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Results for "

expression

" in MCE Product Catalog:

405

Inhibitors & Agonists

6

Screening Libraries

1

Biochemical Assay Reagents

16

Peptides

6

MCE Kits

177

Natural
Products

5

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-134476
    NF-κΒ activator 1

    NF-κB Inflammation/Immunology
    NF-κΒ activator 1 is a potent NF-κΒ activator with an EC50 of 0.9 μM. NF-κΒ activator 1 induces superoxide dismutase (SOD)2 mRNA expression.
  • HY-N1534
    Ponasterone A

    25-Deoxyecdysterone

    Others Others
    Ponasterone A (25-Deoxyecdysterone), an ecdysteroid, has strong affinity for the ecdysone receptor. Ponasterone A is a potent regulator of gene expression in cells and transgenic animals, enabling reporter genes to be turned on and off rapidly.
  • HY-13570A
    Betamethasone hydrochloride

    Glucocorticoid Receptor Apoptosis Inflammation/Immunology Endocrinology
    Betamethasone hydrochloride is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone hydrochloride accelerates fetal lung maturation and induces gene expression and apoptosis.
  • HY-13570
    Betamethasone

    Glucocorticoid Receptor Apoptosis Inflammation/Immunology Endocrinology Cancer
    Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis.
  • 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-N8122
    24-Methylenecycloartanyl ferulate

    Akt Cancer
    24-Methylenecycloartanyl ferulate is a γ-oryzanol compound. 24-Methylenecycloartanyl ferulate promotes parvin-beta expression in human breast cancer cells. 24-Methylenecycloartanyl ferulate is a potential ATP-competitive Akt1 inhibitor (EC50= 33.3μM).
  • HY-106168
    Thymectacin

    NB1011

    Others Cancer
    Thymectacin (NB1011) is an agent selectively targeting tumor cells that have a high expression of thymidylate synthase (TS). Thymectacin is an aryloxy phosphoramidate derivative of BVdU (brivudin).
  • HY-B1238
    Pronethalol

    (±)-Pronethalo

    Adrenergic Receptor Neurological Disease Cardiovascular Disease
    Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs).
  • HY-B1238A
    Pronethalol hydrochloride

    (±)-Pronethalo hydrochloride

    Adrenergic Receptor Neurological Disease Cardiovascular Disease
    Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias, and limits the cerebral arteriovenous malformation (AVMs).
  • HY-121750
    CCG-222740

    Ras ROCK Cancer
    CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
  • HY-N0704
    Agrimol B

    Sirtuin PPAR Metabolic Disease
    Agrimol B is a polyphenol derived from Agrimonia pilosa Ledeb, suppresses adipogenesis via inducing SIRT1 translocation and expression, and reducing PPARγ expression.
  • HY-18292
    ARN2966

    Amyloid-β Neurological Disease
    ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ.
  • HY-121118
    Coronaridine

    Wnt Cancer Neurological Disease
    Coronaridine, an iboga type alkaloid, inhibits the wnt signaling pathway by decreasing β-catenin expression.
  • HY-B0393
    Fudosteine

    Others Inflammation/Immunology
    Fudosteine is a cysteine derivative and a mucoactive agent. Fudosteine inhibits MUC5AC mucin hypersecretion by reducing MUC5AC gene expression.
  • HY-101454
    SR0987

    ROR Cancer Inflammation/Immunology
    SR0987, a SR1078 analog, is a RORγt agonist, with an EC50 of 800 nM. SR0987 increases IL17 expression while repressing the expression of PD-1.
  • HY-N1280
    Semilicoisoflavone B

    Amyloid-β Neurological Disease
    Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β () secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation.
  • 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-N2483
    Hydroprotopine

    Others Cancer
    Hydroprotopine is a alkaloid from Hypecoum leptocarpumand. Leptopidine can suppress growth and induce cytotoxicity in breast cancer cells and that the cytotoxicity of leptopidine may be related to its inhibitory effect on fatty acid synthase expression.
  • HY-N1060
    Yatein

    HSV Apoptosis Cancer Infection
    Yatein is a lignan isolated from A. chilensis, with antiproliferative activity. Yatein suppresses herpes simplex virus type 1 (HSV-1 ) replication by interruption the immediate-early gene expression.
  • HY-B2230
    Hinokitiol

    β-Thujaplicin

    Keap1-Nrf2 DNA Methyltransferase Virus Protease Cancer Infection
    Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.
  • HY-80013A
    THZ1 Hydrochloride

    CDK Cancer
    THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • HY-N0703
    Schaftoside

    Toll-like Receptor (TLR) MyD88 Dynamin Mitochondrial Metabolism Autophagy Inflammation/Immunology
    Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
  • HY-80013
    THZ1

    CDK Cancer
    THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • 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-N6968
    α-Humulene

    Humulene; α-Caryophyllene

    NO Synthase COX Inflammation/Immunology
    α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 µg/mL). α-Humulene inhibits COX-2 and iNOS expression.
  • HY-100596
    AS1842856

    Autophagy Metabolic Disease
    AS1842856, a specific Foxo1 inhibitor (IC50=30 nM), potently suppresses autophagy. AS1842856 only reduces the activity of FoxO1 by binding with it, without affecting its transcription and protein expression.
  • HY-136446
    MYLS22

    Others Cancer Cardiovascular Disease
    MYLS22 is a first-in-class and selective optic atrophy 1 (OPA1) inhibitor. MYLS22 can target endothelial OPA1 to curtail tumor growth and inhibits angiogenesis by impinging on NFkB activity and on angiogenic gene expression.
  • HY-N5123
    α-L-Rhamnose

    Others Others
    α-L-Rhamnose is a terminal residue of steviol glycosides Dulcoside A and Dulcoside B. α-L-Rhamnose recognizing lectin site of human dermal fibroblasts functions as a signal transducer: modulation of Ca 2+ fluxes and gene expression.
  • 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-16182A
    Ecamsule disodium

    Others Others
    Ecamsule disodium is a broad-spectrum UVA filter that can be used in sunscreen product. Ecamsule reduces biological damage caused by solar radiation such as pyrimidine dimer formation, p53 protein accumula-tion, or collagenase 2 expression.
  • HY-16509
    UNBS5162

    CXCR Autophagy Cancer Endocrinology
    UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.
  • HY-126241
    RV01

    Aldehyde Dehydrogenase (ALDH) Inflammation/Immunology
    RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity.
  • HY-134582
    dCBP-1

    PROTACs Epigenetic Reader Domain Cancer
    dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on PROTAC. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression.
  • HY-119692
    Curvulin

    Microtubule/Tubulin Others
    Curvulin is a phytotoxin. Curvularin inhibits microtubule assembly and inhibits iNOS expression.
  • HY-N1389
    Carmine

    Carmine red

    Others Inflammation/Immunology
    Carmine (Carmine red), a natural red dye extracted from the dried females of the insect Dactylopius coccus var. Costa (cochineal). Carmine is a widely used food additive. Carmine provokes both an immediate hypersensitivity and a delayed systemic response with cutaneous expression.
  • HY-N0158
    Oxymatrine

    TGF-beta/Smad Influenza Virus Cancer Infection Inflammation/Immunology
    Oxymatrine, an alkaloid from the roots of Sophora species, with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.
  • HY-13671
    LW6

    HIF-1α inhibitor; LW8

    HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
  • HY-103701
    L-Ascorbic acid 2-phosphate

    2-Phospho-L-ascorbic acid

    Phosphatase Metabolic Disease
    L-ascorbic acid 2-phosphate (2-Phospho-L-ascorbic acid) is a long-acting vitamin C derivative that can stimulate collagen formation and expression. L-ascorbic acid 2-phosphate (2-Phospho-L-ascorbic acid) can be used as a culture medium supplement for the osteogenic differentiation of human adipose stem cells (hASCs). L-ascorbic acid 2-phosphate increases alkaline phosphatase (ALP) activity and expression of runx2A in hASCs during the osteogenic differentiation.
  • HY-133131
    PROTAC BRD4 Degrader-1

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-1 is an efficacious BRD4 degrader with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.
  • HY-120062
    TVB-3664

    Fatty Acid Synthase (FASN) Cancer
    TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.
  • HY-N0532
    Morroniside

    MMP Pyroptosis Apoptosis Metabolic Disease Neurological Disease
    Morroniside has neuroprotective effect by inhibiting neuron apoptosis and MMP2/9 expression.
  • HY-N1157
    Thevetiaflavone

    Apigenin-5-methyl ether

    Bcl-2 Family Caspase Neurological Disease
    Thevetiaflavone could upregulate the expression of Bcl‑2 and downregulate that of Bax and caspase‑3.
  • HY-N0809
    Sesamolin

    p38 MAPK JNK Caspase Metabolic Disease Neurological Disease
    Sesaminol, isolated from Justicia orbiculata, has antioxidative activity, Sesaminol inhibits lipid peroxidation and shows neuroprotection effect. Sesaminol potently inhibits MAPK cascades by preventing phosphorylation of JNK, p38 MAPKs, and caspase-3 but not ERK-MAPK expression.
  • HY-107599
    AEG3482

    JNK Apoptosis Neurological Disease
    AEG3482 is a potent antiapoptotic compound that inhibits Jun kinase (JNK) activity through induced expression of heat shock protein 70 (HSP70). AEG3482 directly binds HSP90, thereby facilitating HSF1-dependent expression of HSP70 and HSP25.
  • HY-114310
    VDR agonist 1

    VD/VDR Apoptosis Cancer
    VDR agonist 1 (compound 28) is a nonsteroidal Vitamin D receptor (VDR) agonist, with an IC50 of 690 nM in MCF-7 cells. VDR agonist 1 arrests the cell cycle through the up-regulation of p21 and p27, promotes apoptosis by increasing the expression of BAX and decrease the expression of Bcl-2.
  • HY-N0249
    Saikosaponin C

    Amyloid-β Neurological Disease
    Saikosaponin C is a bioactive component found in radix bupleuri, targets amyloid beta and tau in Alzheimer's disease. Saikosaponin C inhibits the secretion of both Aβ1-40 and Aβ1-42, and suppresses abnormal tau phosphorylation, but shows no effect on BACE1 activity and expression.
  • HY-N0256
    Hederagenin

    Others Cancer
    Hederagenin is a triterpenoid saponin. It can inhibit LPS-stimulated expression of iNOS, COX-2, and NF-κB.
  • HY-19994
    ML264

    KLF Cancer
    ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.
  • HY-112822
    ON-013100

    CDK Cancer
    ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
  • HY-123076
    Pifithrin-α, p-Nitro, Cyclic

    PFN-α

    MDM-2/p53 Neurological Disease
    Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
  • HY-103701A
    L-Ascorbic acid 2-phosphate magnesium

