1. Search Result

Search Result

Pathways Recommended: Autophagy
Targets Recommended: Autophagy Mitophagy

Results for "Autophagy Activators" in MCE Product Catalog:

1344

Inhibitors & Agonists

15

Screening Libraries

8

Dye Reagents

151

Peptides

1

Inhibitory Antibodies

352

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-B0795
    MHY1485

    mTOR Autophagy Cancer
    MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes
  • HY-10219
    Rapamycin

    Sirolimus; AY-22989

    mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Cancer
    Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-100973A
    Adenosine 5′-diphosphoribose sodium

    ADP ribose sodium

    TRP Channel Autophagy Endocrinology Metabolic Disease
    Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD +) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca 2+-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy.
  • HY-10219S
    Rapamycin-d3

    Sirolimus-d3; AY-22989-d3

    mTOR FKBP Autophagy Cancer
    Rapamycin-d3 (Sirolimus-d3) is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-136064
    4,4'-Dimethoxychalcone

    Autophagy Metabolic Disease
    4,4'-Dimethoxychalcone, isolated from the plant Angelica keiskei koidzumi, acts as a natural autophagy inducer with anti-ageing properties.
  • HY-101923B
    LYN-1604 dihydrochloride

    ULK Autophagy Apoptosis Cancer
    LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).
  • HY-101923A
    LYN-1604 hydrochloride

    ULK Autophagy Apoptosis Cancer
    LYN-1604 hydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).
  • HY-101923
    LYN-1604

    ULK Autophagy Apoptosis Cancer
    LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).
  • HY-N1416
    Pogostone

    Bacterial Apoptosis Autophagy Infection Inflammation/Immunology
    Pogostone is isolated from patchouli with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml . Pogostone induces cell apoptosis and autophagy.
  • HY-112483
    QX77

    Autophagy Cancer
    QX77 is a chaperone-mediated autophagy (CMA) activator.
  • HY-P1328
    TAT-14

    Keap1-Nrf2 Others
    TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
  • HY-U00434
    3BDO

    mTOR Autophagy Apoptosis Cancer
    3BDO is a new mTOR activator which can also inhibit autophagy.
  • HY-125465
    SLLN-15

    Autophagy Cancer
    SLLN-15 is an oral active, selective and potent enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC).
  • HY-17394
    Cisplatin

    CDDP; cis-Diaminodichloroplatinum

    DNA Alkylator/Crosslinker Ferroptosis Autophagy Cancer
    Cisplatin (CDDP) is an antineoplastic chemotherapy agent by cross-linking with DNA and causing DNA damage in cancer cells. Cisplatin activates ferroptosis and induces autophagy.
  • HY-70002
    Enzalutamide

    MDV3100

    Androgen Receptor Autophagy Cancer
    Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator.
  • HY-17471A
    Metformin hydrochloride

    1,1-Dimethylbiguanide hydrochloride

    AMPK Autophagy Mitophagy Metabolic Disease Cardiovascular Disease
    Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy.
  • HY-110228
    Metformin D6 hydrochloride

    1,1-Dimethylbiguanide D6 hydrochloride

    AMPK Autophagy Mitophagy Metabolic Disease Cardiovascular Disease
    Metformin D6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy.
  • HY-P1328A
    TAT-14 TFA

    Keap1-Nrf2 Others
    TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
  • HY-125996
    NR1H4 activator 1

    FXR Inflammation/Immunology
    NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.
  • HY-14374
    GPP78

    CAY10618

    Nampt Autophagy Cancer Inflammation/Immunology
    GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.
  • HY-13018
    MRT67307

    IKK ULK Autophagy Cancer Inflammation/Immunology
    MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells.
  • HY-13018A
    MRT67307 hydrochloride

    IKK ULK Autophagy Cancer Inflammation/Immunology
    MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells.
  • HY-B0627
    Metformin

    1,1-Dimethylbiguanide

    AMPK Autophagy Mitophagy Metabolic Disease Cardiovascular Disease
    Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin can cross the blood-brain barrier and triggers autophagy.
  • HY-100548
    GSK621

    AMPK Autophagy Apoptosis Cancer
    GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
  • HY-13030
    (+)-JQ-1

    JQ1

    Epigenetic Reader Domain Autophagy Ligand for Target Protein for PROTAC Cancer
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
  • HY-135825
    TFEB activator 1

    Autophagy Neurological Disease
    TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.
  • HY-10255AS
    Sunitinib D10

    SU 11248 D10

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-115453
    UBCS039

    Sirtuin Autophagy Cancer
    UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM.
  • HY-N0484
    Liensinine

    Autophagy Mitophagy Cancer Cardiovascular Disease
    Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
  • HY-10162
    Olaparib

    AZD2281; KU0059436

    PARP Autophagy Mitophagy Cancer
    Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
  • HY-117958
    HJC0197

    Others Cancer Metabolic Disease Cardiovascular Disease
    HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.
  • HY-N2149A
    Tomatidine hydrochloride

    NF-κB JNK Autophagy Inflammation/Immunology Cardiovascular Disease
    Tomatidine hydrochloride acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine hydrochloride activates autophagy either in mammal cells or C elegans.
  • HY-N0112
    Dihydromyricetin

    Ampelopsin; Ampeloptin

    mTOR Autophagy Cancer
    Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2).
  • HY-N2149
    Tomatidine

    NF-κB JNK Autophagy Inflammation/Immunology Cardiovascular Disease
    Tomatidine acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine activates autophagy either in mammal cells or C elegans.
  • HY-N0817
    Polyphyllin G

    Apoptosis Autophagy Bacterial Cancer Inflammation/Immunology
    Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs). Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy.
  • 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-13417
    AICAR

    Acadesine; AICA Riboside

    AMPK Autophagy Mitophagy Cancer
    AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy and mitophagy inhibitor.
  • HY-135318
    NBDHEX

    Glutathione Peroxidase Apoptosis Autophagy Cancer
    NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
  • HY-113313
    Aldosterone

    Endogenous Metabolite Cardiovascular Disease
    Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
  • HY-102011
    BMS-1166

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-128892
    EN6

    Autophagy Proton Pump Neurological Disease
    EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H + ATPase (v-ATPase). EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner.
  • HY-111516
    MGV354

    Guanylate Cyclase Inflammation/Immunology Cardiovascular Disease
    MGV354 is a soluble guanylate cyclase (sGC) activator with EC50s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively.
  • HY-15870
    SR 11302

    Others Cancer Inflammation/Immunology
    SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).
  • HY-10999
    Trametinib

    GSK1120212; JTP-74057

    MEK Autophagy Apoptosis Cancer
    Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
  • HY-13856
    (R)-PS210

    PDK-1 Cancer
    (R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.
  • HY-103349
    PETCM

    Caspase Apoptosis Cancer
    PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.
  • HY-10249
    GSK-690693

    Akt AMPK Autophagy Cancer
    GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.
  • HY-13757A
    Tamoxifen

    ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen activates autophagy and induces apoptosis.
  • HY-117917
    (Rac)-MGV354

    Guanylate Cyclase Inflammation/Immunology Cardiovascular Disease
    (Rac)-MGV354 is the racemate of MGV354. MGV354 is a soluble guanylate cyclase (sGC) activator with EC50s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively.
  • HY-N3005
    Britannin

    Apoptosis Autophagy Cancer Inflammation/Immunology
    Britannin, isolated from Inula aucheriana, is a sesquiterpene lactone. Britannin induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. Britannin has anti-proliferative and anti-inflammatory activities.
  • HY-124729A
    (Rac)-BL-918

    ULK Autophagy Neurological Disease
    (Rac)-BL-918 is the racemate of BL-918. BL-918 is a potent activator of UNC-51-like kinase 1 (ULK1), inducing cytoprotective autophagy for Parkinson’s disease treatment.
  • HY-13757
    Tamoxifen Citrate

    ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate activates autophagy and induces apoptosis.
  • HY-12028
    PD98059

    MEK Aryl Hydrocarbon Receptor Autophagy Cancer
    PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits autophagy.
  • HY-16592
    Brefeldin A

    BFA; Cyanein; Decumbin

    Autophagy CRISPR/Cas9 Mitophagy HSV Antibiotic Cancer Infection
    Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
  • HY-N6872
    Actein

    JNK Akt Apoptosis Autophagy Cancer
    Actein is a triterpene glycoside isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in human bladder cancer. Actein has little toxicity in vivo.
  • HY-125197
    BRD5631

    Autophagy Inflammation/Immunology
    BRD5631 is an autophagy enhancer, enhances autophagy through an mTOR-independent pathway. BRD5631 affects several cellular disease phenotypes previously linked to autophagy, including protein aggregation, cell survival, bacterial replication, and inflammatory cytokine production.
  • HY-12545
    Brevetoxin-3

    PbTx-3

    Sodium Channel Inflammation/Immunology
    Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
  • HY-12041
    SP600125

    JNK Autophagy Apoptosis Ferroptosis Cancer
    SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates apoptosis.
  • HY-18980
    Rottlerin

    Mallotoxin; NSC 56346; NSC 94525

    PKC Autophagy Apoptosis Infection Cancer
    Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation.
  • HY-135231
    NL-1

    Mitochondrial Metabolism Autophagy Cancer
    NL-1 is a mitoNEET inhibitor with antileukemic effect. NL-1 inhibits REH and REH/Ara-C cells growth with IC50s of 47.35 µM and 56.26 µM, respectively. NL-1-mediated death in leukemic cells requires the activation of the autophagic pathway.
  • HY-10182B
    CHIR-99021 trihydrochloride

    CT99021 trihydrochloride

    GSK-3 Wnt β-catenin Autophagy Cancer
    CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 trihydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 trihydrochloride induces autophagy.
  • HY-10182
    CHIR-99021

    CT99021

    GSK-3 Wnt β-catenin Autophagy Cancer
    CHIR-99021 (CT99021) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 induces autophagy.
  • HY-10999A
    Trametinib (DMSO solvate)

    GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)

    MEK Apoptosis Cancer
    Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.
  • HY-101920
    Autophinib

    Autophagy Cancer Neurological Disease
    Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.
  • HY-13259
    MG-132

    Z-Leu-leu-leu-al

    Proteasome Autophagy Apoptosis Cancer
    MG-132 (Z-Leu-leu-leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
  • HY-15394
    (Rac)-Rotigotine hydrochloride

    Dopamine Receptor Adrenergic Receptor 5-HT Receptor Endocrinology Neurological Disease
    (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
  • HY-103706
    ROC-325

    Autophagy Apoptosis Cancer
    ROC-325 is a novel inhibitor of autophagy.
  • HY-N0221
    Daurisoline

    (R,R)-Daurisoline

    Autophagy Potassium Channel Cancer
    Daurisoline is a hERG inhibitor and also an autophagy blocker.
  • HY-N4113
    Glycycoumarin

    Autophagy Cancer
    Glycycoumarin is a major bioactive coumarin of licorice. Glycycoumarin inhibits hepatocyte lipoapoptosis through activation of autophagy and inhibition of ER stress-mediated JNK and GSK-3-mediated mitochondrial pathway. Glycycoumarin exerts anti-liver cancer activity by directly targeting T-LAK cell-originated protein kinase .
  • HY-10201
    Sorafenib

    Bay 43-9006

    Raf VEGFR FLT3 Autophagy Apoptosis Ferroptosis Cancer
    Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
  • HY-10201A
    Sorafenib Tosylate

    Bay 43-9006 Tosylate

    Raf VEGFR FLT3 Autophagy Ferroptosis Apoptosis Cancer
    Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator.
  • HY-N0824
    Syringin

    Eleutheroside B

    Autophagy Cardiovascular Disease
    Syringin is a main bioactive phenolic glycoside in Acanthopanax senticosus, with anti-osteoporosis activity. Syringin prevents cardiac hypertrophy induced by pressure overload through the attenuation of autophagy.
  • HY-14165
    Veliflapon

    BAY X 1005; DG-031

    FLAP Leukotriene Receptor Inflammation/Immunology Cardiovascular Disease
    Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.
  • HY-N2527
    Sanshool

    Autophagy Inflammation/Immunology
    Sanshool is a major component in Zanthoxylum bungeanum. Sanshool improves UVB-induced skin photodamage by targeting JAK2/STAT3-dependent autophagy.
  • HY-B0015
    Paclitaxel

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Autophagy Cancer
    Paclitaxel (Taxol) is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy.
  • HY-10182A
    CHIR-99021 monohydrochloride

    CT99021 monohydrochloride

    GSK-3 Wnt β-catenin Autophagy Cancer
    CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 monohydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 monohydrochloride induces autophagy.
  • HY-15531
    Venetoclax

    ABT-199; GDC-0199

    Bcl-2 Family Autophagy Cancer
    Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy.
  • HY-12222
    Obeticholic acid

    INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid

    FXR Autophagy Others
    Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.
  • HY-12795
    Vps34-IN-1

    PI3K Autophagy Cancer
    Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO2012085815A1, compound example 16a, with an IC50 of 4 nM. Vps34-IN-1 modulates autophagy.
  • 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-13629
    Etoposide

    VP-16; VP-16-213

    Topoisomerase Autophagy Mitophagy Bacterial Apoptosis Antibiotic Cancer Infection
    Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
  • HY-18676
    OSU-T315

    Integrin Autophagy Apoptosis Cancer
    OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
  • 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-N4180
    Pennogenin 3-O-beta-chacotrioside

    Autophagy Cancer
    Pennogenin 3-O-beta-chacotrioside is an active component isolated from Paris polyphylla, modulates autophagy via increasing the expressions of autophagy-related proteins LC3 and Beclin-1. Anti-colorectal cancer activity.
  • HY-N2531
    Notoginsenoside Fc

    Autophagy Cardiovascular Disease
    Notoginsenoside Fc, a protopanaxadiol- (PPD-) type saponin isolated from the leaves of Panax notoginseng, effectively counteracts platelet aggregation. Notoginsenoside Fc can accelerate reendothelialization following vascular injury in diabetic rats by promoting autophagy.
  • HY-10256A
    SB 203580 hydrochloride

    RWJ 64809 hydrochloride

    p38 MAPK Autophagy Mitophagy Inflammation/Immunology Cancer
    SB 203580 hydrochloride (RWJ 64809 hydrochloride) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy and mitophagy activator.
  • HY-P2260
    Tat-beclin 1

    Autophagy HIV Infection
    Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
  • HY-13418
    Dorsomorphin dihydrochloride

    Compound C dihydrochloride; BML-275 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-13418A
    Dorsomorphin

    Compound C; BML-275

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin (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-P2260A
    Tat-beclin 1 TFA

    Autophagy HIV Infection
    Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
  • HY-12057
    Vemurafenib

    PLX4032; RG7204; RO5185426

    Raf Autophagy Cancer
    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
  • HY-10358
    MK-2206 dihydrochloride

    MK-2206 (2HCl)

    Akt Autophagy Apoptosis Cancer
    MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy.
  • HY-10256
    SB 203580

    RWJ 64809

    p38 MAPK Autophagy Mitophagy Inflammation/Immunology Cancer
    SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.
  • HY-10108
    LY294002

    PI3K Casein Kinase DNA-PK Autophagy Apoptosis Cancer Infection
    LY294002 (NSC 697286; SF 1101) is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
  • HY-18672
    SMER18

    Autophagy Cancer
    SMER18 is a small molecule enhancer of rapamycin which act as a mTOR-independent autophagy inducer.
  • HY-13027
    DAPT

    GSI-IX

    γ-secretase Amyloid-β Autophagy Notch Apoptosis Cancer Inflammation/Immunology Neurological Disease
    DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and 42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
  • HY-100596
    AS1842856

    Autophagy Metabolic Disease
    AS1842856, a specific Foxo1 inhibitor (IC50=30 nM), potently suppresses autophagy. AS1842856 inhibits FoxO1 activity by suppressing the expression of SIRT1. AS1842856 only reduces the activity of FoxO1 by binding with it, without affecting its transcription and protein expression.
  • HY-10586
    5-Azacytidine

    Azacitidine; 5-AzaC; Ladakamycin

    Nucleoside Antimetabolite/Analog DNA Methyltransferase Bacterial Autophagy Antibiotic Cancer Infection
    5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.
  • HY-112914
    mTOR inhibitor-1

    mTOR Autophagy Cancer
    mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.
  • HY-B0146
    Verteporfin

    CL 318952

    YAP Apoptosis Autophagy Cancer
    Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis. Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation.
  • HY-112698
    CA-5f

    Autophagy Apoptosis Cancer
    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
  • HY-12661A
    AMG PERK 44

    PERK Autophagy Cancer
    AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy.
  • HY-17371
    Oxaliplatin

    DNA Alkylator/Crosslinker Autophagy Cancer
    Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death. Oxaliplatin time-dependently inhibits human melanoma cell lines C32 and G361 with IC50 values of 0.98 μM and 0.14 μM, respectively. Oxaliplatin induces cell autophagy.
  • HY-122404
    Xantocillin

    MEK ERK Autophagy Cancer
    Xanthocillin is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.
  • HY-100200
    SMER28

    Autophagy Cancer
    SMER28 is a positive regulator of autophagy acting via an mTOR-independent mechanism. SMER28 prevents the accumulation of amyloid beta peptide.
  • HY-N6939
    Pseudolaric Acid B

    HBV Fungal Apoptosis Autophagy Ferroptosis Cancer Infection Inflammation/Immunology
    Pseudolaric Acid B is a diterpene isolated from the root of Pseudolarix kaempferi Gorden (pinaceae), has anti-cancer, antifungal, and antifertile activities, and shows immunosuppressive activity on T lymphocytes. Pseudolaric Acid B inhibits hepatitis B virus (HBV) secretion through apoptosis and cell cycle arrest. Pseudolaric Acid B induces autophagy.
  • HY-123056
    EAD1

    Autophagy Apoptosis Cancer
    EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis.
  • HY-15184
    Elaiophylin

    Azalomycin B; Gopalamicin; Efomycin E

    Autophagy Cancer
    Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells.
  • HY-112897
    IITZ-01

    Autophagy PI3K Apoptosis Cancer
    IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
  • HY-129622
    NH2-PEG5-C6-Cl

    PROTAC Linker Cancer
    NH2-PEG5-C6-Cl (K-7) is a PROTAC linker, which refers to the PEG composition. NH2-PEG5-C6-Cl can be used in the synthesis of a series of PROTACs, and it induces degradation of intracellular molecules by autophagy.
  • HY-N0901
    Corynoxine

    Autophagy Cancer
    Corynoxine is an enantiomer of Corynoxine B; induces autophagy in different neuronal cell lines, including N2a and SHSY-5Y cells.
  • HY-111621
    DC661

    Autophagy Apoptosis Cancer
    DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity.
  • HY-15142
    Doxorubicin hydrochloride

    Hydroxydaunorubicin hydrochloride

    Topoisomerase ADC Cytotoxin AMPK Autophagy Apoptosis HIV HBV Mitophagy Bacterial Antibiotic Cancer Infection
    Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy. Doxorubicin hydrochloride inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
  • HY-10115
    PI-103

    PI3K mTOR DNA-PK Autophagy Apoptosis Cancer
    PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.
  • HY-10115A
    PI-103 Hydrochloride

    PI3K mTOR DNA-PK Autophagy Apoptosis Cancer
    PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.
  • HY-N0901A
    Corynoxine B

    Autophagy Cancer
    Corynoxine B is an oxindole alkaloid isolated from Uncaria rhynchophylla (Miq.) Jacks (Gouteng in Chinese); a Beclin-1-dependent autophagy inducer.
  • HY-125848
    Ginsenoside F2

    Apoptosis Autophagy Endogenous Metabolite Cancer
    Ginsenoside F2, a metabolite from Ginsenoside Rb1, induces apoptosis accompanied by protective autophagy in breast cancer stem cells.
  • HY-N2359
    Chelerythrine

    PKC Bcl-2 Family Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology
    Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.
  • HY-135811
    Desethyl chloroquine

    Parasite Toll-like Receptor (TLR) Autophagy Infection
    Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity.
  • HY-10514
    BX795

    PDK-1 IKK Autophagy Cancer
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
  • HY-112818
    S130

    Cathepsin Autophagy Apoptosis Cancer
    S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 µM. S130 suppresses autophagy flux.
  • HY-15893
    DMOG

    Dimethyloxallyl Glycine

    HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
  • HY-12990
    Spautin-1

    Autophagy Apoptosis Cancer
    Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.
  • HY-N4120
    Valechlorine

    Autophagy Metabolic Disease
    Valechlorine, a autophagy enhancer, breaks down lipid droplets. Valechlorine reduces oleic acid (OA)-induced lipid accumulation in an Atg5-dependent manner.
  • HY-135811A
    Desethyl chloroquine diphosphate

    Parasite Toll-like Receptor (TLR) Autophagy Infection
    Desethyl chloroquine diphosphate is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine diphosphate possesses antiplasmodic activity.
  • HY-15425
    PF-543

    Sphingosine Kinase 1 Inhibitor II

    SPHK LPL Receptor Apoptosis Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy.
  • HY-15425B
    PF-543 hydrochloride

    Sphingosine Kinase 1 Inhibitor II hydrochloride

    SPHK LPL Receptor Apoptosis Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
  • HY-13251
    Silvestrol

    (-)-Silvestrol

    Eukaryotic Initiation Factor (eIF) Apoptosis Autophagy Cancer
    Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata. Silvestrol induces autophagy and caspase-mediated apoptosis.
  • HY-129111
    EACC

    Autophagy Infection Neurological Disease
    EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion.
  • HY-N2991
    Dehydropachymic acid

    Autophagy Neurological Disease
    Dehydropachymic acid is one of the major triterpenes isolated from Poria cocos. Dehydropachymic acid is more effective in autophagy-lysosome pathway (ALP) impaired cells rather than normal cells.
  • HY-16966
    SBI-0206965

    ULK Autophagy Apoptosis Cancer
    SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2.
  • HY-N0399
    Wogonoside

    Autophagy Cancer Inflammation/Immunology
    Wogonoside, a flavonoid glycoside isolated from Huangqin, possesses anti-inflammatory effects. Wogonoside induces autophagy in breast cancer cells by regulating MAPK-mTOR pathway.
  • HY-100599
    Urolithin A

    Drug Metabolite Reactive Oxygen Species DNA/RNA Synthesis Autophagy Apoptosis Endogenous Metabolite Cancer
    Urolithin A, a gut-microbial metabolite of ellagic acid, exerts anti-inflammatory, antiproliferative, and antioxidant properties. Urolithin A induces autophagy and apoptosis, suppresses cell cycle progression, and inhibits DNA synthesis.
  • HY-N4176
    Ginkgolide K

    Autophagy Neurological Disease
    Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway. Ginkgolide K possesses neuroprotective activity.
  • HY-100558
    Bafilomycin A1

