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Targets Recommended: LXR P2X Receptor RAR/RXR CXCR

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

118

Inhibitors & Agonists

9

Dye Reagents

9

Peptides

17

Natural
Products

36

Recombinant Proteins

Cat. No. Product Name Target Research Area
  • HY-16590
    X-376

    ALK c-Met/HGFR Cancer
    X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
  • HY-70050
    Alosetron (Hydrochloride(1:X))

    GR 68755 (Hydrochloride(1:X)); GR 68755X (Hydrochloride(1:X))

    5-HT Receptor Neurological Disease
    Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
  • HY-N2001
    Araloside X

    Others Others
    Araloside X (Congmunoside X) is a triterpenoid saponin isolated from Aralia elata.
  • HY-108136A
    Bisindolylmaleimide X hydrochloride

    BIM-X hydrochloride; Ro31-8425 hydrochloride

    PKC CDK Others
    Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM.
  • HY-103714
    Ensartinib

    X-396

    ALK c-Met/HGFR Cancer
    Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  • HY-B1071
    Lasalocid

    Lasalocid-A; Ionophore X-537A; Antibiotic X-537A

    Bacterial Autophagy Infection Cancer
    Lasalocid (Lasalocid-A; Ionophore X-537A; Antibiotic X-537A) is an antibacterial agent and a coccidiostat, used in the feed additives
  • HY-103714A
    Ensartinib hydrochloride

    X-396 hydrochloride

    ALK c-Met/HGFR Cancer
    Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  • HY-112605
    sPLA2-X Inhibitor 31

    Phospholipase Cardiovascular Disease
    sPLA2-X Inhibitor 31 is a selective secreted phospholipase A2 type X (sPLA2-X) inhibitor with IC50s of 26 nM, 310 nM, and 2230 nM for sPLA2-X, sPLA2-IIa, and sPLA2-V, respectively.
  • HY-108522
    PA452

    RAR/RXR Metabolic Disease
    PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.
  • HY-109019
    Vorolanib

    CM082; X-82

    VEGFR PDGFR Cancer
    Vorolanib (CM082; X-82) is an orally active, multikinase VEGFR/PDGFR inhibitor. Vorolanib minimizes toxicity, disrupts tumor angiogenesis and tumor cell proliferation, and induces of tumor cell death.
  • HY-112292
    GW806742X

    Mixed Lineage Kinase VEGFR Others
    GW806742X is a Mixed Lineage Kinase Domain-Like protein (MLKL) inhibitor which binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and has anti-necroptosis activity. GW806742X has activity against VEGFR2.
  • HY-111911
    Xanthocillin X permethyl ether

    Others Neurological Disease
    Xanthocillin X permethyl ether is a natural compound isolated from fungal extracts, with Aβ-42 lowering activity.
  • HY-110390
    GR148672X

    Others Cardiovascular Disease
    GR148672X is a triacyglycerol hydrolase (TGH) inhibitor with an IC50 of 4 nM extracted from patent WO 2001016358 A2.
  • HY-N1724
    Concanamycin A

    Antibiotic X 4357B; Concanamycin; X 4357B

    Proton Pump Cancer
    Concanamycin A (Antibiotic X 4357B) is a macrolide antibiotic and a specific vacuolar type H +-ATPase (V-ATPase) inhibitor.
  • HY-14167
    GW842166X

    Cannabinoid Receptor Inflammation/Immunology Neurological Disease
    GW842166X is a potent and selective cannabinoid receptor 2 (CB2) agonist with IC50 values of 63 and 91 nM for human and rat CB2, respectively.
  • HY-14165
    Veliflapon

    BAY X 1005; DG-031

    FLAP Leukotriene Receptor Inflammation/Immunology Cardiovascular Disease
    Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.
  • HY-19956
    GI254023X

    GI4023; SRI028594

    MMP Cancer
    GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.
  • HY-11003
    GW843682X

    GW843682

    Polo-like Kinase (PLK) Cancer
    GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ∼30 other kinases.
  • HY-13867
    Bisindolylmaleimide I

    GF109203X; Go 6850

    PKC Metabolic Disease Cancer
    Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
  • HY-101588
    Gefapixant

    AF219; MK-7264

    P2X Receptor Inflammation/Immunology
    Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC 50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
  • HY-14483
    AF-353

    Ro-4

    P2X Receptor Cancer
    AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3.
  • HY-117508
    JNJ-54175446

    P2X Receptor Neurological Disease
    JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.
  • HY-15568A
    A-317491 sodium salt hydrate

    P2X Receptor Autophagy Neurological Disease Cancer
    A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.
  • HY-15568
    A-317491

    P2X Receptor Autophagy Neurological Disease Cancer
    A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.
  • HY-14832
    Ataluren

    PTC124

    CFTR Autophagy Metabolic Disease
    Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
  • HY-B0385
    Gabexate mesylate

    FOY

    Factor Xa Proteasome Inflammation/Immunology
    Gabexate mesylate is a Factor X inhibitor; serine protease inhibitor .
  • HY-101910
    PSB-12062

    N-(p-Methylphenylsulfonyl)phenoxazine

    P2X Receptor Neurological Disease
    PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
  • HY-50697
    A-740003

    P2X Receptor Neurological Disease
    A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively.
  • HY-15488
    A 438079

    P2X Receptor Neurological Disease
    A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
  • HY-108652
    α,β-Methylene ATP trisodium

