1. Search Result

Search Result

Pathways Recommended: Stem Cell/Wnt
Targets Recommended: Wnt

Results for "Ar wnt Inhibitors" in MCE Product Catalog:

207

Inhibitors & Agonists

4

Screening Libraries

8

Peptides

25

Natural
Products

2

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-N6703
    ar-Turmerone

    (+)-Ar-Turmerone

    Apoptosis Cancer Inflammation/Immunology
    ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities. ar-turmerone ((+)-ar-Turmerone) activates apoptotic protein in human lymphoma U937 cells. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation and constitutes a promising therapeutic agent for various neurologic disorders.
  • HY-15564
    AR 231453

    GPR119 Metabolic Disease
    AR 231453 is a potent, selective and orally available GPR119 agonist.
  • HY-U00371
    AR-08

    Adrenergic Receptor Neurological Disease Endocrinology
    AR-​08 is an agonist of α2-adrenergic receptor, used for the treatment of attention deficit hyperactivety disorder (ADHD).
  • HY-12798C
    AR-13324 M1 metabolite

    Others Others
    AR-13324 M1 metabolite is a hydrolysis metabolite of AR-13324 mesylate.
  • HY-133127
    AR453588

    Glucokinase Metabolic Disease
    AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity.
  • HY-16758
    Verosudil

    Ar-12286

    ROCK Neurological Disease
    Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. AR-12286 lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork.
  • HY-101106
    AR7

    RAR/RXR Autophagy Neurological Disease
    AR7 is a retinoic acid receptor α (RARα) antagonist.
  • HY-136073
    Wnt pathway activator 2

    Wnt Cancer
    Wnt pathway activator 2 is a potent Wnt activator extracted from patent WO2012024404A1, compound 2, has an IC50s of 13 nM.
  • HY-114321
    Wnt/β-catenin agonist 1

    Wnt Cancer
    Wnt/β-catenin agonist 1 (compound 3f) is a Wnt/β-catenin signalling pathway agonist, with an EC50 of 0.27 μM.
  • HY-135516
    Wnt pathway activator 1

    Wnt Cancer
    Wnt pathway activator 1 is a potent Wnt activator extracted from patent WO2012024404A1, compound 1, has an IC50s of 28-29 nM.
  • HY-17545
    LGK974

    wnt974

    Porcupine Cancer
    LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM.
  • HY-10512
    AR-A014418

    Ar 0133418; GSK 3β inhibitor VIII; Ar 014418

    GSK-3 Metabolic Disease Cancer
    AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor with an IC50 of 104 nM。
  • HY-133127A
    AR453588 hydrochloride

    Glucokinase Metabolic Disease
    AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity.
  • HY-15659
    Wnt-C59

    C59

    Porcupine Wnt Cancer
    Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
  • HY-111848
    PROTAC AR Degrader-4

    SNIPER PROTAC Androgen Receptor Cancer
    PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
  • HY-120006A
    (rel)-AR234960

    ERK Cardiovascular Disease
    (rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
  • HY-18776
    A2AR-agonist-1

    Adenosine Receptor Neurological Disease
    A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.39 and 3.47 for A2AR and ENT1.
  • HY-U00391
    β3-AR agonist 2

    Adrenergic Receptor Metabolic Disease Endocrinology
    β3-AR agonist 2 is a potent and selective β3-adrenergic receptor (β3-AR) agonist with an EC50 of 8 nM.
  • HY-101039A
    AR-M 1000390 hydrochloride

    Opioid Receptor Neurological Disease
    AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
  • HY-B1114
    Gliquidone

    Ar-DF 26

    Others Metabolic Disease
    Gliquidone (AR-DF 26) is an anti-diabetic drug in the sulfonylurea class, used in the treatment of diabetes mellitus type 2.
  • HY-12122A
    AR-C102222 hydrochloride

    NO Synthase Inflammation/Immunology Neurological Disease
    AR-C102222 hydrochloride is a potent, competitive, orally active and highly selective inducible nitric oxide synthase (iNOS) inhibitor, with an IC50 of 37 nM. AR-C102222 hydrochloride has antinociception and anti-inflammatory activities.
  • HY-13248
    AR-C155858

    Monocarboxylate Transporter Others
    AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Kis of 2.3 nM and 10 nM, respectively.
  • HY-130845
    AR antagonist 1

    Ligand for E3 Ligase Cancer
    AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
  • HY-107018
    AR-A 2