    (-)-Bafilomycin A1

    Proton Pump Bacterial Autophagy Apoptosis Antibiotic Cancer Infection
    Bafilomycin A1, a macrolide antibiotic isolated from the Streptomyces species, is a specific inhibitor of vacuolar-type H + ATPase (V-ATPase). Bafilomycin A1 inhibits autophagy and induces apoptosis.
  • HY-N6038
    Gartanin

    Others Cancer
    Gartanin is a natural xanthone of mangosteen, with antioxidant, anti-inflammatory, antifungal, neuroprotective and antineoplastic properties. Gartanin induces cell cycle arrest and autophagy and suppresses migration in human glioma cells.
  • HY-13003
    Torin 1

    mTOR Autophagy Cancer
    Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM. Torin 1 is an effective inducer of autophagy.
  • HY-U00141
    ABTL-0812

    α-Hydroxylinoleic acid

    Autophagy Metabolic Disease
    ABTL-0812 (α-Hydroxylinoleic acid) induces endoplasmic reticulum (ER) stress-mediated autophagy. ABTL-0812 is a first-in-class small molecule with anti-cancer activity.
  • HY-12496
    NS-1619

    Potassium Channel Cardiovascular Disease
    NS-1619 is a selective large conductance Ca2+-activated K+-channel activator.
  • HY-15425A
    PF-543 Citrate

    Sphingosine Kinase 1 Inhibitor II Citrate

    SPHK LPL Receptor Apoptosis Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy.
  • HY-N6002
    3'-Hydroxypterostilbene

    Apoptosis Autophagy Cancer
    3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.
  • HY-100008
    Peretinoin

    NIK333

    RAR/RXR SPHK Autophagy HCV Cancer Infection
    Peretinoin is an oral acyclic retinoid retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM.
  • HY-N0103
    Sophocarpine

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-N6074
    Soyasapogenol B

    Autophagy Apoptosis Cancer
    Soyasapogenol B, an ingredient of soybean, exerts anti-proliferative, anti-metastatic activities. Soyasapogenol B triggers endoplasmic reticulum stress, which mediates apoptosis and autophagy in colorectal cancer.
  • HY-129652
    Halo PROTAC 1

    PROTAC Autophagy Cancer
    Halo PROTAC 1 is a PROTAC, which is a ligand having activity to bind to an intracellular proteins fused with HaloTag and a structure having activity to induce autophagy of an intracellular molecule are linked via a PEG linker.
  • HY-N2593
    Isorhapontigenin

    Autophagy Cancer Inflammation/Immunology
    Isorhapontigenin, an orally bioavailable dietary polyphenol isolated from the Chinese herb Gnetum cleistostachyum, displays anti-inflammatory effects. Isorhapontigenin induces autophagy and inhibits invasive bladder cancer formation.
  • HY-12831
    Ampkinone

    AMPK Metabolic Disease
    Ampkinone is an indirect AMP-activated protein kinase (AMPK) activator.
  • HY-12884
    OAC2

    Oct3/4 Others
    OAC2 is an Oct4-activating compound which activates expression through the Oct4 gene promoter.
  • HY-122760
    Bax activator-1

    Bcl-2 Family Apoptosis Cancer
    Bax activator-1 (compound 106) is a Bax activator that induces Bax-dependent tumor cell apoptosis.
  • HY-128340
    Autogramin-2

    Autophagy Cancer
    Autogramin-2 potently inhibits autophagy induced by either starvation (IC50=0.27 μM) or mTORC1 inhibition (Rapamycin; IC50=0.14 μM).
  • HY-128339
    Autogramin-1

    Autophagy Cancer
    Autogramin-1 potently inhibits autophagy induced by either starvation (IC50=0.17 μM) or mTORC1 inhibition (Rapamycin; IC50=0.44 μM).
  • HY-19734
    NK-252

    Keap1-Nrf2 Cancer
    NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
  • HY-N0336
    3-Butylidenephthalide

    Butylidenephthalide

    Parasite Infection
    3-Butylidenephthalide (Butylidenephthalide) is a phthalic anhydride derivative identified in Ligusticum chuanxiong Hort, and has larvicidal activity (LC50 of 1.56 mg/g for Spodoptera litura larvae).
  • HY-10542A
    (Z)-GW 5074

    Raf Neurological Disease
    (Z)-GW 5074 is a compound which interacts with both mHTT (mutant huntingtin protein) and LC3, but not but not with the wild-type HTT protein. (Z)-GW 5074 inhibits c-Raf, shows no effect on autophagy, and is effective for neurodegenerative disorder.
  • HY-N0730
    Diosgenin glucoside

    Autophagy Inflammation/Immunology Neurological Disease
    Diosgenin glucoside, a saponin compound extracted from Tritulus terrestris L., provides neuroprotection by regulating microglial M1 polarization. Diosgenin glucoside protects against spinal cord injury by regulating autophagy and alleviating apoptosis .
  • HY-12031A
    U0126

    MEK Autophagy Mitophagy Influenza Virus Cancer
    U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.
  • HY-N0103A
    Sophocarpine monohydrate

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-101788
    Glucokinase activator 1

    Glucokinase Metabolic Disease
    Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.
  • HY-12048
    Chelerythrine chloride

    PKC Bcl-2 Family Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology
    Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy.
  • HY-19312
    3-Methyladenine

    3-MA

    PI3K Autophagy Mitophagy Endogenous Metabolite Cancer
    3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K.
  • HY-19826
    Isofistularin-3

    DNA Methyltransferase ADC Cytotoxin Autophagy Apoptosis Cancer
    Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
  • HY-13103
    NS 11021

    Potassium Channel Others
    NS 11021 is a potent and specific Ca 2-activated big-conductance K Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials.
  • HY-15122
    Sinomenine

    NF-κB Opioid Receptor Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Sinomenine, an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
  • HY-100508
    ITSA-1

    HDAC Cancer
    ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation.
  • HY-12689
    Mitapivat

    Pyruvate Kinase Cancer
    Mitapivat is a pyruvate kinase isoenzyme M2 (PKM2) activator.
  • HY-114490
    ULK-101

    ULK Cancer
    ULK-101 is a potent and selective ULK1 inhibitor, with IC50 values of 1.6 nM and 30 nM for ULK1 and ULK2, respectively. ULK-101 suppresses autophagy and sensitizes cancer cells to nutrient stress.
  • HY-108701
    Nampt-IN-3

    Nampt HDAC Autophagy Apoptosis Cancer
    Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.
  • HY-B0497C
    Niclosamide olamine

    BAY2353 olamine

    STAT Parasite Antibiotic Autophagy
    Niclosamide olamine is an anthelmintic that disrupts mitochondrial metabolism in parasitic worms and animal models. Niclosamide olamine inhibits STAT3 (IC50 = 0.25 μM) and stimulates autophagy by reversibly inhibiting mammalian target of Rapamycin complex 1 (mTORC1) signaling.
  • HY-116506
    Bigelovin

    RAR/RXR Reactive Oxygen Species Apoptosis Autophagy Cancer
    Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.
  • HY-P1308
    SLIGRL-NH2

    Protease-Activated Receptor-2 Activating Peptide

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • HY-15122A
    Sinomenine hydrochloride

    Cucoline hydrochloride

    NF-κB Opioid Receptor Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
  • HY-P0283
    Protease-Activated Receptor-2, amide

    Protease-Activated Receptor (PAR) Cancer
    Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.
  • HY-107988
    MK-3903

    AMPK Metabolic Disease
    MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM.
  • HY-N0277
    Aconine

    Jesaconine

    NF-κB Inflammation/Immunology Cancer
    Aconine inhibits receptor activator of nuclear factor (NF)-κB ligand (RANKL)-induced NF-κB activation.
  • HY-N6631
    7-Methoxyisoflavone

    AMPK Metabolic Disease Cancer
    7-Methoxyisoflavone is an isoflavone derivative and also an activator of adenosine monophosphate-activated protein kinase (AMPK).
  • HY-114304
    COH000

    E1/E2/E3 Enzyme Cancer
    COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
  • HY-12855A
    Lys05

    Lys01 trihydrochloride

    Autophagy Cancer
    Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.
  • HY-P1308A
    SLIGRL-NH2 TFA

    Protease-Activated Receptor-2 Activating Peptide TFA

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • HY-13971
    GPR40 Activator 1

    GPR40 Metabolic Disease
    GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.
  • HY-122203
    PCS1055 dihydrochloride

    mAChR AChE Neurological Disease
    PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively.
  • HY-121546
    ALLO-1

    Autophagy Cancer
    ALLO-1, an autophagy receptor, is essential for autophagosome formation around paternal organelles and directly binds to the worm LC3 homologue LGG-1 through its LC3-interacting region (LIR) motif.
  • HY-P0297
    Protease-Activated Receptor-4

    Protease-Activated Receptor (PAR) Others
    Protease-Activated Receptor-4 is the agonist of proteinase-activated receptor-4 (PAR4).
  • HY-117656
    ESI-05

    NSC 116966

    Others Others
    ESI-05 (NSC 116966) is a specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 µM. ESI-05 (NSC 116966) inhibits cAMP-mediated activation of EPAC2 as well as EAPC2 mediated Rap1 activation.
  • HY-124873
    SERCA2a activator 1

    Calcium Channel Cardiovascular Disease
    SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.
  • HY-N1446
    Oleic acid

    9-cis-Octadecenoic acid; 9Z-Octadecenoic acid

    Na+/K+ ATPase Endogenous Metabolite Apoptosis Cancer Metabolic Disease
    Oleic acid is an abundant monounsaturated fatty acid. Oleic acid is a Na +/K + ATPase activator.
  • HY-108330
    AG126

    Tyrphostin AG126

    ERK Inflammation/Immunology
    AG126 is a tyrosine kinase inhibitor which can prevent the activation of mitogen-activated protein kinase p42MAPK (ERK2).
  • HY-12031
    U0126-EtOH

    MEK Autophagy Mitophagy Influenza Virus Cancer
    U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.
  • HY-N0072
    Brazilin

    Apoptosis Autophagy Cancer Inflammation/Immunology
    Brazilin is a red dye precursor obtained from the heartwood of several species of tropical hardwoods. Brazilin inhibits the cells proliferation, promotes apoptosis, and induces autophagy through the AMPK/mTOR pathway. Brazilin shows chondroprotective and anti-inflammatory activities.
  • HY-N2099
    Onjisaponin B

    Autophagy Neurological Disease
    Onjisaponin B is a natural product derived from Radix Polygalae. Onjisaponin B enhances autophagy and accelerates the degradation of mutant α-synuclein and huntingtin in PC-12 cells, and exbibits potential therapeutic effects on Parkinson disease and Huntington disease.
  • HY-12406
    VLX600

    Mitochondrial Metabolism Autophagy Cancer
    VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. Anticancer activity.
  • HY-19635A
    G-5555 hydrochloride

    PAK Cancer
    G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
  • HY-15336
    AG 555

    Tyrphostin AG 555

    EGFR Reverse Transcriptase Cancer
    AG 555, a potent antiretroviral drug, is a potent and selective inhibitor of EGFR and blocks Cdk2 activation.
  • HY-104038
    Gcase activator 1

    Glucosidase Neurological Disease
    Gcase activator 1 is an activator of glucocerebrosidase (Gcase) extracted from patent WO 2017192841 A1.
  • HY-18739
    Phorbol 12-myristate 13-acetate

    PMA

    PKC SPHK Inflammation/Immunology
    Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator.
  • HY-N6779
    Patulin

    Terinin

    Bacterial Apoptosis Antibiotic Infection
    Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin (Terinin) induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage.
  • HY-B1479C
    Emetine hydrochloride

    Parasite DNA/RNA Synthesis Autophagy Bacterial Antibiotic Infection
    Emetine hydrochloride, derived from the ipecac root, is a potent anti-protozoal and emetic agent. Emetine hydrochloride inhibits viral polymerases and inhibits Zika and Ebola virus infections. Emetine hydrochloride potently inhibits autophagy and has anti-malarial, anti-bacterial and anti-amoebic effect.
  • HY-B1479
    Emetine

    Parasite DNA/RNA Synthesis Autophagy Bacterial Antibiotic Infection
    Emetine, derived from the ipecac root, is a potent anti-protozoal and emetic agent. Emetine inhibits viral polymerases and inhibits Zika and Ebola virus infections. Emetine potently inhibits autophagy and has anti-malarial, anti-bacterial and anti-amoebic effect.
  • HY-13636
    Fulvestrant

    ICI 182780; ZD 9238; ZM 182780

    Estrogen Receptor/ERR Autophagy Apoptosis Cancer
    Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
  • HY-B1479B
    Emetine dihydrochloride hydrate

    Parasite DNA/RNA Synthesis Autophagy Bacterial Antibiotic Infection Cancer
    Emetine dihydrochloride hydrate, derived from the ipecac root, is a potent anti-protozoal and emetic agent. Emetine dihydrochloride hydrate inhibits viral polymerases and inhibits Zika and Ebola virus infections. Emetine dihydrochloride hydrate potently inhibits autophagy and has anti-malarial, anti-bacterial and anti-amoebic effect.
  • HY-110153
    NS19504

    Potassium Channel Neurological Disease
    NS19504 is a Ca 2+-activated K + channel (BK channel, KCa1.1 channel) activator (EC50=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.
  • HY-101047
    D-erythro-Sphingosine

    Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine

    PKC Phosphatase Endogenous Metabolite Cancer
    D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
  • HY-100221
    AM-2394

    Glucokinase Metabolic Disease
    AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.
  • HY-B0493
    Niflumic acid

    Chloride Channel Inflammation/Immunology
    Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.
  • HY-111383
    LX2343

    Beta-secretase PI3K Amyloid-β Autophagy Neurological Disease
    LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of clearance.
  • HY-N3442
    Juglanin

    JNK Cancer
    Juglanin is a JNK activator.
  • HY-N0625A
    Alpinetin

    PPAR Inflammation/Immunology Cancer
    Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.
  • HY-12070
    DPH

    Bcr-Abl Cancer
    DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.  
  • HY-10484
    Pevonedistat hydrochloride

    MLN4924 hydrochloride

    NEDD8-activating Enzyme Cancer
    Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM.
  • HY-100381
    Nigericin sodium salt

    Potassium Channel NOD-like Receptor (NLR) Bacterial Antibiotic Cancer Infection
    Nigericin sodium salt is an antibiotic from Streptomyces hygroscopicus that works by acting as an H +, K +, and Pb 2+ ionophore, a NLRP3 activator.
  • HY-B0167A
    Sodium Salicylate

    Salicylic acid sodium salt; 2-Hydroxybenzoic acid sodium salt

    COX Autophagy Apoptosis Inflammation/Immunology Cancer
    Sodium Salicylate (Salicylic acid sodium salt) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation.
  • HY-135884
    PKR activator 2

    Pyruvate Kinase Cardiovascular Disease
    PKR activator 2 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035863A1, compound 385.
  • HY-70062
    Pevonedistat

    MLN4924

    NEDD8-activating Enzyme Cancer
    Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM.
  • HY-136251
    BRD0539

    CRISPR/Cas9 Infection
    BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay.
  • HY-102052
    DCEBIO

    Potassium Channel Inflammation/Immunology
    DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl secretion in T84 colonic cells. DCEBIO stimulates Cl secretion via the activation of hIK1 K channels and the activation of an apical membrane Cl conductance.
  • HY-12303
    OAC1

    Oct3/4 Others
    OAC1 is a Octamer-binding transcription factor 4 (Oct4)-activating compound; enhances the iPSC reprogramming efficiency and accelerated the reprogramming process.
  • HY-14754
    Salirasib

    S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS

    Ras Autophagy Cancer
    Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
  • HY-108593
    BMS-191011

    BMS-A

    Potassium Channel Neurological Disease
    BMS-191011 (BMS-A) is an opener of the large-conductance, Ca 2+-activated potassium (maxi-K) channel, effective in stroke models.
  • HY-14714
    NSC-207895

    XI-006

    MDM-2/p53 Cancer
    NSC-207895 (XI-006), a DNA damaging agent, is an anticancer agent and p53 activator.
  • HY-17538
    ZLN005

    PGC-1α Autophagy Metabolic Disease
    ZLN005 is a potent activator of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α).
  • HY-U00441
    DPBQ

    MDM-2/p53 Cancer
    DPBQ is a p53 activator.
  • HY-15597
    Salinomycin

    Procoxacin

    Bacterial Wnt β-catenin Mitophagy Autophagy Apoptosis Antibiotic Cancer
    Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin (Procoxacin) shows selective activity against human cancer stem cells.
  • HY-10218
    Everolimus

    RAD001; SDZ-RAD

    mTOR FKBP Autophagy Apoptosis Cancer
    Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
  • HY-N2312
    Mogrol

    ERK STAT Cancer
    Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
  • HY-B0167
    Salicylic acid

    2-Hydroxybenzoic acid

    COX Autophagy Mitophagy Apoptosis Endogenous Metabolite Inflammation/Immunology Cancer
    Salicylic acid (2-Hydroxybenzoic acid) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation.
  • 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-15027
    5-Aminosalicylic Acid

    Mesalamine; 5-ASA; Mesalazine

    PPAR PAK NF-κB Endogenous Metabolite Inflammation/Immunology Cancer
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-135883
    PKR activator 1

    Pyruvate Kinase Cardiovascular Disease
    PKR activator 1 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035865A1, compound E7-93.
  • HY-13417A
    AICAR phosphate

    Acadesine phosphate; AICA Riboside phosphate

    AMPK Autophagy Mitophagy Cancer
    AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AMPK Activator.
  • HY-103368
    Eact

    Chloride Channel Neurological Disease
    Eact is a selective and potent activator of TMEM16A, directly activates the TRPV1 channels in sensory nociceptors and produces itch, acute nociception and thermal hypersensitivity.
  • HY-N0509
    Astilbin

    Keap1-Nrf2 TNF Receptor NF-κB Inflammation/Immunology Cancer
    Astilbin, a flavonoid compound, is isolated from the rhizome of Smilax glabra. Astilbin enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
  • HY-N2632
    Uvarigrin

    Apoptosis Cancer
    Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation.
  • HY-104047
    LM22B-10

    Trk Receptor Akt ERK Neurological Disease
    LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.
  • HY-N0712
    Typhaneoside

    Autophagy Inflammation/Immunology Cardiovascular Disease
    Typhaneoside, extracted from Typha angustifolia L., Typhaneoside can inhibit the excessive autophagy of hypoxia/reoxygenation cells and increase the phosphorylation of Akt and mTOR. Typhaneoside has certain effects on the cardiovascular system, including lowering blood lipid levels, promoting antiatherosclerosis activities, as well as improving immune and coagulation function.
  • HY-13630
    Etoposide phosphate

    BMY-40481

    Topoisomerase Bacterial Autophagy Apoptosis Cancer Infection Neurological Disease
    Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
  • HY-100489
    TBHQ

    tert-Butylhydroquinone

    Keap1-Nrf2 ERK Autophagy Apoptosis Ferroptosis Cancer
    TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma.
  • HY-136172
    ESI-08

    Ras Cancer Metabolic Disease Cardiovascular Disease
    ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation.
  • HY-B0341
    Nicorandil

    SG-75

    Potassium Channel Cardiovascular Disease
    Nicorandil (SG-75) is potassium channel activator.
  • HY-104073
    CAY10602

    Sirtuin Metabolic Disease Inflammation/Immunology
    CAY10602 is a SIRT1 activator.
  • HY-15723A
    NSC 23766 trihydrochloride

    Ras Apoptosis Cancer
    NSC 23766 trihydrochloride is an inhibitor of Rac1 activation.
  • HY-101594
    Tulopafant

    RP 59227

    Others Cardiovascular Disease
    Tulopafant is a platelet activating factor (PAF) antagonist.
  • HY-101675
    Setipafant

    BN-50727; LAU-0901

    Others Cardiovascular Disease
    Setipafant is a platelet-activating factor (PAF) antagonist.
  • HY-14290A
    Pinacidil monohydrate

    Potassium Channel Others
    Pinacidil monohydrate, an antihypertensive drug, is a potassium channel activator.
  • HY-B0664
    Ciprofibrate

    Win35833

    PPAR Cancer
    Ciprofibrate is a peroxisome proliferator-activated receptor agonist.
  • HY-128895
    NQO1 activator 1

    Others Metabolic Disease
    NQO1 activator 1 is an orally available NAD + modulator. It reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD + levels via NADH oxidation. Elevated NAD + levels triggers the activation of SIRT1 and AMPK, and subsequently activates PGC-1α. NQO1 activator 1 improves energy metabolism and mitochondrial dysfunction in MELAS fibroblasts.
  • HY-75342
    Methyl vanillate

    Wnt Reactive Oxygen Species Endogenous Metabolite Inflammation/Immunology Cancer
    Methyl vanillate, one of the ingredients in Hovenia dulcis Thunb, is a Wnt/β-catenin pathway activator. A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite.
  • HY-U00292
    AMPK activator 1

    AMPK Metabolic Disease
    AMPK activator 1 is an AMPK activator extracted from patent WO2013116491A1, compound No.1-75, has an EC50 of <0.1μM.
  • HY-12647
    GPR40 Activator 2

    GPR40 Metabolic Disease
    GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
  • HY-15542B
    FRAX486

    PAK Cancer
    FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
  • HY-N4182
    Licochalcone E

    Akt p38 MAPK Autophagy Inflammation/Immunology
    Licochalcone E, a flavonoid compound isolated from Glycyrrhiza inflate, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation.
  • HY-19635
    G-5555

    PAK Cancer
    G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.
  • HY-101069
    Y-26763

    Potassium Channel Cardiovascular Disease
    Y-26763 is a K + channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K + (KATP) channel activator.
  • HY-128574
    GLUT4 activator 1

    GLUT Metabolic Disease
    GLUT4 activator 1 (Compound 26b) is a potent glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM.
  • HY-B0006A
    Carvedilol phosphate hemihydrate

    BM 14190 phosphate hemihydrate

    Adrenergic Receptor Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is a non-selective β/α-1 blocker. Carvedilol phosphate hemihydrate inhibits lipid peroxidation with an IC50 of 5 μM. Carvedilol phosphate hemihydrate is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol phosphate hemihydrate is an autophagy inducer that inhibits the NLRP3 inflammasome.
  • HY-50895
    Gefitinib

    ZD1839

    EGFR Autophagy Cancer
    Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-50895A
    Gefitinib hydrochloride

    ZD-1839 hydrochloride

    EGFR Cancer
    Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity.
  • HY-136073
    Wnt pathway activator 2

    Wnt Cancer
    Wnt pathway activator 2 is a potent Wnt activator extracted from patent WO2012024404A1, compound 2, has an IC50s of 13 nM.
  • HY-N1380
    Guaiacol

    2-Methoxyphenol

    COX NF-κB Endogenous Metabolite Inflammation/Immunology
    Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.
  • HY-14233
    Omecamtiv mecarbil

