
    Acetylarenobufagin

    HIF/HIF Prolyl-Hydroxylase Cancer
    Acetylarenobufagin is a steroidal hypoxia inducible factor-1 (HIF-I) modulator.
  • HY-15586
    L67

    DNA Ligase Inhibitor

    DNA/RNA Synthesis Cancer
    L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM.
  • HY-12777
    Asivatrep

    PAC-14028

    TRP Channel Inflammation/Immunology
    Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.
  • HY-13758A
    TAS-103 dihydrochloride

    BMS-247615 dihydrochloride

    Topoisomerase Cancer
    TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
  • HY-B1756
    Rotenone

    Mitochondrial Metabolism Autophagy Apoptosis Neurological Disease Cancer
    Rotenone is an mitochondrial electron transport chain complex I inhibitor. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.
  • HY-126332
    NED-3238

    Arginase Metabolic Disease
    NED-3238 is a highly potent arginase I and II inhibitor with IC50 values of 1.3 nM and 8.1 nM, respectively.
  • HY-111634
    Epsilon-momfluorothrin

    Others Cancer
    Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats.
  • HY-112729
    HC-056456

    3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide

    Others Others
    HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na +]i rise is slowed by HC-056456 (IC50~3 µM).
  • HY-W012382
    N-Acetyl-L-tyrosine

    Endogenous Metabolite Metabolic Disease
    N-Acetyl-L-tyrosine originates from tyrosine through an AA acetylase, is associated with aromatic L-amino acid decarboxylase deficiency and tyrosinemia I.
  • HY-114161
    H-Val-Pro-Pro-OH

    Angiotensin Receptor Metabolic Disease Inflammation/Immunology Endocrinology
    H-Val-Pro-Pro-OH, a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM.
  • HY-16711
    SB225002

    CXCR Inflammation/Immunology Endocrinology Cancer
    SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
  • HY-P1533A
    CRF, bovine TFA

    Corticotropin Releasing Factor bovine TFA

    CRFR Inflammation/Immunology Endocrinology
    CRF, bovine (TFA) is a potent agonist of CRF receptor, and displaces [ 125I-Tyr]ovine CRF with a Ki of 3.52 nM.
  • HY-U00068
    PPARα-MO-1

    PPAR Metabolic Disease
    PPARα-MO-1 is a potent PPARα modulator extracted from patent WO/2004/110982A1, formula I.
  • HY-13277
    IRAK inhibitor 3

    IRAK Inflammation/Immunology
    IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.
  • HY-15542A
    FRAX597

    PAK Cancer
    FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
  • HY-113166
    Dodecanoylcarnitine

    Endogenous Metabolite Metabolic Disease
    Dodecanoylcarnitine is present in fatty acid oxidation disorders such as long-chain acyl CoA dehydrogenase deficiency, carnitine palmitoyltransferase I/II deficiency, and is also associated with celiac disease.
  • HY-128575
    BNC375

    nAChR Neurological Disease
    BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM.
  • HY-78349
    A 77-01

    TGF-β Receptor Cancer
    A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
  • HY-113005
    Glutarylcarnitine

    Endogenous Metabolite Metabolic Disease
    Glutarylcarnitine is the diagnostic metabolite for malonic aciduria and glutaric aciduria type I monitored in most tandem mass spectrometry newborn screening programmes.
  • HY-13432
    Nanatinostat

    CHR-3996

    HDAC Cancer
    Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM.
  • HY-12163
    Entinostat

    MS-275; SNDX-275

    HDAC Apoptosis Autophagy Cancer
    Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively.
  • HY-114161A
    H-Val-Pro-Pro-OH TFA

    Angiotensin Receptor Metabolic Disease Inflammation/Immunology Endocrinology
    H-Val-Pro-Pro-OH (TFA), a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM.
  • HY-N0275
    (±)-10-Hydroxycamptothecin

    (±)-10-HCPT

    Topoisomerase Cancer
    (±)-10-Hydroxycamptothecin, an indole alkaloid isolated from Camptotheca acuminate, inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.
  • HY-13462
    LY-364947

    HTS466284

    TGF-β Receptor Cancer
    LY-364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
  • HY-111451
    ATR inhibitor 1

    ATM/ATR Cancer
    ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a Ki value below 1 µΜ.
  • HY-19637
    SW044248

    Topoisomerase Cancer
    SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
  • HY-18623
    VI 16832