    2-Phospho-L-ascorbic acid magnesium

    Phosphatase Metabolic Disease
    L-Ascorbic acid 2-phosphate magnesium (2-Phospho-L-ascorbic acid magnesium) is a long-acting vitamin C derivative that can stimulate collagen formation and expression. L-Ascorbic acid 2-phosphate magnesium (2-Phospho-L-ascorbic acid magnesium) can be used as a culture medium supplement for the osteogenic differentiation of human adipose stem cells (hASCs). L-Ascorbic acid 2-phosphate magnesium (2-Phospho-L-ascorbic acid magnesium) increases alkaline phosphatase (ALP) activity and expression of runx2A in hASCs during the osteogenic differentiation.
  • HY-N0554
    Escin IA

    HIV Protease Cancer Infection
    Escin IA is a triterpene saponin isolated from horse chestnut, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression.
  • HY-N2273
    Gymnestrogenin

    LXR Metabolic Disease
    Gymnestrogenin is a pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br. Gymnestrogenin is a LXR antagonist with IC50s of 2.5 and 1.4 μM for LXRα and LXRβ transactivation, respectively. Gymnestrogenin reduces the transcriptional activity of LXR even on its own promoter, thus reducing the mRNA expression.
  • HY-132304
    CC-90005

    PKC Inflammation/Immunology
    CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression.
  • HY-129113
    α-​Chaconine

    COX Inflammation/Immunology
    α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
  • HY-N1967
    Dihydrocurcumin

    Fatty Acid Synthase (FASN) Metabolic Disease
    Dihydrocurcumin, a major metabolites of curcumin, reduces lipid accumulation and oxidative stress. Dihydrocurcumin regulates mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increases protein expression levels of pAKT and PI3K, and reduced the levels of cellular NO and ROS via Nrf2 signaling pathways.
  • HY-19694
    BRD7552

    Others Endocrinology
    BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function.
  • HY-100495
    FT011

    Others Inflammation/Immunology
    FT011 is an anti-fibrotic agent, reduces mRNA expression of collagens I and III and inhibits collagen synthesis.
  • HY-N0184A
    Dipotassium glycyrrhizinate

    Glycyrrhizic acid dipotassium; Dipotassium glycyrrhizate

    Virus Protease Inflammation/Immunology
    Dipotassium glycyrrhizinate is a natural compound, inhibits atopic dermatitis-related gene expression with anti-anti-inflammatory activity.
  • HY-16079
    AZD3514

    Androgen Receptor Cancer
    AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.
  • HY-12884
    OAC2

    Oct3/4 Others
    OAC2 is an Oct4-activating compound which activates expression through the Oct4 gene promoter.
  • HY-N0509
    Astilbin

    Keap1-Nrf2 TNF Receptor NF-κB Inflammation/Immunology Cancer
    Astilbin is a flavonoid compound and enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
  • HY-B2184
    Sofalcone

    Autophagy Bacterial Infection Inflammation/Immunology
    Sofalcone, a gastric antiulcer agent, is known to induce the expression of Heme oxygenase-1 (HO-1) in gastric epithelium.
  • HY-N0246
    Saikosaponin A

    LXR Bacterial Inflammation/Immunology Cancer
    Saikosaponin A is an active component of Bupleurum falcatum, up-regulates LXRα expression, with potent anti-inflammatory activity.
  • HY-N2252
    Licarin A

    (+)-Licarin A

    TNF Receptor Prostaglandin Receptor COX Metabolic Disease Inflammation/Immunology Neurological Disease
    Licarin A ((+)-Licarin A), a neolignan, significantly and dose-dependently reduces TNF-α production (IC50=12.6 μM) in dinitrophenyl-human serum albumin (DNP-HSA)-stimulated RBL-2H3 cells. Anti-allergic effects. Licarin A reduces TNF-α and PGD2 production, and COX-2 expression.
  • HY-14648
    Dexamethasone

    Hexadecadrol; Prednisolone F

    Glucocorticoid Receptor SARS-CoV Autophagy Complement System Mitophagy Bacterial Antibiotic Cancer Infection Endocrinology Inflammation/Immunology
    Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
  • HY-N6675
    Gardenia yellow

    Sirtuin Neurological Disease Cancer
    Gardenia yellow is an active member of crocin, increases mRNA expression of SIRT3, and acts as an orally active antidepressant agent.
  • HY-Y0078
    Cinnamyl Alcohol

    PPAR Metabolic Disease
    Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, with anti-obesity activity.
  • HY-W014522
    Dichlormid

    Others Others
    Dichlormid is a herbicide safener. Dichlormid up-regulates expression of ZmGST27 and ZmMRP1 and increases ZmGT1.
  • HY-15615
    TIC10 isomer

    ONC201 isomer

    Others Others
    TIC10 isomer is the isomer of TIC10. TIC10 isomer does not possess the reported biological activity of inducing TRIAL expression.
  • HY-19999A
    PF-CBP1 hydrochloride

    Epigenetic Reader Domain Histone Acetyltransferase Neurological Disease
    PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC50 of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1βIL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.
  • HY-12725
    ML324

    Histone Demethylase HSV CMV Cancer
    ML324 is a potent JMJD2 demethylase inhibitor with antiviral activity. ML324 also exhibits inhibition for the histone demethylase KDM4B, with an IC50 of 4.9 μM. ML324 has potent anti-viral activity against both herpes simplex virus (HSV) and human cytomegalovirus (hCMV) infection via inhibition viral IE gene expression.
  • HY-101931
    hVEGF-IN-1

    VEGFR Cancer
    hVEGF-IN-1, a quinazoline derivative, could specifically bind to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilize the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression.
  • HY-19808
    C-DIM12

    Apoptosis Neurological Disease Cancer
    C-DIM12 is a synthetic Nurr1 activaor induces Nurr1 and DA gene expression in cell lines and primary neurons.
  • HY-N5118
    Chimonanthine

    (-)-Chimonanthine

    Tyrosinase Cancer
    Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis.
  • HY-112582
    N1-Methylpseudouridine

    1-Methylpseudouridine

    Others Inflammation/Immunology
    N1-methyl-pseudouridine (1-Methylpseudouridine), a methylpseudouridine, outperforms 5 mC and 5 mC/N1-methyl-pseudouridine in translation. N1-methyl-pseudouridine in mRNA enhances translation through eIF2α-dependent and independent mechanisms by increasing ribosome density.
  • HY-100218A
    RSL3

    (1S,3R)-RSL3

    Glutathione Peroxidase Ferroptosis Cancer
    RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.
  • HY-B1026
    Adelmidrol

    NF-κB COX PPAR Inflammation/Immunology
    Adelmidrol exerts important anti-inflammatory effects that are partly dependent on PPARγ. Adelmidrol reduces NF-κB translocation, and COX-2 expression.
  • HY-12702
    10058-F4

    c-Myc Autophagy Cancer
    10058-F4 is a c-Myc inhibitor that prevents c-Myc-Max dimerization and transactivation of c-Myc target gene expression.
  • HY-N0774
    Isofraxidin

    COX MMP Toll-like Receptor (TLR) Inflammation/Immunology
    Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.
  • HY-N0604
    Ginsenoside Rh1

    Prosapogenin A2; Sanchinoside B2; Sanchinoside Rh1

    PPAR TNF Receptor Interleukin Related Endogenous Metabolite Inflammation/Immunology
    Ginsenoside Rh1 (Prosapogenin A2) inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
  • HY-126482
    Telomerase-IN-2

    Telomerase Cancer
    Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC50 of 0.89 µM. Anti-cancer activity.
  • HY-N0648
    Monotropein

    Others Inflammation/Immunology
    Monotropein is an iridoid glycoside isolated Morinda officinalis. Monotropein inhibits the expression of inflammatory mediators in dextran sulfate sodium (DSS)-induced colitis mouse model.
  • HY-N1380
    Guaiacol

    2-Methoxyphenol

    COX NF-κB Endogenous Metabolite Inflammation/Immunology
    Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.
  • HY-N5015
    Rosmanol

    Others Inflammation/Immunology Cancer
    Rosmanol could inhibit the oxidation of low density lipoprotein (LPL) and significantly inhibit lipopolysaccharide induced iNOS and COX-2 expression, with anti-inflammatory effect.
  • HY-N1902
    4-Hydroxyphenylacetic acid

    Keap1-Nrf2 Endogenous Metabolite Metabolic Disease
    4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2.
  • HY-10211
    Tanespimycin

    17-AAG; NSC 330507; CP 127374

    HSP Autophagy Mitophagy Bacterial Apoptosis Antibiotic Cancer Infection
    Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.
  • HY-N6064
    Polygalacin D

    Apoptosis IAP Cancer
    Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum (Jacq.) with anticancer and anti-proliferative properties. PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis
  • HY-N2205
    Esculentoside H

    NF-κB JNK Cancer
    Esculentoside H (EsH) is a saponin isolated from the root extract of perennial plant Phytolacca esculenta. Esculentoside H (EH) has anti-tumor activity, the mechanism is related to the capacity for TNFrelease. Esculentoside H (EsH) suppresses colon cancer cell migration through blockage of the JNK1/2 and NF-κB signaling-mediated matrix metalloproteinases-9 (MMP-9) expression.
  • HY-112234
    L-Sepiapterin

    Sepiapterin

    Endogenous Metabolite Cancer
    L-Sepiapterin (Sepiapterin) is a precursor of the endothelial nitric oxide synthase (eNOS) cofactor tetrahydrobiopterin (BH4). L-Sepiapterin improves endothelial dysfunction in small mesenteric arteries from db/db mice, and induces angiogenesis. L-Sepiapterin inhibits cell proliferation and migration of ovarian cancer cells via down-regulation of p70 S6K-dependent VEGFR-2 expression.
  • HY-N0197
    Baicalin

    Baicalein 7-O-β-D-glucuronide

    NF-κB Autophagy HIV Inflammation/Immunology Cancer
    Baicalin, as a flavonoid glycoside, is an allosteric carnitine palmityl transferase 1 (CPT1) activator. Baicalin reduces the expression of NF-κB.
  • HY-N0686
    Pseudoprotodioscin

    Fatty Acid Synthase (FASN) MicroRNA Metabolic Disease
    Pseudoprotodioscin, a furostanoside, inhibits SREBP1/2 and microRNA 33a/b levels and reduces the gene expression regarding the synthesis of cholesterol and triglycerides.
  • HY-N2057
    Steviol

    Others Metabolic Disease
    Steviol is a major metabolite of the sweetening compound stevioside. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation.
  • 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-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-135581
    Raloxifene 6-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-135582
    Raloxifene 4'-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-111784
    Inobrodib

    CCS1477

    Epigenetic Reader Domain Cancer
    Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain inhibitor. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.
  • HY-103484
    GATA4-NKX2-5-IN-1

    Others Cardiovascular Disease
    GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.
  • HY-18371
    TC-S 7009

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ≫ 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression.
  • HY-N7421
    Smilagenin acetate

    Others Neurological Disease
    Smilagenin acetate is a sapogenin derivative extracted from patent US20030004147A1. Smilagenin acetate increases the expression of acetylcholine m2 receptors and can be used for the research of dementia.
  • HY-N7067
    Revaprazan hydrochloride

    Bacterial COX Infection
    Revaprazan hydrochloride is a novel acid pump antagonist (APA). Revaprazan hydrochloride reduces COX-2 expression and has significant anti-inflammatory actions activities in H. pylori infection.
  • HY-N0011
    Baohuoside I