    CK-1827452

    Myosin Cardiovascular Disease
    Omecamtiv mecarbil is a selective cardiac myosin activator.
  • HY-P0240
    Tuftsin

    Endogenous Metabolite Inflammation/Immunology
    Tuftsin is a tetrapeptide. Tuftsin is a macrophage/microglial activator.
  • HY-15976
    P7C3

    Nampt Neurological Disease
    P7C3 is a NAMPT activator.
  • HY-100490
    Rilmenidine

    Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy Cardiovascular Disease
    Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
  • HY-10197
    Wortmannin

    SL-2052; KY-12420

    PI3K Polo-like Kinase (PLK) Autophagy Cancer
    Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively.
  • HY-135516
    Wnt pathway activator 1

    Wnt Cancer
    Wnt pathway activator 1 is a potent Wnt activator extracted from patent WO2012024404A1, compound 1, has an IC50s of 28-29 nM.
  • HY-B0289
    Erdosteine

    RV 144

    NF-κB Bacterial Infection Metabolic Disease Inflammation/Immunology
    Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects.
  • HY-N2432
    Paederoside

    HBV Cancer Infection
    Paederoside is a monoterpene S-methyl thiocarbonate isolated from Paederia pertomentosa. Paederoside shows a high anti-tumor promoting activity against the Epstein-Barr virus activation.
  • HY-13764
    Tetrandrine

    NSC-77037; d-Tetrandrine

    Calcium Channel Potassium Channel Cancer Inflammation/Immunology
    Tetrandrine (NSC-77037; d-Tetrandrine) is a bis-benzyl-isoquinoline alkaloid, which inhibits voltage-gated Ca 2+ current (ICa) and Ca 2+-activated K + current.
  • HY-17589
    Chloroquine phosphate

    Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Antibiotic Cancer Infection Inflammation/Immunology
    Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
  • HY-17589B
    Chloroquine dihydrochloride

    Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Antibiotic Cancer Infection Inflammation/Immunology
    Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
  • HY-12481
    SAR405

    PI3K Autophagy Cancer
    SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.
  • HY-13630A
    Etoposide phosphate disodium

    BMY-40481 disodium

    Topoisomerase Autophagy Apoptosis Cancer Neurological Disease
    Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
  • HY-B0006
    Carvedilol

    BM 14190

    Adrenergic Receptor Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
  • HY-17589A
    Chloroquine

    Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Antibiotic Cancer Infection Inflammation/Immunology
    Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
  • HY-100783A
    (-)-Bicuculline methochloride

    l-Bicuculline methochloride

    GABA Receptor Neurological Disease
    (-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
  • HY-P1536
    Thrombin Receptor Activator for Peptide 5 TRAP-5

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Thrombin Receptor Activator for Peptide 5 (TRAP-5) is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD).
  • HY-100472
    ZYZ-488

    Caspase Cancer
    ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3.
  • HY-18749
    SC79

    Akt Cancer Inflammation/Immunology Neurological Disease
    SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt.
  • HY-100783
    (-)-Bicuculline methobromide

    l-Bicuculline methobromide

    GABA Receptor Neurological Disease
    (-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
  • HY-P1376
    G-Protein antagonist peptide

    mAChR Adrenergic Receptor
    G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
  • HY-N6892
    3'-​O-​Acetylhamaudol

    Others Cancer
    3'-O-Acetylhamaudol, isolated from Angelica japonica roots, exhibits anti-tumor activity through dual actions, anti-angiogenesis and intestinal intraepithelial lymphocyte activation.
  • HY-14452
    Fatostatin

    125B11

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-111363
    MK8722

    AMPK Metabolic Disease
    MK8722 is a potent and systemic pan-AMPK activator.
  • HY-19121A
    TCV-309 chloride

    Others Cancer
    TCV-309 (chloride) is a platelet activating factor (PAF) antagonist.
  • HY-14255
    Levcromakalim

    (-)-Cromakalim; BRL 38227

    Potassium Channel Cardiovascular Disease
    Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K + channel (KATP) activator.
  • HY-112878
    CL656

    c-[2’FdAMP(S)-2’FdIMP(S)]

    STING Inflammation/Immunology
    CL656 is an activator of stimulator of interferon genes (STING).
  • HY-N0019
    Daidzein

    PPAR Endogenous Metabolite Endocrinology Cancer
    Daidzein is a soy isoflavone, which acts as a PPAR activator.
  • HY-15964
    Tirasemtiv

    CK-2017357

    Others Neurological Disease
    Tirasemtiv is an activator of the fast skeletal muscle troponin complex.
  • HY-P0136
    SAMS

    AMPK Metabolic Disease
    SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK).
  • HY-N0865
    Ingenol

    (-)-Ingenol

    PKC Cancer
    Ingenol is a PKC activator, with a Ki of 30 μM, with antitumor activity.
  • HY-10164
    E-​6123

    Others Inflammation/Immunology
    E-​6123 is a platelet-activating factor (PAF) receptor antagonist.
  • HY-104027
    ML402

    Potassium Channel Neurological Disease
    ML402 is a selective TREK-1 activator.
  • HY-U00040
    PAF-AN-1

    Others Inflammation/Immunology Cardiovascular Disease
    PAF-AN-1 is a platelet activating factor receptor (PAF) antagonist.
  • HY-12695
    Guanosine 5'-triphosphate trisodium salt

    5'-GTP trisodium salt

    Endogenous Metabolite Others
    Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) is an activator of the signal transducing G proteins which are involved in various cellular processes including proliferation, differentiation, and activation of several intracellular kinase cascades.
  • HY-B1221
    Flufenamic acid

    COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels.
  • HY-N6065
    Praeruptorin A

    NF-κB Inflammation/Immunology
    Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation.
  • HY-123879
    BAA473

    Others Inflammation/Immunology
    BAA473 is a bile acid analog and is a potent activator of the pyrin inflammasome that induces the secretion of interleukin 18 (IL-18) through activation of the inflammasome in both myeloid and intestinal epithelial cells.
  • HY-17397
    Strontium Ranelate

    Distrontium renelate; S12911

    CaSR Metabolic Disease
    Strontium Ranelate (S12911) is an antiosteoporotic agent that acts by reducing bone resorption and promoting bone formation, thereby inducing a positive bone balance. Strontium Ranelate also can activate the calcium-sensing receptor (CaSR) in non skeletal cells, resulting in the activation of inositol 1, 4, 5-triphosphate production and mitogen-activated protein kinase signaling.
  • HY-N0831
    Jaceosidin

    Bcl-2 Family COX Apoptosis Cancer Inflammation/Immunology
    Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin exhibits anti-cancer, anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation.
  • HY-16915
    RPR-260243

    Potassium Channel Cardiovascular Disease
    RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
  • HY-15416
    NS309

    Potassium Channel Cardiovascular Disease
    NS309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels); increases Ca2+ sensitivity. Displays no activity at BK channels.
  • HY-P1847
    IKKγ NBD Inhibitory Peptide

    NF-κB Cancer
    IKKγ NBD Inhibitory Peptide is a NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region, which is shown to block TNF-alpha-induced NF-kB activation.
  • HY-N6258
    Kahweol

    AMPK Apoptosis Metabolic Disease
    Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
  • HY-N0052A
    Sanguinarine chloride

    Pseudochelerythrine chloride; Sanguinarium chloride

    Apoptosis Autophagy Bacterial Parasite Cancer
    Sanguinarine chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
  • HY-P1376A
    G-Protein antagonist peptide TFA

    mAChR Adrenergic Receptor
    G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
  • HY-18633
    MDK83190

    Apoptosis Cancer
    MDK83190 is a potent apoptosis activator, induces Apaf-1 oligomerization, increases procaspase-9 processing and subsequent caspase-3 activation in a cyto c-dependent Manner.
  • HY-N0052
    Sanguinarine

    Pseudochelerythrine; Sanguinarin

    Apoptosis Autophagy Cancer
    Sanguinarine, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
  • HY-10969
    Obatoclax Mesylate

    GX15-070 Mesylate

    Bcl-2 Family Autophagy Parasite Cancer Infection
    Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.
  • HY-13516
    Aloperine

    Apoptosis Autophagy Filovirus HIV Cancer Infection Inflammation/Immunology
    Aloperine is an alkaloid in sophora plants such as Sophora alopecuroides L, which has shown anti-cancer, anti-inflammatory and anti-virus properties. Aloperine is widely used to treat patients with allergic contact dermatitis eczema and other skin inflammation in China. Aloperine induces apoptosis and autophagy in HL-60 cells.
  • HY-133779
    Gefitinib impurity 5

    Others Others
    Gefitinib impurity 5 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-131257
    Gefitinib impurity 1

    Others Others
    Gefitinib impurity 1 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-10969A
    Obatoclax

    GX15-070

    Bcl-2 Family Autophagy Parasite Cancer Infection
    Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.
  • HY-B1197
    Amcinonide

    CL-34699

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    Amcinonide inhibit NO release from activated microglia with IC50 3.38 nM.
  • HY-U00442
    CTX1

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    CTX1 is a novel small molecule p53 activator.
  • HY-14909
    Bardoxolone

    CDDO; RTA 401

    Keap1-Nrf2 Cancer
    Bardoxolone is a novel nuclear regulator factor (Nrf-2) activator.
  • HY-59047
    Tolimidone

    MLR-1023

    Src Metabolic Disease
    Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.
  • HY-112060
    Saccharin 1-methylimidazole

    DNA/RNA Synthesis Cancer
    Saccharin 1-methylimidazole is an activator for DNA/RNA Synthesis.
  • HY-15300
    Skepinone-L

    CBS3830

    p38 MAPK Autophagy Inflammation/Immunology
    Skepinone-L (CBS3830) is a selective p38 mitogen-activated protein kinase inhibitor.
  • HY-12376
    BAY 41-2272

    Guanylate Cyclase Inflammation/Immunology
    BAY 41-2272 is a soluble guanylate cyclases (sGC) activator.
  • HY-14256
    BMS-191095

    Potassium Channel Metabolic Disease
    BMS-191095 is an activators of mitochondrial ATP-sensitive potassium (mitoKATP) channels.
  • HY-13529
    Globalagliatin

    LY2608204

    Glucokinase Metabolic Disease
    Globalagliatin (LY2608204) is a activator of glucokinase (GK) with EC50 of 42 nM.
  • HY-110105
    NS8593 hydrochloride

    Potassium Channel Neurological Disease
    NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
  • HY-128591
    DIPQUO

    Others Metabolic Disease
    DIPQUO is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.
  • HY-P1847A
    IKKγ NBD Inhibitory Peptide TFA

    NF-κB Inflammation/Immunology
    IKKγ NBD Inhibitory Peptide TFA is a NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region, which is shown to block TNF-alpha-induced NF-kB activation.
  • HY-123962
    G6PD activator AG1

    Others Metabolic Disease
    G6PD activator AG1 is a glucose-6-phosphate dehydrogenase (G6PD) activator with an EC50 of 3 µΜ, extracted from patent WO2019023264A1, compound AG1.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-P0256
    Apamin

    Apamine

    Potassium Channel Inflammation/Immunology Neurological Disease
    Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca 2+-activated K + (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.
  • HY-107406
    Antimycin A1

    Mitochondrial Metabolism Cancer
    Antimycin A1 is a specific electron transfer inhibitor of ubiquinol-cytochrome c oxidoreductase. Antimycin A1 inhibits angiogenesis through decrease in VEGF production caused by inhibition of HIF-1α activation.
  • HY-117962
    (Rac)-BI 703704

    Guanylate Cyclase Metabolic Disease
    (Rac)-BI 703704 is a potent soluble guanylyl cyclase (sGC) activator. (Rac)-BI 703704 reduces progression of renal damage in the ZSF1 rat, and highlight the potential of sGC activation as an effective therapy for diabetic nephropathy.
  • HY-N6688
    Verruculogen

    Potassium Channel Bacterial Antibiotic Infection
    Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca 2+-activated K + channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle.
  • HY-N0699
    Daphnoretin

    Dephnoretin; Thymelol

    PKC Influenza Virus Infection
    Daphnoretin (Dephnoretin), isolated from Wikstroemia indica, possesses antiviral activity. Daphnoretin likes PMA, may direct activation of protein kinase C which in turn activated NADPH oxidase and elicited respiratory burst.
  • HY-12754
    ML228

    CID-46742353

    HIF/HIF Prolyl-Hydroxylase Cancer
    ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.
  • HY-136173
    TNO155

    Phosphatase Cancer
    TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
  • HY-100234A
    DREADD agonist 21 dihydrochloride

    mAChR Neurological Disease
    DREADD agonist 21 dihydrochloride is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
  • HY-W018781
    Benzamidine hydrochloride

    Ser/Thr Protease Cancer
    Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 µM, 21 µM, 20 µM and 110 µM for uPA, trypsin, tryptase and factor Xa, respectively.
  • HY-135303
    GLPG1205

    GPR84 Inflammation/Immunology
    GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
  • HY-100234
    DREADD agonist 21

    mAChR Neurological Disease
    DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
  • HY-14452A
    Fatostatin hydrobromide

    125B11 hydrobromide

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-12762
    QS11

    Others Cancer
    QS11 is a GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor.
  • HY-100602
    HJC0152 hydrochloride

    STAT Apoptosis Cancer
    HJC0152 hydrochloride is a signal transducers and activators of transcription 3 (STAT3) inhibitor.
  • HY-19987
    BML-284

    Wnt Cancer
    BML-284 is selective and cell-permeable Wnt signaling activator.
  • HY-N3463
    Isopimaric acid

    Potassium Channel
    Isopimaric acid is a potent opener of large conductance calcium activated K + (BK) channels.
  • HY-N0553
    Gypenoside XVII

    Gynosaponin S

    Estrogen Receptor/ERR Endogenous Metabolite Cardiovascular Disease
    Gypenoside XVII, a novel phytoestrogen belonging to the gypenosides, can activate estrogen receptors.
  • HY-12848B
    SAG hydrochloride

    Smo Cancer
    SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
  • HY-N0441
    Neferine

    (-)-Neferine

    NF-κB Autophagy Apoptosis Metabolic Disease Cancer
    Neferine is a major bisbenzylisoquinline alkaloid. Neferine strongly inhibits NF-κB activation.
  • HY-115685
    3-Methyl-GABA

    GABA Receptor
    3-Methyl-GABA is an activator of GABA aminotransferase with anticonvulsant activity.
  • HY-101214
    UK-371804

    PAI-1 Inflammation/Immunology
    UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
  • HY-101738A
    Peliglitazar racemate

    BMS 426707-01 racemate

    PPAR Metabolic Disease
    Peliglitazar racemate is the racemate of Peliglitazar. Peliglitazar is a novel dual α/γ PPAR activator.
  • HY-100295
    (4-Acetamidocyclohexyl) nitrate

    BM121307

    Guanylate Cyclase Cardiovascular Disease
    (4-Acetamidocyclohexyl) nitrate (BM121307) is a guanylate cyclase activator.
  • HY-N0933
    Androsterone

    5α-Androstan-3α-ol-17-one

    FXR Endogenous Metabolite Autophagy Metabolic Disease Neurological Disease
    Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).
  • HY-100153
    48740 RP

    RP-55778

    Others Inflammation/Immunology
    48740 RP (RP-55778) is a platelet-activating factor (PAF) antagonist.
  • HY-W040129
    Chromomycin A3

    Bacterial Fungal Antibiotic Cancer Infection
    Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 forms dimeric complexes with divalent cations, such as Mg 2+, which strongly binds to the GC rich sequence of DNA to inhibit DNA replication and transcription. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor.
  • HY-126147
    J22352

    HDAC Cancer
    J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1.
  • HY-50856
    Ruxolitinib

    INCB18424

    JAK Autophagy Mitophagy Apoptosis Cancer
    Ruxolitinib (INCB18424) is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.
  • HY-10971
    Alisertib

    MLN 8237

    Aurora Kinase Autophagy Apoptosis Cancer
    Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
  • HY-B0099S
    Edaravone D5

    MCI-186 D5

    MMP Apoptosis Neurological Disease
    Edaravone D5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
  • HY-N0608
    Myrislignan

    NF-κB Inflammation/Immunology
    Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
  • HY-10255A
    Sunitinib

    SU 11248

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-P0256A
    Apamin TFA

    Apamine TFA

    Potassium Channel Inflammation/Immunology Neurological Disease
    Apamin TFA (Apamine TFA) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca 2+-activated K + (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.
  • HY-131265
    Mesalamine impurity P

    PPAR PAK NF-κB Cancer Inflammation/Immunology
    Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-N2433
    Paederosidic acid methyl ester

    Potassium Channel Neurological Disease
    Paederosidic acid methyl ester is a ATP‐sensitive K + channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K + channel in the brain and spinal cord level.
  • HY-101346
    ZD7288

    ICI D7288

    HCN Channel Neurological Disease
    ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.
  • HY-12848
    SAG

    Smo Cancer
    SAG is a potent Smo receptor agonist which activates the Hedgehog signaling pathway with a Kd of 59 nM.
  • HY-14181
    Cinaciguat

    BAY 58-2667

    Guanylate Cyclase Cardiovascular Disease
    Cinaciguat is an activator of guanylate cyclase (sGC), and used for acute decompensated heart failure.
  • HY-76847
    Chenodeoxycholic Acid

    CDCA

    FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
  • HY-B1058
    Benfluorex hydrochloride

    JP-992 hydrochloride

    Others Metabolic Disease Cardiovascular Disease
    Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.
  • HY-100242
    Mivotilate

    YH439

    Aryl Hydrocarbon Receptor Others
    Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.
  • HY-B0809
    Theophylline

    1,3-Dimethylxanthine; Theo-24

    Adenosine Receptor Phosphodiesterase (PDE) Autophagy Endogenous Metabolite Cancer
    Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
  • HY-101804
    (E)-Alprenoxime

    CDDD-1815

    Others Cardiovascular Disease
    (E)-Alprenoxime is the isomer of the Alprenoxime. Alprenoxime is a site-activated ocular β-blocker.
  • HY-128642
    FAPI-2

    Others Cancer
    FAPI-2 is a fibroblast activation protein (FAP) inhibitor for cancer research.
  • HY-100415
    UKI-1

    UKI-1C

    Others Infection
    UKI-1 is a novel synthetic inhibitor of the urokinase-type plasminogen activator system.
  • HY-12359
    TPPB

    PKC Neurological Disease
    TPPB is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM.
  • HY-14181A
    Cinaciguat hydrochloride

    BAY 58-2667 hydrochloride

    Guanylate Cyclase Cardiovascular Disease
    Cinaciguat hydrochloride is a potent soluble guanylate cyclase (GC) activator with EC50 of 15 nM in platelets.
  • HY-19706
    ARS-853

    Ras Apoptosis Cancer
    ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
  • HY-136059
    Desfluoro-ezetimibe

    Keap1-Nrf2 Autophagy Cancer Cardiovascular Disease
    Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
  • HY-W006230
    Anthraflavic acid

    Others Cancer
    Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
  • HY-103666
    CY-09

    NOD-like Receptor (NLR) Inflammation/Immunology
    CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation.
  • HY-B0167S
    Salicylic acid-D6

    2-Hydroxybenzoic acid-D6

    COX Autophagy Mitophagy Apoptosis Cancer Inflammation/Immunology
    Salicylic acid-D6 (2-Hydroxybenzoic acid-D6) is a deuterium labeled Salicylic acid. Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation.
  • HY-128920
    Phortress free base

    Cytochrome P450 Cancer
    Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.
  • HY-108573
    P-1075

    Potassium Channel Cardiovascular Disease
    P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.
  • HY-117727
    Leriglitazone

    Hydroxypioglitazone

    PPAR Metabolic Disease
    Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM,induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM.
  • HY-100932
    ML-9

    Myosin Cancer
    ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
  • HY-12203
    PFK-158

    Autophagy Apoptosis Cancer
    PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria.
  • HY-122614
    S29434

    NMDPEF

    Autophagy Neurological Disease
    S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 (NMDPEF) induces autophagy and inhibits QR2-mediated ROS production.
  • HY-17589AS
    Chloroquine D5

    Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Cancer Infection Inflammation/Immunology
    Chloroquine D5 is deuterium labeled Chloroquine. Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
  • HY-135388
    ent-Ezetimibe

    ent-SCH 58235

    Drug Metabolite Cardiovascular Disease
    ent-Ezetimibe (ent-SCH 58235) is the RRS-enantiomer of Ezetimibe. Ezetimibe is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
  • HY-N0608A
    (Rac)-Myrislignan

    NF-κB Inflammation/Immunology
    (Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
  • HY-101180
    C2 Ceramide

    Ceramide 2

    Phosphatase Mitochondrial Metabolism Apoptosis Endocrinology Metabolic Disease
    C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.
  • HY-103000
    HSF1A

    HSP Cancer Cardiovascular Disease
    HSF1A is a cell-permeable activator of heat shock transcription factor 1 (HSF1).
  • HY-N6577
    Astragaloside VI

    EGFR Inflammation/Immunology Neurological Disease
    Astragaloside VI could activate EGFR/ERK signalling pathway to improve wound healing.
  • HY-100447
    TM5275 sodium

    PAI-1 Cancer Cardiovascular Disease
    TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.
  • HY-U00458
    K-80003

    TX-803

    Akt Cancer
    K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
  • HY-B1140
    Diazoxide

    Sch-6783; SRG-95213

    Potassium Channel Autophagy Cardiovascular Disease
    Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.
  • HY-50662
    A-769662

    AMPK Cancer
    A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM.
  • HY-B0664S
    Ciprofibrate D6

    PPAR Cancer
    Ciprofibrate D6 is deuterium labeled Ciprofibrate, which is a peroxisome proliferator-activated receptor agonist.
  • HY-U00411
    PSN-GK1

    Glucokinase Metabolic Disease
    PSN-GK1 is a potent glucokinase activator with an EC50 of 0.13 μM.
  • HY-15341
    BAM7

    Bcl-2 Family Cancer
    BAM7 is a direct and selective activator of proapoptotic BAX with an IC50 of 3.3 μM.
  • HY-B0162A
    Ivabradine hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Ivabradine hydrochloride is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
  • HY-136094
    SRT3657

    Sirtuin Neurological Disease
    SRT3657 is a brain-permeable activator of SIRT1, with neuroprotective effect.
  • HY-16271
    Kevetrin hydrochloride

    4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride

    MDM-2/p53 Cancer
    Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
  • HY-104005
    ML335

    Potassium Channel Neurological Disease
    ML335 is a selective activator of both TREK-1 and TREK-2.
  • HY-16397A
    Phenformin hydrochloride

    Phenethylbiguanide hydrochloride

    AMPK Autophagy Cancer
    Phenformin hydrochloride is an anti-diabetic drug from the biguanide class, can activate AMPK activity.
  • HY-101625
    Recilisib