    Ar-A 000002

    5-HT Receptor Neurological Disease
    AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
  • HY-111151
    AR-9281

    APAU

    Epoxide Hydrolase Metabolic Disease
    AR9281 is a potent and selective inhibitor of soluble epoxide hydrolase (s-EH), with potential for the treatment of hypertension and type 2 diabetes.
  • HY-101854
    N6-(2-Phenylethyl)adenosine

    N6-Phenethyladenosine; N6-Phenylethyladenosine

    Adenosine Receptor Cancer Inflammation/Immunology
    N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine), an adenosine derivative, is a potent adenosine receptors (AR) agonist with Ki values of 11.8 nM, 30.1 nM, 0.63 nM for rat A1AR, human A1AR and hA3AR, respectively.
  • HY-119996A
    AR-C141990 hydrochloride

    Monocarboxylate Transporter Inflammation/Immunology
    AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pKi values of 7.6, 6.6 for MCT-1 and MCT-2, respectively. AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response.
  • HY-101514
    β3-AR agonist 1

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).
  • HY-114936
    Piericidin A

    Ar-054

    Bacterial ADC Cytotoxin Antibiotic 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-P1454A
    Fz7-21 TFA

    Ac-LPSDDLEFWCHVMY-NH2 TFA

    Wnt Cancer
    Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA , a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
  • HY-P1454
    Fz7-21

    Ac-LPSDDLEFWCHVMY-NH2

    Wnt Cancer
    Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2), a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
  • HY-70002
    Enzalutamide

    MDV3100

    Androgen Receptor Autophagy Cancer
    Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-N2907
    Atranorin

    Ras Endogenous Metabolite Cancer
    Atranorin is a lichen secondary metabolite. Atranorin inhibits lung cancer cell motility and tumorigenesis by affecting AP-1, Wnt, and STAT signaling and suppressing RhoGTPase activity.
  • HY-136242
    UT-34

    Androgen Receptor Cancer Endocrinology
    UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy.
  • HY-18959
    CWP232228

    β-catenin Wnt Cancer
    CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
  • HY-15746
    Dobutamine hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion.
  • HY-108642B
    AMG-548 dihydrochloride

    p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
  • HY-108642
    AMG-548

    p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
  • HY-108642A
    AMG-548 hydrochloride

    p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
  • 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-14300A
    Vilanterol trifenatate

    GW642444 trifenatate

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Vilanterol trifenatate (GW642444 trifenatate) is a long-acting β2-adrenoceptor 2-AR) agonist with inherent 24-hour activity. The pEC50s for β2-AR, β1-AR and β3-AR are 10.37, 6.98 and 7.36, respectively.
  • HY-B1866
    Linuron

    Androgen Receptor Endocrinology
    Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor.
  • HY-14300
    Vilanterol

    GW642444

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Vilanterol (GW642444) is a long-acting β2-adrenoceptor 2-AR) agonist with 24 h activity. The pEC50s for β2-AR,β1-AR and β3-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.
  • HY-P1416
    Foxy-5

    Wnt Cancer
    Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
  • HY-P1416A
    Foxy-5 TFA

    Wnt Cancer
    Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
  • HY-N1943
    Ailanthone

    Δ13-DehydrochapArrinone

    Androgen Receptor Cancer Inflammation/Immunology
    Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
  • HY-19334
    L755507

    Adrenergic Receptor CRISPR/Cas9 Cancer Endocrinology
    L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM.
  • HY-101986
    BIIE-0246

    Ar-H 053591

    Neuropeptide Y Receptor Metabolic Disease Endocrinology
    BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 of 15 nM.
  • HY-17439
    Salinomycin sodium salt

    Salinomycin sodium; Sodium salinomycin

    Wnt β-catenin Bacterial Autophagy Apoptosis Antibiotic Cancer
    Salinomycin sodium salt (Salinomycin sodium), an antibiotic potassium ionophore, is a potent inhibitor of Wnt/β-catenin signaling. Salinomycin sodium salt (Salinomycin sodium) acts on the Wnt/Fzd/LRP complex, blocks Wnt-induced LRP6 phosphorylation, and causes degradation of the LRP6 protein. Salinomycin sodium salt (Salinomycin sodium) shows selective activity against human cancer stem cells.
  • HY-12111
    BMS-564929

    Androgen Receptor Endocrinology
    BMS-564929 is an androgen receptor (AR) agonist, binds to androgen receptor (AR) with a Ki of 2.11±0.16 nM.
  • HY-B1016
    Trapidil