    Icariin-II; Icariside-II

    CXCR Apoptosis Cancer Inflammation/Immunology Endocrinology
    Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
  • HY-18623
    VI 16832

    Others Cancer
    VI 16832 is a broad spectrum Type I kinase inhibitor which can be used as an enrichment tool for the comparative expression analysis of protein kinases in different cancer cell lines.
  • HY-N6878
    Cauloside D

    Others Inflammation/Immunology
    Cauloside D is a triterpene glycoside isolated from Caulophyllum robustum Max. Cauloside D exerts anti-inflammatory effects through the inhibition of expression of iNOS and proinflammatory cytokines.
  • HY-118660
    Anhydrotetracycline hydrochloride

    Antibiotic Bacterial Infection
    Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells.
  • 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-N2518
    Agnuside

    Agnoside

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Agnuside is a compound isolated from Vitex negundo, down-regulates pro-inflammatory mediators PGE2 and LTB4, and reduces the expression of cytokines, with anti-arthritic activity.
  • HY-N6741
    β-Zearalenol

    Others Infection Endocrinology
    β-Zearalenol is a non-steroidal estrogenic mycotoxin synthesized by Fusarium species. β-Zearalenol potentially influences transcription and effects gene expression on translational level.
  • HY-19696
    Tauroursodeoxycholate

    Tauroursodeoxycholic acid; TUDCA; UR 906

    ERK Caspase Endogenous Metabolite Apoptosis Cancer
    Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
  • HY-N6919
    Cauloside C

    Others Inflammation/Immunology
    Cauloside C is a triterpene glycoside isolated from Caulophyllum robustum Max. Cauloside C exerts anti-inflammatory effects through the inhibition of expression of iNOS and proinflammatory cytokines.
  • HY-N0040
    Ginsenoside Rb2

    Ginsenoside C

    GPR120 Influenza Virus Endogenous Metabolite Infection Metabolic Disease Inflammation/Immunology
    Ginsenoside Rb2 is one of the main bioactive components of ginseng extracts. Rb2 can upregulate GPR120 gene expression. Ginsenoside Rb2 has antiviral effects.
  • HY-122808
    (-)-Camphoric acid

    mGluR Metabolic Disease
    (-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1.
  • HY-135849
    Catalase

    Reactive Oxygen Species Cancer
    Catalase is a key enzyme in the metabolism of H2O2 and reactive oxygen species (ROS), and its expression and localization is markedly altered in tumors. Free oxygen radical scavenger.
  • HY-13030A
    (R)-(-)-JQ1 Enantiomer

    Epigenetic Reader Domain Cancer
    (R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (R)-(-)-JQ1 Enantiomer has no effect.
  • HY-N0635
    Prim-O-glucosylcimifugin

    NO Synthase COX Inflammation/Immunology
    Prim-O-glucosylcimifugin exerts anti-inflammatory effects through the inhibition of iNOS and COX-2 expression by through regulating JAK2/STAT3 signaling.
  • HY-19696A
    Tauroursodeoxycholate sodium

    Tauroursodeoxycholic acid sodium; TUDCA sodium; UR 906 sodium

    ERK Caspase Apoptosis Cancer
    Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
  • HY-128583
    G150

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor for repression of dsDNA-triggered interferon expression, with an IC50 of 10.2 nM.
  • HY-N2897
    Dihydrokaempferol

    Apoptosis Bcl-2 Family Inflammation/Immunology
    Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic drugs.
  • HY-N7688
    Regaloside B

    NO Synthase COX Inflammation/Immunology
    Regaloside B is a phenylpropanoid isolated from Lilium longiflorum. Regaloside B can inhibit the expression of iNOS and COX-2. Regaloside B has anti-inflammatory activity.
  • HY-N2989
    3-O-Acetyl-16α-hydroxydehydrotrametenolic acid

    NO Synthase Inflammation/Immunology
    3-O-Acetyl-16α-hydroxydehydrotrametenolic acid, an anti-inflammatory triterpenoid, inhibits NO production and iNOS expression in LPS-stimulated Raw264.7 cells.
  • 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-14959
    Ulipristal

    CDB-3236; Deacetyl CDB-2914

    Progesterone Receptor Cancer Endocrinology
    Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system.
  • HY-136568
    Stafia-1-dipivaloyloxymethyl ester

    STAT Others
    Stafia-1-dipivaloyloxymethyl ester (compound 27, 0-200 μM) decreases pSTAT5a expression significantly, and has no obvious inhibition on pSTAT5b.
  • HY-14571
    E7820

    ER68203-00

    Integrin Cancer
    E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.
  • HY-N0060B
    (E)-Ferulic acid

    (E)-Coniferic acid

    β-catenin Bcl-2 Family Ferroptosis Endogenous Metabolite Cancer
    (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.
  • HY-U00441
    DPBQ

    MDM-2/p53 Apoptosis Cancer
    DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells.
  • HY-N1949
    Homoplantaginin

    TNF Receptor NF-κB Inflammation/Immunology
    Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.
  • HY-N0596
    Panaxadiol

    20(R)-Panaxadiol

    Others Cancer
    Panaxadiol is found in the roots of Panax ginseng, activities neuroprotective and anti-tumour functions. Panaxadiol inhibits programmed cell death-ligand 1(PD-L1) expression and tumour proliferation.
  • HY-12743A
    K-7174 dihydrochloride

    Others Inflammation/Immunology
    K-7174 dihydrochloride is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
  • HY-B0360
    Rebamipide

    OPC12759; Proamipide

    COX Prostaglandin Receptor Cancer Inflammation/Immunology
    Rebamipide (OPC12759) is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner.
  • HY-N1988
    Cucurbitacin IIa

    Hemslecin A

    Survivin Apoptosis Cancer
    Cucurbitacin IIa is a triterpene isolated from Hemsleya amalils Diels, induces apoptosis of cancer cells, reduces expression of survivin, reduces phospho-Histone H3 and increases cleaved PARP in cancer cells.
  • HY-12743
    K-7174

    Others Inflammation/Immunology
    K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
  • 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-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-B0141
    Estradiol

    β-Estradiol; E2; 17β-Estradiol; 17β-Oestradiol

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
  • HY-B1776
    Spermidine

    Endogenous Metabolite Metabolic Disease
    Spermidine maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine significantly decreases the H2O2 and O2 .- contents.
  • HY-107805
    Dihydroactinidiolide

    Others Cancer Infection Neurological Disease
    Dihydroactinidiolide, existing in plant leaves and fruits, is a potent plant growth inhibitor, a regulator of gene expression and is responsible for photo acclimation in Arabidopsis. Dihydroactinidiolide has antioxidant activity, antibacterial activity, anticancer activity and neuroprotective effect.
  • HY-N0847
    Micheliolide

    NF-κB 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-19696B
    Tauroursodeoxycholate dihydrate

    Tauroursodeoxycholic acid dihydrate; TUDCA dihydrate; UR 906 dihydrate

    ERK Caspase Apoptosis Cancer
    Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
  • HY-B1776A
    Spermidine trihydrochloride

    Others Metabolic Disease
    Spermidine trihydrochloride maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine trihydrochloride significantly decreases the H2O2 and O2 .- contents.
  • 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-N0042
    Ginsenoside Rc

    Panaxoside Rc

    GABA Receptor TNF Receptor Interleukin Related Cancer Inflammation/Immunology Neurological Disease
    Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
  • HY-N1963
    Curzerene

    Gutathione S-transferase Apoptosis Cancer
    Curzerene is a sesquiterpene is isolated from the rhizome of Curculigo orchioides Gaertn with anti-cancer activity. Curzerene inhibits glutathione S-transferase A1 (GSTA1) mRNA and protein expression. Curzerene induces cell apoptosis.
  • HY-111444
    Auxinole

    Others Others
    Auxinole is a potent auxin antagonist of TIR1/AFB receptors, binding TIR1 to block the formation of the TIR1-IAA-Aux/IAA complex and so inhibits auxin-responsive gene expression.
  • HY-N2110
    Phellopterin

    Others Inflammation/Immunology
    Phellopterin is a natural product isolated from P. trifoliata. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
  • HY-13992
    AP20187

    B/B Homodimerizer

    FKBP Metabolic Disease
    AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein (FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.
  • HY-137067
    IMT1B

    LDC203974

    Others Cancer
    IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.
  • HY-18772
    O4I2

    Oct3/4 Others
    O4I2 is a potent Oct3/4 inducer. O4I2 induces the expression of pluripotent-associated genes Lin28, Sox2 and Nanog, and suppresses Rex1.
  • HY-136341
    7,8-Dihydroneopterin

    Apoptosis NO Synthase Endogenous Metabolite Inflammation/Immunology Neurological Disease
    7,8-Dihydroneopterin, an inflammation marker, induces cellular apoptosis in astrocytes and neurons via enhancement of nitric oxide synthase (iNOS) expression. 7,8-Dihydroneopterin can be used in the research of neurodegenerative diseases.
  • HY-125129
    Carlinoside

    Others Others
    Carlinoside is a flavone glycoside with hepatoprotective efficiency. Carlinoside reduces hepatic bilirubin accumulation by stimulating bilirubin-UGT activity through Nrf2 gene expression. Carlinoside has the potential to intervene hyperbilirubinemia due to liver dysfunction.
  • HY-N1940
    β-Anhydroicaritin

    Interleukin Related TNF Receptor MMP Inflammation/Immunology
    β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
  • HY-100008
    Peretinoin

    NIK333

    RAR/RXR SphK Autophagy HCV Cancer Infection
    Peretinoin is an oral acyclic 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-124237A
    N-Octanoyl-L-homoserine lactone

    Bacterial Infection
    N-octanoyl-L-Homoserine lactone is a small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and affecting cellular metabolism. N-octanoyl-L-Homoserine lactone can be used for the infection prevention and regulation of virulence in cystic fibro.
  • HY-136409
    N-Decanoyl-L-homoserine lactone

    Bacterial Infection
    N-Decanoyl-L-homoserine lactone is a member of N-acyl-homoserine lactone family. N-Acylhomoserine lactones (AHL) regulate gene expression in Gram-negative bacteria, such as Echerichia and Salmonella, and are involved in quorum sensing, cell to cell communication among bacteria.
  • HY-N1506
    Ganodermanontriol

    Others Cancer
    Ganodermanontriol, a sterol isolated from Ganoderma lucidum, induces anti-inflammatory activity in tert-butyl hydroperoxide (t-BHP)-damaged hepatic cells through the expression of HO-1. Ganodermanontriol exhibits hepatoprotective activity.
  • HY-N6782
    Oligomycin

    ATP Synthase Fungal Antibiotic Cancer Infection
    Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
  • HY-N0001
    (-)-Epicatechin

    (-)-Epicatechol; Epicatechin; epi-Catechin

    COX Ferroptosis Endogenous Metabolite Cancer Inflammation/Immunology
    (-)-Epicatechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.
  • HY-N0364
    Falcarindiol