    Ex-RAD; ON 01210

    Akt PI3K Cancer
    Recilisib is a radioprotectant, which can activate AKT, PI3K activities in cells.
  • HY-128643
    FAPI-4

    Others Cancer
    FAPI-4 is a fibroblast activation protein (FAP) inhibitor used in cancer research.
  • HY-19739
    JW74

    Wnt Cancer
    JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.
  • HY-123054
    BTSA1

    Bcl-2 Family Apoptosis Cancer
    BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.
  • HY-P0190
    Iberiotoxin

    Potassium Channel Cardiovascular Disease
    Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.
  • HY-10255
    Sunitinib Malate

    SU 11248 Malate

    PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-12316
    20(S)-Hydroxycholesterol

    20α-Hydroxycholesterol

    Smo Endogenous Metabolite Cancer
    20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
  • HY-B0968A
    Trimetazidine

    Autophagy Cardiovascular Disease
    Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
  • HY-11109
    Resatorvid

    TAK-242; CLI-095

    Toll-like Receptor (TLR) TNF Receptor Interleukin Related Autophagy Inflammation/Immunology Cancer
    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-R and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.
  • HY-N0485
    Liensinine Diperchlorate

    Autophagy Mitophagy Cardiovascular Disease
    Liensinine Diperchlor​ate is a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn. Liensinine Diperchlor​ate inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. Liensinine Diperchlor​ate has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
  • HY-12248
    Telaglenastat

    CB-839

    Glutaminase Autophagy Cancer
    Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inudces autophagy and has antitumor activity.
  • HY-N2500
    Deoxypodophyllotoxin

    Microtubule/Tubulin Apoptosis Autophagy Infection Cardiovascular Disease
    Deoxypodophyllotoxin (DPT), a derivative of podophyllotoxin, is a lignan with potent antimitotic, anti-inflammatory and antiviral properties isolated from rhizomes of Sinopodophullumhexandrum (Berberidaceae). Deoxypodophyllotoxin, targets the microtubule, has a major impact in oncology not only as anti-mitotics but also as potent inhibitors of angiogenesis. Deoxypodophyllotoxin induces cell autophagy and apoptosis. Deoxypodophyllotoxin evokes increase of intracellular Ca 2+ concentrations in DRG neurons.
  • HY-B0968
    Trimetazidine dihydrochloride

    Autophagy Cardiovascular Disease
    Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
  • HY-W017212
    Methyl cinnamate

    Methyl 3-phenylpropenoate

    Tyrosinase Bacterial AMPK Infection Metabolic Disease
    Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway.
  • HY-N3807
    Enniatin B1

    Acyltransferase ERK NF-κB Cancer Infection Cardiovascular Disease
    Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
  • HY-15477
    YS-49

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-N1990
    Gypenoside XLIX

    PPAR Inflammation/Immunology Cardiovascular Disease
    Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
  • HY-109121
    Reldesemtiv

    CK-2127107

    Others Cardiovascular Disease
    Reldesemtiv (CK-2127107) is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in a heart failure model.
  • HY-113673
    A-935142

    Potassium Channel Cardiovascular Disease
    A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization.
  • HY-108638
    NSC 146109 hydrochloride

    MDM-2/p53 Cancer
    NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and could be of value in treating breast cancer. NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes[1].
  • HY-116330A
    Hyperforin dicyclohexylammonium salt

    Hyperforin DCHA

    TRP Channel Calcium Channel Neurological Disease
    Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
  • HY-77251
    TAK1/MAP4K2 inhibitor 1

    MAP4K MAP3K Cancer
    TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
  • HY-114363A
    SRI 31215 TFA

    c-Met/HGFR Cancer
    SRI 31215 (TFA), a triplex inhibitor of matriptase, hepsin and hepatocyte growth factor activator (HGFA) with IC50s of 0.69 μM, 0.65 μM, 0.3 μM, blocks pro-HGF activation and thus mimics the activity of HAI-1/2.
  • HY-P1260
    FSLLRY-NH2

    Protease-Activated Receptor (PAR) Neurological Disease
    FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-112473
    NAV-2729

    Others Cancer
    NAV-2729 is a dual Arf1/Arf6 activation inhibitor.
  • HY-P0252
    α-Melanocyte-Stimulating Hormone (MSH), amide

    Adenylate Cyclase Metabolic Disease
    α-Melanocyte-Stimulating Hormone (MSH), amide stimulates melanocortin 1 receptor that results in the activation of adenylyl cyclase.
  • HY-108599
    DCP-LA

    FR236924

    PKC Neurological Disease
    DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε.
  • HY-32348
    Doxercalciferol

    1.alpha.-Hydroxyvitamin D2

    VD/VDR Metabolic Disease Cancer
    Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.
  • HY-18965
    TAS-301

    PKC Cardiovascular Disease
    TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.
  • HY-111441
    1,4-Chrysenequinone

    Chrysene-1,4-dione

    Aryl Hydrocarbon Receptor Cancer
    1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR).
  • HY-B0131
    Prostaglandin E1

    PGE1

    Prostaglandin Receptor Endogenous Metabolite Metabolic Disease Endocrinology
    Prostaglandin E1 (PGE1) is a potent vasodilator and activates the prostaglandin E1 (EP) receptor.
  • HY-15252
    Reparixin L-lysine salt

    Repertaxin L-lysine salt

    CXCR Cancer Inflammation/Immunology Endocrinology
    Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.
  • HY-B0345A
    ATP disodium salt

    Disodium adenosine triphosphate; Adenosine 5'-triphosphate disodium salt

    P2X Receptor Metabolic Disease
    ATP disodium salt is a phosphate-group donor for substrate activation in metabolic reactions and the coenzyme for a large number of kinases.
  • HY-107854
    N-Acetyl-5-hydroxytryptamine

    N-Acetylserotonin; Normelatonin; O-Demethylmelatonin

    Endogenous Metabolite Trk Receptor Neurological Disease
    N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor.
  • HY-15840
    YLF-466D

    C24

    AMPK Cancer
    YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
  • HY-B0236
    6-Aminocaproic acid

    EACA; Epsilon-Amino-n-caproic Acid; 6-Aminohexanoic acid

    Others Metabolic Disease
    6-Aminocaproic acid is an antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.
  • HY-106199
    Adenosine A1 receptor activator T62

    Adenosine Receptor Inflammation/Immunology Neurological Disease
    Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain.
  • HY-N0492
    α-Lipoic Acid

    Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid

    NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.
  • HY-110302
    6'-GNTI dihydrochloride

    Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
  • HY-103697
    Gardiquimod

    Toll-like Receptor (TLR) HIV Cancer Infection
    Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM.
  • HY-N0279
    Cardamonin

    Cardamomin; Alpinetin chalcone

    NOD-like Receptor (NLR) Aryl Hydrocarbon Receptor Inflammation/Immunology Cancer
    Cardamonin (Cardamomin), a natural flavone isolated from Alpinia katsumadai Hayata, acts as an aryl hydrocarbon receptor (AhR) activator. Cardamonin alleviates inflammatory bowel disease by the inhibition of NLRP3 inflammasome activation via an AhR/Nrf2/NQO1 pathway.
  • HY-P1740
    RGD peptide (GRGDNP)

    Integrin Apoptosis Inflammation/Immunology
    RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
  • HY-12519
    Oltipraz

    RP 35972; NSC 347901

    HIF/HIF Prolyl-Hydroxylase HIV Keap1-Nrf2 Cancer
    Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
  • HY-10119
    Vorapaxar

    SCH 530348

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
  • HY-P1375
    [D-Trp7,9,10]-Substance P

    mAChR
    [D-Trp7,9,10]-Substance P is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P does not inhibit Gi/o activation by M2 ACh receptors.
  • HY-P0316
    TP508

    Thrombin NO Synthase Cardiovascular Disease
    TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 activates endothelial cells and stem cells to revascularize and regenerate tissues.
  • HY-W015445
    SD-169

    p38 MAPK Metabolic Disease
    SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
  • HY-N0107
    Cyclovirobuxine D

    Apoptosis Autophagy mTOR Akt Cardiovascular Disease
    Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR. Cyclovirobuxine D inhibits cell proliferation of gastric cancer cells through suppression of cell cycle progression and inducement of mitochondria-mediated apoptosis. Cyclovirobuxine D is beneficial for heart failure induced by myocardial infarction.
  • HY-15477A
    YS-49 monohydrate

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-112558
    AZ3451

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  • HY-124960
    CTPB

    Histone Acetyltransferase Cancer
    CTPB is a good activator of p300 histone acetyl transferase (HAT) enzyme.
  • HY-17517
    Tiadinil

    Bacterial Infection
    Tiadinil is a plant activator of systemic acquired resistance, boosts the production of herbivore-induced plant volatiles; fungicide.
  • HY-101790
    ZM223

    NEDD8-activating Enzyme Cancer
    ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active.
  • HY-W040055
    D-(+)-Neopterin

    2-Amino-6-((1S,2R)-1,2,3-trihydroxypropyl)pteridin-4(3H)-one

    Endogenous Metabolite Inflammation/Immunology
    D-(+)-Neopterin, a catabolic product of guanosine triphosphate (GTM), serves as a marker of cellular immune system activation.
  • HY-N6630
    6-Methylflavone

    GABA Receptor Neurological Disease
    6-Methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.
  • HY-15577
    GSK3787

    PPAR Cancer
    GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
  • HY-P1260A
    FSLLRY-NH2 TFA

    Protease-Activated Receptor (PAR) Neurological Disease
    FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-12639
    Bephenium

    Parasite Infection
    Bephenium is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator.
  • HY-10590
    TWS119

    GSK-3 Autophagy Neurological Disease Cancer
    TWS119 is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
  • HY-101371
    Hesperin

    Keap1-Nrf2 Cancer
    Hesperin is a bioactive ingredient present in Japanese horseradish (wasabi) and has been shown to be an Nrf2 activator.
  • HY-100181
    PF-04991532

    Glucokinase Metabolic Disease
    PF-04991532 is a potent, hepatoselective glucokinase activator with EC50s of 80 and 100 nM in human and rat, respectively.
  • HY-10257
    BAY 11-7085

    BAY 11-7083

    NF-κB Ferroptosis Apoptosis Cancer
    BAY 11-7085 is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.
  • HY-12885A
    ADU-S100 disodium salt

    MIW815 disodium salt; ML RR-S2 CDA disodium salt

    STING Inflammation/Immunology
    ADU-S100 disodium salt (MIW815 disodium salt) is an activator of stimulator of interferon genes (STING).
  • HY-117793
    I-191

    Protease-Activated Receptor (PAR) Cancer
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
  • HY-P0249A
    Phe-Met-Arg-Phe amide trifluoroacetate

    Potassium Channel Neurological Disease
    Phe-Met-Arg-Phe amide trifluoroacetate is an activator of K + current, with ED50 of 23 nM in the peptidergic caudodorsal neurons.
  • HY-B1399
    3-Methylsalicylic acid

    o-Cresotic acid; Hydroxytoluic acid

    Others Cardiovascular Disease
    3-Methylsalicylic acid is a salicylic acid derivative compound with marked fibrinolytic activity in human plasma by activating its fibrinolytic system.
  • HY-114398
    BAY-293

    Ras Cancer
    BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.
  • HY-100581
    CORM-3

    NF-κB NOD-like Receptor (NLR) Inflammation/Immunology
    CORM-3, a water-soluble carbon monoxide-releasing molecule, attenuates NF-κB p65 nuclear translocation, reduces ROS generation and enhances intracellular glutathione and superoxide dismutase levels. CORM-3 reduces NLRP3 inflammasome activation.
  • HY-136477
    Pentagamavunon-1

    PGV-1

    Apoptosis COX VEGFR NF-κB Cancer
    Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.
  • HY-10119A
    Vorapaxar sulfate

    SCH 530348 sulfate

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
  • HY-103697A
    Gardiquimod diTFA

    Toll-like Receptor (TLR) HIV Cancer Infection
    Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
  • HY-P1375A
    [D-Trp7,9,10]-Substance P TFA

    mAChR
    [D-Trp7,9,10]-Substance P TFA is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P TFA does not inhibit Gi/o activation by M2 ACh receptors.
  • HY-B1816
    Zaprinast

    M&B 22948

    Phosphodiesterase (PDE) Neurological Disease Cardiovascular Disease Endocrinology
    Zaprinast (M&B 22948) is an inhibitor of cGMP-selective Phosphodiesterases(PDEs). Zaprinast is a G protein-coupled receptor (GPR) 35 agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.
  • HY-P1740A
    RGD peptide (GRGDNP) (TFA)

    Integrin Apoptosis Inflammation/Immunology Cancer
    RGD peptide (GRGDNP) (TFA) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) (TFA) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
  • HY-112769
    EX229

    AMPK Metabolic Disease
    EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.
  • HY-N2485
    4'-Methoxyresveratrol

    4'-O-Methylresveratrol

    Others Inflammation/Immunology
    4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.
  • HY-N0896
    Inulicin

    1-O-Acetylbritannilactone

    NF-κB COX Cancer Inflammation/Immunology
    Inulicin (1-O-Acetylbritannilactone) is an active compound isolated from Inula Britannica L. Inulicin (1-O-Acetylbritannilactone) inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone) inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
  • HY-124748A
    ENMD-1068 hydrochloride

    Protease-Activated Receptor (PAR) Inflammation/Immunology Cardiovascular Disease
    ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist with antiangiogenic and anti-inflammatory activities. ENMD-1068 hydrochloride reduces epatic stellate cells (HSCs) activation and collagen expression through the inhibiton of TGF-β1/Smad signal transduction.
  • HY-100932A
    ML-9 Free Base

    Myosin Cancer
    ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
  • HY-N2959
    Brevilin A

    JAK STAT Apoptosis Autophagy Cancer
    Brevilin A is a sesquiterpene lactone isolated from Centipeda minima with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM) in Cancer Cells. Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.
  • 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-N6979
    Crustecdysone

    20-Hydroxyecdysone

    Caspase Autophagy Endogenous Metabolite Cardiovascular Disease
    Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Cyanotis arachnoides C.B.Clarke which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP. Crustecdysone exhibits regulatory or protective roles in the cardiovascular system. Crustecdysone is an active metabolite of Ecdysone (α-Ecdysone; HY-N0179)
  • HY-12639A
    Bephenium hydroxynaphthoate

    Parasite Infection
    Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator.
  • HY-19800
    ML-098

    CID-7345532

    Ras Cancer
    ML-098 (CID-7345532) is an activator of the GTP-binding protein Rab7 with an EC50 of 77.6 nM.
  • HY-17613
    Evocalcet

    KHK7580

    CaSR Metabolic Disease
    Evocalcet has an activating effect on calcium sensing receptor (CaSR) extracted from patent WO 2017061621 A1, compound A.
  • HY-N0897
    Corylifol A

    Corylifol-A; Corylinin

    STAT Others
    Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC50 of 0.81 μM.
  • HY-B1897A
    Menadione bisulfite sodium

    Menadione sodium bisulfite; Vitamin K3 sodium bisulfite

    Others
    Menadione bisulfite (sodium) is used as an agent to induce acute oxidative stress, and to function as a plant-defense activator against several pathogens.
  • HY-A0070
    Liothyronine sodium

    Triiodothyronine sodium; 3,3',5-Triiodo-L-thyronine sodium; T3 sodium

    Thyroid Hormone Receptor Cancer Endocrinology
    Liothyronine sodium is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity.
  • HY-100941
    CCCP

    Carbonyl cyanide 3-chlorophenylhydrazone; Carbonyl Cyanide m-Chlorophenylhydrazone

    STING IFNAR Mitochondrial Metabolism Bacterial Cancer Inflammation/Immunology
    CCCP is an oxidative phosphorylation uncoupler. CCCP induces activation of PINK1 leading to Parkin Ser65 phosphorylation.
  • HY-N2506
    Ginsenoside Ra1

    Others Cardiovascular Disease
    Ginsenoside Ra1 is a component from ginseng, inhibits protein tyrosine kinase (PTK) activation induced by hypoxia/reoxygenation.
  • HY-16696
    SN 2

    TRP Channel Others
    SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8±0.13 μM.
  • HY-14645A
    (+)-DHMEQ

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

    Keap1-Nrf2 Inflammation/Immunology
    (+)-DHMEQ is an activator of antioxidant transcription factor Nrf2. (+)-DHMEQ is the enantiomer of (-)-DHMEQ. (-)-DHMEQ inhibits NF-kB than its enantiomer (+)-DHMEQ.
  • HY-N0486
    L-Leucine

    mTOR Metabolic Disease
    L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.
  • HY-P0078
    TRAP-6

    PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    TRAP-6 (PAR-1 agonist peptide) is a protease-activated receptor 1 (PAR1) agonist.
  • HY-108599A
    DCPLA-ME

    DCPLA methyl ester

    PKC Neurological Disease
    DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases.
  • HY-18723
    Yoda 1

    Others Cardiovascular Disease
    Yoda 1 is a Piezo1 agonist. Yoda 1 activates purified Piezo1 channels.
  • HY-A0070A
    Liothyronine

    Triiodothyronine; 3,3',5-Triiodo-L-thyronine; T3

    Thyroid Hormone Receptor Endogenous Metabolite Cancer Endocrinology
    Liothyronine is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity.
  • HY-112125A
    KRN2 bromide

    Others Inflammation/Immunology
    KRN2 (bromide) is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM.
  • HY-101746
    GSK376501A

    PPAR Metabolic Disease
    GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
  • HY-15530
    CID-2858522

    NF-κB Inflammation/Immunology Cancer
    CID-2858522 is a highly potent and selective antigen receptor-mediated NF-κB activation inhibitor with an IC50 of 70 nM.
  • HY-P0195
    Bombesin

    Bombesin Receptor Metabolic Disease Neurological Disease
    Bombesin is a tetradecapeptide originally isolated from frog skin; plays an important role in the release of gastrin and the activation of G-protein receptors.
  • HY-50703
    MK-2461

    c-Met/HGFR Cancer
    MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.
  • HY-111202
    Pyributicarb

    TSH-888

    Cytochrome P450 Inflammation/Immunology
    Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
  • HY-P0316A
    TP508 TFA

    Thrombin NO Synthase Cardiovascular Disease
    TP508 TFA is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 TFA activates endothelial cells and stem cells to revascularize and regenerate tissues.
  • HY-108586
    NS3623

    Potassium Channel Neurological Disease
    NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels.
  • HY-50694
    Senicapoc

    ICA-17043

    Potassium Channel Others
    Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca 2+-activated K + channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca 2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
  • HY-N6241
    (S)-Falcarinol

    (S)-Panaxynol; (S)-Carotatoxin

    Keap1-Nrf2 Cancer Cardiovascular Disease
    (S)-Falcarinol ((S)-Panaxynol), one of the major polyacetylenes isolated from Panax ginseng, has antitumor activity. (S)-Falcarinol is the most potent antiplatelet agent in ginseng and its mechanism of action is chiefly due to the inhibition of thromboxane formation. (S)-Falcarinol is a potent Nrf2 activator.
  • HY-14994
    SCH79797 dihydrochloride

    Protease-Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
  • HY-14600
    Rosiglitazone maleate

    BRL 49653C

    PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology
    Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
  • HY-N7526
    Naphthazarin

    DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone

    Apoptosis Cancer Neurological Disease
    Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects.
  • HY-117433
    4-Hydroperoxy cyclophosphamide

    DNA Alkylator/Crosslinker Apoptosis Reactive Oxygen Species Drug Metabolite
    4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide is used to treat lymphomas and autoimmune disorders.
  • HY-100410
    FCCP

    Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone

    Mitochondrial Metabolism Cancer
    FCCP is an uncoupler of oxidative phosphorylation in mitochondria. FCCP induces activation of PINK1 leading to Parkin Ser65 phosphorylation.
  • HY-N0516
    Casticin

    Vitexicarpin

    STAT Inflammation/Immunology
    Casticin is a methyoxylated flavonol isolated from Viticis Fructus, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
  • HY-101396
    ICA-069673

    Potassium Channel Neurological Disease
    ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM.
  • HY-13719
    Oleandrin

    Na+/K+ ATPase Apoptosis Cancer
    Oleandrin inhibits the Na +, K +-ATPase activity with an IC50 of 620 nM. Oleandrin induces apoptosis via activating endoplasmic reticulum stress.
  • HY-128586A
    TAS4464 hydrochloride

    NEDD8-activating Enzyme Cancer
    TAS4464 (hydrochloride) is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.
  • HY-13423
    Tenovin-1

    Sirtuin MDM-2/p53 Autophagy Cancer
    Tenovin-1 is an inhibitor of sirtuin 1 and sirtuin 2, an activator of p53 and may have potential in the management of cancer.
  • HY-N1411
    Platycodin D

    AMPK Metabolic Disease
    Platycodin D is a saponin isolated from Platycodi Radix, acts as an activator of AMPKα, with anti-obesity property.
  • HY-B0887
    Permethrin

    NRDC-143

    Parasite Infection
    Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
  • HY-114481
    Imidazole ketone erastin

    IKE

    Ferroptosis Cancer
    Imidazole ketone erastin (IKE) is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system Xc - and an activator of ferroptosis.
  • HY-13523
    PAC-1

    Procaspase activating compound 1

    Caspase Autophagy Apoptosis Cancer
    PAC-1 is an activator of procaspase-3 induces apoptosis in cancer cells with EC50 of 2.08 μM.
  • HY-P1534
    Adrenomedullin (1-50), rat

    CGRP Receptor Cardiovascular Disease
    Adrenomedullin (1-50), rat is a 50 amino acid peptide, which induces a selective arterial vasodilation via activation of CGRP1 receptor.
  • HY-N0674A
    Dehydrocorydaline chloride

    13-Methylpalmatine chloride

    p38 MAPK Autophagy Cancer
    Dehydrocorydaline chloride is an alkaloidal that has anti-inflammatory and anti-cancer activities. Dehydrocorydaline chloride can elevate p38 MAPK activation.
  • HY-136352
    Adenosine 5'-succinate

    Others Others
    Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin.
  • HY-17363
    Dimethyl fumarate

    DMF

    Keap1-Nrf2 Endogenous Metabolite Inflammation/Immunology
    Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
  • HY-N1913
    Danshensu

    Dan shen suan A; Salvianic acid A

    Keap1-Nrf2 Autophagy Apoptosis Cardiovascular Disease Cancer
    Danshensu, an active ingredient of Salvia miltiorrhiza, shows wide cardiovascular benefit by activating Nrf2 signaling pathway.
  • HY-103638
    3-Methoxytyramine hydrochloride

    3-O-methyl Dopamine hydrochloride

    Drug Metabolite Endogenous Metabolite Neurological Disease
    3-Methoxytyramine hydrochloride is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1).
  • HY-111498
    RGX-104

    LXR Cancer Inflammation/Immunology
    RGX-104 is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-128586
    TAS4464

    NEDD8-activating Enzyme Cancer
    TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.
  • HY-19097
    Ro-24-4736