    Others Cancer
    VI 16832 is a broad spectrum Type I kinase inhibitor which can be used as an enrichment tool for the comparative expression analysis of protein kinases in different cancer cell lines.
  • HY-100223
    Calpeptin

    Cathepsin Apoptosis Proteasome Inflammation/Immunology
    Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.
  • HY-N0167
    Gynostemma Extract

    Ginsenoside C-Mx1; Gynosaponin I; Gypenoside IX

    Others Cancer
    Gynostemma Extract (Ginsenoside C-Mx1) is a natural product.
  • HY-15146
    NSC 74859

    S3I-201

    STAT Cancer
    NSC 74859 is a selective Stat3 inhibitor with an IC50 of 86 μM.
  • HY-14394
    TBB

    NSC 231634; Casein Kinase II Inhibitor I

    Casein Kinase Cancer
    TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
  • HY-15508
    JANEX-1

    WHI-P131; Jak3 inhibitor I

    JAK Cancer
    JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
  • HY-101489
    GZD856

    PDGFR Bcr-Abl Cancer
    GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities. Also a Bcr-Abl T315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant.
  • HY-128704A7
    c-Kit-IN-3 tartrate

    c-Kit Cancer
    c-Kit-IN-3 tartrate (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC50 of 4 nM) and a broad spectrum of drug-resistant mutants (IC50 of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability.
  • HY-114170
    ML604440

    Proteasome Inflammation/Immunology
    ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
  • HY-N2198
    Podocarpusflavone A

    Topoisomerase Apoptosis Cancer
    Podocarpusflavone A is a DNA topoisomerase I inhibitor, have moderated anti-proliferative activity induce cell apoptosis in MCF-7, is developing anti-tumor drugs target: DNA topoisomerase I In vitro: podocarpusflavone-A show significant inhibitions against DLD, KB, MCF-7, HEp-2 tumor cell lines (ED50 4.56-16.24 μg/mL) and induce cell apoptosis in MCF-7 via mainly sub-G1/S phase arrest.
  • HY-128704A1
    c-Kit-IN-3 hydrochloride

    c-Kit Cancer
    c-Kit-IN-3 hydrochloride (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC50 of 4 nM) and a broad spectrum of drug-resistant mutants (IC50 of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability.
  • HY-W009310
    9-cis-Retinal

    Endogenous Metabolite Others
    9-cis-Retinal is a natural retinoid. Dietary 9-cis-β-carotene generates 9-cis-retinoids via cleavage into 9-cis-retinal. 9-cis Retinal binds to cellular retinol-binding protein-I (CRBP-I) and CRBP-II with Kds of 8 nM and 5 nM, respectively. 9-cis-Retinal expedites differentiation and maturation of rod photoreceptors in retinal organoids.
  • HY-N4237
    Saikogenin D

    Prostaglandin Receptor Potassium Channel Inflammation/Immunology
    Saikogenin D is isolated from Bupleurum chinense, has anti-inflammatory effects. Saikogenin D activates epoxygenases that converts arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and the metabolites secondarily inhibit prostaglandin E2 (PGE2) production. Saikogenin D results in an elevation of [Ca 2+]i due to Ca 2+ release from intracellular stores.
  • HY-129966
    PROTAC IRAK4 degrader-1

    PROTAC IRAK Cancer
    PROTAC IRAK4 degrader-1 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively.
  • HY-128704A5
    c-Kit-IN-3 D-tartrate

    c-Kit Cancer
    c-Kit-IN-3 (D-tartrate) (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC50 of 4 nM) and a broad spectrum of drug-resistant mutants (IC50 of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability.
  • HY-13522
    Fimepinostat

    CUDC-907

    PI3K Apoptosis HDAC Cancer
    Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
  • HY-70063
    Buparlisib

    NVP-BKM120; BKM120

    Apoptosis PI3K Cancer
    Buparlisib (NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
  • HY-112951
    ChX710

    STING Cancer
    ChX710 could prime the type I interferon response to cytosolic DNA, which induces the ISRE promoter sequence, specific cellular Interferon-Stimulated Genes (ISGs), and the phosphorylation of Interferon Regulatory Factor (IRF) 3.
  • HY-13555
    β-Lapachone

    ARQ-501; NSC-26326

    Topoisomerase Autophagy Apoptosis Cancer
    β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.
  • HY-114233
    MC-GGFG-DX8951