    Apoptosis Autophagy PPAR Cancer Infection Metabolic Disease Inflammation/Immunology
    Falcarindiol, an orally active polyacetylenic oxylipin, activates PPARγ and increases the expression of the cholesterol transporter ABCA1 in cells. Falcarindiol induces apoptosis and autophagy. Falcarindiol has anti-inflammatory, antifungal, anticancer and antidiabetic properties.
  • HY-N0656
    Usnic acid

    Bacterial Cancer Infection
    Usnic acid, a lichen-derived secondary metabolite, has a unique dibenzofuran skeleton. Usnic acid has excellent anticancer and antimicrobial properties. Usnic acid significantly inhibits RANKL-mediated osteoclast formation and function by reducing the transcriptional and translational expression of NFATc1.
  • 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-N9391
    7,3′,5′-Trihydroxyflavanone

    Apoptosis Cancer
    7,3′,5′-Trihydroxyflavanone, a flavanoid derivative, induces the apoptotic cell death of MCF-7 cells by increasing Bax expression level. 7,3′,5′-Trihydroxyflavanone also exhibits antioxidant activity.
  • 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-N6893
    Ergolide

    NF-κB Inflammation/Immunology
    Ergolide is a sesquiterpene lactone isolated from the dried flowers of Inula Britannica. Ergolide inhibits inducible nitric oxide synthase and cyclo-oxygenase-2 expression in RAW 264.7 macrophages through the inactivation of NF-κB.
  • HY-13580
    Budesonide

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
  • 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-N2342
    Procyanidin C1

    Apoptosis Cancer
    Procyanidin C1 is a natural polyphenol, causes DNA damage, cell cycle arrest, and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells.
  • HY-19306
    SB-267268

    Integrin Cancer
    SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
  • HY-N7674A
    Angoline hydrochloride

    STAT Cancer
    Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
  • HY-N3063
    Pimaric acid

    Others Cardiovascular Disease
    Pimaric acid is a resin acid that has been found in A. cordata and various pines. Pimaric acid reduces mRNA expression, protein levels, and promoter activity of matrix metalloproteinase-9 (MMP-9) in TNF-α-stimulated human aortic smooth muscle cells (HASMCs).
  • HY-N7038
    Phytohemagglutinin

    PHA-M

    Others Inflammation/Immunology
    Phytohemagglutinin (PHA-M), the major seed lectin of the common bean, Phaseolus vulgaris, accumulates in the parenchyma cells of the cotyledons. Phytohemagglutinin is a T-cell activator. Stimulation of human mononuclear leukocytes by Phytohemagglutinin induces the expression of ChAT mRNA, and potentiated ACh synthesis.
  • HY-N7674
    Angoline

    STAT Cancer
    Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
  • HY-101491
    SR-18292

    PGC-1α Autophagy Metabolic Disease
    SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
  • HY-N0698
    Crocin II

    NO Synthase COX Cancer Inflammation/Immunology Neurological Disease
    Crocin II is isolated from the fruit of Gardenia jasminoides with antioxidant, anticancer, and antidepressant activity. Crocin II inhibits NO production with an IC50 value of 31.1 μM. Crocin II suppresses the expressions of protein and m-RNA of iNOS and COX-2.
  • HY-115393A
    N-Heptanoyl-L-homoserine lactone

    Bacterial Infection
    N-Heptanoyl-L-homoserine lactone is a member of N-acyl-homoserine lactone family. N-acyl-homoserine lactones (AHL) can regulate gene expression in gram-negative bacteria, such as Echerichia and Salmonella, and are involved in quorum sensing, cell to cell communication among bacteria.
  • HY-N0896
    Inulicin

    1-O-Acetylbritannilactone

    NF-κB COX Cancer Inflammation/Immunology
    Inulicin (1-O-Acetylbritannilactone) is an active compound that 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-N0602
    Ginsenoside Rg2

    Chikusetsusaponin I; Panaxoside Rg2; Prosapogenin C2

    NF-κB Amyloid-β Neurological Disease Cardiovascular Disease Cancer
    Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 inhibits VCAM-1 and ICAM-1 expressions stimulated with lipopolysaccharide (LPS). Ginsenoside Rg2 also reduces 1-42 accumulation.
  • HY-Y1620
    3-(3,4-Dimethoxyphenyl)propanoic acid

    Others Cardiovascular Disease
    3-(3,4-Dimethoxyphenyl)propanoic acid is an orally active short-chain fatty acids (SCFAs). 3-(3,4-Dimethoxyphenyl)propanoic acid stimulates γ globin gene expression, erythropoiesis in vivo and is used for the β hemoglobinopathies and other anemias.
  • HY-106443A
    Arimoclomol maleate

    BRX-220

    HSP Metabolic Disease Inflammation/Immunology Neurological Disease
    Arimoclomol maleate (BRX-220) is a co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.
  • HY-121356
    Carebastine

    Histamine Receptor Cancer Endocrinology
    Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner. Carebastine suppresses the expression of macrophage migration inhibitory factor.
  • HY-136476
    Mg(II) protoporphyrin IX

    Others Others
    Mg(II) protoporphyrin IX is a precursor of chlorophyll in Chlorella. Mg(II) protoporphyrin IX is a negative effector of nuclear photosynthetic gene expression. Mg(II) protoporphyrin IX can be used for the research of signaling molecule implicated in plastid-to-nucleus communication.
  • HY-N0830
    Palmitic acid

    Endogenous Metabolite HSP Metabolic Disease Neurological Disease Cardiovascular Disease Cancer
    Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells.
  • HY-N1934
    Dihydroberberine

    Potassium Channel HSP Cancer Inflammation/Immunology Cardiovascular Disease
    Dihydroberberine inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces heat shock protein 90 (Hsp90) expression and its interaction with hERG. Dihydroberberine has anti-inflammatory, anti-atherosclerotic, hypolipidemic and antitumor activities.
  • HY-138946
    XY028-140

    CDK PROTACs Cancer
    XY028-140 is a selective CDK4/CDK6 degrader. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells.
  • HY-N0617
    Sanggenon C

    NF-κB Cancer Inflammation/Immunology Cardiovascular Disease
    Sanggenon C is a flavanone Diels-Alder adduct compound, which is isolated from the root bark of Morus cathayana. Sanggenon C exerts protective effects against cardiac hypertrophy and fibrosis via suppression of the calcineurin/NFAT2 pathway. Sanggenon C inhibits inducible nitric oxide synthase expression in RAW264.7 cells, and tumor necrosis factor-α-stimulated cell adhesion and vascular cell adhesion molecule-1 expression, by suppressing NF-κB activity. Sanggenon C possesses antioxidant, anti-inflammatory activities and inhibits Pancreatic lipase (PL) with the an IC50 of 3.00 μM.
  • HY-N6954
    Garcinone C

    ATM/ATR STAT CDK Cancer
    Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia Champ that is used as an anti-inflammatory, analgesia, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner.
  • HY-N9536
    Cinnamtannin A2

    Others Metabolic Disease
    Cinnamtannin A2, a tetrameric procyanidin, can increases GLP-1 and insulin secretion in mice. Cinnamtannin A2 could upregulate the expression of corticotrophin releasing hormone. Cinnamtannin A2 exhibits antioxidant, anti-diabetic and nephroprotective effect.
  • 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-108638
    NSC 146109 hydrochloride

    MDM-2/p53 Apoptosis Cancer
    NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and can be used for breast cancer research. NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes.
  • HY-117407
    ALLO-2

    Smo Cancer
    ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.
  • HY-N0506
    Rosarin

    Others Neurological Disease
    Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice .
  • HY-121149
    Droloxifene

    3-Hydroxytamoxifen

    Estrogen Receptor/ERR Apoptosis Cancer
    Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
  • HY-N0582
    Qingyangshengenin B

    Others Neurological Disease
    Qingyangshengenin B, a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic activity.
  • HY-106443
    Arimoclomol

    BRX-220 free base

    HSP Metabolic Disease Inflammation/Immunology Neurological Disease
    Arimoclomol (BRX-220 free base) is a co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.
  • HY-N2160
    6‴-Feruloylspinosin

    Others Neurological Disease
    6‴-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6‴-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons.
  • HY-B0230
    Phenylbutazone

    COX Inflammation/Immunology
    Phenylbutazone is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Phenylbutazone, a hepatotoxin, is a nonsteroidal anti-inflammatory drug (NSAID). Phenylbutazone induces muscle blind-like protein 1 (MBNL1) expression and has the potential for ankylosing spondylitis research.
  • HY-100226
    A-205804

    Integrin Inflammation/Immunology
    A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.
  • HY-B0360S
    Rebamipide D4

    OPC12759 D4; Proamipide D4

    COX Prostaglandin Receptor Cancer Inflammation/Immunology
    Rebamipide D4 (OPC12759 D4) is deuterium labeled Rebamipide. Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner.
  • HY-N0600
    Ginsenoside F3

    Interleukin Related IFNAR Inflammation/Immunology
    Ginsenoside F3, a component of PPTGs (an minor saponin in the leaves of Panax ginseng), has immunoenhancing activity by regulating production and gene expression of type 1 cytokines (IL-2, IFN-gamma) and type 2 cytokines (IL-4 and IL-10).
  • HY-N3584
    Paris saponin VII

    Chonglou Saponin VII

    Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Apoptosis 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-N0908
    Ginsenoside Rg5

    IGF-1R NF-κB COX Cancer Inflammation/Immunology Cardiovascular Disease Endocrinology
    Ginsenoside Rg5 is the main component of Red ginseng. Ginsenoside blocks binding of IGF-1 to its receptor with an IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
  • HY-N2454
    β-Elemonic acid

    Apoptosis Reactive Oxygen Species COX Cancer Inflammation/Immunology
    β-Elemonic acid is a triterpene isolated from Boswellia papyrifera. β-Elemonic acid induces cell apoptosis, reactive oxygen species (ROS) and COX-2 expression and inhibits prolyl endopeptidase. β-Elemonic acid exhibits anticancer and anti-inflammatory effects.
  • HY-14590
    Kaempferol

    Kempferol; Robigenin

    Estrogen Receptor/ERR Autophagy Mitophagy Apoptosis HIV Parasite Endogenous Metabolite Cancer
    Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.
  • HY-106443B
    Arimoclomol citrate

    BRX-220 citrate

    HSP Metabolic Disease Inflammation/Immunology Neurological Disease
    Arimoclomol citrate (BRX-220 citrate) is a co-inducer of heat shock proteins (HSP). Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.
  • HY-18619
    YL-109

    Aryl Hydrocarbon Receptor Cancer
    YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness.
  • HY-15066
    CNQX

    FG9065

    iGluR Neurological Disease
    CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist. CNQX blocks the expression of fear-potentiated startle in rats.
  • HY-19359
    ZED-1227

    Glutaminase Inflammation/Immunology
    ZED-1227 is a specific and orally active transglutaminase 2 (TG2) inhibitor, with an IC50 of 45 nM. ZED-1227 can block inflammation-induced TG2 expression and activity. ZED-1227 can be used for the research of celiac disease (CeD).
  • 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-P1453
    CMD178