    Others Cardiovascular Disease
    Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action.
  • HY-101580
    Paliroden

    SR 57667

    Others Neurological Disease
    Paliroden is an orally bioactive neurotrophic, non-peptidic compound that activates synthesis of endogenous neurotrophines, used for treatment of Alzheimer's Disease and Parkinson's.
  • HY-N6971
    Cimiracemoside C

    Cimicifugoside M

    AMPK Metabolic Disease
    Cimiracemoside C is an active component of Cimicifuga racemosa, activates AMPK, has the potential activity against diabetes.
  • HY-N2318
    Podocarpic acid

    TRP Channel Neurological Disease
    Podocarpic acid is a natural product, which has the best all-round positive effect and acts as a novel TRPA1 activator.
  • HY-100407
    JNJ16259685

    mGluR Neurological Disease
    JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
  • HY-N0290
    Mangiferin

    NF-κB Keap1-Nrf2 Apoptosis Cancer
    Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50.
  • HY-121618
    α-Thujone

    GABA Receptor Reactive Oxygen Species Parasite Apoptosis Autophagy Cancer Infection Neurological Disease
    α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
  • HY-117102
    ANI-7

    Aryl Hydrocarbon Receptor Checkpoint Kinase (Chk) Cancer
    ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
  • HY-124037
    SRT 1460

    Sirtuin Cancer
    SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues.
  • HY-130354
    Dibutyryl-cGMP sodium

    Bt2cGMP sodium

    Potassium Channel Cardiovascular Disease
    Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels.
  • HY-15002
    AST 487

    NVP-AST 487

    RET FLT3 VEGFR c-Kit Bcr-Abl Cancer
    AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
  • HY-14590
    Kaempferol

    Kempferol; Robigenin

    Estrogen Receptor/ERR Autophagy Mitophagy Apoptosis HIV Parasite Endogenous Metabolite Cancer
    Kaempferol inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK.
  • HY-108594
    PD-118057

    Potassium Channel Metabolic Disease
    PD-118057 is a human ether-a-go-go-related gene (hERG) channel activator that does not cause hERG blockade.
  • HY-19354
    Aglafoline

    Aglafolin; Rocaglamide U; (-)-Methyl rocaglate

    Others Cardiovascular Disease
    Aglafoline inhibits in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor).
  • HY-N0628
    Kaempferitrin

    Lespedin; Lespenephryl

    Insulin Receptor Cancer Metabolic Disease Endocrinology
    Kaempferitrin is a natural flavonoid, possesses antinociceptive, anti-inflammatory, anti-diabetic, antitumoral and chemopreventive effects, and activates insulin signaling pathway.
  • HY-15251
    Reparixin

    Repertaxin; DF 1681Y

    CXCR Inflammation/Immunology Endocrinology Cancer
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
  • HY-14351
    AC-264613

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC50 of 7.5.
  • HY-107004A
    Amotosalen hydrochloride

    S-59

    Others Inflammation/Immunology
    Amotosalen hydrochloride (S-59) is a light-activated, DNA-, RNA-crosslinking psoralen compound, which is used to neutralise pathogens.
  • HY-19330
    DASA-58

    Pyruvate Kinase Cancer
    DASA-58 is a potent activator of pyruvate kinase M2 (PKM2) with an AC90 of 680 nM, and an AC50 of 38 nM.
  • HY-103683
    PF-06409577

    AMPK Metabolic Disease
    PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.
  • HY-B0686
    Eptifibatide

    Integrin Cardiovascular Disease
    Eptifibatide is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity.
  • HY-18377
    Bioymifi

    DR5 Activator

    TNF Receptor Cancer
    Bioymifi(DR5 Activator) is the first novel and potent small-molecule activatior of the TRAIL receptor DR5 in human cancer cells.
  • HY-19793
    RS-1

    RAD51 CRISPR/Cas9 Cancer
    RS-1 is a RAD51 activator, and also increases CRISPR/Cas9-mediated knock-in efficiencies.
  • HY-18985
    Phorbol 12,13-dibutyrate

    Phorbol dibutyrate; PDBu

    PKC Cancer
    Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter.
  • HY-128588
    STAT3-IN-3

    STAT Cancer
    STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3).
  • HY-108634
    Apafant

    WEB 2086

    Others Inflammation/Immunology
    Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
  • HY-N2065
    Withaferin A

    NF-κB Ferroptosis Cancer Inflammation/Immunology
    Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities.
  • HY-B0686A
    Eptifibatide acetate

    Integrin Cardiovascular Disease
    Eptifibatide acetate is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity.
  • HY-15869
    Inauhzin

    INZ

    Sirtuin MDM-2/p53 Cancer
    Inauhzin is a dual SirT1/IMPDH2 inhibitor, and acts as an activator p53, used in the research of cancer.
  • HY-14831
    Arhalofenate

    MBX 102; JNJ 39659100

    PPAR Metabolic Disease
    Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
  • HY-12524
    Bikinin

    Abrasin

    GSK-3 Others
    Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling.
  • HY-13519
    TRAM-34

    Potassium Channel Neurological Disease
    TRAM-34 is a highly selective blocker of intermediate-conductance calcium-activated K + channel (IKCa1) (Kd=20 nM).
  • HY-78131B
    (R)-(-)-Ibuprofen

    (R)-Ibuprofen

    NF-κB Inflammation/Immunology Cancer
    (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
  • HY-N6946
    Mitraphylline

    Others Inflammation/Immunology
    Mitraphylline is the major pentacyclic oxindolic alkaloid presented in Uncaria tomentosa. Mitraphylline inhibits lipopolysaccharide-mediated activation of primary human neutrophils.
  • HY-101790A
    ZM223 hydrochloride

    NEDD8-activating Enzyme Cancer
    ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.
  • HY-N1372A
    Fangchinoline

    HIV FAK Apoptosis Autophagy Cancer Infection
    Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer.
  • HY-135887
    ZX-29

    ALK Apoptosis Autophagy Cancer
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
  • HY-10224
    Panobinostat

    LBH589; NVP-LBH589

    HDAC Autophagy HIV Apoptosis Cancer
    Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma.
  • HY-10029
    Nutlin-3a

    MDM-2/p53 E1/E2/E3 Enzyme Autophagy Apoptosis Cancer
    Nutlin-3a, an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas.
  • HY-107818
    4-Hydroxychalcone

    NF-κB Inflammation/Immunology Cardiovascular Disease
    4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice.
  • HY-B1546
    Benzamil

    Benzylamiloride

    Sodium Channel Na+/Ca2+ Exchanger Neurological Disease
    Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
  • HY-114372
    Lycopodine

    Lipoxygenase Caspase Apoptosis Cancer
    Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  • HY-B1546A
    Benzamil hydrochloride

    Benzylamiloride hydrochloride

    Na+/Ca2+ Exchanger Sodium Channel Neurological Disease
    Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
  • HY-126429
    Nav1.1 activator 1

    Sodium Channel Neurological Disease
    Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant τ of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.
  • HY-W011641
    (±)-Naringenin

    Potassium Channel Cardiovascular Disease
    (±)-Naringenin is a naturally-occurring flavonoid. (±)-Naringenin displays vasorelaxant effect on endothelium-denuded vessels via the activation of BKCa channels in myocytes.
  • HY-16785
    Veledimex

    INXN-1001; RG-115932

    Interleukin Related Cytochrome P450 Inflammation/Immunology Cancer
    Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
  • HY-16785A
    Veledimex racemate

    INXN-1001 racemate; RG-115932 racemate

    Interleukin Related Cytochrome P450 Cancer Inflammation/Immunology
    Veledimex racemate (INXN-1001 racemate) is the racemate of veledimex. Veledimex is an orally available, small-molecule activator ligand for the RheoSwitch Therapeutic System.
  • HY-B0513
    Methylthiouracil

    MTU

    NF-κB TNF Receptor Interleukin Related ERK Inflammation/Immunology Cancer
    Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
  • 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-15285
    Doxercalciferol-D3

    VD/VDR Metabolic Disease
    Doxercalciferol-D3 is the deuterated form of Doxercalciferol, which is a Vitamin D2 analog that acts as a vitamin D receptor activator (VDRA).
  • HY-N2283
    Deltonin

    ERK Akt Endogenous Metabolite Cancer
    Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis Wright, with antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
  • HY-N0593
    Deoxycholic acid

    Cholanoic Acid; Desoxycholic acid

    GPCR19 Endogenous Metabolite Metabolic Disease
    Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
  • HY-32735
    Triptolide

    PG490

    NF-κB Apoptosis Cancer
    Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory and antiproliferative effects. Triptolide is a NF-κB activation inhibitor.
  • HY-15725
    CDDO-Im

    RTA-403; TP-235; CDDO-Imidazolide

    Keap1-Nrf2 PPAR Ferroptosis Cancer
    CDDO-Im (RTA-403) is an activator of Nrf2 and PPAR, with Kis of 232 and 344 nM for PPARα and PPARγ.
  • HY-111789
    TAK-981

    E1/E2/E3 Enzyme Cancer Inflammation/Immunology
    TAK-981 is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
  • HY-12213
    CDDO-EA

    CDDO ethyl amide; TP319; RTA 405

    Keap1-Nrf2 Cancer
    CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator.
  • HY-19205A
    CMI-392

    Lipoxygenase Inflammation/Immunology
    CMI-392 is a dual 5-lipoxygenese inhibitor and platelet-activating factor (PAF) receptor antagonist with IC50s of 100 and 10 nM, respectively.
  • HY-Y1683
    DL-Menthol

    Racementhol

    GABA Receptor Others
    DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol induces surgical anesthesia for fish that relates to the activation of GABAA receptor.
  • HY-N2084
    Perillartine

    DL-Perillartine

    Endogenous Metabolite Others
    Perillartine is a sweetener, which activates the taste receptor type 1 member 2 (Tas1r2) subunit in a species-dependent manner.
  • HY-N0593A
    Deoxycholic acid sodium salt

    Sodium deoxycholate

    GPCR19 Endogenous Metabolite Metabolic Disease
    Deoxycholic acid sodium salt is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
  • HY-N2337
    11beta-Hydroxyprogesterone

    11β-Hydroxyprogesterone

    Endogenous Metabolite Cardiovascular Disease
    11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.
  • HY-P0249
    Phe-Met-Arg-Phe, amide

    Potassium Channel Neurological Disease
    Phe-Met-Arg-Phe, amide dose dependently (ED50=23 nM) activates a K + current in the peptidergic caudodorsal neurons.
  • HY-13694
    Methionine

    MRX-1024; D-Methionine

    GABA Receptor Cancer Neurological Disease
    Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
  • HY-131281
    Ivabradine impurity 1

    Others Others
    Ivabradine impurity 1 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
  • HY-P1562
    PUMA BH3

    Bcl-2 Family Cancer
    PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
  • HY-B0923
    Danthron

    Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone

    AMPK Autophagy Bacterial Virus Protease Cancer
    Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.
  • HY-Y0152
    Cinchonine

    (8R,9S)-Cinchonine; LA40221

    Apoptosis Parasite Cancer
    Cinchonine is a natural compound present in Cinchona bark. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
  • HY-101833
    YM-264

    Others Inflammation/Immunology
    YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
  • HY-W007355
    Skatole

    3-Methylindole; 3-Methyl-1H-indole

    Aryl Hydrocarbon Receptor p38 MAPK Endogenous Metabolite Autophagy Bacterial Fungal Others
    Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38.
  • HY-N0629
    Maslinic acid

    Crategolic acid; 2α-Hydroxyoleanolic acid

    NF-κB Bacterial HIV Inflammation/Immunology Cancer
    Maslinic acid can inhibit the DNA-binding activity of NF-κB p65 and abolish the phosphorylation of IκB-α, which is required for p65 activation.
  • HY-131282
    Ivabradine impurity 2

    Others Others
    Ivabradine impurity 2 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
  • HY-N0892
    AKBA

    Acetyl-11-keto-β-boswellic acid

    HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species Endogenous Metabolite Cancer
    AKBA (Acetyl-11-keto-β-boswellic acid) is an active triterpenoid compound from the extract of Boswellia serrate and a novel Nrf2 activator.
  • HY-N7452
    Coumermycin A1

    Bacterial Metabolic Disease
    Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.
  • HY-N2025
    Oroxin A

    PARP Glucosidase Metabolic Disease
    Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE), activates peroxisome proliferator-activated receptor γ (PPARγ) by docking into the PPARγ protein ligand-binding domain. Oroxin A exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.
  • HY-N7018
    20-Hydroxyganoderic Acid G

    Others Inflammation/Immunology
    20-Hydroxyganoderic Acid G is a lanostane triterpenoid obtained from the EtOH extract of fruiting bodies of the Ganoderma curtisii. 20-Hydroxyganoderic Acid G inhibits BV-2 microglia cells activated by LPS with an IC50 of 21.33 μM. 20-Hydroxyganoderic Acid G has therapeutic potential in the drug discovery of nerve inflammation diseases associated with microglia activated by LPS.
  • HY-103370
    Talniflumate

    BA 7602-06

    Chloride Channel Inflammation/Immunology
    Talniflumate (BA 7602-06) is the prodrug of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase. Talniflumate is an orally active Ca 2+-activated Cl - channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome.
  • HY-116084
    Trimethylamine N-oxide

    NOD-like Receptor (NLR) Reactive Oxygen Species TGF-beta/Smad Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
  • HY-100487
    TAK-243

    MLN7243

    E1/E2/E3 Enzyme NF-κB Apoptosis Cancer
    TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
  • HY-16312
    MDL-29951

    iGluR Neurological Disease
    MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [ 3H]glycine binding in vitro and in vivo.
  • HY-N0377
    Liquiritigenin

    4',7-Dihydroxyflavanone

    Estrogen Receptor/ERR Cancer Inflammation/Immunology Neurological Disease
    Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC50 of 36.5 nM for activation of the ERE tk-Luc.
  • HY-16511
    Upamostat

    WX-671

    Ser/Thr Protease PAI-1 Cancer
    Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
  • HY-B0837
    Emamectin Benzoate

    MK-244

    GABA Receptor Infection
    Emamectin Benzoate (MK-244) works as a chloride channel activator by binding gamma aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods.
  • HY-N0168
    Hesperetin

    p38 MAPK Apoptosis Autophagy Neurological Disease Cancer
    Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
  • HY-50714
    Quiflapon sodium

    MK-591 sodium

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
  • HY-112331
    SJ000291942

    TGF-β Receptor Cancer
    SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
  • HY-15707
    NS6180

    Potassium Channel Inflammation/Immunology
    NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.
  • HY-127018
    Maltoheptaose

    Others Metabolic Disease
    Maltoheptaose is an activator of phosphorylase B to prepare heptulose-2-phosphate. Maltoheptaose is a maltooligosaccharide contanins seven glucose units.
  • HY-117962A
    BI 703704

    Guanylate Cyclase Metabolic Disease
    BI 703704 is a potent soluble guanylate cyclase (sGC) activator. BI 703704 inhibits the progression of diabetic nephropathy in the ZSF1 rat.
  • HY-15253
    Tiplaxtinin

    PAI-039; Tiplasinin

    PAI-1 Apoptosis Metabolic Disease Cancer
    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
  • HY-131283
    8-Demethyl Ivabradine

    Drug Metabolite Endocrinology
    8-Demethyl Ivabradine is a metabolite of Ivabradine. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
  • HY-109128
    Danicamtiv

    Myosin Cancer
    Danicamtiv, an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.
  • HY-N0708
    Vanillic acid

    NF-κB Bacterial Endogenous Metabolite Infection Inflammation/Immunology
    Vanillic acid is a flavoring agent found in edible plants and fruits. Vanillic acid inhibits NF-κB activation. Anti-inflammatory, antibacterial, and chemopreventive effects.
  • HY-127018A
    Maltoheptaose hydrate

    Others Metabolic Disease
    Maltoheptaose hydrate is an activator of phosphorylase B to prepare heptulose-2-phosphate. Maltoheptaose hydrate is a maltooligosaccharide contanins seven glucose units.
  • HY-12306
    8-Bromo-cAMP sodium salt

    8-Br-Camp sodium salt

    PKA Cancer
    8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA).
  • HY-N0606
    Ginsenoside Rh3

    Keap1-Nrf2 Inflammation/Immunology
    Ginsenoside Rh3 is a bacterial metabolite of Ginsenoside Rg5. Ginsenoside Rh3 treatment in human retinal cells induces Nrf2 activation.
  • HY-13294
    Impurity C of Alfacalcidol

    VD/VDR Metabolic Disease
    Impurity of Alfacalcidol. Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) is a non-selective VDR activator medication.
  • HY-100611
    CaCCinh-A01

    Chloride Channel Inflammation/Immunology Cancer
    CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively.
  • HY-N6913
    3α-Hydroxymogrol

    AMPK Metabolic Disease
    3α-Hydroxymogrol is a triterpenoid isolated from Siraitia grosvenorii Swingle, acts as a potent AMPK activator, and enhances AMPK phosphorylation.
  • HY-112920
    TM-25659

    Others Metabolic Disease
    TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.
  • HY-B0099
    Edaravone

    MCI-186

    MMP Apoptosis Neurological Disease
    Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
  • HY-129364
    5-A-RU hydrochloride

    5-Amino-6-(D-ribitylamino)uracil hydrochloride

    Others Inflammation/Immunology
    5-A-RU hydrochloride (5-Amino-6-(D-ribitylamino)uracil hydrochloride), a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU hydrochloride forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways.
  • HY-19356
    Rocaglamide

    Roc-A

    NF-κB HSP Eukaryotic Initiation Factor (eIF) Cancer
    Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.
  • HY-129364A
    5-A-RU

    5-Amino-6-(D-ribitylamino)uracil

    Others Inflammation/Immunology
    5-A-RU (5-Amino-6-(D-ribitylamino)uracil), a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways.
  • HY-122214
    AC-73

    Autophagy Cancer
    AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells. AC-73 is also an anti-proliferative drug and an inducer of autophagy in leukemic cells.
  • HY-10181
    Dasatinib

    BMS-354825

    Bcr-Abl Src Autophagy Apoptosis Cancer
    Dasatinib (BMS-354825) is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor with IC50s of 0.6 nM, 0.8 nM, respectively. Dasatinib also inhibits Abl, Src, Fyn, c-Kit and c-Kit D816V with IC50s of 2.8 nM, 79 nM and 37 nM, respectively. Dasatinib also induces apoptosis and autophagy. Dasatinib shows potently antitumor activity and has the potential for chronic myelogenous leukemia (CML) treatment.
  • HY-12695B
    Guanosine 5'-triphosphate trisodium salt hydrate

    5'-GTP trisodium salt hydrate

    Others Others
    5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
  • HY-P1333
    Dynorphin A

    Opioid Receptor Neurological Disease
    Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors,  such as mu (MOR) and delta (DOR).
  • HY-111098
    GSK1702934A

    TRP Channel Cardiovascular Disease
    GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.
  • HY-118266
    BTdCPU

    Phosphatase Apoptosis Cancer
    BTdCPU is a potent heme-regulated eIF2α kinase (HRI) activator. BTdCPU promotes eIF2α phosphorylation and induced apoptosis in resistant cell.
  • HY-15098
    Apoptozole

    Apoptosis Activator VII

    HSP Apoptosis Cancer
    Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
  • HY-112675
    4-Octyl Itaconate

    Keap1-Nrf2 Inflammation/Immunology
    4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1.
  • HY-75041
    Calcitriol Impurities A

    VD/VDR Metabolic Disease
    Calcitriol Impurities A is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
  • HY-15718A
    Istaroxime hydrochloride

    PST2744 hydrochloride

    Na+/K+ ATPase Calcium Channel Cardiovascular Disease
    Istaroxime hydrochloride is a Na +/K +-ATPase inhibitor (IC50=0.11 μM) and a sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator.
  • HY-133127
    AR453588

    Glucokinase Metabolic Disease
    AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity.
  • HY-B1378
    Ethosuximide

    Calcium Channel Neurological Disease
    Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
  • HY-N2209
    Angeloylgomisin H

    PPAR Metabolic Disease
    Angeloylgomisin H, as a major lignin extract of Schisandra rubriflora, has the potential to improve insulin-stimulated glucose uptake by activating PPAR-γ.
  • HY-19770
    GSK2981278

    ROR Inflammation/Immunology
    GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
  • HY-P0004
    Lysipressin

    Lysine vasopressin; [Lys8]-Vasopressin

    Others Others
    Lysipressin is Antidiuretic hormone that have been found in pigs and some marsupial families. Induces contraction of the rabbit urinary bladder smooth muscle, activate adenylate-cyclase.
  • HY-133127A
    AR453588 hydrochloride

    Glucokinase Metabolic Disease
    AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity.
  • HY-101929
    CU-CPT17e

    Toll-like Receptor (TLR) Cancer Inflammation/Immunology
    CU-CPT17e is a potent multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9.
  • HY-12885
    ADU-S100

    MIW815; ML RR-S2 CDA

    STING Inflammation/Immunology
    ADU-S100 (MIW815), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.
  • HY-12357
    Bempedoic acid

    ETC-1002; ESP-55016

    ATP Citrate Lyase AMPK Metabolic Disease
    Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor. Bempedoic acid (ETC-1002) activates AMPK.
  • HY-100965
    Diphenyleneiodonium chloride

    DPI

    TRP Channel NADPH Oxidase Reactive Oxygen Species Inflammation/Immunology Neurological Disease
    Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC50 of 1 to 3 μM. Diphenyleneiodonium chloride selectively inhibits intracellular reactive oxygen species.
  • HY-10595
    Ro 28-1675

    Glucokinase Metabolic Disease
    Ro 28-1675 (Ro 0281675) is a potent allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM.
  • HY-B0649
    Propofol

    2,6-Diisopropylphenol

    GABA Receptor Endogenous Metabolite Neurological Disease
    Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
  • HY-13296
    PYR-41

    E1/E2/E3 Enzyme Apoptosis Cancer
    PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
  • HY-19084
    Ro-24-0238

    Others Inflammation/Immunology
    Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF.
  • HY-75992
    trans-Doxercalciferol

    Others Others
    trans-Doxercalciferol is an isomer of Doxercalciferol. Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.
  • HY-108596
    BL-1249

    Potassium Channel Inflammation/Immunology
    BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM).
  • HY-124151
    Adenosine-2'-monophosphate

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

    Adenosine Receptor Endogenous Metabolite Neurological Disease
    Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
  • HY-P1061
    Colivelin

    STAT Amyloid-β Neurological Disease
    Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
  • HY-110247
    TRAF-STOP inhibitor 6877002

    TNF Receptor NF-κB Inflammation/Immunology Cardiovascular Disease
    TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques.
  • HY-16708A
    ZLN024 hydrochloride

    AMPK Metabolic Disease
    ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
  • HY-16708
    ZLN024