    Ar-12008

    PDGFR Cardiovascular Disease Cancer
    Trapidil is a vasodilator, is an antiplatelet drug with specific platelet-derived growth factor.
  • HY-101479
    Iclaprim

    Ar-100

    Bacterial Infection
    Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
  • HY-122816
    HLY78

    Wnt Cancer Neurological Disease
    HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction.
  • HY-15314
    Ranirestat

    AS-3201

    Aldose Reductase Metabolic Disease Neurological Disease
    Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC50s of 11 nM and 15 nM for rat lens AR and recombinant human AR, respectively, and a Ki of 0.38 nM for recombinant human AR. Ranirestat has the potential for diabetic sensorimotor polyneuropathy treatment. Ranirestat also has a neuroprotective effect on diabetic retinas.
  • HY-112895
    UT-155

    Androgen Receptor Cancer
    UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
  • HY-B0659
    Brimonidine

    UK 14304; AGN190342

    Adrenergic Receptor Endocrinology
    Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
  • HY-120675
    SSTC3

    Casein Kinase Wnt Cancer
    SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
  • HY-16060
    Apalutamide

    ArN-509

    Androgen Receptor Cancer
    Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
  • HY-15721
    FH535

    PPAR Wnt β-catenin Cancer
    FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.
  • HY-103705
    iCRT3

    Wnt Apoptosis Cancer
    iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.
  • HY-12879
    IWP-4

    Wnt Cancer
    IWP-4 is a small molecule Wnt inhibitor with an IC50 of 25 nM.
  • HY-B0659A
    Brimonidine tartrate

    UK 14304 tArtrate; AGN190342 tArtrate

    Adrenergic Receptor Endocrinology
    Brimonidine tartrate (UK 14304 tartrate) is a full α2-adrenergic receptor (α2-AR) agonist.
  • HY-19987
    BML-284

    Wnt Cancer
    BML-284 is selective and cell-permeable Wnt signaling activator.
  • HY-12238
    IWR-1

    endo-IWR 1; IWR-1-endo

    Wnt Cancer
    IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
  • HY-A0293
    Pyrvinium pamoate

    Pyrvinium embonate

    Wnt Cancer
    Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.
  • HY-136596
    Apalutamide-COOH

    Others Cancer
    Apalutamide-COOH can be used to synthesis Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-123875A
    Ralaniten triacetate

    EPI-506

    Androgen Receptor Cancer
    Ralaniten triacetate (EPI-506), the pro-drug of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7.
  • HY-17453
    Salmeterol xinafoate

    GR 33343X xinafoate

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Salmeterol xinafoate is a long-acting beta-2 adrenergic receptor (β2AR) agonist, with Ki of 1.5 nM for WT β2AR, and used for asthma treatment.
  • HY-100408
    GNF-6231

    Porcupine Cancer
    GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.
  • HY-101090
    KYA1797K

    Wnt β-catenin Cancer
    KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.
  • HY-101275
    EMT inhibitor-1

    Hippo (MST) TGF-beta/Smad Wnt Cancer
    EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
  • HY-19739
    JW74

    Wnt Cancer
    JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.
  • HY-130992
    Androgen receptor antagonist 1

    Androgen Receptor Ligand for Target Protein for PROTAC Cancer
    Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
  • HY-N4089
    Quercetin 3-gentiobioside

    Aldose Reductase Metabolic Disease
    Quercetin 3-gentiobioside is isolated from A. iwayomogi, AR and AGE formation inhibitor, demonstrates biological activities against Aldose reductase (AR) and the formation of advanced glycation endproducts (AGEs).
  • HY-130492
    ARCC-4

    PROTAC Androgen Receptor Cancer
    ARCC-4 is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.
  • HY-133020
    ARD-266

    PROTAC Androgen Receptor Cancer
    ARD-266 is a a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
  • HY-15597
    Salinomycin

    Procoxacin

    Bacterial Wnt β-catenin Mitophagy Autophagy Apoptosis Antibiotic Cancer
    Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin (Procoxacin) shows selective activity against human cancer stem cells.
  • HY-111809
    N6-Ethyladenosine

    Adenosine Receptor Others
    N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively.
  • HY-16060S
    Apalutamide D4

    ArN-509 D4

    Androgen Receptor Cancer
    Apalutamide D4 (ARN-509 D4) is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
  • HY-101300
    Cirazoline hydrochloride