    STAT Cancer
    CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 also is an inhibitor of STAT5 and inhibit Treg cell development.
  • HY-B1245
    Salsalate

    Salicylsalicylic acid; Disalicylic acid

    Reactive Oxygen Species Inflammation/Immunology
    Salsalate, a non-acetylated salicylate, is an effective antirheumatic drug that bypasses gastric absorption and also avoids cyclooxygenase inhibition. Salsalate has anti-inflammatory activity and reduces glucose levels, insulin resistance, and cytokine expression. Salsalate can be used in the research of type 2 diabetes.
  • HY-N6636
    Valencene

    NF-κB Inflammation/Immunology
    Valencene is a sesquiterpene isolated from Cyperus rotundus, possesses antiallergic, antimelanogenesis, anti-infammatory, and antioxidant activitivies. Valencene inhibits the exaggerated expression of Th2 chemokines and proinflammatory chemokines through blockade of the NF-κB pathway. Valencene is used to flavor foods and drinks.
  • HY-P1453A
    CMD178 TFA

    STAT Inflammation/Immunology
    CMD178 (TFA) is a lead peptide that consistently reduces the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 (TFA) also is an inhibitor of STAT5 and inhibits Tregcells development.
  • HY-N0613
    Sauchinone

    NF-κB Inflammation/Immunology
    Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity.
  • HY-128579
    DW14800

    Histone Methyltransferase Cancer
    DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
  • HY-B1000A
    L-SelenoMethionine

    Endogenous Metabolite Apoptosis Cancer
    L-SelenoMethionine, an L-isomer of Selenomethionine, is a major natural food-form of selenium. L-SelenoMethionin is a cancer chemopreventive agent that can reduce cancer incidence by dietary supplementation and induce apoptosis of cancer cells. L-SelenoMethionine also can increase expression of glutathione peroxidase.
  • HY-107222
    Lysionotin

    Others Inflammation/Immunology
    Lysionotin is a flavonoid isolated from few flower lysionotus herbs. Lysionotin efficiently inhibit α-Toxin (a pore-forming protein) expression and shows significant protection against S. aureus in vitro and in vivo. Lysionotin has the potential for the treatment of S. aureus induced pneumonia.
  • HY-136561
    GRK5-IN-2

    Others Metabolic Disease
    GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research.
  • HY-W015782
    4-Ethylresorcinol

    Others Metabolic Disease
    4-Ethylresorcinol, a derivative of resorcinol, can act as substrates of tyrosinase. 4-Ethylresorcinol possess hypopigmentary effects. 4-Ethylresorcinol attenuates mRNA and protein expression of tyrosinase-related protein (TRP)-2, and possessed antioxidative effect by inhibiting lipid peroxidation.
  • HY-100859
    LSD1-IN-5

    Histone Demethylase Cancer
    LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-126236
    3,5-Diiodothyropropionic acid

    Thyroid Hormone Receptor Cardiovascular Disease Endocrinology
    3,5-Diiodothyropropionic acid is a thyroid hormone analog, induces α-myosin heavy chain mRNA expression, binds to thyroid hormone receptor (TR), with Ka of 2.40 and 4.06 M -1 for TRα1 and TRβ1, respectively.
  • HY-100860
    LSD1-IN-6

    Histone Demethylase Cancer
    LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-107471
    CB2 receptor agonist 3

    Cannabinoid Receptor Cancer
    CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells.
  • HY-101246
    RPI-1

    RET Cancer
    RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity.
  • HY-N0577
    Apiin

    Others Inflammation/Immunology
    Apiin, a major constituent of Apium graveolens leaves with anti-inflammatory properties. Apiin shows significant inhibitory activity on nitrite (NO) production (IC50 = 0.08 mg/mL) in-vitro and iNOS expression (IC50 = 0.049 mg/ mL) in LPS-activated J774.A1 cells.
  • HY-124771
    RH01386

    Others Metabolic Disease
    RH01386 is a small molecule that can prevent ER stress-induced β cell dysfunction and death, and inhibits proapoptotic gene expression. RH01386 restores ER stress-impaired glucose-stimulated insulin secretion responses. RH01386 has the potential for type 2 diabetes treatment.
  • HY-N0781
    Linderalactone

    Apoptosis Cancer
    Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM.
  • HY-10450
    Dapagliflozin

    BMS-512148

    SGLT Metabolic Disease Cancer
    Dapagliflozin (BMS-512148), a new type of drug used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine. Dapagliflozin induces HIF1 expression and attenuates renal IR injury.
  • HY-N1346
    Robinin

    Toll-like Receptor (TLR) Inflammation/Immunology
    Robinin is present in flavonoid fraction of Vigna unguiculata leaf. Robinin inhibits upregulated expression of TLR2 and TLR4. Robinin ameliorates oxidized low density lipoprotein (Ox-LDL) induced inflammatory insult through TLR4/NF-κB pathway.
  • HY-12422
    Voruciclib

    CDK Cancer
    Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
  • 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-12422A
    Voruciclib hydrochloride

    CDK Cancer
    Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
  • HY-131723
    Pregnenolone 16α-carbonitrile

    Cytochrome P450 Metabolic Disease
    Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P4503A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults.
  • HY-139149
    NiCur

    Histone Acetyltransferase Cancer
    NiCur is a potent and selective CBP histone acetyltransferase (HAT) inhibitor with an IC50 value of 0.35 μΜ. NiCur, which blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins.
  • HY-B0167A
    Sodium Salicylate

    Salicylic acid sodium salt; 2-Hydroxybenzoic acid sodium salt

    COX NF-κB Ribosomal S6 Kinase (RSK) 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. Sodium Salicylate is also a S6K inhibitor.Sodium Salicylate is a NF-κB inhibitor that decreases inflammatory gene expression and improves repair in aged muscle.
  • HY-12185
    BRD7389

    Ribosomal S6 Kinase (RSK) Cancer Metabolic Disease
    BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells.
  • HY-107404
    SID 7969543

    Others Endocrinology
    SID 7969543 is a selective SF-1 (steroidogenic factor 1, NR5A1) inhibitor with an IC50 of 760 nM. SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 of 30 nM. SF-1 is a transcription factor belonging to the nuclear receptor superfamily.
  • HY-N0401A
    (Z)-Ligustilide

    Bacterial Infection Metabolic Disease
    (Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6. (Z)-Ligustilide inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) .
  • HY-N1356
    Reticuline

    JAK STAT NF-κB Inflammation/Immunology Cardiovascular Disease
    Reticuline shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3. Reticuline exhibits cardiovascular effects.
  • 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-125171
    IAXO-102

    Toll-like Receptor (TLR) Inflammation/Immunology
    IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.
  • HY-N2098
    Obtusifolin

    NF-κB Cancer
    Obtusifolin, isolated from the seeds of Cassia obtusifolia, regulates the gene expression and production of MUC5AC mucin in airway epithelial cells via inhibiting NF-kB pathway. Obtusifolin suppresses phthalate esters-induced breast cancer bone metastasis by targeting parathyroid hormone-related protein.
  • HY-112483
    QX77

    Autophagy Cancer
    QX77 is a chaperone-mediated autophagy (CMA) activator and upregulates LAMP2A expression in vitro. QX77 induces Rab11 upregulation, rescues Rab11 down-regulation and trafficking deficiency in cystinotic cells. QX77 can impede self-renewal and promote differentiation of ES cells.
  • HY-P1098
    Ac2-26

    NF-κB Inflammation/Immunology
    Ac2-26, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
  • HY-120878A
    (R,R)-CXCR2-IN-2

    CXCR Inflammation/Immunology
    (R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively.
  • HY-130243
    RORγt Inverse agonist 6

    ROR Inflammation/Immunology
    RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.
  • HY-139400
    FTX-6058

    Histone Methyltransferase Cardiovascular Disease
    FTX-6058 is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 can induce HbF protein expression in cell and murine models. FTX-6058 can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia.
  • HY-N0262
    Cordycepin

    3'-Deoxyadenosine

    MMP Bacterial Autophagy Antibiotic Cancer Infection Inflammation/Immunology
    Cordycepin (3'-Deoxyadenosine) is a nucleoside derivative and inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner. Cordycepin kills Mycobacterium tuberculosis through hijacking the bacterial adenosine kinase.
  • HY-13965
    Parmodulin 2

    ML161

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
  • HY-N6901
    Luteolin 7-sulfate

    Others Metabolic Disease
    Luteolin 7-sulfate is isolated from Phyllospadix iwatensis Makino, a marine plant. Luteolin 7-sulfate attenuates TYR gene expression through the intervention of a cAMP-responsive element binding protein (CREB)- and microphthalmia-associated transcription factor (MITF)-mediated signaling pathway, leading to the decreased melanin synthesis.
  • HY-15066A
    CNQX disodium

    FG9065 disodium

    iGluR Neurological Disease
    CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist. CNQX disodium blocks the expression of fear-potentiated startle in rats.
  • HY-133537
    Hygrolidin

    Antibiotic Fungal ADC Cytotoxin Cancer Infection
    Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity.
  • HY-110084
    BTZO-1

    Apoptosis Cardiovascular Disease
    BTZO-1 binds to Macrophage migration inhibitory factor (MIF) with a Kd value of 68.6 nM, and its binding requires the N-terminal Pro1. BTZO-1 can activate antioxidant response element (ARE)-mediated gene expression and suppress oxidative stress-induced cardiomyocyte apoptosis in vitro.
  • HY-139400A
    FTX-6058 hydrochloride

    Histone Methyltransferase Cardiovascular Disease
    FTX-6058 hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 hydrochloride can induce HbF protein expression in cell and murine models. FTX-6058 hydrochloride can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia.
  • HY-N5112B
    β,β-Dimethylacrylshikonin

    Isoarnebin I

    Others Cancer
    β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative isolated from Arnebia nobilis, promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway.β,β-Dimethylacrylshikonin has anti-tumor activity.
  • HY-18981
    Decursin

    (+)-Decursin

    PKC Apoptosis Cancer Inflammation/Immunology
    Decursin ((+)-Decursin) is a cytotoxic agent and a potent protein kinase C activator from the Root of Angelica gigas. Decursin inhibits tumor growth, migration, and invasion in gastric cancer by down-regulating CXCR7 expression. Decursin inhibits the growth of HepG2 cells via Hippo/YAP signaling pathway.
  • HY-17363
    Dimethyl fumarate

    DMF

    Keap1-Nrf2 Reactive Oxygen Species HIV Autophagy Endogenous Metabolite Cancer Infection Inflammation/Immunology Neurological Disease
    Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.
  • HY-112210
    Shield-1

    FKBP Others
    Shield-1 is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize the entire fusion protein.
  • HY-N2036
    Mosloflavone

    Enterovirus Bacterial Infection
    Mosloflavone is a flavonoid isolated from Scutellaria baicalensis Georgi with  anti-EV71 activity. Mosloflavone  inhibits VP2 virus replication and protein expression during the initial stage of virus infection and inhibits viral VP2 capsid protein synthesis. Mosloflavone is a promising biocide and inhibits P. aeruginosa virulence and biofilm formation.
  • HY-N2008
    Luteolin 5-O-glucoside