    Drug-Linker Conjugates for ADC Cancer
    MC-GGFG-DX8951 is a drug-linker conjugate for ADC with antitumor activity by using DX8951 (a DNA topoisomerase I inhibitor), linked via the protease cleavable MC-GGFG linker.
  • HY-N0642
    α-L-Rhamnose monohydrate

    Others Infection Metabolic Disease Cancer
    α-L-Rhamnose monohydrate is a component of the plant cell wall pectic polysaccharides rhamnogalacturonan I and rhamnogalacturonan II. α-L-Rhamnose monohydrate is also a component of bacterial polysaccharides where it plays an important role in pathogenicity.
  • HY-10964
    Vadimezan

    DMXAA; ASA-404

    STING Interleukin Related Cancer
    Vadimezan (DMXAA; ASA-404), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines.
  • HY-13955
    Telmisartan

    BIBR 277

    Angiotensin Receptor Autophagy Cardiovascular Disease Endocrinology
    Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
  • HY-A0276
    Gentamicin sulfate

    Bacterial Infection
    Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC50 of 0.57 mM.
  • HY-100954
    2,4-Diamino-6-hydroxypyrimidine

    Others Inflammation/Immunology
    2,4-Diamino-6-hydroxypyrimidine is a specific GTP cyclohydrolase I inhibitor (the rate-limiting enzyme in de novo pterin synthesis), blocks BH4 synthesis and suppresses NO production.
  • HY-13631D
    Dxd

    Exatecan derivative for ADC

    Topoisomerase ADC Cytotoxin Cancer
    Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
  • HY-16134A
    Celgosivir hydrochloride

    MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride

    Glucosidase HCV HIV Infection
    Celgosivir hydrochloride (MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
  • HY-P1016A
    BQ-3020 TFA

    Endothelin Receptor Cardiovascular Disease Endocrinology
    BQ-3020 (TFA) is a selective agonist of ETB receptor, inhibits [ 125I]ET-1 binding to ETB receptor with an IC50 of 0.2 nM in cerebellum, and causes vasoconstriction.
  • HY-N2217
    Rotundic acid

    Akt mTOR p38 MAPK Apoptosis Inflammation/Immunology Cardiovascular Disease Cancer
    Rotundic acid, a triterpenoid obtained from I. rotunda, induces DNA damage and cell apoptosis in hepatocellular carcinoma through AKT/mTOR and MAPK Pathways. Rotundic acid possesses anti-inflammatory and cardio-protective abilities.
  • HY-114192
    TGFβRI-IN-1

    TGF-β Receptor Cancer
    TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .
  • HY-18819
    BCR-ABL-IN-2

    Bcr-Abl Cancer
    BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1 native and ABL1 T315I, respectively.
  • HY-19348
    Pimelic Diphenylamide 106

    RGFA-8; TC-H 106; Histone Deacetylase Inhibitor VII

    HDAC Cancer
    Pimelic Diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and 370 nM, respectively), demonstrating no activity against class II HDACs.
  • HY-13592
    HDAC-IN-7

    Chidamide impurity

    HDAC Cancer
    HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.
  • HY-12293
    LY2857785

    Apoptosis CDK Cancer
    LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
  • HY-128589
    CHMFL-KIT-033

    c-Kit Cancer
    CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM.
  • HY-16100
    BI99179

    Fatty Acid Synthase (FAS) Cancer Metabolic Disease
    BI99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats.
  • HY-100183
    GSK2239633A

    CCR Inflammation/Immunology Endocrinology
    GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [ 125I]-TARC to human CCR4 with a pIC50 of 7.96 ± 0.11.
  • HY-119370
    CHMFL-ABL-121

    Bcr-Abl Apoptosis Cancer
    CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively.
  • HY-13513
    U-104

    NSC-213841; MST-104

    Carbonic Anhydrase Cancer
    U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM; low inhibition for CA I and CA II.
  • HY-10339
    KW-2449

    FLT3 FGFR Bcr-Abl Apoptosis Aurora Kinase Cancer
    KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABL T315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
  • HY-13704
    SN-38

    NK012

    Topoisomerase ADC Cytotoxin Autophagy Cancer
    SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
  • HY-12508
    CMPDA

    iGluR Neurological Disease
    CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.4 ± 4.2 nM/63.4 ± 5.6 nM for GluA2i/GluA2o receptor.
  • HY-16134
    Celgosivir

    MBI 3253; MDL 28574; MX3253

    Glucosidase HCV HIV Infection
    Celgosivir (MBI 3253; MDL 28574; MX3253) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
  • HY-N0141
    Parthenolide