    AMPK Metabolic Disease
    ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
  • HY-P1314
    2-Furoyl-LIGRLO-amide

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0..
  • HY-N0233
    Bavachin

    Corylifolin

    Estrogen Receptor/ERR Cancer
    Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
  • HY-119240
    CCT020312

    PERK Autophagy Cancer Neurological Disease
    CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
  • HY-101255
    ODQ

    Guanylate Cyclase Apoptosis Cancer
    ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
  • HY-N3196
    Neotuberostemonine

    Others Infection Inflammation/Immunology
    Neotuberostemonine, one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, attenuates bleomycin-induced pulmonary fibrosis by suppressing the recruitment and activation of macrophages.
  • HY-10535
    Evofosfamide

    TH-302

    Apoptosis Cancer
    Evofosfamide (TH-302) is a hypoxia-activated prodrug with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.
  • HY-N4322
    Decursinol angelate

    PKC Cancer Inflammation/Immunology
    Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities.
  • HY-77274
    Calcitriol Impurities D

    VD/VDR Metabolic Disease
    Calcitriol Impurities D is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
  • HY-12005
    Fingolimod hydrochloride

    FTY720

    LPL Receptor PAK Inflammation/Immunology Cancer
    Fingolimod hydrochloride is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride also is a pak1 activator.
  • HY-133739
    NBD-125

    RAR/RXR Cancer
    NBD-125 (B-12), a berberine analogue, is an RXRα activator, with an IC50 of 31.10 μM in KM12C cell.
  • HY-W011890
    Cridanimod

    Progesterone Receptor IFNAR Inflammation/Immunology
    Cridanimod is a potent progesterone receptor (PR) activator mediated through induction of IFNα and IFNβ expression. Cridanimod is a small-molecule immunomodulator and interferon inducer.
  • HY-109030
    Dorzagliatin

    HMS5552

    Glucokinase Metabolic Disease
    Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes.
  • HY-16642A
    LY2828360

    Cannabinoid Receptor Neurological Disease
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
  • HY-112929
    DT-061

    Phosphatase Cancer
    DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
  • HY-12343
    ML277

    CID-53347902

    Potassium Channel Cardiovascular Disease
    ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.
  • HY-N2370
    24-Hydroxycholesterol

    iGluR LXR Neurological Disease
    24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
  • HY-19700
    trans-Zeatin

    MEK ERK Endogenous Metabolite Others
    trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
  • HY-N0436
    Engeletin

    NF-κB Infection Inflammation/Immunology
    Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
  • HY-N6046
    Kamebakaurin

    NF-κB Cancer Inflammation/Immunology
    Kamebakaurin is a natural compound isolated from Isodon japonicus. Kamebakaurin is a potent inhibitor of NF-κB activation by directly targeting DNA-binding activity of p50.
  • HY-13108
    Bz 423

    BZ48

    Bcl-2 Family Inflammation/Immunology
    Bz 423 is a pro-apoptotic 1,4-benzodiazepine with therapeutic properties in murine models of lupus demonstrating selectivity for autoreactive lymphocytes, and activates Bax and Bak.
  • HY-N2530
    Notoginsenoside Fa

    Others Neurological Disease
    Notoginsenoside Fa, a protopanaxadiol (ppd)-type saponin isolated from P. notoginseng, could possibly activate and recover the function of degenerated brain.
  • HY-111498A
    RGX-104 free Acid

    LXR Cancer Inflammation/Immunology
    RGX-104 free Acid is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-P0233
    Melittin

    Phospholipase Cancer Inflammation/Immunology
    Melittin is a PLA2 activator, stimulates the activity of the low molecular weight PLA2, while it does not the increase activity of the high molecular weight PLA2.
  • HY-15145
    SRT 1720 Hydrochloride

    Sirtuin Autophagy Metabolic Disease
    SRT 1720 Hydrochloride is a selective activator of SIRT1 with an EC50 of 0.10 μM, and shows less potent activities on SIRT2 and SIRT3.
  • HY-B1560
    Bismuth subgallate

    Others Others
    Bismuth subgallate, a hemostatic agent, acts on coagulation factor XII (Hageman factor), leading to the activation of the coagulation cascade and improving early formation of a fibrin clot.
  • HY-P1061A
    Colivelin TFA

    STAT Amyloid-β Neurological Disease
    Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
  • HY-112671
    CDDO-dhTFEA

    RTA dh404

    Keap1-Nrf2 NF-κB Inflammation/Immunology
    CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB. CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats.
  • HY-124697
    BMP signaling agonist sb4

    TGF-β Receptor Cancer
    BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.
  • HY-16561
    Resveratrol

    trans-Resveratrol; SRT501

    IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Cancer Infection Inflammation/Immunology
    Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor.
  • HY-N1469
    Kaurenoic acid

    Others Inflammation/Immunology Neurological Disease
    Kaurenoic acid is a diterpene from Sphagneticola trilobata, inhibits Inflammatory Pain by the inhibition of cytokine production and activation of the NO–cyclic GMP–PKG–ATP-sensitive potassium channel signaling pathway.
  • HY-N0014
    Icariin

    Ieariline

    Phosphodiesterase (PDE) PPAR Autophagy Inflammation/Immunology Cardiovascular Disease Cancer
    Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
  • HY-N6781
    Ophiobolin A

    Phosphodiesterase (PDE) Cancer Infection
    Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity.
  • HY-N0177
    Diosgenin

    STAT Metabolic Disease
    Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57.
  • HY-W011303
    Phytosphingosine

    Apoptosis Cancer
    Phytosphingosine is a phospholipid and has anti-cancer activities. Phytosphingosine induces cell apoptosis via caspase 8 activation and Bax translocation in cancer cells.
  • HY-15398
    Cholecalciferol

    Vitamin D3; Colecalciferol

    VD/VDR Endogenous Metabolite Cancer
    Cholecalciferol(Vitamin D3) is a naturally occuring form of vitamin D; Reported that upon metabolic activation, Cholecalciferol induces cell differentiation and prevents proliferation of cancer cells.
  • HY-13772
    Valrubicin

    AD-32

    PKC Cancer Inflammation/Immunology
    Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
  • HY-N0754
    Eupalinolide A

    HSP Inflammation/Immunology
    Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
  • HY-N0168A
    (Rac)-Hesperetin

    p38 MAPK Apoptosis Autophagy Cancer Neurological Disease
    (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
  • HY-104049
    Lanifibranor

    IVA337

    PPAR Metabolic Disease Cancer
    Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.
  • HY-N6018
    Beta-Eudesmol

    TRP Channel Metabolic Disease
    Beta-Eudesmol is a natural oxygenated sesquiterpene, activates hTRPA1, with an EC50 of 32.5 μM. Beta-Eudesmol increases appetite through TRPA1.
  • HY-131096
    L-Proline 4-methoxy-β-naphthylamide hydrochloride

    H-Pro-4MβNA hydrochloride

    Others Cancer
    L-Proline 4-methoxy-β-naphthylamide hydrochloride (H-Pro-4MβNA hydrochloride) can be used for Fap-activated anti-tumor compounds preparaction.
  • HY-N0518
    Toddalolactone

    PAI-1 Cardiovascular Disease
    Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
  • HY-A0084
    Procainamide hydrochloride

    Autophagy Cancer
    Procainamide hydrochloride is an anti-arrhythmic agent and is used to treat cardiac arrhythmia; induces rapid block of the batrachotoxin(BTX)-activated sodium channels of the heart muscle and acts as antagonist to long gating closures.
  • HY-15004
    AUZ 454

    K03861

    CDK Cancer
    AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
  • HY-11063
    Fingolimod

    FTY720 free base

    LPL Receptor PAK Cancer Inflammation/Immunology
    Fingolimod is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.
  • HY-110192
    ML 297

    VU 0456810; CID 56642816

    Potassium Channel Neurological Disease
    ML 297 (VU 0456810) is a potent and selective GIRK1/2 activator, with an EC50 of 0.16 μM. ML 297 is potential for the treatment of epilepsy.
  • HY-P1333A
    Dynorphin A TFA

    Opioid Receptor Neurological Disease
    Dynorphin A TFA, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A TFA also serve as an agonist for other opioid receptors,  such as mu (MOR) and delta (DOR).
  • HY-120261
    GB-88

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca 2+ release with an IC50 of 2 µM.
  • HY-15332
    Alfacalcidol-D6

    VD/VDR Metabolic Disease
    Alfacalcidol-D6, a deuterated Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3), is a non-selective VDR activator medication.
  • HY-12809
    Optovin

    TRP Channel Others
    Optovin is a reversible photoactive TRPA1 activator; stimulates human TRPA1 channels in vitro and enables repeated photoactivation of motor behaviors in wild-type zebrafish (EC50 = 2 μM).
  • HY-103640
    WR-1065 dihydrochloride

    MDM-2/p53 Cancer
    WR-1065 dihydrochloride can protect normal tissues from the toxic effects of certain cancer drugs and activate p53 through a JNK-dependent signaling pathway.
  • HY-P1314A
    2-Furoyl-LIGRLO-amide TFA

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    2-Furoyl-LIGRLO-amide TFA is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0..
  • HY-107780
    Cyclic-di-GMP

    c-di-GMP; cyclic diguanylate; 5GP-5GP

    STING Endogenous Metabolite Cancer
    Cyclic-di-GMP (c-di-GMP) is a STING activator and a ubiquitous second messenger that regulates biofilm formation, motility, and virulence in diverse bacterial species.
  • HY-135013
    Umbellulone

    TRP Channel Neurological Disease
    Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.
  • HY-112816
    MA242

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    MA242 is a dual inhibitor of murine double minute 2 (MDM2) and nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy.
  • HY-100316
    CP-96486

    Leukotriene Receptor Inflammation/Immunology
    CP-96486 is a potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with Kis of 20 and 24 nM, respectively.
  • HY-12885B
    ADU-S100 ammonium salt

    MIW815 ammonium salt; ML RR-S2 CDA ammonium salt

    STING Inflammation/Immunology
    ADU-S100 ammonium salt (MIW815 ammonium salt), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.
  • HY-N0050
    Allomatrine

    (+)-Allomatrine

    Others Neurological Disease
    Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors.
  • HY-18286
    NCGC00229600

    TSH Receptor Endocrinology
    NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
  • HY-103097
    ST271

    Phospholipase Others
    ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
  • HY-P1562A
    PUMA BH3 TFA

    Bcl-2 Family Cancer
    PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
  • HY-19752A
    VU0357017 hydrochloride

    CID-25010775

    mAChR Neurological Disease
    VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).
  • HY-136351
    THZ-P1-2

    Autophagy Cancer
    THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
  • HY-100671
    L002

    Histone Acetyltransferase STAT Cancer Inflammation/Immunology
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.
  • HY-121629
    PS210

    PDK-1 Cancer
    PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.
  • HY-102011A
    BMS-1166 hydrochloride

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-N1970
    5,7-Dihydroxychromone

    Keap1-Nrf2 Arenavirus Caspase PARP Neurological Disease
    5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells.
  • HY-133558
    VII-31

    E1/E2/E3 Enzyme Apoptosis Cancer
    VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways.
  • HY-101860
    GIBH-130

    Interleukin Related Neurological Disease
    GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM).
  • HY-16677A
    Mofegiline hydrochloride

    MDL72974A

    Monoamine Oxidase Neurological Disease
    Mofegiline hydrochloride (MDL72974A) is a potent and selective enzyme-activated irreversible inhibitor of MAO-B; shows marked selectivity for the B form (IC50 = 680 and 3.6 nM for MAO-A and MAO-B).
  • HY-N0474
    Tyrosol

    NF-κB Endogenous Metabolite Inflammation/Immunology
    Tyrosol is a derivative of phenethyl alcohol. Tyrosol attenuates pro-inflammatory cytokines from cultured astrocytes and NF-κB activation. Anti-oxidative and anti-inflammatory effects.
  • HY-103087
    FIN56

    Ferroptosis Others
    FIN56 is a specific inducer of ferroptosis. FIN56 induces ferroptosis by inducing degradation of GPX4. FIN56 also binds to and activates squalene synthase.
  • HY-13595
    Chrysophanol

    Chrysophanic acid

    EGFR Cancer
    Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
  • HY-12212
    Omaveloxolone

    RTA 408

    Keap1-Nrf2 STING Apoptosis Cancer Inflammation/Immunology
    Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.
  • HY-15675
    AZD1656

    Glucokinase Metabolic Disease
    AZD1656 is a potent, selective and orally active glucokinase activator with an EC50 of 60 nM. AZD1656 has the potential for type 2 diabetes research.
  • HY-B0021
    Doxifluridine

    Ro 21-9738; 5-Fluoro-5'-deoxyuridine; 5'-DFUR

    Nucleoside Antimetabolite/Analog Cancer
    Doxifluridine(Ro 21-9738; 5'-DFUR) is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
  • HY-19937
    Saroglitazar

    PPAR Metabolic Disease
    Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
  • HY-13008
    MK-0354

    GPR109A Cardiovascular Disease
    MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.
  • HY-18936
    Alda-1

    Aldehyde Dehydrogenase (ALDH) Apoptosis Cancer
    Alda-1 is a potent ALDH2 agonist, which activates wild-type ALDH2 and restores near wild-type activity to ALDH2*2.
  • HY-136065
    bpV(phen)

    PTEN Phosphatase HIV Parasite Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology
    bpV(phen) is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B. bpV(phen) is an insulin-mimetic agent following insulin-receptor tyrosine kinase hyperphosphorylation and activation. bpV(phen) activates HIV-1 transcription and replication via NF-κB-dependent and independent mechanisms. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
  • HY-N1912
    Andropanolide

    NF-κB Inflammation/Immunology
    Andrographolide (Andro) is a small antagonist for NF-κB activation by covalent modifying reduced cysteine 62 of p50. Andrographolide is a bicyclic diterpenoid lactone mainly produced from the plant Andrographis (Andrographis paniculate). Andrographolide suppresses the activation of NF-κB in stimulated endothelial cells, which reduces the expression of cell adhesion molecule E-selectin and prevents E-selectin-mediated leukocyte adhesion, but has no effect on IκBα degradation, p50 and p65 nuclear translocation.
  • HY-136190
    TRPC6-PAM-C20

    TRP Channel
    TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca 2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).
  • HY-126675A
    AS2863619

    CDK STAT Inflammation/Immunology
    AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.
  • HY-105118A
    Zaldaride maleate

    CGS-9343B; KW 5617

    nAChR Metabolic Disease Inflammation/Immunology Neurological Disease
    Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR.
  • HY-128358
    MR-L2

    Phosphodiesterase (PDE) Neurological Disease
    MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM.
  • HY-127019
    Nigericin

    Sodium Channel NOD-like Receptor (NLR) Bacterial Apoptosis Antibiotic Cancer Infection
    Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K +/H + ionophore, promoting K +/H + exchange across mitochondrial membranes.Nigericin can be a NLRP3 activator that induces the release of IL-1β as a NALP3-dependent manner. Nigericin triggers eryptosis, an effect paralleled by ROS formation, and in part due to induction of oxidative stress. Nigericin triggers apoptosis.
  • HY-13324
    Bardoxolone methyl

    RTA 402; NSC 713200; CDDO Methyl ester

    Keap1-Nrf2 Autophagy Apoptosis Ferroptosis Cancer
    Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.
  • HY-N6651
    Isocryptotanshinone

    STAT Phosphatase Cancer
    Isocryptotanshinone is a potent signal transducer and activator of transcription 3 (STAT3) and protein tyrosine phosphatase 1B PTP1B inhibitor, with an IC50 of 56.1 μM for PTP1B.
  • HY-P2228
    Chlamydocin

    HDAC Apoptosis Cancer
    Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3.
  • HY-126382
    Hesperidin methylchalcone

    NF-κB Inflammation/Immunology
    Hesperidin methylchalcone (Hesperidin methyl chalcone) inhibits oxidative stress, cytokine production and NF-κB activation. Hesperidin methylchalcone inhibits inflammation and pain. Hesperidin methylchalcone exhibits vasoprotective activity.
  • HY-16031
    AFP464 free base

    NSC710464 free base

    HIF/HIF Prolyl-Hydroxylase Cancer
    AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
  • HY-19937A
    Saroglitazar Magnesium

    PPAR Metabolic Disease
    Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
  • HY-17376
    Ezetimibe

    SCH 58235

    Keap1-Nrf2 Autophagy Cardiovascular Disease Cancer
    Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
  • HY-10003
    Alfacalcidol

    1-hydroxycholecalciferol; 1.alpha.-Hydroxyvitamin D3

    VD/VDR Metabolic Disease
    Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis.
  • HY-122816
    HLY78

    Wnt Cancer Neurological Disease
    HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction.
  • HY-18935A
    CBL0137 hydrochloride

    Curaxin-137 hydrochloride; CBL-C137 hydrochloride

    MDM-2/p53 NF-κB Cancer
    CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.
  • HY-112606
    ML-290

    Others Others
    ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC50 of 94 nM.
  • HY-W015026
    Isobutylparaben

    Isobutyl 4-hydroxybenzoate

    Bacterial Inflammation/Immunology
    Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics.
  • HY-113204
    N-Oleoyl glycine

    Endogenous Metabolite Cannabinoid Receptor Akt Metabolic Disease
    N-Oleoyl glycine is a lipoamino acid, which stimulates adipogenesis associated with activation of CB1 receptor and Akt signaling pathway in 3T3-L1 adipocyte.
  • HY-12641
    Pyrantel tartrate

    Parasite Antibiotic Infection
    Pyrantel tartrate is an antinematodal thiophene; nicotinic receptor agonist and can elicit spastic muscle paralysis in parasitic worms due to prolonged activation of the excitatory nicotinic acetylcholine (nACh) receptors on body wall muscle.
  • HY-18657
    TEPP-46

    ML-265

    Pyruvate Kinase Cancer
    TEPP-46 is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR.
  • HY-15124
    (S)-(-)-Bay-K-8644

    Calcium Channel Cardiovascular Disease
    (S)-(-)-Bay-K-8644 is an agonist of L-type Ca 2+ channel. (S)-(-)-Bay-K-8644 activates Ba 2+ currents (IBa) (EC50=32 nM).
  • HY-103667
    2-HBA

    Caspase Cancer
    2-HBA is a potent inducer of NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1) which can also activate caspase-3 and caspase-10.
  • HY-N6673
    Okanin

    Toll-like Receptor (TLR) NF-κB Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways.
  • HY-10167A
    Tecalcet Hydrochloride

    R-568 (hydrochloride)

    CaSR Others
    Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+.
  • HY-114330A
    ZK824859 hydrochloride

    PAI-1 Inflammation/Immunology
    ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.
  • HY-12741
    LDN-212320

    LDN/OSU-0212320; LDN-0212320; OSU-0212320

    EAAT2 Neurological Disease
    LDN-212320(OSU-0212320) is a glutamate transporter EAAT2 activator; enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.
  • HY-P1955
    Etelcalcetide

    AMG 416; KAI-4169

    CaSR Endocrinology
    Etelcalcetide (AMG 416) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis.
  • HY-13255A
    TAME hydrochloride

    APC Cancer
    TAME hydrochloride is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest.
  • HY-105170B
    ABT-418 hydrochloride

    nAChR Neurological Disease
    ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease.
  • HY-N1713
    29-Nor-20-oxolupeol

    Others Neurological Disease
    29-Nor-20-oxolupeol, extracted from Impatiens basamina, reduces NO levels in LPS-activated murine microglial cells with an IC50 of 44.21 µM.
  • HY-N0773
    Isovitexin

    Saponaretin; Homovitexin

    JNK NF-κB Inflammation/Immunology
    Isovitexin is a flavonoid isolated from rice hulls of Oryza sativa, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
  • HY-N0847
    Micheliolide

    Others Others
    Micheliolide could effectively attenuate the high glucose-stimulated activation of NF-κB, the degradation of IκBα, and the expression of MCP-1, TGF-β1 and FN in rat mesangial cells (MCs).
  • HY-P0318
    Hemorphin-7

    Opioid Receptor Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).
  • HY-N2247A
    (+)-Guaiacin

    Others Metabolic Disease
    (+)-Guaiacin is a compound extracted of the bark of Machilus wangchiana Chun. (Lauraceae). (+)-Guaiacin shows potent in vitro activities against the release of β-glucuronidase in rat polymorphonuclear leukocytes (PMNs) induced by platelet-activating factor (PAF) .
  • HY-123963
    C-178

    STING Inflammation/Immunology
    C-178 is a potent and selective covalent inhibitor of STING. C-178 binds to Cys91 and suppresses the STING responses elicited by distinct bona fide activators in mouse but not human.
  • HY-114330
    ZK824859

    PAI-1 Inflammation/Immunology
    ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.
  • HY-136447
    ASP4132

    AMPK Cancer
    ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
  • HY-33350
    Clofilium tosylate

    Potassium Channel Apoptosis Cancer Cardiovascular Disease
    Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent.
  • HY-N7439
    Mogroside VI B

    PGC-1α Metabolic Disease
    Mogroside VI B, a cucurbitane glucoside, separated from the crude extract of Siraitia grosvenorii. Mogroside VI B shows effect on activating PGC-1α transcription.
  • HY-18937
    WEHI-345

    RIP kinase Cancer
    WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.
  • HY-13255
    TAME

    APC Cancer
    TAME is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest.
  • HY-128400
    4'-Methoxychalcone

    PARP Metabolic Disease Cancer
    4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity.
  • HY-12825
    BHPI

    Estrogen Receptor/ERR Cancer
    BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
  • HY-108908
    (Rac)-Modipafant

    UK-74505

    Others Infection Inflammation/Immunology
    (Rac)-Modipafant (UK-74505) is an orally active, selective, long-acting irreversible platelet activating factor receptor (PAFR) antagonist. (Rac)-Modipafant prevents dengue infection.
  • HY-14608
    (S)-Glutamic acid

    (+)-L-Glutamic acid

    Endogenous Metabolite iGluR Ferroptosis Apoptosis Neurological Disease
    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  • HY-101455
    CDN1163

    Calcium Channel Metabolic Disease
    CDN1163 is an allosteric sarco/endoplasmic reticulum Ca 2+-ATPase (SERCA) activator that improves Ca 2+ homeostasis. CDN1163 attenuates diabetes and metabolic disorders.
  • HY-B0260
    Methylprednisolone

    U 7532

    Glucocorticoid Receptor Autophagy SARS-CoV Cancer Infection Endocrinology Inflammation/Immunology
    Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.
  • HY-P1955A
    Etelcalcetide hydrochloride

    AMG 416 hydrochloride; KAI-4169 hydrochloride

    CaSR Endocrinology
    Etelcalcetide hydrochloride (AMG 416 hydrochloride) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide hydrochloride is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis.
  • HY-U00036A
    Naveglitazar

    LY519818

    PPAR Metabolic Disease
    Naveglitazar (LY519818) is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models.
  • HY-P1594
    Dynorphin A 1-10