    NO Synthase Reactive Oxygen Species Inflammation/Immunology
    Luteolin 5-O-glucoside, a major flavonoidfrom Cirsium maackii, possesses anti-inflammatory activity. Luteolin 5-O-glucoside inhibits LPS-induced NO production and t-BHP-induced ROS generation. Luteolin 5-O-glucoside suppresses the expression of iNOS and COX-2 in macrophages.
  • HY-120395
    UC-514321

    STAT Apoptosis Cancer Inflammation/Immunology
    UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.
  • HY-N0643
    Carnosol

    Ribosomal S6 Kinase (RSK) Keap1-Nrf2 Cancer
    Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1).
  • HY-134477
    NF-κΒ activator 2

    NF-κB Neurological Disease
    NF-κΒ activator 2 is a potent and orally active NF-ҡB activator, with an EC50 of 1.58 μM. NF-κΒ activator 2 induces SOD2 through increasing NF-ҡB expression and activation. NF-κΒ activator 2 can be used for the research of amyotrophic lateral sclerosis (ALS).
  • 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-18773
    Oct3/4-inducer-1

    Oct3/4 Inflammation/Immunology
    Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer. Oct3/4-inducer-1 promotes expression and stabilization of Oct3/4, and enhances its transcriptional activity in diverse human somatic cells.
  • HY-N2609
    7,4'-Dihydroxyflavone

    CCR NF-κB Inflammation/Immunology Endocrinology
    7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid isolated from Glycyrrhiza uralensis, the eotaxin/CCL11 inhibitor, has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production. 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2. 7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM.
  • HY-N2106
    Dehydroevodiamine

    NF-κB COX PGE synthase NO Synthase Inflammation/Immunology
    Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
  • HY-B0230S
    Phenylbutazone(diphenyl-d10)

    COX Inflammation/Immunology
    Phenylbutazone-d10 (diphenyl) is the deuterium labeled Phenylbutazone. Phenylbutazone is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Phenylbutazone, a hepatotoxin, is a nonsteroidal anti-inflammatory drug (NSAID). Phenylbutazone induces muscle blind-like protein 1 (MBNL1) expression and has the potential for ankylosing spondylitis research.
  • HY-B1238S
    Pronethalol-d6

    Adrenergic Receptor Neurological Disease Cardiovascular Disease
    Pronethalol-d6 ((±)-Pronethalo-d6) is the deuterium labeled Pronethalol. Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs).
  • HY-131364
    Nur77 modulator 1

    Others Cancer
    Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity.
  • HY-120028
    GNE-207

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
  • HY-111753
    WDR5-IN-4

    Histone Methyltransferase Cancer
    WDR5-IN-4 is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
  • HY-P1098A
    Ac2-26 TFA

    NF-κB Inflammation/Immunology
    Ac2-26 TFA, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
  • HY-124069
    M-525

    Epigenetic Reader Domain Cancer
    M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity.
  • HY-B0557
    Bisacodyl

    Others Metabolic Disease
    Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.
  • HY-N6663
    3-Carene

    Others Inflammation/Immunology
    3-Carene is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene inhibits nociceptive stimulus-induced inflammatory infiltrates and COX-2 overexpression, and with antinociceptive effect. 3-Carene stimulates the activity and expression of alkaline phosphatase that is an early phase marker of osteoblastic differentiation.
  • HY-125911
    Gossypin

    NF-κB Cancer Inflammation/Immunology Cardiovascular Disease
    Gossypin is a flavone isolated from Hibiscus vitifolius and has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, analgesic and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits RANKL-induced osteoclastogenesis both in mouse primary bone marrow cells and RAW 264.7 cells in vitro.
  • HY-B0011
    Docetaxel

    RP-56976

    Microtubule/Tubulin Apoptosis Endogenous Metabolite Cancer
    Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity.
  • HY-P2048A
    MOTS-c(human) acetate

    AMPK GLUT Metabolic Disease
    MOTS-c(human) acetate is a mitochondrial-derived peptide. MOTS-c(human) acetate induces the accumulation of AMP analog AICAR, increases activation of AMPK and expression of its downstream GLUT4. MOTS-c(human) acetate induces glucose uptake and improves insulin sensitivity. MOTS-c(human) acetate has implications in the regulation of obesity, diabetes, exercise, and longevity.
  • HY-104037
    Cintirorgon

    LYC-55716

    ROR Cancer
    Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
  • 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-W010231
    β-Cyclocitral

    Others Others
    β-Cyclocitral, a volatile oxidized derivative of β-carotene, is a grazer defence signal unique to the Cyanobacterium Microcystis. β-Cyclocitral, one of the predominant volatile terpenoid compounds, can upregulate the expression of defence genes to enhance excess light (EL) acclimation. β-Cyclocitral is a powerful repellent.
  • HY-N0069
    Solamargine

    Solamargin; δ-Solanigrine

    P-glycoprotein Apoptosis Cancer
    Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity.
  • HY-N0510
    Aristolochic acid A

    Aristolochic acid I; TR 1736

    NF-κB Cancer
    Aristolochic acid A (Aristolochic acid I; TR 1736) is the main component of plant extract Aristolochic acids, which are found in various herbal plants of genus Aristolochia and Asarum. Aristolochic acid A significantly reduces both activator protein 1 (AP-1) and NF-κB activities. Aristolochic acid A reduces BLCAP gene expression in human cell lines.
  • HY-115579
    MALAT1-IN-1

    Others Cancer
    MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
  • HY-119695A
    Simvastatin acid ammonium

    Tenivastatin ammonium

    Endogenous Metabolite Cardiovascular Disease
    Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
  • HY-124418
    SBI-477

    Others Metabolic Disease
    SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain–containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
  • HY-P1131
    M617

    Neuropeptide Y Receptor Cardiovascular Disease
    M617 is a selective galanin receptor 1 (GAL1) agonist, with Kis of 0.23 and 5.71 nM for GAL1 and GAL2, respectively. M617, acting through its central GAL1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats.
  • HY-111753A
    WDR5-IN-4 TFA

    Histone Methyltransferase Cancer
    WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
  • HY-12741
    LDN-212320

    LDN-0212320; OSU-0212320

    EAAT2 Neurological Disease
    LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC[1]
  • HY-N2459
    Peonidin chloride

    YGM-6 chloride

    COX Cancer
    Peonidin chloride is an O-methylated anthocyanidin that functions as a primary plant pigment, endowing purplish-red hues to flowers such as the peony, from which it takes its name, as well as berries and vegetables. Peonidin chloride exhibits chemopreventive, as well as anti-inflammatory activities on cancer cells in vitro, blocking COX-2 expression and transformation in JB6 P+ mouse epidermal cells.
  • HY-114180
    RU.521

    RU320521

    Cyclic GMP-AMP Synthase Metabolic Disease
    RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 700 nM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).
  • HY-131179
    Influenza A virus-IN-1

    Influenza Virus Infection
    Influenza A virus-IN-1 is a dihydropyrrolidones derivative and is a potent inhibitor against wide subtypes of influenza A virus (IAV) with IC50 values from 3.11 μM to 7.13 μM. Influenza A virus-IN-1 efficiently inhibits replication of IAV, up-regulates the expression of key antiviral cytokines IFN-β and antiviral protein MxA.
  • HY-W012123
    3,4,5-Trimethoxycinnamic acid

    GABA Receptor Endogenous Metabolite Neurological Disease
    3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits.
  • HY-110258
    ML334

    LH601A

    Keap1-Nrf2 Cancer
    ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
  • HY-N0331
    Ziyuglycoside I

    MDM-2/p53 Apoptosis Cancer
    Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics. Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential drug candidate for treating triple-negative breast cancer (TNBC).
  • HY-128932
    Cefminox sodium

    MT-141

    Bacterial PPAR Prostaglandin Receptor Antibiotic Infection Cardiovascular Disease Endocrinology
    Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension.
  • HY-10254
    Mirdametinib

    PD0325901; PD325901

    MEK Autophagy Apoptosis Cancer
    Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts.
  • HY-124958
    NDMC101

    NF-κB Dipeptidyl Peptidase Metabolic Disease Inflammation/Immunology
    NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene expression. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al.
  • HY-B0185A
    Lidocaine hydrochloride

    Lignocaine hydrochloride

    Sodium Channel MEK ERK NF-κB Apoptosis Cancer Cardiovascular Disease
    Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative commonly used to anesthetize. hydrochloride is a a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
  • HY-114170
    ML604440

    Proteasome Inflammation/Immunology
    ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
  • HY-123522
    PAT-048

    Phosphodiesterase (PDE) Inflammation/Immunology
    PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. PAT-048 reduces dermal fibrosis in vivo.
  • HY-19333
    OG-L002

    Histone Demethylase Monoamine Oxidase HSV Infection
    OG-L002 is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 is a potent monoamine oxidases (MAO) inhibitor with IC50s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 potently inhibits the expression of HSV IE genes.
  • HY-N1440
    Koumine

    Others Cancer Inflammation/Immunology
    Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells. Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities, protects against the development of arthritis in Rheumatoid arthritis (RA) animal models.
  • HY-N6790
    Nonactin

    Ammonium ionophore I

    Potassium Channel Mitochondrial Metabolism Bacterial Influenza Virus Apoptosis Antibiotic Cancer Infection
    Nonactin is a naturally occurring macrotetrolide antibiotic from Streptomyces griseus. Nonactin acts as an ionophore for monovalent cations, including K +, and NH4 +. Nonactin is able to uncouple the oxidative phosphorylation (OXPHOS) of mitochondria. Nonactin selectively induces apoptosis in cell lines harboring active mutant β-catenin. Nonactin inhibits the surface expression of endogenous HSP60.
  • HY-12323
    ISX-9

    Isoxazole 9

    Calcium Channel Neurological Disease
    ISX-9 (Isoxazole 9) is a potent inducer of adult neural stem cell differentiation. ISX-9 activates Ca 2+ influx through both voltage-gated Ca 2+ channels and NMDA receptors and increases neuroD expression. ISX-9 also induces cardiomyogenic differentiation of Notch-activated epicardium-derived cells (NECs).
  • HY-112288
    C188-9

    STAT Apoptosis Cancer
    C188-9 is a STAT3 inhibitor, with a Kd of 4.7 nM. C188-9 inhibits G-CSF-induced STAT3 activation and STAT3-dependent gene expression. C188-9 induces apoptosis in AML cell lines and primary samples and inhibits colony formation by primary AML blasts.
  • HY-N4103
    Fucosterol

    PARP Endogenous Metabolite Cancer Metabolic Disease
    Fucosterol is a sterol isolated from algae, seaweed or diatoms. Fucosterol exhibits various biological activities, including antioxidant, anti-adipogenic, blood cholesterol reducing, anti-diabetic and anti-cancer activities. Fucosterol regulates adipogenesis via inhibition of PPARα and C/EBPα expression and can be used for anti-obesity agents development research.
  • HY-101872A
    GSK-872 hydrochloride