    (-)-Parthenolide

    NF-κB Autophagy Apoptosis Mitophagy Cancer
    Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
  • HY-101653
    MHP 133

    AChE mAChR 5-HT Receptor Others
    MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
  • HY-19529
    Ro 46-2005

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.
  • HY-P1104A
    FC131 TFA

    CXCR HIV Infection Endocrinology
    FC131 TFA is a CXCR4 antagonist, inhibits [ 125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
  • HY-100409
    PHCCC

    mGluR Cancer
    PHCCC is a Group I metabotropic glutamate receptor antagonist with EC 50 of 6 uM and a positive allosteric modulator of mGluR4. Also as a potent to antagonism for mGluR2 and mGluR8.
  • HY-N1935
    Worenine

    Others Metabolic Disease
    Worenine is isolated from Coptis chinensis. Worenine in rat shows dehydrogenization, hydrogenation, hydroxylation, and demethylene reactions in phase I metabolism. The phase II metabolism sulfation and glucuronidation reactions.
  • HY-15666
    GZD824

    HQP1351

    Bcr-Abl Cancer
    GZD824 (HQP1351) is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl (WT) and Bcr-Abl (T315I) with IC50s of 0.34 nM and 0.68 nM, respectively.
  • HY-112441
    Prolyl Hydroxylase inhibitor 1

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM. Antianemia agent.
  • HY-125990
    SLC13A5-IN-1

    Sodium Channel Metabolic Disease Cardiovascular Disease
    SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of  14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5.
  • HY-N4267
    Yangambin

    Calcium Channel Infection Cardiovascular Disease
    Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+ influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM.
  • HY-124726
    Aumitin

    Autophagy Cancer Neurological Disease
    Aumitin is a diaminopyrimidine-based autophagy inhibitor which inhibits mitochondrial respiration by targeting complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively.
  • HY-N0613
    Sauchinone

    NF-κB Inflammation/Immunology
    Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity.
  • HY-50847
    ZSTK474

    PI3K Autophagy Cancer
    ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
  • HY-129997
    Luteolinidin chloride

    Others Inflammation/Immunology
    Luteolinidin is a natural deoxyanthocyanidin, isolated from mosses and ferns. Luteolinidin is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.
  • HY-13744
    Rubitecan

    RFS 2000; 9-Nitrocamptothecin

    Topoisomerase Cancer
    Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
  • HY-N6865
    Groenlandicine

    Topoisomerase Cancer Metabolic Disease
    Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR). Groenlandicine selectively induces topoisomerase I-mediated DNA cleavage.
  • HY-100620
    RPR121056

    APC

    Topoisomerase AChE Cancer
    RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE.
  • HY-N2306A
    Aclacinomycin A hydrochloride

    Aclarubicin hydrochloride

    Proteasome Topoisomerase Cancer
    Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors.
  • HY-P2093
    S961

    Insulin Receptor Metabolic Disease
    S961 is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.
  • HY-12071A
    LDN193189 Tetrahydrochloride

    TGF-β Receptor Cancer
    LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
  • HY-13634B
    TLK117

    TER117

    Gutathione S-transferase Cancer Inflammation/Immunology
    TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.
  • HY-107096
    CH-0793076

    TP3076

    Topoisomerase Cancer
    CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein).
  • HY-125331
    DRF-1042

    Topoisomerase ADC Cytotoxin Cancer
    DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.
  • HY-12071
    LDN193189

    DM-3189

    TGF-β Receptor Cancer
    LDN193189 is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
  • HY-13521
    SB-505124

    TGF-β Receptor Cancer
    SB-505124 is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
  • HY-N2237
    Piceatannol 3'-O-glucoside

    Quzhaqigan

    NO Synthase Arginase Cardiovascular Disease
    Piceatannol 3'-O-glucoside, an active component of Rhubarb, activates endothelial nitric oxide (NO) synthase through inhibition of arginase activity with IC50s of 11.22 µM and 11.06 µM against arginase I and arginase II, respectively.
  • HY-13026
    Idelalisib

    CAL-101; GS-1101

    PI3K Autophagy Cancer
    Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
  • HY-13024
    Rebastinib

    DCC-2036

    Bcr-Abl FLT3 Apoptosis Src Cancer
    Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1 WT and Abl1 T315I with IC50 of 0.8 nM and 4 nM, also inhibits SRC, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit.
  • HY-100530
    Rp-cAMPS triethylammonium salt