    Opioid Receptor iGluR Neurological Disease
    Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
  • HY-107780A
    Cyclic-di-GMP sodium

    c-di-GMP sodium; cyclic diguanylate sodium; 5GP-5GP sodium

    STING Endogenous Metabolite Cancer
    Cyclic di-GMP sodium (c-di-GMP sodium) is a STING activator and a global bacterial second messenger, which regulates biofilm formation, motility, and virulence in diverse bacterial species.
  • HY-101572
    MHP

    Methyl caprooyl tyrosinate

    SPHK Inflammation/Immunology
    MHP (Methyl caprooyl tyrosinate) is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production. MHP (Methyl caprooyl tyrosinate) enhances antimicrobial defense and innate immunity.
  • HY-B0711
    Carglumic Acid

    N-Carbamyl-L-glutamic acid

    Others Cancer
    Carglumic acid (N-Carbamyl-L-glutamic acid), a functional analogue of N-acetylglutamate (NAG) and a carbamoyl phosphate synthetase 1 (CPS1) activator, is used to treat acute and chronic hyperammonemia associated with NAG synthase (NAGS) deficiency.
  • HY-13812
    QNZ

    EVP4593

    NF-κB TNF Receptor Inflammation/Immunology Neurological Disease
    QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel.
  • HY-P0172A
    ATI-2341 TFA

    CXCR Cancer Inflammation/Immunology Endocrinology
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
  • HY-15598
    20-HETE

    20-hydroxy Arachidonic Acid

    Potassium Channel NF-κB NO Synthase Reactive Oxygen Species NADPH Oxidase Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    20-HETE (20-hydroxy Arachidonic Acid) is a CYP450 metabolite and a potent vasoconstrictor. 20-HETE is an endogenous inhibitor of the large-conductance Ca 2+-activated K + channel in renal arterioles. 20-HETE constricts smooth muscles, stimulates smooth muscle proliferation and migration. 20-HETE increases NADPH oxidase, ROS, and NF-κB activity. 20-HETE also inhibits endothelial NO synthase and inhibits apoptosis of pulmonary artery smooth muscle cells.
  • HY-P0172
    ATI-2341

    CXCR Inflammation/Immunology Endocrinology Cancer
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
  • HY-101287
    MPT0B392

    Microtubule/Tubulin JNK Apoptosis Caspase Cancer
    MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
  • HY-117163
    FzM1.8

    Wnt β-catenin Cancer
    FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
  • HY-16591
    Birinapant

    TL32711

    IAP Apoptosis HIV Cancer
    Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
  • HY-N1490
    14-Deoxy-11,12-didehydroandrographolide

    14-dehydro Andrographolide; AP10

    NF-κB Inflammation/Immunology Cancer
    14-Deoxy-11,12-didehydroandrographolide is an analogue of Andrographolide that can be isolated from A. paniculata. 14-Deoxy-11,12-didehydroandrographolide inhibits NF-κB activation.
  • HY-112108
    Chitosan oligosaccharide

    COS

    AMPK Cancer Metabolic Disease
    Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.
  • HY-B1218
    Sulfaphenazole

    Bacterial Infection
    Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
  • HY-U00201
    KRN4884

    Potassium Channel Cardiovascular Disease
    KRN4884 is a K + channel opener. In the presence of intracellular ATP (1 mM), KRN4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM).
  • HY-13735A
    Quinacrine dihydrochloride

    Mepacrine dihydrochloride; SN-390 dihydrochloride

    Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine dihydrochloride (Mepacrine dihydrochloride) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
  • HY-12885C
    ADU-S100 enantiomer ammonium salt

    MIW815 enantiomer ammonium salt; ML RR-S2 CDA enantiomer ammonium salt

    Others Inflammation/Immunology
    ADU-S100 enantiomer ammonium salt (MIW815 enantiomer ammonium salt) is the less active enantiomer of ADU-S100. ADU-S100 is an activator of stimulator of interferon genes (STING).
  • HY-15272
    WAY-600

    mTOR Cancer Inflammation/Immunology
    WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC50 of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.
  • HY-N0139
    Troxerutin

    Trihydroxyethylrutin

    NOD-like Receptor (NLR) Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species (ROS) and depress ER stress-mediated NOD activation.
  • HY-126361
    ZK824190

    Ser/Thr Protease PAI-1 Inflammation/Immunology
    ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
  • HY-120675
    SSTC3

    Casein Kinase Wnt Cancer
    SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
  • HY-13735B
    Quinacrine hydrochloride hydrate

    Mepacrine hydrochloride hydrate; SN-390 hydrochloride hydrate

    Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
  • HY-N2310
    Domoic acid

    (-)-Domoic acid; L-Domoic acid

    iGluR Neurological Disease
    Domoic acid ((-)-Domoic acid; L-Domoic acid) is an excitatory neurotransmitter isolated from a form of marine vegetation, Nitzschia pungens. Domoic acid produces neurotoxic effect through activating kainate receptor.
  • HY-124293
    AA147

    Others Metabolic Disease
    AA147, a small molecule endoplasmic reticulum (ER) proteostasis regulator, selectively activates ATF6 arm of the unfolded protein response (UPR) extracted from patent WO2017117430A1, compound 147*.
  • HY-N0341
    Scopolin

    Sirtuin Metabolic Disease
    Scopolin is a coumarin isolated from Arabidopsis thaliana (Arabidopsis) roots. Scopolin attenuated hepatic steatosis through activation of SIRT1-mediated signaling cascades.
  • HY-N7117
    1,4-Cineole

    TRP Channel Endogenous Metabolite Cancer Inflammation/Immunology
    1,4-Cineole is a widely distributed, natural, oxygenated monoterpene. 1,4-Cineole, present in eucalyptus oil, activates both human TRPM8 and human TRPA1.
  • HY-N4171
    Dihydrocucurbitacin B

    Others Inflammation/Immunology
    Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity.
  • HY-124108
    Eicosatetraynoic acid

    ETYA

    COX PPAR Others
    Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM.
  • HY-112823B
    HS-10296 hydrochloride

    EGFR Cancer
    HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
  • HY-N3026
    Soyasaponin Ab

    Others Metabolic Disease
    Soyasaponin Ab is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).
  • HY-101731
    CP-96021 hydrochloride

    Leukotriene Receptor Inflammation/Immunology
    CP-96021 hydrochloride is a balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with Ki values of 34 nM and 37 nM, respectively.
  • HY-N3027
    Soyasaponin Aa

    Others Metabolic Disease
    Soyasaponin Aa is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).
  • HY-108036
    Pro-xylane

    Hydroxypropyl tetrahydropyrantriol

    Others Metabolic Disease
    Pro-xylane (Hydroxypropyl tetrahydropyrantriol) is a biologically active C-glycoside in aqueous media, acts as an activator of glycosaminoglycans (GAGs) biosynthesis. Pro-xylane is the first example of 'Green' chemical used in cosmetic.
  • HY-18711A
    SCR-1481B1

    c-Met inhibitor 2

    c-Met/HGFR VEGFR Cancer
    SCR-1481B1 (c-Met inhibitor 2) is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.
  • HY-78869
    Mutated EGFR-IN-1

    Osimertinib analog

    EGFR Cancer
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
  • HY-N0141
    Parthenolide

    (-)-Parthenolide

    NF-κB Autophagy Mitophagy Apoptosis 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-112125
    KRN2

    Others Inflammation/Immunology
    KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis.
  • HY-W001174
    2,5-Dihydroxyacetophenone

    ERK NF-κB Inflammation/Immunology
    2,5-Dihydroxyacetophenone, isolated from Rehmanniae Radix Preparata, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways.
  • HY-14608A
    L-Glutamic acid monosodium salt

    Monosodium glutamate

    iGluR Apoptosis Ferroptosis Neurological Disease
    L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  • HY-N0815
    Resibufogenin

    Bufogenin; Recibufogenin

    Others Cancer
    Resibufogenin, a component of huachansu, has been shown to exhibit the anti-proliferative effect against cancer cells, and this may be attributed to the degradation of cyclin D1 caused by the activation of GSK-3β.
  • HY-N6681
    15-Acetoxyscirpenol

    Caspase Bacterial Apoptosis Antibiotic Infection
    15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3.
  • HY-12290
    Arg-Gly-Asp-Ser

    RGDS peptide; Fibronectin tetrapeptide

    Integrin Inflammation/Immunology
    Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function, decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS and MMP-9.
  • HY-N4202
    Dihydrorotenone

    Mitochondrial Metabolism Apoptosis Neurological Disease
    Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway.
  • HY-N4225
    Aaptamine

    Adrenergic Receptor Cancer Endocrinology
    Aaptamine, a spongean alkaloid isolated from a sea sponge Aaptos aaptos, is a competitive antagonist of α-adrenoceptor and activates the p21 promoter in a p53-independent manner.
  • HY-N0109
    Salidroside

    Rhodioloside

    mTOR Apoptosis Cancer
    Salidroside is a prolyl endopeptidase Inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
  • HY-114384
    NV-5138

    mTOR Neurological Disease
    NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 possesses rapid antidepressant effects.
  • HY-108908A
    Modipafant

    UK-80067

    Others Inflammation/Immunology
    Modipafant (UK-80067), the (+)-enantiomer of UK-74505, is a potent, orally active, and selective platelet-activating factor (PAF) antagonist. Modipafant exhibits approximately double the intrinsic potency of UK-74505.
  • HY-100227
    E 64c

    Cathepsin SARS-CoV Metabolic Disease
    E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
  • HY-N6261
    Epimagnolin B

    Others Inflammation/Immunology
    Epimagnolin B is a bisepoxylignan isolated from Magnolia fargesii, with anti-inflammatory activity and antiallergic effects. Epimagnolin B inhibits NO production in LPS-activated microglia. Epimagnolin B exhibited antiallergic effects.
  • HY-13293
    Impurity C of Calcitriol

    VD/VDR Cancer
    Impurity C of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
  • HY-13292
    Impurity B of Calcitriol

    1β,25-Dihydroxyvitamin-D3; 1-Epicalcitriol

    VD/VDR Cancer
    Impurity B of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
  • HY-B0190A
    Nafamostat mesylate

    FUT-175

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease Cancer
    Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat mesylate supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat mesylate blocks activation of SARS-CoV-2..
  • HY-N2119
    Sciadopitysin

    NF-κB Inflammation/Immunology
    Sciadopitysin is a type of biflavonoids in leaves from ginkgo biloba. Sciadopitysi inhibits RANKL-induced osteoclastogenesis and bone loss by inhibiting NF-κB activation and reducing the expression of c-Fos and NFATc1.
  • HY-B0190
    Nafamostat

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease
    Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2.
  • HY-B0190B
    Nafamostat hydrochloride

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease
    Nafamostat hydrochloride, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat hydrochloride supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat hydrochloride blocks activation of SARS-CoV-2..
  • HY-N0250
    Saikosaponin D

    STAT NF-κB Estrogen Receptor/ERR Bacterial Cancer Infection Inflammation/Immunology
    Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
  • HY-16785B
    Veledimex (S enantiomer)

    INXN-1001 (S enantiomer); RG-115932 (S enantiomer)

    Interleukin Related Cytochrome P450 Cancer
    Veledimex S enantiomer (INXN-1001 S enantiomer) is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
  • HY-103269
    BAI1

    Bcl-2 Family Cancer
    BAI1 is a selective and allosteric inhibitor of BAX activation. BAI1 demonstrates inhibition of tBID (HY-100464)-induced BAX-mediated membrane permeabilization with an IC50 of 3.3 μΜ.
  • HY-N0048
    Polyphyllin II

    Apoptosis Cancer
    Polyphyllin II is one of the most significant saponins in Rhizoma Paridis and has toxic effects on kinds of cancer cells. Polyphyllin II induces apoptosis through caspases activation and cell-cycle arrest.
  • HY-N0020
    Echinacoside

    Wnt Reactive Oxygen Species Neurological Disease
    Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche salsa, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.
  • HY-U00036
    Naveglitazar racemate

    LY519818 racemate

    PPAR Metabolic Disease
    Naveglitazar racemate (LY519818 racemate) is the racemate of Naveglitazar. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models.
  • HY-P1594A
    Dynorphin A (1-10) (TFA)

    Opioid Receptor iGluR Neurological Disease
    Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
  • HY-N0826
    Corynoline

    AChE Keap1-Nrf2 Inflammation/Immunology Neurological Disease Cancer
    Corynoline, isolated from Corydalis incise (Papaveraceae), is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM. Corynoline exhibits anti-inflammatory activity by activating Nrf2.
  • HY-111617
    BTR-1

    Apoptosis Cancer
    BTR-1 is an active anti-cancer agent, causes S phase arrest, and affects DNA replication in leukemic cells. BTR-1 activates apoptosis and induces cell death.
  • HY-N1485
    Astramembrangenin

    Cyclosieversigenin

    Apoptosis Inflammation/Immunology Neurological Disease
    Astramembrangenin (Cycloastragenol) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus (Fisch.) Bunge. Astramembrangenin is orally safe and has broad Extensive pharmacological effects, including telomerase activation, telomere elongation, anti-inflammatory and anti-oxidative properties. Astramembrangenin has antiaging properties, CAG stimulates telomerase activity in human neonatal keratinocytes and rat neuronal cells, and induces CREB activation followed by tert and bcl2 expression. Cycloastragenol (CAG) may have a novel therapeutic role in depression.
  • HY-15340
    LG100268

    LG268

    RAR/RXR Autophagy Metabolic Disease
    LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy.
  • HY-N6257
    Cafestol

    ERK PGE synthase COX NF-κB Cancer Inflammation/Immunology
    Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects.
  • HY-110353
    CU-T12-9

    Toll-like Receptor (TLR) Cancer Infection Inflammation/Immunology
    CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
  • HY-126675
    AS2863619 free base

    CDK STAT Inflammation/Immunology
    AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
  • HY-W010737
    Guanosine-5'-triphosphate disodium salt

    5'-GTP disodium salt

    Endogenous Metabolite Metabolic Disease
    Guanosine-5'-triphosphate disodium salt (5'-GTP trisodium salt) is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
  • HY-15874A
    Fiboflapon sodium

    GSK2190915 sodium salt; AM-803 sodium

    FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
  • HY-136319
    OSu-PEG4-VC-PAB-Duocarmycin SA

    Drug-Linker Conjugates for ADC DNA Alkylator/Crosslinker Cancer
    SA is a drug-linker conjugate for ADC with potent antitumor activity by using Duocarmycin SA (a potent DNA alkylation activator), linked via the cleavable ADC linker OSu-PEG4-VC-PAB.
  • HY-113134
    25-Hydroxycholesterol

    Endogenous Metabolite Inflammation/Immunology
    25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells.
  • HY-136651
    BNTA

    Others Inflammation/Immunology
    BNTA is a small molecule with extracellular matrix (ECM) modulatory properties, and it facilitates cartilage structural molecule synthesis on chondrocytes by activating superoxide dismutase 3 (SOD3). BNTA is a potential therapeutic agent in osteoarthritis.
  • HY-101843
    ML213

    Potassium Channel Neurological Disease
    ML213 is a selective activator of Kv7.2 and Kv7.4 channels, enhances Kv7.2 and Kv7.4 channels with EC50s of 230 and 510 nM, respectively.
  • HY-128344
    BR102375

    PARP Apoptosis Metabolic Disease
    BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28 μM and Amax ratio of 98%.
  • HY-124867
    D3-βArr

    TSH Receptor Endocrinology
    D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
  • HY-129527
    GNE-9278

    iGluR Neurological Disease
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.
  • HY-112823
    HS-10296

    EGFR Cancer
    HS-10296, an orally available and third-generation EGFR-activating mutations and T790M-resistant mutation inhibitor, shows limited activity against wild-type EGFR.
  • HY-N5083
    Saponarin

    Others Inflammation/Immunology
    Saponarin is a natural flavonoid isolated from Gypsophila trichotoma, with antioxidant, anti-inflammatory and hepatoprotective activities. Saponarin activates AMPK in a calcium-dependent manner, thus regulating gluconeogenesis and glucose uptake.
  • HY-115658
    VU0420373

    Bacterial Infection Metabolic Disease
    VU0420373 is a potent heme sensor system (HssRS) activator with an EC50 of 10.7 μM and a pEC50 of 4.97. VU0420373 induces heme biosynthesis, and is toxic to fermenting S. aureus.
  • HY-108036A
    (S)-Pro-xylane

    (S)-Hydroxypropyl tetrahydropyrantriol

    Others Others
    (S)-Pro-xylane ((S)-Hydroxypropyl tetrahydropyrantriol) is the S-enantiomer of Pro-xylane (HY-108036). Pro-xylane is a biologically active C-glycoside in aqueous media, acts as an activator of glycosaminoglycans (GAGs) biosynthesis.
  • HY-17376S
    Ezetimibe D4

    SCH 58235 D4

    Others Cardiovascular Disease Cancer
    Ezetimibe D4 (SCH 58235 D4) is the deuterium labeled Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
  • HY-N6826
    Asatone

    NF-κB Inflammation/Immunology
    Asatone is an active component isolated from Radix et Rhizoma Asari, with anti-inflammatory effect via activation of NF-κB and donwn regulation of p-MAPK (ERK, JNK and p38) pathways.
  • HY-B0285
    Amiloride

    MK-870

    Sodium Channel TRP Channel Apoptosis Metabolic Disease Cardiovascular Disease
    Amiloride (MK-870) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride is a blocker of polycystin-2 (PC2; TRPP2) channel.
  • HY-15874
    Fiboflapon

    GSK2190915; AM-803

    FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
  • HY-B0285A
    Amiloride hydrochloride

    MK-870 hydrochloride

    Sodium Channel TRP Channel Apoptosis Metabolic Disease Cardiovascular Disease
    Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride is a blocker of polycystin-2 (PC2; TRPP2) channel.
  • HY-136093
    HL271

    AMPK Neurological Disease
    HL271, a chemical derivative of metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment in animal model.
  • HY-103490
    Takinib

    MAP3K Apoptosis Cancer
    Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.
  • HY-12764
    6-OAU

    GTPL5846

    GPR84 Inflammation/Immunology
    6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.
  • HY-N2585
    Isodeoxyelephantopin

    Reactive Oxygen Species NF-κB Autophagy Cancer
    Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer.
  • HY-13520
    Nocodazole

    Oncodazole; R17934

    Microtubule/Tubulin Bcr-Abl CRISPR/Cas9 Autophagy Apoptosis Cancer
    Nocodazole is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
  • HY-100164
    SDZ-MKS 492

    MKS 492

    Phosphodiesterase (PDE) Inflammation/Immunology
    SDZ-MKS 492 (MKS 492) is a selective type III isozyme inhibitor of cyclic nucleotide phosphodiesterase, effective in allergic bronchoconstriction and platelet activating factor (PAF) or LTB4-induced inflammatory reactions in animals.
  • HY-N0605
    Ginsenoside Rh2

    20(S)-Ginsenoside Rh2; 20(S)-Rh2; Ginsenoside-Rh2

    Caspase Apoptosis Endogenous Metabolite Cancer
    Ginsenoside Rh2 is isolated from the root of Ginseng. Ginsenoside Rh2 induces the activation of caspase-8 and caspase-9. Ginsenoside Rh2 induces cancer cell apoptosis in a multi-path manner.
  • HY-N0802
    Tenuigenin

    Senegenin

    NF-κB Infection Inflammation/Immunology
    Tenuigenin is a major active component isolated from the root of the Chinese herb Polygala tenuifolia. Tenuigenin protects against S.aureus-induced pneumonia by inhibiting NF-κB activation. Tenuigenin has anti-inflammatory effect.
  • HY-P2319
    OVA-E1 peptide

    p38 MAPK JNK Inflammation/Immunology
    OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes.
  • HY-17363S
    Dimethyl fumarate D6

    DMF D6

    Keap1-Nrf2 Inflammation/Immunology
    Dimethyl fumarate D6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
  • HY-122445
    Resorcinolnaphthalein

    Angiotensin-converting Enzyme (ACE) Inflammation/Immunology Cardiovascular Disease
    Resorcinolnaphthalein is a specific angiotensin-converting enzyme 2 (ACE2) enhancer and activates ACE2 activity with an EC50 value of 19.5 μM. Resorcinolnaphthalein can be used for the investigation of hypertension and renal fibrosis.
  • HY-102004
    Rilapladib

    SB 659032

    Phosphatase Inflammation/Immunology Neurological Disease
    Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM. Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist.
  • HY-112800
    cyt-PTPε Inhibitor-1

    Phosphatase Metabolic Disease
    cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.
  • HY-108539
    CE3F4

    Others Metabolic Disease
    CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
  • HY-N0220
    Dauricine

    NF-κB Apoptosis Cancer Inflammation/Immunology
    Dauricine, a bisbenzylisoquinoline alkaloid in Asiatic Moonseed Rhizome, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer.
  • HY-135808
    BIZ 114

    NF-κB Inflammation/Immunology
    BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases.
  • HY-119931
    2-Hydroxychalcone

    Bcl-2 Family Apoptosis NF-κB Cancer Metabolic Disease
    2-hydroxychalcone, a natural flavonoid, is a potent antioxidant, inhibiting lipid peroxidation. 2-Hydroxychalcone induces apoptosis by Bcl-2 downregulation. 2-Hydroxychalcone inhibits the activation of NF-kB.
  • HY-122700
    Factor D inhibitor 6

    Complement System Inflammation/Immunology
    Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
  • HY-109011
    Rosiptor

    AQX-1125

    Phosphatase Cancer
    Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.
  • HY-107414
    SKA-121

    Potassium Channel Cardiovascular Disease
    SKA-121 is a selective KCa3.1 activator. SKA-121 exhibits EC50s of 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively.
  • HY-P2319A
    OVA-E1 peptide TFA

    p38 MAPK JNK Inflammation/Immunology
    OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes.
  • HY-108439
    Neurodazine

    Wnt Hedgehog Neurological Disease
    Neurodazine is an imidazole-based small molecule, serve as a promoter of neurogenesisin pluripotent cells. Neurodazine promotes neurogenesis by activating Wnt and Shh signaling pathways. Neurodazine selectively suppresses astrocyte differentiation of P19 cells.
  • HY-109079A
    Abeprazan hydrochloride

    DWP14012 hydrochloride

    Proton Pump Metabolic Disease
    Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.
  • HY-136093A
    IM156

    HL156A

    AMPK Neurological Disease
    IM156 (HL156A), a chemical derivative of metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model.
  • HY-126114
    Lupeol acetate

    Others Inflammation/Immunology
    Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.
  • HY-N0039
    Ginsenoside Rb1

    Gypenoside III

    Na+/K+ ATPase IRAK NF-κB Autophagy Mitophagy HSV Inflammation/Immunology Cancer
    Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na +, K +-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .
  • HY-106916
    Unoprostone