    RIP kinase Inflammation/Immunology
    GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
  • HY-B0185
    Lidocaine

    Lignocaine

    Sodium Channel MEK ERK NF-κB Apoptosis Cancer Cardiovascular Disease
    Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative commonly used to anesthetize. Lidocaine is a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
  • HY-18669
    ML346

    HSP Cancer
    ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 induces specific increases in genes and protein effectors of the heat shock response (HSR), including chaperones such as Hsp70, Hsp40, and Hsp27.
  • HY-13425
    Deguelin

    (-)-Deguelin; (-)-cis-Deguelin

    Akt Autophagy Apoptosis Cancer
    Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.
  • HY-N0074
    Byakangelicol

    COX Inflammation/Immunology
    Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory drug on airway inflammation.
  • HY-B0011A
    Docetaxel Trihydrate

    RP-56976 Trihydrate

    Microtubule/Tubulin Apoptosis Cancer
    Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis.
  • HY-N0801
    Polygalacic acid

    MMP AChE Inflammation/Immunology Neurological Disease
    Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment . Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex.
  • HY-101872
    GSK-872

    RIP kinase Inflammation/Immunology
    GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
  • HY-N0603
    20(S)-Ginsenoside Rg3

    20(S)-Propanaxadiol; S-ginsenoside Rg3

    Sodium Channel Potassium Channel NF-κB COX Amyloid-β Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    20(S)-Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na + and hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits levels, NF-κB activity, and COX-2 expression.
  • HY-110266
    GN44028

    HIF/HIF Prolyl-Hydroxylase Cancer
    GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.
  • HY-16291
    APTO-253

    LOR-253; LT-253

    c-Myc KLF Apoptosis Cancer Inflammation/Immunology
    APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor. APTO-253 has antiarthritic activity.
  • 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-α 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-N2007
    Veratric acid

    3,4-Dimethoxybenzoic acid

    COX Reactive Oxygen Species Inflammation/Immunology Cardiovascular Disease
    Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant and anti-inflammatory activities. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.
  • HY-134923
    CA77.1

    Autophagy Neurological Disease
    CA77.1 is a potent, brain-penetrant and orally active chaperone-mediated autophagy (CMA) activator with favorable pharmacokinetics. CA77.1 is a derivative of AR7 (HY-101106) and can increase the expression of the lysosomal receptor LAMP2A in lysosomes. CA77.1 improves behavior and neuropathology in PS19 mice model and can be used for alzheimer's disease research.
  • HY-129601
    MYCi975

    NUCC-0200975

    c-Myc Cancer Inflammation/Immunology
    MYCi975 (NUCC-0200975) is an orally active MYC inhibitor, which disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 (NUCC-0200975) exhibits potent anti-tumor efficacy with good tolerability, increases tumor immune cell infiltration, and sensitizes tumors to anti-PD1 immunotherapy.
  • HY-10496
    SC75741

    NF-κB Influenza Virus Infection Cancer
    SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65. SC75741 blocks influenza viruses (IV) replication. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins.
  • HY-16560
    Camptothecin

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

    Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic Cancer Infection
    Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
  • HY-N7118
    Clindamycin hydrochloride monohydrate

    Bacterial Antibiotic Infection
    Clindamycin hydrochloride monohydrate is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin hydrochloride monohydrate resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin hydrochloride monohydrate decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla).
  • HY-127090
    Muramyl dipeptide

    MDP

    p38 MAPK ERK JNK Inflammation/Immunology
    Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. Muramyl dipeptide is an inducer of bone formation through induction of Runx2. Muramyl dipeptide directly enhances osteoblast differentiation by up-regulating Runx2 gene expression through MAPK pathways. Muramyl dipeptide indirectly attenuates osteoclast differentiation through a decreased RANKL/OPG ratio.
  • HY-P3245
    HXR9

    Apoptosis Cancer
    HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells.
  • HY-N6022
    Byakangelicin

    Others Metabolic Disease
    Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.
  • HY-114936
    Piericidin A

    AR-054

    Bacterial ADC Cytotoxin Antibiotic Mitochondrial Metabolism Cancer Infection Neurological Disease
    Piericidin A (AR-054) is a natural mitochondrial NADH-ubiquinone oxidoreductase (complex I) inhibitor. Piericidin A is a potent neurotoxin and inhibits mitochondrial respiration by disrupting the electron transport system through its action on NADH-ubiquinone reductase. Piericidin A is also a potential quorum-sensing inhibitor that suppresses the expression of the virulence genes of Erwinia carotovora subsp. atroseptica (Eca). Piericidin A is an ADC cytotoxin and has anti-bacterial, anticancer, insecticidal activity.
  • HY-113618A
    RO2959 hydrochloride

    CRAC Channel Interleukin Related Cardiovascular Disease
    RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
  • HY-N0265
    Asperosaponin VI

    Caspase Apoptosis Cardiovascular Disease
    Asperosaponin VI, A saponin component from Dipsacus asper wall, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway. Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB.
  • 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-B1455
    Clindamycin

    Bacterial Antibiotic Infection
    Clindamycin is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla).
  • HY-N4126
    6-Demethoxytangeretin

    ALK Cancer Inflammation/Immunology Neurological Disease
    6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus depressa. 6-Demethoxytangeretin exerts anti-inflammatory activity and anti-allergic activity, suppresses production and gene expression of interleukin-6 in human mast cell-1 via anaplastic lymphoma kinase (ALK) and mitogen-activated protein kinase (MAPK) pathways. 6-Demethoxytangeretin facilitates the CRE-mediated transcription associated with learning and memory in cultured hippocampal neurons.
  • HY-13518
    Piceatannol

    Astringenin; trans-Piceatannol

    Syk Autophagy Apoptosis Cancer
    Piceatannol is a well-known Syk inhibitor and reduces the expression of iNOS induced by TNF. Piceatannol is an effective agent for research of acute lung injury (ALI). Piceatannol is a naturally occurring polyphenolic stilbene found in various fruits and vegetables and exhibits anticancer and anti-inflammatory properties. Piceatannol induces apoptosis in DLBCL cell lines. Piceatannol induces autophagy and apoptosis in MOLT-4 human leukemia cells.
  • HY-129611
    Bromelain

    Apoptosis Cancer Inflammation/Immunology
    Bromelain is an anti-inflammatory drug derived from pineapple stem that acts through down-regulation of plasma kininogen, inhibition of Prostaglandin E2 expression, degradation of advanced glycation end product receptors and regulation of angiogenic biomarkers as well as antioxidant action upstream in the COX-pathway. Bromelain exhibits various fibrinolytic, antiedematous, antithrombotic, and anti-inflammatory activities. Bromelain also possesses some anticancerous activities and promotes apoptotic cell death.
  • HY-111520
    NVS-SM2

    DNA/RNA Synthesis Neurological Disease
    NVS-SM2 is a potent, orally active and brain-penetrant SMN2 splicing enhancer with an EC50 of 2 nM for SMN. NVS-SM2 enhances U1-pre-mRNA association. NVS-SM2 promotes exon 7 inclusion and restores normal survival motor neuron (SMN) protein expression. NVS-SM2 can be used for spinal muscular atrophy (SMA) research.
  • 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-N0407
    Picroside I

    6'-Cinnamoylcatalpol

    STAT Inflammation/Immunology
    Picroside I is the major ingredient of Picrorhiza kurroa. Picrorhiza kurroa is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II. Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ.
  • HY-15614A
    SC144 hydrochloride

    Interleukin Related Apoptosis Cancer
    SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells.
  • HY-135646
    Eleutheroside B1

    Influenza Virus Infection Inflammation/Immunology
    Eleutheroside B1, a coumarin compound, has a wide spectrum of anti-human influenza virus efficacy, with an IC50 value of 64-125 µg/ml. Eleutheroside B1 mediates its anti-influenza activity through POLR2A and N-glycosylation. Eleutheroside B1 inhibits the mRNA expression of several chemokine genes and the influenza nucleoprotein (NP) gene, and exhibits low cytotoxicity. Antiviral and anti-inflammatory activities.
  • HY-135794
    11-Ketodihydrotestosterone

    11-KDHT; 5α-Dihydro-11-keto testosterone

    Androgen Receptor Endocrinology
    11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
  • HY-15614
    SC144

    Interleukin Related Apoptosis Cancer
    SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells.
  • HY-128598
    MD2-TLR4-IN-1

    Toll-like Receptor (TLR) Cancer Inflammation/Immunology
    MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
  • HY-N0674A
    Dehydrocorydaline chloride

    13-Methylpalmatine chloride

    Bcl-2 Family Caspase PARP p38 MAPK Parasite Autophagy Cancer Infection
    Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline chloride shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
  • HY-115461
    MID-1

    Insulin Receptor Metabolic Disease
    MID-1 is a disruptor of MG53-IRS-1 (Mitsugumin 53-insulin receptor substrate-1) interaction. MID-1 disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1 expression level and increased insulin signaling and glucose uptake.
  • HY-N0385
    Gomisin J

    AMPK Calcium Channel Metabolic Disease Cardiovascular Disease
    Gomisin J is a small molecular weight lignan found in Schisandra chinensis and has been demonstrated to have vasodilatory activity. Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca 2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells. gomisin J has potential benefits in treating nonalcoholic fatty liver disease.
  • HY-112780
    UC2288

    MDM-2/p53 Cancer
    UC2288 is a novel, cell-permeable, and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 decreases p21 mRNA expression independently of p53, and attenuates p21 protein levels with minimal effect on p21 protein stability. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM.
  • HY-130851
    HS-27

    HSP Cancer
    HS-27, a fluorescently-tethered Hsp90 inhibitor, assays surface Hsp90 expression on intact tissue specimens. HS-27 is made up of the core elements of SNX-5422, an Hsp90 inhibitor, tethered via a PEG linker to a fluorescein derivative (fluorescein isothiocyanate or FITC), that binds to ectopically expressed Hsp90. HS-27 has potential use in a see-and-treat paradigm in breast cancer.
  • 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-124745
    KY-05009

    MAP4K Wnt Apoptosis Cancer
    KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.
  • HY-W018643
    Ferulic acid methyl ester

    Methyl ferulate

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease Cancer
    Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties. Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders. Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages.
  • HY-115463
    EB-3D

    AMPK Apoptosis Cancer
    EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
  • HY-113618B
    RO2959 monohydrochloride

    CRAC Channel Interleukin Related Cardiovascular Disease
    RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
  • HY-N2557
    Euphorbia Factor L1

    Apoptosis Cancer Cardiovascular Disease
    Euphorbia Factor L1 is a diterpenoid from Euphorbia lathyris L., reduces the expression of Bcl-2, PI3K, AKT and mTOR protein and mRNA, upregulates cleaved caspase-9 and caspase-3 levels, buts shows no effect on pro-caspase-9 and pro-caspase-3. Euphorbia Factor L1 induces apoptosis, has anticancer, antiadipogenesis, antiosteoclastogenesis and multidrug resistance-modulating effect.
  • HY-N1511
    Ganoderic acid D