    LD 3098 hydrochloride

    Adenosine Receptor Neurological Disease
    Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM).
  • HY-103184
    Proxalutamide

    GT0918

    Androgen Receptor Cancer
    Proxalutamide (GT0918) is a potent androgen receptor (AR) antagonist.
  • HY-10590
    TWS119

    GSK-3 Autophagy Neurological Disease Cancer
    TWS119 is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
  • HY-12292
    IM-12

    GSK-3 Cancer
    IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.
  • HY-13236
    LUF6000

    Adenosine Receptor Cardiovascular Disease
    LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR).
  • HY-U00244
    Benzquinamide

    P2647; BZQ; Benzoquinamide

    Adrenergic Receptor Metabolic Disease Endocrinology
    Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively.
  • HY-100853
    IWP-O1

    Porcupine Wnt Cancer
    IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells. IWP-O1 prevents the secretion of Wnt proteins. IWP-O1 suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-U00205
    Dopexamine hydrochloride

    FPL60278Ar

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Dopexamine hydrochloride is a β2 adrenergic receptor agonist.
  • HY-15758
    3,3'-Diindolylmethane

    DIM; Arundine; HB 236

    Androgen Receptor Autophagy Cancer
    3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.
  • HY-10122
    Silodosin

    KAD 3213; KMD 3213

    Adrenergic Receptor Cancer Endocrinology
    Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.
  • HY-101130
    PNU-74654

    Wnt β-catenin Apoptosis Cancer
    PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
  • HY-19337
    ORM-15341

    Androgen Receptor Endocrinology
    ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.
  • HY-19319
    MI-136

    Androgen Receptor Apoptosis Cancer
    MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes.
  • HY-N2037
    Higenamine

    Norcoclaurine

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine (Norcoclaurine) has anti-apoptotic effects.
  • HY-N2037A
    Higenamine hydrochloride

    Norcoclaurine hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Higenamine hydrochloride (Norcoclaurine hydrochloride), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine hydrochloride (Norcoclaurine hydrochloride) has anti-apoptotic effects.
  • HY-N0400
    Wogonin

    CDK Wnt Autophagy Apoptosis Cancer Inflammation/Immunology
    Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
  • HY-133045
    VHL Ligand 8

    Ligand for E3 Ligase Cancer
    VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
  • HY-18285
    Longdaysin

    Casein Kinase ERK CDK Cancer
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
  • HY-101980
    AZD4635

    HTL1071

    Adenosine Receptor Cancer
    AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors.
  • HY-16910
    WIKI4

    PARP β-catenin Cancer
    WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM.
  • HY-13912
    IWP-2

    Wnt Casein Kinase Cancer
    IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ.
  • HY-110136A
    PMX 205 Trifluoroacetate

    Complement System Inflammation/Immunology
    PMX 205 Trifluoroacetate is a potent complement C5a receptor (C5aR; CD88) antagonist.
  • HY-11027
    MK-0773

    PF-05314882

    Androgen Receptor Endocrinology
    MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.
  • HY-110136
    PMX 205

    Complement System Inflammation/Immunology
    PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.
  • HY-116042
    FSCPX

    Adenosine Receptor Neurological Disease
    FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modifies the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium.
  • HY-16665
    iCRT 14

    Wnt Cancer
    iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-120090
    MRS1177

    Adenosine Receptor Inflammation/Immunology
    MRS1177 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 0.3 nM.
  • HY-N0138
    Theobromine

    3,7-Dimethylxanthine

    Adenosine Receptor Endogenous Metabolite Neurological Disease
    Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
  • HY-118678
    MRS1186

    Adenosine Receptor Inflammation/Immunology
    MRS1186 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 7.66 nM.
  • HY-12715
    Yohimbine

    Adrenergic Receptor Neurological Disease Endocrinology
    Yohimbine is a potent and relatively nonselective alpha 2-adrenergic receptor (AR) antagonist, with IC50 of 0.6 μM.
  • 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-N2523
    Gigantol

    Wnt Cancer
    Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the Wnt/β-catenin pathway.
  • HY-102028
    KY1220

    Wnt β-catenin Cancer
    KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
  • HY-75342
    Methyl vanillate

    Wnt Reactive Oxygen Species Endogenous Metabolite Inflammation/Immunology Cancer
    Methyl vanillate, one of the ingredients in Hovenia dulcis Thunb, is a Wnt/β-catenin pathway activator. A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite.
  • HY-10593
    IQ 1