    Potassium Channel Neurological Disease
    Unoprostone, a prostaglandin F2α analogs (PGAs), activates BK channels to reduce oxidative stress- and light-induced retinal cell death, and phagocytotic dysfunction. Unoprostone reduces intraocular pressure and is used topically for glaucoma or ocular hypertension.
  • HY-76814
    Calcitriol D6

    VD/VDR Metabolic Disease
    Calcitriol D6 is the deuterated form of Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ), which is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
  • HY-75161
    (-)-Menthol

    TRP Channel Endogenous Metabolite 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-N0499
    Cyanidin Chloride

    IdB 1027

    Others Cancer
    Cyanidin Chloride (IdB 1027), a subclass of anthocyanin, displays antioxidant and anti-carcinogenesis properties. Cyanidin Chloride (IdB 1027) inhibits osteoclast formation, hydroxyapatite resorption, and receptor activator of NF-κB ligand (RANKL)-induced osteoclast marker gene expression.
  • HY-109041
    Razuprotafib

    Phosphatase Inflammation/Immunology
    Razuprotafib, a protein tyrosine phosphatase ß (HPTPß) inhibitor, extracted from patent WO2019165349A1, compound AA34, has an IC50 of 50 nM. Razuprotafib is effective for activation of Tie-2, and is protective against acute kidney injury.
  • HY-109079
    Abeprazan

    DWP14012

    Proton Pump Metabolic Disease
    Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.
  • HY-N4097
    Incensole

    Others Neurological Disease
    Incensole, a 14-membered diterpenoid, is isolated from both essential oils and resins of frankincense. Incensole has shown anti-inflammatory and anti-depression activities due to their ability to activate ion channels in the brain to alleviate anxiety or depression.
  • HY-N0589
    Dehydrodiisoeugenol

    NF-κB COX Bacterial Infection Inflammation/Immunology
    Dehydrodiisoeugenol is isolated from Myristica fragrans Houtt, shows anti-inflammatory and anti-bacterial actions. Dehydrodiisoeugenol inhibits LPS- stimulated NF-κB activation and cyclooxygenase (COX)-2 gene expression in murine macrophages.
  • HY-B0764A
    Bucladesine calcium

    Dibutyryl cAMP calcium salt; DBcAMP calcium salt

    PKA Phosphodiesterase (PDE) Apoptosis Others
    Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
  • HY-N0447
    8-Gingerol

    TRP Channel Infection Inflammation/Immunology Cancer
    8-Gingerol, found in the rhizomes of ginger (Z. officinale) with oral bioavailability, activates TRPV1, with an EC50 of 5.0 µM. 8-Gingerol inhibits COX-2, and inhibits the growth of H. pylori in vitro.
  • HY-N2006
    Ganoderic acid B

    HIV Protease Infection
    Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease.
  • HY-N6679A
    10,11-Dehydrocurvularin

    HSP TGF-beta/Smad Cancer Infection
    10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
  • HY-N0791
    Tectoridin

    Estrogen Receptor/ERR Cancer
    Tectoridin is a isoflavone isolated from Maackia amurensis. Tectoridin is a phytoestrogen and activates estrogen and thyroid hormone receptors. Tectoridin exerts the estrogenic effects via ER-dependent genomic pathway and GPR30-dependent nongenomic pathway.
  • HY-N6748
    Roquefortine C

    P-glycoprotein Cytochrome P450 Bacterial Cancer Infection
    Roquefortine C, a fungal cyclopeptide isolated from Penicillium roquefortii, activates P-gp and also inhibits P450-3A and other haemoproteins. Roquefortine C has bacteriostatic activities against Gram-positive bacteria.
  • HY-101942
    CM-4620

    CRAC Channel Neurological Disease
    CM-4620 is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.
  • HY-125021
    2BAct

    Eukaryotic Initiation Factor (eIF) Neurological Disease
    2BAct is a highly selective, CNS-permeable, and orally active eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response.
  • HY-N1504
    Loureirin B

    PAI-1 Potassium Channel ERK JNK Metabolic Disease
    Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
  • HY-19702
    PKR-IN-2

    Others Cancer
    PKR-IN-2 is a pyruvate kinase (PKR) activator, extracted from patent WO2014139144A1, compound 160, has an IC50 of <100 nM for. PKR (R510Q), PKR (R532W), PKR (WT), and PKR (WT Cell Based).
  • HY-100016
    AZD0156

    ATM/ATR Apoptosis Cancer
    AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.
  • HY-B0285B
    Amiloride hydrochloride dihydrate

    MK-870 hydrochloride dihydrate

    Sodium Channel Apoptosis TRP Channel Metabolic Disease Cardiovascular Disease
    Amiloride hydrochloride dihydrate (MK-870 hydrochloride dihydrate) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride dihydrate is a blocker of polycystin-2 (PC2; TRPP2) channel.
  • HY-14854
    Tecarfarin

    ATI-5923

    Others Cardiovascular Disease
    Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin has the antithrombotic activity .
  • HY-N2078
    Yamogenin

    Neodiosgenin

    LXR Metabolic Disease
    Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes.
  • HY-136278
    NOC 18

    NO Synthase
    NOC 18 is a nitric oxide donor and activates an inward current in cultured rat cerebellar granules cells. NOC 18 increases cGMP production in cultured vascular smooth muscle cells. NOC 18 reduces contractility of cardiac muscle preparations in vitro.
  • HY-105940
    IQB-782

    Others Cardiovascular Disease
    IQB-782 is a cysteine derivative. IQB-782 has inhibition for thrombin activatable fibrinolysis inhibitor (TAFI), with an Ki(app) of 0.14 μM. IQB-782 shows a potent mucolytic-expectorant activity.
  • HY-N7041
    11-Oxomogroside IIa

    HSV Infection
    11-Oxomogroside IIa (11-oxomogroside II A1) is a cucurbitane glycoside extracted from the fruits of Siraitia grosVenorii. 11-Oxomogroside IIa has inhibitory effects against the Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), shows weak inhibitory effects on activation of (+/-)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexemide (NOR 1), a nitric oxide (NO) donor.
  • HY-107738
    Guggulsterone

    Z/E-Guggulsterone

    Apoptosis JNK Akt Caspase FXR Autophagy Cancer
    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.
  • HY-17537
    APY29

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-115576
    P62-mediated mitophagy inducer

    PMI

    Mitophagy Neurological Disease
    P62-mediated mitophagy inducer is a mitophagy regulator which activates mitophagy without recruiting Parkin or collapsing ΔΨm and retains activity in cells devoid of a fully functional PINK1/Parkin pathway.
  • HY-136179
    ZAP-180013

    Tyrosinase Inflammation/Immunology
    ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs).
  • HY-112126
    KRN5

    Others Inflammation/Immunology
    KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis.
  • HY-122727
    STL127705

    DNA-PK Cancer
    STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM).
  • HY-15510B
    Tenovin-6 Hydrochloride

    Sirtuin MDM-2/p53 Autophagy Cancer
    Tenovin-6 Hydrochloride is an inhibitor of SIRT1 and SIRT2, slightly inhibits HDAC8, and is also a potent activator of p53, with IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively.
  • HY-N2344
    Procyanidin A1

    Proanthocyanidin A1

    PKC Inflammation/Immunology
    Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.
  • HY-N1419
    Vaccarin

    AMPK Metabolic Disease
    Vaccarin is an active flavonoid glycoside associated with various biological functions. Vaccarin significantly promote wound healing and endothelial cells and fibroblasts proliferation in the wound site. Vaccarin ameliorates insulin resistance and steatosis by activating the AMPK signaling pathway.
  • HY-50937
    ST 2825

    MyD88 Inflammation/Immunology
    ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity.
  • HY-113926
    BAY 60-2770

    Guanylate Cyclase Cardiovascular Disease
    BAY 60-2770 is a potent, selective, and orally active soluble guanylyl cyclase (sGC) activator. BAY 60-2770 increases the activity of sGC in a nitric oxide-independent manner. BAY 60-2770 shows antifibrotic effect.
  • 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-114739
    MA-0204

    PPAR Metabolic Disease
    MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
  • HY-119339
    SX-682

    CXCR Cancer Inflammation/Immunology Endocrinology
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
  • HY-U00280
    Potassium Channel Activator 1

    Others Neurological Disease
    Potassium Channel Activator 1 is an agent for treating, one or more disorders or conditions wherein the dopaminergic system is disrupted, such as one or more disorders or conditions independently selected from the group consisting of: schizophrenia and other psychotic states; mood disorders ADHD; aggression; movement disorders.
  • HY-N7015
    Zerumbone

    HSV Infection
    Zerumbone is a monocyclic sesquiterpene compound isolated from the rhizomes of Zingiber zerumbet Smith. Zerumbone potently inhibits the activation of Epstein-Barr virus with an IC50 of 0.14 mM. Zerumbone has anti-cancer, antioxidant, anti-inflammatory and anti-proliferative activity.
  • HY-N4053
    Heraclenin

    Others Inflammation/Immunology
    Heraclenin, a natural furanocoumarin, isolated from the root parts of the plant Prangos pabularia. Heraclenin significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
  • HY-118532
    Tyrphostin AG30

    AG30

    EGFR Cancer
    Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.
  • HY-P1179
    Guanylin(human)

    Guanylate Cyclase Endogenous Metabolite Cancer Endocrinology
    Guanylin(human), a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.
  • HY-N0431
    Astragaloside IV

    MMP ERK JNK Cancer
    Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
  • HY-110249
    CINPA1

    Others Metabolic Disease
    CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.
  • HY-15510
    Tenovin-6

    Sirtuin MDM-2/p53 Autophagy Cancer
    Tenovin-6 is an inhibitor of SIRT1 and SIRT2, slightly inhibits HDAC8, and is also a potent activator of p53, with IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively.
  • HY-128900
    11-cis-Vaccenyl acetate

    Endogenous Metabolite Others
    11-cis-Vaccenyl acetate is male-specific lipid that mediates aggregation behavior in both male and female flies, which activates a few dozen olfactory neurons located in T1 sensilla on the antenna of both male and female flies.
  • HY-N0674
    Dehydrocorydaline

    13-Methylpalmatine

    Bcl-2 Family Caspase PARP Cancer
    Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP.
  • HY-N3584
    Paris saponin VII

    Chonglou Saponin VII

    Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Cancer
    Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
  • HY-N0651
    Spinosin

    Others Neurological Disease
    Spinosyn a C-glycoside flavonoid isolated from the seeds of Zizyphus jujube, with neuroprotective effects. Spinosin inhibits Aβ1-42 production and aggregation via activating Nrf2/HO-1 pathway.
  • HY-19843
    MK-0941

    Glucokinase Metabolic Disease
    MK-0941 is a potent, orally active and allosteric glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 has potential in the treatment of type 2 diabetes.
  • HY-N2941
    Bisandrographolide C

    TRP Channel Metabolic Disease Inflammation/Immunology
    Bisandrographolide C is an unusual dimer of ent-labdane diterpenoid isolated and identified from Andrographis paniculata. Bisandrographolide C activates TRPV1 and TRPV3 channels with Kd values of 289 and 341 μM respectively, and protects cardiomyocytes from hypoxia-reoxygenation injury.
  • HY-108635
    C16-PAF

    PAF (C16)

    Endogenous Metabolite
    C16-PAF is an endogenous platelet-activating factor (PAF) and ligand for PAF receptors. C16-PAF is produced by inflammatory cells and a potent chemoattractant for polymorphonuclear neutrophils. C16-PAF induces increased vascular permeability.
  • HY-115545
    DBCO-NHS ester 3

    ADC Linker Cancer
    DBCO-NHS ester 3 (Compound 12) is a cleavable linker that is used for making antibody-drug conjugate (ADC). DBCO-NHS ester 3 is a derivative of Dibenzylcyclooctyne (DBCO) obtained by activation of N-hydroxysuccinimide by the carboxylic acid moiety of both methyl-oxanorbornadiene (MeOND) and dibenzoazacyclooctyne (DIBAC).
  • HY-14854A
    Tecarfarin sodium

    ATI-5923 sodium

    Others Metabolic Disease
    Tecarfarin sodium (ATI-5923 sodium) is a novel orally active non-competitive vitamin K epoxide reductase (VKOR) antagonist, impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin sodium has the antithrombotic activity.
  • HY-N5018
    Nepodin

    Musizin

    Parasite AMPK Infection
    Nepodin (Musizin) is a quinone oxidoreductase (PfNDH2) inhibitor isolate from Rumex crispus.Nepodin (Musizin) stimulates the translocation of GLUT4 to the plasma membrane by activation of AMPK.Nepodin (Musizin) has antidiabetic and antimalarial activities.
  • 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-N3376
    Liriodenine

    Spermatheridine; VLT045

    Others Cancer
    Liriodenine (Spermatheridine; VLT045) is an aporphine alkaloid isolated from the plant Mitrephora sirikitiae and has anti-cancer activities. Liriodenine induces cell apoptosis, activates the intrinsic pathway by induction of caspase-3 and caspase-9.
  • HY-101379A
    8-Bromo-cGMP sodium

    Calcium Channel Neurological Disease
    8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator and significantly inhibits Ca 2+ macroscopic currents and impairs insulin release stimulated with high K +. 8-Bromo-cGMP sodium has antinociceptive effects.
  • HY-P1149
    Epithalon

    Telomerase Cancer Neurological Disease
    Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa.
  • HY-W008956
    Myoseverin

    Microtubule/Tubulin Inflammation/Immunology
    Myoseverina, a microtubule-binding molecule, induces the reversible fission of multinucleated myotubes into mononucleated fragments. Myoseverina affects the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with the activation of pathways involved in wound healing and tissue regeneration.
  • HY-N0722
    Neochlorogenic acid

    trans-5-O-Caffeoylquinic acid

    NF-κB Interleukin Related TNF Receptor COX Inflammation/Immunology Cancer
    Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and IL-1β. Neochlorogenic acid suppresses iNOS and COX-2 protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.
  • HY-10532
    SRT 1720

    Sirtuin Autophagy Metabolic Disease
    SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities agaiinst SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.
  • HY-112820
    Chlorantraniliprole

    Others Others
    Chlorantraniliprole is an insecticide that potently and selectively activates insect ryanodine receptor, with EC50s of 40 nM and 50 nM for Drosophila melanogaster and H. virescens ryanodine receptor, and ∼300-fold more potent than that in the mouse myoblast cell line, C2C12 (EC50, 14 μM).
  • HY-118628
    N-(p-amylcinnamoyl) Anthranilic Acid

    ACA

    Phospholipase TRP Channel Cardiovascular Disease
    N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia.
  • HY-N6807
    Elemicin

    Stearoyl-CoA Desaturase (SCD) Influenza Virus Cancer Infection
    Elemicin is a alkenylbenzene widely distributed in many herbs and spices. Elemicin inhibits Stearoyl-CoA Desaturase 1 (SCD1) by metabolic activation. Elemicin is one of the main components in aromatic food and has antimicrobial, antioxidant, and antiviral activities. Elemicin possesses genotoxicity and carcinogenicity.
  • HY-N0191
    Andrographolide

    Andrographis

    NF-κB SARS-CoV Influenza Virus Autophagy Cancer Infection Inflammation/Immunology
    Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
  • HY-13297
    PYZD-4409

    E1/E2/E3 Enzyme Cancer
    PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
  • HY-N2374
    Eupatorin

    Others Cancer
    Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage.
  • HY-N6641
    Monascin

    Others Cancer Inflammation/Immunology
    Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor).
  • HY-P1179A
    Guanylin(human) TFA

    Guanylate Cyclase Endogenous Metabolite
    Guanylin(human) TFA, a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) TFA is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.
  • HY-114335
    Triphala

    NF-κB Fungal Cancer Infection Inflammation/Immunology
    Triphala, an Ayurvedic polyherbal formulation comprising of equiproportional fruit parts of Terminalia chebula, Terminalia bellerica, and Phyllanthus emblica. Triphala inhibits NF-κB activation. Triphala exerts antifungal action. Anti-adipogenic, anti-inflammatory, and anti-neoplastic activities.
  • HY-121538
    CUDA

    Epoxide Hydrolase PPAR Cardiovascular Disease
    CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
  • HY-15262
    SRT 2104

    Sirtuin Metabolic Disease Neurological Disease Cancer
    SRT 2104 is a first-in-class, highly selective and brain-permeable activator of the NAD + dependent deacetylase Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 mRNA. Used in the research of diabetes mellitus and Huntington’s disease.
  • HY-103254
    ML221

    Others Neurological Disease
    ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
  • HY-N0479
    Licarin B

    (-)-Licarin B

    PPAR GLUT Metabolic Disease
    Licarin B, a nitric oxide production inhibitor extracted from the component of the seeds of Myristica fragrans, improves insulin sensitivity via PPARγ and activation of GLUT4 in the IRS-1/PI3K/AKT pathway.
  • HY-N6861
    Lucidenic acid B

    Apoptosis Cancer
    Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells.
  • HY-19837
    BMS-986120

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects.
  • HY-N2116
    Ginkgolic acid C17:1

    PTEN Phosphatase Cancer
    Ginkgolic acid C17:1, extracted from Ginkgo biloba Leaves, suppresses constitutive and inducible STAT3 activation through induction of PTEN and SHP-1 tyrosine phosphatase. Ginkgolic acid C17:1 has anticancer effects.
  • HY-13649
    Indibulin

    ZIO 301; D 24851

    Microtubule/Tubulin Apoptosis Cancer Neurological Disease
    Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.
  • HY-126585
    SAICAR

    Endogenous Metabolite Cancer
    SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions.
  • HY-111549
    Bragsin1

    Others Cancer
    Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.
  • HY-P1219
    Jingzhaotoxin-III

    Sodium Channel Neurological Disease
    Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype[1] [2] .
  • 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-18982
    Anisomycin

    Flagecidin; Wuningmeisu C

    DNA/RNA Synthesis JNK Bacterial Apoptosis Antibiotic Cancer Infection
    Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system. Anisomycin is a JNK activator, which increases phospho-JNK. Anisomycin is a bacterial antibiotic isolated from Streptomyces griseolus.
  • HY-B0258
    Gemfibrozil

    CI-719

    PPAR Cytochrome P450 Metabolic Disease Cardiovascular Disease
    Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering drug; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
  • HY-N0003
    Honokiol

    NSC 293100

    Akt ERK Autophagy HCV Cancer
    Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2. Honokiol can readily cross the blood brain barrier.
  • HY-121685A
    Tipepidine hydrochloride

    Potassium Channel Neurological Disease
    Tipepidine hydrochloride reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine hydrochloride subsequently activates VTA dopamine neuron. Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect.
  • HY-N3806
    Enniatin B

    Acyltransferase ERK Cancer Infection Cardiovascular Disease
    Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes. Enniatins B decreases the activation of ERK (p44/p42).
  • HY-P0175A
    740 Y-P TFA

    740YPDGFR TFA; PDGFR 740Y-P TFA

    PI3K Autophagy Cancer
    740 Y-P TFA is a potent and cell-permeable PI3K activator. 740 Y-P TFA readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
  • HY-119917
    Gossypetin

    p38 MAPK Bacterial Cancer Infection
    Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities.
  • HY-10936
    S 18986

    iGluR Neurological Disease
    S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
  • HY-N0592
    Demethyleneberberine

    NF-κB AMPK Metabolic Disease Inflammation/Immunology
    Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD).
  • HY-N2497
    Isoliquiritin apioside

    NF-κB MMP p38 MAPK Cancer
    Isoliquiritin apioside, a component isolated from Glycyrrhizae radix rhizome, significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells.
  • HY-18686
    AS1949490

    Phosphatase Metabolic Disease
    AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM. AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes.
  • HY-10619B
    Niraparib tosylate

    MK-4827 tosylate

    PARP Apoptosis Cancer
    Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-131187
    BMS-1166-N-piperidine-COOH

    Ligand for Target Protein for PROTAC Cancer
    BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-120528A
    GB-110 hydrochloride

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-117541
    Glycyl-glutamine

    Glycyl-L-glutamine

    Others Neurological Disease
    Glycyl-glutamine (Glycyl-L-glutamine), as a enzymatic cleavage product of β-endorphin, is apparently an endogenous antagonist of beta-endorphin(1-31) in several systems. Glycyl-glutamine (Glycyl-L-glutamine) is an activate and stable glutamine-containing neuropeptide over glutamine (Gln).
  • HY-W009724
    2-Aminoethyl diphenylborinate

    2-APB

    Calcium Channel TRP Channel Infection
    2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca 2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
  • HY-P1149A
    Epithalon TFA

    Telomerase Cancer Neurological Disease
    Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa.
  • HY-125827
    13-Methylberberine chloride

    13-Methylberberinium chloride

    Others Cancer Metabolic Disease
    13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS.
  • HY-100612
    T16Ainh-A01

    Chloride Channel Others
    T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).
  • HY-B0764
    Bucladesine sodium

    Dibutyryl cAMP sodium salt; DBcAMP sodium salt

    PKA Phosphodiesterase (PDE) Inflammation/Immunology
    Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.
  • HY-15415
    KB-R7943 mesylate

    Na+/Ca2+ Exchanger Autophagy Cancer
    KB-R7943 mesylate is a widely used inhibitor of the reverse Na +/Ca 2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.
  • HY-N0496
    Ruscogenin

    NOD-like Receptor (NLR) Cardiovascular Disease
    Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway and exerts significant anti-inflammatory and anti-thrombotic activities.
  • HY-13459
    PF-5274857

    Smo Cancer
    PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
  • HY-120528
    GB-110

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-15271
    WYE-687

    mTOR PI3K Cancer
    WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
  • HY-13757AS
    Tamoxifen-​d5

    ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
  • HY-111926
    N6-Methyladenosine 5'-monophosphate disodium salt

    Others Metabolic Disease
    N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM. N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor.
  • HY-B1899A
    Taurodeoxychloic Acid sodium hydrate

    Sodium taurodeoxycholate monohydrate

    Caspase Metabolic Disease Inflammation/Immunology
    Taurodeoxychloic Acid sodium hydrate (Sodium taurodeoxycholate monohydrate) prevents apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxychloic Acid sodium hydrate is investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.
  • HY-N0393
    Glabridin

    PPAR Reactive Oxygen Species Bacterial Cancer Infection Inflammation/Immunology
    Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds to and activates PPARγ, with an EC50 of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.
  • HY-10529
    Betulinic acid

    Lupatic acid; Betulic acid

    Apoptosis Topoisomerase HIV Autophagy Mitophagy NF-κB Endogenous Metabolite 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-120111
    MW-150

    MW01-18-150SRM

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-15615A
    TIC10

    ONC-201

    TNF Receptor Apoptosis Cancer
    TIC10 is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier.
  • HY-114645
    PDK1-IN-RS2

    PDK-1 Cancer
    PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1.
  • HY-10619
    Niraparib