    PKA Neurological Disease
    Rp-cAMPS triethylammonium salt is an analog of cAMP which acts as a potent, competitive and cell-permeable antagonist of cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 6.05 µM and 9.75 µM, respectively). Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.
  • HY-N6714
    Alternariol

    Topoisomerase Cancer Infection
    Alternariol is a mycotoxin produced by Alternaria species. AOH inhibits the catalytic activity of topoisomerase I and topoisomerase II enzymes. Alternariol exhibits a variety of therapeutic and biological properties such as phytotoxicity, cytotoxicity, anti-HIV, anti-cancer, and anti-microbial properties.
  • HY-100748
    CXD101

    HDAC Cancer
    CXD101 is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. CXD101 has no activity against HDAC class II. CXD101 has antitumor activity.
  • HY-100371
    (RS)-MCPG

    alpha-MCPG

    mGluR Neurological Disease
    (RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.
  • HY-14852
    Tafamidis

    Others Neurological Disease
    Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis.
  • HY-75800
    VX-222

    VCH-222

    HCV Infection
    VX-222 (VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L.
  • HY-15897
    LDN-212854

    TGF-β Receptor Cancer
    LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.
  • HY-133114
    Ezetimibe ketone

    EZM-K

    Keap1-Nrf2 Autophagy Cancer Cardiovascular Disease
    Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor.
  • HY-120118
    Metarrestin

    ML246

    DNA/RNA Synthesis Cancer
    Metarrestin (ML246) disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin is a first-in-class perinucleolar compartment inhibitor with a favorable PK profile, which effectively suppresses metastasis.
  • HY-123872
    MSC1094308

    p97 Others
    MSC1094308 is a reversible and allosteric inhibitor of the type II AAA ATPase human ubiquitin-directed unfoldase (VCP)/p97 and the type I AAA ATPase VPS4B, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively.
  • HY-16012
    Domatinostat tosylate

    4SC-202

    HDAC Cancer
    Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
  • HY-15778A
    AVE 0991 sodium salt

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [ 125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50 of 21±35 nM.
  • HY-13323A
    CX-5461 dihydrochloride

    DNA/RNA Synthesis Cancer
    CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM).
  • HY-15180
    Buparlisib Hydrochloride

    BKM120 Hydrochloride; NVP-BKM120 Hydrochloride

    PI3K Apoptosis Cancer
    Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
  • HY-P1985A
    Notch 1 TFA

    Notch Cancer Cardiovascular Disease
    Notch 1 TFA (Notch homolog 1, translocation-associated) is a human gene. This gene encodes a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types.
  • HY-16526
    Pilaralisib

    XL-147; SAR245408

    PI3K Cancer
    Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
  • HY-19615B
    MS023 dihydrochloride

    Histone Methyltransferase Cancer
    MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
  • HY-10221
    Vorinostat

    SAHA; Suberoylanilide hydroxamic acid

    HDAC Mitophagy Autophagy Cancer
    Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis.
  • HY-P2093A
    S961 TFA

    Insulin Receptor Metabolic Disease
    S961 TFA is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.
  • HY-114303
    CM-675

    Phosphodiesterase (PDE) HDAC Neurological Disease
    CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer’s disease.
  • HY-13323
    CX-5461

    DNA/RNA Synthesis Cancer
    CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively.
  • HY-12278
    K02288

    TGF-β Receptor Others
    K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.
  • HY-13521A
    SB-505124 hydrochloride

    TGF-β Receptor Cancer
    SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
  • HY-16012A
    Domatinostat

    4SC-202 (free base)

    HDAC Cancer
    Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
  • HY-19615
    MS023

    Histone Methyltransferase Cancer
    MS023 is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
  • HY-100435
    Oxaquin

    MCB-3837; DNV3837

    Bacterial Infection
    Oxaquin (MCB-3837) is a water-soluble, injectable prodrug that is rapidly converted to the active sub-stance MCB3681 in vivo following intravenous (i.v.) administration, active against Gram-positive bacterial species. Oxaquin (MCB-3837) itself has no antimicrobial effects.
  • HY-10583
    Y-27632 dihydrochloride

    Apoptosis ROCK Cancer
    Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 dihydrochloride induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
  • HY-10529
    Betulinic acid

    Lupatic acid; Betulic acid

    Apoptosis Topoisomerase HIV Autophagy Mitophagy NF-κB Cancer Infection Inflammation/Immunology
    Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid acts as a new activator of NF-kB.
  • HY-14776
    Quarfloxin