    Wnt Cancer
    IQ 1 has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on.
  • HY-14302
    Salmeterol

    GR33343X

    Adrenergic Receptor Endocrinology
    Salmeterol is a long-acting beta2-adrenergic receptor (beta 2AR) agonist used clinically to treat asthma.
  • HY-19436
    Solabegron

    GW 427353

    Adrenergic Receptor Metabolic Disease Endocrinology
    Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-10064
    Ticagrelor

    AZD6140; Ar-C 126532XX

    P2Y Receptor Cardiovascular Disease Cancer
    Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.
  • HY-101085
    SKL2001

    Wnt β-catenin Cancer
    SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.
  • HY-16985
    Darolutamide

    ODM-201; BAY-1841788

    Androgen Receptor Cancer
    Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
  • HY-13604
    Cyproterone acetate

    Androgen Receptor Endocrinology
    Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.
  • HY-70002B
    Enzalutamide carboxylic acid

    MDV3100 cArboxylic acid

    Drug Metabolite Cancer
    Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist.
  • HY-106178
    PMX-53

    3D53

    Complement System Cancer Inflammation/Immunology Cardiovascular Disease
    PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.
  • HY-B1001A
    Todralazine hydrochloride

    EcArazine hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Todralazine hydrochloride (Ecarazine hydrochloride) is an anti-hypertensive agent, acts as a β2AR blocker, with antioxidant and free radical scavenging activity.
  • HY-B1001
    Todralazine

    EcArazine

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Todralazine (Ecarazine) is an anti-hypertensive agent, acts as a β2AR blocker, with antioxidant and free radical scavenging activity.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-117163
    FzM1.8

    Wnt β-catenin Cancer
    FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
  • HY-111847
    Androstanolone acetate

    Androgen Receptor Ligand for Target Protein for PROTAC Cancer
    Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs.
  • HY-135732
    SK33

    Androgen Receptor Cancer
    SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity.
  • HY-70002S
    Enzalutamide D3

    MDV3100 D3

    Androgen Receptor Autophagy Cancer
    Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
  • HY-109049
    Adavivint

    SM04690; Lorecivivint

    Wnt Inflammation/Immunology Cancer
    Adavivint (SM04690; Lorecivivint) is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.
  • HY-N0020
    Echinacoside

    Wnt Reactive Oxygen Species Neurological Disease
    Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche salsa, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.
  • HY-17497A
    Acebutolol hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Acebutolol hydrochloride is a β1 adrenergic receptor (β1AR) antagonist. Acebutolol hydrochloride is used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
  • HY-B1486
    Oxprenolol hydrochloride

    Ba 39089

    Adrenergic Receptor Cardiovascular Disease
    Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
  • HY-128934
    Antitumor agent-2

    Others Cancer Inflammation/Immunology
    Antitumor agent-2 is sourced from patent CN102250203, compound 6a-r, has antitumor action and anti-inflammatory action.
  • HY-121251
    BI-167107

    Adrenergic Receptor Cancer Neurological Disease Endocrinology
    BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
  • HY-B0573
    Propranolol hydrochloride

    Adrenergic Receptor Neurological Disease Endocrinology
    Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used to control hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • 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-B0573B
    Propranolol

    Adrenergic Receptor Neurological Disease Cardiovascular Disease Endocrinology
    Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used to control hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-19532
    ZM241385

    Adenosine Receptor Neurological Disease Cancer
    ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM.
  • HY-N0008
    Orcinol glucoside

    Others Neurological Disease
    Orcinol glucoside (OG) is an active constituent isolated from Rhizoma Curculiginis, with antidepressant effects. Orcinol glucoside facilitates the shift of MSC fate to osteoblast and prevents adipogenesis via Wnt/β-catenin signaling pathway.
  • HY-135813
    LtaS-IN-1

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

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-102076
    0990CL

    Others Others
    0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP.
  • HY-101978
    CPI-444

    V81444; ciforadenant

    Adenosine Receptor Cancer
    CPI-444 (V81444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.
  • HY-108439
    Neurodazine

    Wnt Hedgehog Neurological Disease
    Neurodazine is an imidazole-based small molecule, serve as a promoter of neurogenesisin pluripotent cells. Neurodazine promotes neurogenesis by activating Wnt and Shh signaling pathways. Neurodazine selectively suppresses astrocyte differentiation of P19 cells.
  • HY-12681
    CCT251545