    Sirtuin Apoptosis Cancer
    Ganoderic acid D, a highly oxygenated tetracyclic triterpenoid, is the major active component of Ganoderma lucidum. Ganoderic acid D upregulates the protein expression of SIRT3 and induces the deacetylated cyclophilin D (CypD) by SIRT3. Ganoderic acid D inhibits the energy reprogramming of colon cancer cells including glucose uptake, lactate production, pyruvate and acetyl-coenzyme production in colon cancer cells. Ganoderic acid D induces HeLa human cervical carcinoma apoptosis.
  • HY-N0619
    Mulberroside A

    TNF Receptor Interleukin Related Tyrosinase Inflammation/Immunology
    Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
  • 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-B0185AS
    Lidocaine-d10 hydrochloride

    Sodium Channel MEK ERK NF-κB Apoptosis Cancer Cardiovascular Disease
    Lidocaine-d10 (Lignocaine-d10) hydrochloride is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative commonly used to anesthetize. hydrochloride is a a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
  • HY-N0551
    Wedelolactone

    Caspase Lipoxygenase Apoptosis Cancer Inflammation/Immunology
    Wedelolactone, a natural product from Ecliptae herba, suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK Complex. Wedelolactone inhibits 5-lipoxygenase (5-Lox) (IC50~2.5 μM) activity by an oxygen radical scavenging mechanism. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Anti-cancer, anti-inflammatory, and antioxidant activities.
  • HY-N4238
    Dehydrocorydaline nitrate

    13-Methylpalmatine nitrate

    Bcl-2 Family Caspase PARP p38 MAPK Parasite Autophagy Cancer Infection
    Dehydrocorydaline nitrate (13-Methylpalmatine nitrate) is an alkaloid. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline nitrate elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline nitrate shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
  • HY-N1942
    5-O-Demethylnobiletin

    5-Demethylnobiletin

    Lipoxygenase Leukotriene Receptor Inflammation/Immunology Neurological Disease Cancer
    5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Sideritis tragoriganum, is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM.
  • HY-122653
    CCT367766

    PROTACs Cancer
    CCT367766 is a potent and the third generation heterobifunctional and PROTAC-based pirin targeting protein degradation probe (PDP), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein.
  • HY-N2118
    Bilobetin

    PPAR PKA Metabolic Disease
    Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
  • HY-128850
    N-Acetyl-D-mannosamine

    N-Acetylmannosamine; ManNAc

    Bacterial Neurological Disease
    N-Acetyl-D-mannosamine (ManNAc) is an essential precursor of N-acetylneuraminic acid (NeuAc), the specific monomer of bacterial capsular polysialic acid (PA). N-Acetyl-D-mannosamine (ManNAc) can be metabolized by GNE and GlcNAc 2-epimerase (Renin binding protein, RnBP), into ManNAc-6-phosphate and GlcNAc, respectively.  N-Acetyl-d-mannosamine (ManNAc) and its derivatives activates hypocretin (HCRT) gene expression in the orexin neurons, providing a potential model for the testing of a therapy for neural disorders.
  • HY-N0674
    Dehydrocorydaline

    13-Methylpalmatine

    Bcl-2 Family Caspase PARP p38 MAPK Parasite Autophagy Cancer Infection
    Dehydrocorydaline (13-Methylpalmatine) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
  • HY-108672
    NF157

    P2Y Receptor Inflammation/Immunology
    NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).
  • HY-114421
    FKBP12 PROTAC dTAG-13

    dTAG-13

    PROTACs FKBP Epigenetic Reader Domain Cancer
    FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader. FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
  • HY-W063968
    RO8191

    CDM-3008; RO4948191

    IFNAR JAK STAT HCV HBV Infection
    RO8191 (CDM-3008), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 directly binds to IFNα/β receptor 2 (IFNAR2) and activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon. RO8191 is a cccDNA modulator (CDM) through interferon-like activity and has anti-HBV activity.
  • HY-137443
    Ipivivint

    CDK Wnt Cancer
    Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer.
  • HY-10450A
    Dapagliflozin ((2S)-1,2-propanediol, hydrate)

    BMS-512148 (2S)-1,2-propanediol, hydrate

    SGLT Cancer Metabolic Disease
    Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of drug used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine. Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury.
  • HY-N0811
    Anemarsaponin B

    NO Synthase COX NF-κB MEK Inflammation/Immunology
    Anemarsaponin B is a steroidal saponin. Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
  • 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-N2187
    Deoxyshikonin

    Bacterial HIF/HIF Prolyl-Hydroxylase Cancer Infection Cardiovascular Disease
    Deoxyshikonin is isolated from Lithospermum erythrorhizon Sieb with antitumor activity. Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF, indicates a prolymphangiogenesis as well as a proangiogenesis effect in vitro. Deoxyshikonin shows significant synergic antimicrobial activity against S. pneumonia (MIC=17 μg/mL), also shows significantly inhibitory activities against MRSA.
  • HY-128851
    Coenzyme A

    Endogenous Metabolite Cancer Neurological Disease
    Coenzyme A is is an obligatory cofactor in all living cells synthesised from pantothenate (Vitamin B5), adenosine triphosphate (ATP) and cysteine. Covalent binding of Coenzyme A to Peroxiredoxin 5 (Prdx5) results in complete inhibition of its peroxidase activity, which is reversed by reduction with DTT.Coenzyme A and its thioester derivatives are key players in major catabolic and anabolic pathways and the regulation of gene expression. Many human pathologies, including cancer, diabetes and neurodegeneration, have been associated with abnormal biosynthesis and homeostasis of CoA and its derivatives.
  • HY-N0619A
    cis-Mulberroside A

    Mulberroside D

    TNF Receptor Interleukin Related Tyrosinase Inflammation/Immunology
    cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
  • HY-N2503
    Ginsenoside F4

    Apoptosis MMP Inflammation/Immunology
    Ginsenoside F4 (GF4), ginseng saponinis, isolated from notoginseng or red ginseng. Ginsenoside F4 (GF4) has inhibitory effect on human lymphocytoma JK cell by inducing its apoptosis. Ginsenoside F4 (GF4) inhibits matrix metalloproteinase 13 (MMP 13) expression in IL-1β-treated chondrocytes and blocks cartilage breakdown in rabbit cartilage tissue culture, shows therapeutic potential for preventing cartilage collagen matrix breakdown in diseased tissues.
  • HY-123941
    FKBP12 PROTAC dTAG-7

    dTAG-7

    PROTACs FKBP Epigenetic Reader Domain Cancer
    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
  • HY-123931
    ZLDI-8

    Notch Phosphatase Apoptosis Cancer
    ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
  • HY-100574A
    Cl-amidine hydrochloride

    Protein Arginine Deiminase Apoptosis MicroRNA Cancer Inflammation/Immunology
    Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
  • HY-N6791
    KT5823

    PKA PKC Bacterial Apoptosis Antibiotic Infection Inflammation/Immunology
    KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
  • HY-100574
    Cl-amidine

    Protein Arginine Deiminase Apoptosis MicroRNA Cancer Inflammation/Immunology
    Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
  • HY-N1445
    Isoquercetin

    Quercetin 3-glucoside

    NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway. Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies.
  • HY-P2657
    Verucopeptin

    HIF/HIF Prolyl-Hydroxylase Proton Pump Endogenous Metabolite Cancer
    Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
  • HY-17504A
    Rosuvastatin

    ZD 4522

    HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Metabolic Disease Cardiovascular Disease
    Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
  • HY-106353
    Smilagenin

    Endogenous Metabolite mAChR Neurological Disease
    Smilagenin (SMI) is a small-molecule steroidal sapogenin from Rhizoma anemarrhenae and Radix asparagi widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases. Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density. Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD.
  • HY-104040
    MKC8866

    IRE1 Cancer
    MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.
  • HY-114504
    RVX-297

    Epigenetic Reader Domain Inflammation/Immunology
    RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
  • HY-120878
    CXCR2-IN-2

    CXCR Inflammation/Immunology
    CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
  • HY-17504
    Rosuvastatin Calcium

    Rosuvastatin hemicalcium; ZD 4522 Calcium

    HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Metabolic Disease Cardiovascular Disease
    Rosuvastatin Calcium (Rosuvastatin hemicalcium) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
  • HY-17504C
    (3R,5R)-Rosuvastatin

    HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Metabolic Disease Cardiovascular Disease
    (3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
  • HY-17504D
    (3S,5R)-Rosuvastatin

    HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Metabolic Disease Cardiovascular Disease
    (3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
  • HY-100574B
    Cl-amidine TFA

    Protein Arginine Deiminase Apoptosis MicroRNA Cancer Inflammation/Immunology
    Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
  • HY-N2038
    3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone

    Others Cancer Neurological Disease
    3,5,6,7,8,3',4'-heptamethoxyflavone, a flavonoid in C. unshiu peels, exhibits anti-tumor-initiating effect and Anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-heptamethoxyflavone inhibits collagenase activity and increased type I procollagen content in HDFn cells. 3,5,6,7,8,3',4'-heptamethoxyflavone induces brain-derived neurotrophic factor (BDNF) expression via cAMP/ERK/CREB signaling and reduces phosphodiesterase activity in C6 cells.
  • HY-13453
    BAY 11-7082

    BAY 11-7821

    IKK Deubiquitinase Autophagy Apoptosis Cancer Inflammation/Immunology
    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
  • HY-N0515
    Ophiopogonin D

    PPAR NF-κB Calcium Channel Inflammation/Immunology Cardiovascular Disease
    Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
  • HY-N0043
    Ginsenoside Rd

    Gypenoside VIII

    NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease Cancer
    Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
  • HY-101257B
    YKL-5-124 TFA

    CDK Cancer
    YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-101257
    YKL-5-124

    CDK Cancer
    YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-10624
    THIQ

    Melanocortin Receptor Metabolic Disease
    THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants.
  • HY-112544
    IK1 inhibitor PA-6

    PA-6

    Potassium Channel Cardiovascular Disease
    IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia.
  • HY-N7012
    7,3',4'-Tri-O-methylluteolin

    5-Hydroxy-3',4',7-trimethoxyflavone

    TNF Receptor Interleukin Related COX Cancer Metabolic Disease Inflammation/Immunology
    7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid from the herb Lippia nodiflora L. (Verbenaceae) which has been documented to exhibit anti-inflammatory, antipyretic, antitussive, antidiabetic, anticancer, and antimelanogenesis properties. 7,3',4'-Tri-O-methylluteolin obviously reduces the prodn of pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-1β in a concentration-dependent manner. 7,3',4'-Tri-O-methylluteolin significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2, representing that inhibition occurs at the transcriptional level.
  • HY-103241
    Ro 90-7501

    Amyloid-β ATM/ATR Phosphatase Apoptosis Cancer Neurological Disease
    Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces 42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
  • HY-P1110
    AF12198

    Interleukin Related Inflammation/Immunology
    AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo.
  • HY-122578
    P53R3

    MDM-2/p53 Cancer
    P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53 R175H, p53 R248W and p53 R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53 M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research.