    CX-3543

    DNA/RNA Synthesis Cancer
    Quarfloxin (CX-3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template.
  • HY-125773
    β-cyano-L-Alanine

    Beta-cyano-l-alanine

    Others Neurological Disease
    β-cyano-L-Alanine (Beta-cyano-l-alanine), a nitrile of widespread occurrence in higher plants, is enzymatically produced by cyanoalanine synthase from cyanide and cysteine as substrates. β-cyano-L-Alanine abolishes the protective effect of ethanol on cerebral ischemia/reperfusion (I/R) injury.
  • HY-50514
    AT9283

    JAK Aurora Kinase Bcr-Abl FLT3 Apoptosis Autophagy Cancer
    AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
  • HY-11012
    TDZD-8

    GSK-3β Inhibitor I; NP 01139

    GSK-3 Cancer
    TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
  • HY-N0602
    Ginsenoside Rg2

    Chikusetsusaponin I; Panaxoside Rg2; Prosapogenin C2

    NF-κB Amyloid-β Neurological Disease Cardiovascular Disease Cancer
    Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 acts as a NF-κB inhibitor. Ginsenoside Rg2 also reduces 1-42 accumulation.
  • HY-P1295
    Urocortin, human

    Urocortin (human); Human urocortin; Human urocortin 1; Human urocortin I

    CRFR Neurological Disease Endocrinology
    Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF and mCRF, respectively.
  • HY-N0077
    Ginkgolic Acid

    Ginkgolic acid (15:1); Ginkgolic acid I; Romanicardic acid

    E1/E2/E3 Enzyme Cancer
    Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
  • HY-N1201
    Apigenin

    4',5,7-Trihydroxyflavone; Apigenol; C.I. Natural Yellow 1

    Autophagy Cytochrome P450 Inflammation/Immunology Cancer
    Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
  • HY-P1792A
    Angiotensin II (1-4), human TFA

    Angiotensin Receptor Endocrinology Metabolic Disease
    Angiotensin II (1-4), human (TFA) is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
  • HY-12868
    Bimiralisib

    PQR309

    PI3K mTOR Cancer
    Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
  • HY-N0095
    (S)-10-Hydroxycamptothecin

    10-HCPT; 10-Hydroxycamptothecin

    Topoisomerase Apoptosis Cancer
    (S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.
  • HY-50101A
    Mavorixafor trihydrochloride

    AMD-070 trihydrochloride

    CXCR HIV Infection Endocrinology
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-50673
    Dactolisib

    BEZ235; NVP-BEZ235

    PI3K mTOR Autophagy Cancer
    Dactolisib (BEZ235) is a dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
  • HY-W009732
    Sinapinic acid

    Sinapic acid

    HDAC Angiotensin-converting Enzyme (ACE) Reactive Oxygen Species Apoptosis Cancer Metabolic Disease
    Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. Sinapinic acid shows antioxidant and antidiabetic activities. Sinapinic acid reduces total cholesterol, triglyceride, and HOMA-IR index, and also normalizes some serum parameters of antioxidative abilities and oxidative damage in ovariectomized rats.
  • HY-N6791
    KT5823

    PKA PKC Apoptosis Others
    KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
  • HY-124729
    BL-918

    ULK Autophagy Neurological Disease
    BL-918 (compound 33i) 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-128943
    MAC glucuronide phenol-linked SN-38

    Drug-Linker Conjugates for ADC Cancer
    MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) drug linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.
  • HY-128717A
    GSK3368715 dihydrochloride

    EPZ019997 dihydrochloride

    Histone Methyltransferase Cancer
    GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
  • HY-12164
    Mocetinostat

    MGCD0103

    HDAC Apoptosis Autophagy 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-14852A
    Tafamidis meglumine

    Fx-1006A

    Others Neurological Disease
    Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis.
  • HY-13948
    Angiotensin II human

    Angiotensin II; Ang II; DRVYIHPF

    Angiotensin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Angiotensin II human (Angiotensin II) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis.
  • HY-15900
    Voxtalisib

    XL765; SAR245409

    PI3K mTOR Cancer
    Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.
  • HY-128942
    MAC glucuronide α-hydroxy lactone-linked SN-38

    Drug-Linker Conjugates for ADC Cancer
    MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 99 and 105 ng/mL, respectively.
  • HY-N4104
    Agaric acid