    Wnt Cancer
    CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
  • HY-10858
    WAY 316606

    sFRP-1 Cancer
    WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.
  • HY-B0573S
    Propranolol D7 hydrochloride

    Adrenergic Receptor Endocrinology Neurological Disease Cardiovascular Disease
    Propranolol D7 hydrochloride is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used to control hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-N0166
    Gramine

    Donaxine

    Adiponectin Receptor Adrenergic Receptor Reverse Transcriptase Cancer Infection Metabolic Disease Endocrinology
    Gramine (Donaxine) is a natural alkaloid isolated from giant reed, acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 µM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist. Gramine (Donaxine) has anti-tumor, anti-viral and anti-inflammatory properties.
  • HY-133044
    Boc-Pip-alkyne-Ph-COOH

    PROTAC Linker Cancer
    Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
  • HY-12707
    Piribedil

    Adrenergic Receptor Dopamine Receptor Neurological Disease Endocrinology
    Piribedil is a dopamine D2 receptor (D2R) agonist which also displays antagonist property at 1A-adrenoceptor (1A-AR).
  • HY-13613
    Dutasteride

    GG 745; GI 198745

    5 alpha Reductase Apoptosis Cancer
    Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
  • HY-P2272
    NLS-StAx-h

    Wnt β-catenin Cancer
    NLS-StAx-h is a selective, stapled peptide inhibitor of Wnt signaling with an IC50 of 1.4 μM. NLS-StAx-h efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h inhibits proliferation and migration of colorectal cancer cells.
  • HY-112799
    DK419

    Wnt β-catenin Cancer
    DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC50 of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK.
  • HY-116214
    Cyprodinil

    Fungal Androgen Receptor
    Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
  • HY-P1345
    TLQP-21

    Complement System Endocrinology Neurological Disease
    TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.
  • HY-119751
    Hematein

    Casein Kinase Akt Wnt Apoptosis Cancer
    Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.
  • HY-112256
    ACP-105

    Androgen Receptor Inflammation/Immunology
    ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
  • HY-B1276A
    Metaproterenol

    Orciprenaline

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease Endocrinology
    Metaproterenol (Orciprenaline) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol also has anti-inflammatory activity.
  • HY-50289
    Sorbinil

    Aldose Reductase Metabolic Disease
    Sorbinil, is an Aldose reductase inhibitor (ARI). Sorbinil plays therapeutic role in treating diabetes and diabetic complications, decreases AR activity and inhibits polyol pathway, it to be found comparatively safer than other ARIs for human use.
  • HY-101918
    DS-1040 Tosylate

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

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-N2375
    L-Quebrachitol

    Wnt β-catenin Metabolic Disease
    L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway.
  • 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-B1276
    Metaproterenol hemisulfate

    Orciprenaline hemisulfate

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease Endocrinology
    Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity.
  • HY-125839
    OP-3633

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism.
  • HY-P1345A
    TLQP-21 TFA

    Complement System Endocrinology Neurological Disease
    TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.
  • HY-N7045
    Isosilybin B

    Androgen Receptor Apoptosis Cancer
    Isosilybin B, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-136145
    FIDAS-3

    Wnt Cancer
    FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities.
  • HY-17042S
    Cetirizine D4

    Histamine Receptor Inflammation/Immunology
    Cetirizine D4 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-17042S1
    Cetirizine D8

    Histamine Receptor Inflammation/Immunology
    Cetirizine D8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-17042A
    Cetirizine dihydrochloride

    P071

    Histamine Receptor Inflammation/Immunology Endocrinology
    Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-17042AS1
    Cetirizine D8 dihydrochloride

    Histamine Receptor Inflammation/Immunology
    Cetirizine D8 dihydrochloride is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-100661
    Cetirizine Impurity D

    Histamine Receptor Endocrinology Inflammation/Immunology
    Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-17042
    Cetirizine

    Histamine Receptor Inflammation/Immunology Endocrinology
    Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-129393
    AB928

    Adenosine Receptor Inflammation/Immunology
    AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. AB928 relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities.
  • HY-126248
    Tankyrase-IN-2

    PARP Cancer
    Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model.
  • HY-116035
    Nimbolide