    Agaricinic Acid

    Mitochondrial Metabolism Metabolic Disease
    Agaric acid (Agaricinic Acid) is obtained from various plants of the fungous tribe, i.e. Polyporus officinalis and Polyporus igniarius. Agaric acid induces mitochondrial permeability transition through its interaction with the adenine nucleotide translocase. Agaric acid promotes efflux of accumulated Ca 2+, collapse of transmembrane potential, and mitochondrial swelling. Agaric acid is used to regulate lipid metabolism.
  • HY-19834
    Fenebrutinib

    GDC-0853

    Btk Cancer
    Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.
  • HY-P1792
    Angiotensin II (1-4), human

    Angiotensin Receptor Metabolic Disease Endocrinology
    Angiotensin II (1-4), human is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
  • HY-123963
    C-178

    STING Inflammation/Immunology
    C-178, a covalent inhibitor of STING, binds to Cys91, potently and selectively suppresses the STING responses elicited by distinct bona fide activators in mouse but not human. C-178 significantly reduces STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity. C-178 blocks palmitoylation (PMA)-induced clustering of STING; inhibits the CMA-induced phosphorylation of TBK1 (downstream protein kinase of STING).
  • HY-N6972
    Cepharanthine

    HIV Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Cepharanthine, an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities. Cepharanthine attenuates muscle and kidney injuries induced by limb ischemia/reperfusion (I/R). Cepharanthine induces autophagy, apoptosis and cell cycle arrest in breast cancer cells. Cepharanthine inhibits the HIV-1 entry process by reducing plasma membrane fluidity.
  • HY-135283
    ABT-546

    A-216546

    Endothelin Receptor Endocrinology Cardiovascular Disease
    ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively.
  • HY-13246
    Apitolisib

    GDC-0980; GNE 390; RG 7422

    PI3K Apoptosis mTOR Cancer
    Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
  • HY-12598A
    DHPG

    (RS)-3,5-DHPG

    mGluR Neurological Disease
    DHPG ((RS)-3,5-DHPG) is an amino acid, which acts as a selective and potent agonist of group I mGluR (mGluR 1 and mGluR 5), shows no effect on Group II or Group III mGluRs. DHPG ((RS)-3,5-DHPG) is also an effective antagonist of mGluRs linked to phospholipase D.
  • HY-N1971
    Ungeremine

    Topoisomerase Caspase Ferroptosis Autophagy Cancer
    Ungeremine, a phenanthridine type alkaloid, is extracted of the bulbs of Pancratium Illyricum. Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases. Ungeremine displays cytotoxic activity towards the 9 cancer cell lines, including drug-sensitive and MDR phenotypes. Ungeremine induced ferroptosis, necroptosis, autophagy as well as apoptosis mediated by caspase activation, MMP alteration and increase ROS production.
  • HY-14183
    Vernakalant Hydrochloride

    RSD1235 hydrochloride

    Potassium Channel Cardiovascular Disease
    Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
  • HY-12513
    LY3023414

    PI3K DNA-PK mTOR Autophagy Cancer
    LY3023414 potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. LY3023414 potently inhibits mTORC1/2 at low nanomolar concentrations.
  • HY-107139
    JNJ-10229570

    Melanocortin Receptor Others Endocrinology
    JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
  • HY-109015
    Tucidinostat

    Chidamide; HBI-8000; CS 055

    HDAC Cancer
    Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9.
  • HY-119939
    CHDI-390576

    HDAC Cancer
    CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histonedeacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform.
  • HY-128704A6
    c-Kit-IN-3 L-tartrate

    c-Kit Cancer
    c-Kit-IN-3 L-tartrate (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 L-tartrate displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops.
  • HY-15346
    Copanlisib

    BAY 80-6946

    PI3K Cancer
    Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.
  • HY-16992A
    W-54011

    Complement System Reactive Oxygen Species Inflammation/Immunology
    W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively.
  • HY-126350
    CL2-SN-38

    Drug-Linker Conjugates for ADC Cancer
    CL2-SN-38 is a part of the antibody drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is a DNA topoisomerase I inhibitor. The anti-Trop-2 hRS7-CL2A-SN-38 ADC provides significant and specific antitumor effects against a range of human solid tumor types.
  • HY-15371
    Forskolin

    Coleonol; Colforsin

    Adenylate Cyclase FXR Autophagy Cancer Endocrinology Metabolic Disease Inflammation/Immunology
    Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
  • HY-126247
    BI-2852