    NF-κB CDK Apoptosis Cancer
    Nimbolide is a triterpene derived from the leaves and flowers of neem (Azadirachta indica L). Nimbolide induces apoptosis through inactivation of NF-κB. Nimbolide inhibits CDK4/CDK6 kinase activity. Nimbolide suppresses the NF-κB, Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.
  • HY-123940
    SGC-AAK1-1

    Wnt Cancer
    SGC-AAK1-1, a chemical probe, is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC50 of 270 nM and a Ki of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-133028
    CKI-7 free base

    Casein Kinase CDK SGK Ribosomal S6 Kinase (RSK) Cancer
    CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.
  • HY-12170
    Prinomastat

    AG3340; KB-R9896

    MMP Cancer
    Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
  • HY-12170A
    Prinomastat hydrochloride

    AG3340 hydrochloride; KB-R9896 hydrochloride

    MMP Cancer
    Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
  • HY-15147
    XAV-939

    β-catenin PARP Cancer
    XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC50s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kds of 99 and 93 nM, respectively).
  • HY-N0665
    Specnuezhenide

    (8E)-Nuezhenide

    NF-κB Wnt Inflammation/Immunology
    Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA).
  • HY-112052
    Aminomalonic acid

    Endogenous Metabolite Cancer
    Aminomalonic acid is an amino endogenous metabolite, acts as a strong inhibitor of L-asparagine synthetase from Leukemia 5178Y/AR (Ki= 0.0023 M) and mouse pancreas (Ki= 0.0015 M) in vitro. Aminomalonic acid is a potential biomarker to discriminate between different stages of melanoma metastasis.
  • HY-106420
    16,16-Dimethyl prostaglandin E2

    16,16-dimethyl PGE2

    Prostaglandin Receptor Inflammation/Immunology
    16,16-Dimethyl prostaglandin E2 (16,16-dimethyl PGE2) is an orally active vertebrate Hematopoietic stem cells (HSCs) homeostasis critical regulator. 16,16-Dimethyl prostaglandin E2 can act through EP2/EP4 and has an interaction with the Wnt pathway.
  • HY-N7043
    Isosilybin A

    Apoptosis Cancer
    Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-133046
    VHL Ligand-Linker Conjugates 17

    E3 Ligase Ligand-Linker Conjugate Cancer
    VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader.
  • HY-N6883
    6-Methoxytricin

    Aldose Reductase Metabolic Disease
    6-Methoxytricin (Compound 6) is an flavonoid isolated from Artemisia iwayomogi. 6-Methoxytricin (Compound 6) is an inhibitor on aldose reductase (AR) and advanced glycation endproduct (AGE) formation activities with IC50 values of 30.29 μM and 134.88 μM, respectively. 6-Methoxytricin (Compound 6) has potential as an anti-diabetic complications agent.
  • HY-111372
    Finerenone

    BAY 94-8862

    Mineralocorticoid Receptor Cardiovascular Disease
    Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.
  • HY-111024
    2,2,5,7,8-Pentamethyl-6-Chromanol

    PMC

    Androgen Receptor Cancer
    2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.
  • HY-10182B
    CHIR-99021 trihydrochloride

    CT99021 trihydrochloride

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

    CT99021

    GSK-3 Wnt β-catenin Autophagy Cancer
    CHIR-99021 (CT99021) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 induces autophagy.
  • HY-B0845
    Prochloraz

    BTS 40542

    Fungal Estrogen Receptor/ERR Androgen Receptor Aryl Hydrocarbon Receptor
    Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s = 25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50 = 1 μM).
  • HY-10182A
    CHIR-99021 monohydrochloride

    CT99021 monohydrochloride

    GSK-3 Wnt β-catenin Autophagy Cancer
    CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 monohydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 monohydrochloride induces autophagy.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-B0846
    Dimethomorph

    Fungal Androgen Receptor
    Dimethomorph is a morpholine fungicide that inhibits fungal cell wall formation. Dimethomorph inhibits mycelial growth of the oomycete fungi P. citrophthora, P. parasitica, P. capsici, and P. infestans (EC50s=0.14 µg/mL, 0.38 µg/mL, <0.1 µg/mL, and 0.16-0.3 µg/mL, respectively) but is less active against the green algae species C. vulgaris or S. obliquus in vitro (EC50s=47.46 µg/mL and 44.87 µg/mL, respectively). Dimethomorph inhibits androgen receptor (AR) activity in a reporter assay in MDA-kb2 human breast cancer cells but not in a yeast antiandrogen screen (IC20s=0.263 µM and 38.5 µM, respectively).
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.