    Ras Cancer
    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRAS G12C inhibitor (binds to switch II pocket) because it binds to a different pocket present in both the active and inactive forms of KRAS. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
  • HY-130538
    1-Naphthohydroxamic acid

    HDAC Cancer
    1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity.1-Naphthohydroxamic acid can induce tubulin acetylation.
  • HY-128717
    GSK3368715

    EPZ019997

    Histone Methyltransferase Cancer
    GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
  • HY-N0173
    Cinchonidine

    α-Quinidine

    Parasite Serotonin Transporter Infection
    Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
  • HY-15346A
    Copanlisib dihydrochloride

    BAY 80-6946 dihydrochloride

    PI3K Cancer
    Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity.
  • HY-50101
    Mavorixafor

    AMD-070

    CXCR HIV Infection Endocrinology
    Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-13768
    Topotecan

    SKF 104864A; NSC 609669

    Topoisomerase Autophagy Cancer
    Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87.
  • HY-N6716
    Filipin complex

    Fungal Others
    Filipin, produced as a mixture of related compounds known as the filipin complex (filipins I-IV) in nature, is a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure. Filipin III is the major component of Filipin.
  • HY-128704
    c-Kit-IN-3

    c-Kit Cancer
    c-Kit-IN-3 (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops.
  • HY-117287
    BMS-986165

    JAK Interleukin Related Inflammation/Immunology
    BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. BMS-986165 inhibits IL-12/23 and type I IFN pathways.
  • HY-122537A
    Arotinolol

    Adrenergic Receptor 5-HT Receptor Cardiovascular Disease
    Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
  • HY-128946
    CL2A-SN-38

    Drug-Linker Conjugates for ADC Cancer Inflammation/Immunology
    CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.
  • HY-14850
    Sograzepide

    Netazepide; YF 476; YM-220

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively.
  • HY-107353
    Gadopentetic acid

    Gd-DTPA; gadolinium complex

    Others Others
    Gadopentetic acid (Gd-DTPA) is an paramagnetic contrast agent commonly implemented by a bolus intravenous injection (i.v.) in Dynamic contrast-enhanced MRI (DCE-MRI) studies. The initial concentration of Gadopentetic acid (Gd-DTPA) in the plasma ([Gd-DTPA0]) is an important parameter for DCE-MRI. [Gd-DTPA0] is related to the administered bolus dose and varies with subjects. A bolus of 0.025 mmol/kg Gd-DTPA offers shorter acquisition time and less exposure of subjects, with a half-life of 37.3 mins, a mean residence time of 53.8 mins, and an AUC of 3.37 ± 0.47 mmol/min/L.
  • HY-12326
    c-di-AMP

    Cyclic diadenylate; Cyclic-di-AMP

    Bacterial STING Inflammation/Immunology
    c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP (Cyclic diadenylate) is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP (Cyclic diadenylate) acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
  • HY-103241
    Ro 90-7501

    Amyloid-β ATM/ATR Phosphatase Apoptosis Cancer Neurological Disease
    Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces 42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
  • HY-N2038
    3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone

    Others Cancer Neurological Disease
    3,5,6,7,8,3',4'-heptamethoxyflavone, a flavonoid in C. unshiu peels, exhibits anti-tumor-initiating effect and Anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-heptamethoxyflavone inhibits collagenase activity and increased type I procollagen content in HDFn cells. 3,5,6,7,8,3',4'-heptamethoxyflavone induces brain-derived neurotrophic factor (BDNF) expression via cAMP/ERK/CREB signaling and reduces phosphodiesterase activity in C6 cells.
  • HY-112608
    CHMFL-PI3KD-317

    PI3K Cancer
    CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.
  • HY-N6800A
    Netropsin dihydrochloride

    DNA/RNA Synthesis Inflammation/Immunology
    Netropsin (dihydrochloride) is a small-molecule MGB (minor-groove binder), inhibits the catalytic activity of isolated topoisomerase and interferes with the stabilization of the cleavable complexes of topoisomerase II and I in nuclei. Netropsin (dihydrochloride) has potential antibiotic and antiviral properties by binding to dsDNA in a non-intercalative manner, it improves survival from murine endotoxaemia by attenuating NOS2 induction through interference with HMGA1 DNA binding to the core NOS2 promoter. Netropsin (dihydrochloride) in solutions of DNA has radioprotective ability against radiation-induced damage due to its high binding affinity and high structural stabilization, hydroxyl radical (OH*) generated by ionizing radiation cannot radiolyse the netropsin-DNA complex.