    Others Others
    α,β-Methylene ATP trisodium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand.
  • HY-15488A
    A 438079 hydrochloride

    P2X Receptor Neurological Disease
    A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
  • HY-12222
    Obeticholic acid

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

    FXR Autophagy Others
    Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.
  • HY-101418
    JNJ-47965567

    P2X Receptor Neurological Disease
    JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.
  • HY-109096
    Nidufexor

    FXR Autophagy Others
    Nidufexor is a farnesoid X receptor (FXR) agonist.
  • HY-15470
    GW791343 trihydrochloride

    P2X Receptor Neurological Disease
    GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-15469
    GW791343 dihydrochloride

    P2X Receptor Neurological Disease
    GW791343 dihydrochloride is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-100483
    A-804598

    P2X Receptor Cancer
    A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
  • HY-15487
    CE-224535

    PF-04905428

    P2X Receptor Neurological Disease
    CE-224535 is a selective P2X7 receptor antagonist.
  • HY-107399
    CD3254

    RAR/RXR Cancer Metabolic Disease
    CD3254 a potent and selective retinoid-X-receptor (RXR) agonist.
  • HY-N2371
    27-Hydroxycholesterol

    Estrogen Receptor/ERR LXR Endogenous Metabolite Cancer
    27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
  • HY-N0933
    Androsterone

    5α-Androstan-3α-ol-17-one

    FXR Endogenous Metabolite Autophagy Metabolic Disease Neurological Disease
    Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).
  • HY-14302
    Salmeterol

    GR33343X

    Adrenergic Receptor Others Endocrinology
    Salmeterol is a long-acting beta2-adrenergic receptor (beta 2AR) agonist used clinically to treat asthma.
  • 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-13954
    A 839977

    P2X Receptor Neurological Disease Inflammation/Immunology
    A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
  • HY-130605
    BAY-1797

    P2X Receptor Neurological Disease
    BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC50 of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects.
  • HY-N1478
    Gardenoside

    Others Neurological Disease
    Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis.
  • HY-14854A
    Tecarfarin sodium

    ATI-5923 sodium

    Others Metabolic Disease
    Tecarfarin sodium (ATI-5923 sodium) is a novel orally active non-competitive vitamin K epoxide reductase (VKOR) antagonist, impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin sodium has the antithrombotic activity.
  • HY-16322
    Minodronic acid

    YM-529

    P2X Receptor Apoptosis Cancer
    Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain.
  • HY-14854
    Tecarfarin

    ATI-5923

    Others Cardiovascular Disease
    Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin has the antithrombotic activity .
  • HY-108669
    AZ10606120 dihydrochloride

    P2X Receptor Cancer Neurological Disease
    AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth.
  • HY-112154
    CXCR7 modulator 2

    CXCR Cardiovascular Disease Endocrinology
    CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), with a Ki of 13 nM.
  • HY-B0924
    Anisindione

    Others Cardiovascular Disease
    Anisindione is a synthetic anticoagulant, prevents the formation of active procoagulation factors II, VII, IX, and X.
  • HY-135399
    Tauro-Obeticholic acid

    FXR Inflammation/Immunology
    Tauro-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
  • HY-135400
    Glyco-Obeticholic acid

    FXR Inflammation/Immunology
    Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist.
  • HY-109565
    ASTX660

    IAP Cancer
    ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
  • HY-109073
    Rovazolac

    LXR Inflammation/Immunology
    Rovazolac is a liver x receptor (LXR) modulator extracted from patent WO2013130892A1.
  • HY-N3216
    Nagilactone B

    LXR Cardiovascular Disease
    Nagilactone B, extracted from the root bark of Podocarpus nagi, is a liver X receptor (LXR) agonist.
  • HY-10627A
    GW3965 hydrochloride

    LXR Cardiovascular Disease Cancer
    GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC50s of 190 and 30 nM for hLXRα and hLXRβ , respectively.
  • HY-10627
    GW3965

    LXR Cardiovascular Disease
    GW3965 is a potent, selective liver X receptor (LXR) agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.
  • HY-10912
    Fexaramine

    FXR Autophagy Others
    Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds.
  • HY-16972
    SR9243

    LXR Cancer
    SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
  • HY-101442
    SR9238

    LXR Metabolic Disease
    SR9238 is a synthetic liver X receptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.
  • HY-14171
    Bexarotene

    LGD1069

    RAR/RXR Autophagy Cancer
    Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
  • HY-111202
    Pyributicarb

    TSH-888

    Cytochrome P450 Inflammation/Immunology
    Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
  • HY-114392
    Gly-β-MCA

    FXR Autophagy Metabolic Disease
    Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders.
  • HY-111408
    EOAI3402143

    Deubiquitinase Cancer
    EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.
  • HY-19427A
    AZD9056 hydrochloride

    P2X Receptor Inflammation/Immunology
    AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.
  • HY-135103
    Tauro-β-muricholic acid sodium

    T-βMCA sodium

    FXR Cancer
    Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
  • HY-100652A
    O-Desmethyl apixaban sulfate sodium

    Factor Xa Cardiovascular Disease
    O-Desmethyl apixaban sulfate sodium is a major circulating metabolite of Apixaban in humans. O-Desmethyl apixaban sulfate sodium inhibits factor X (FXa) with a Ki of 58 μM.
  • HY-111498A
    RGX-104 free Acid

    LXR Cancer Inflammation/Immunology
    RGX-104 free Acid is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-B1071A
    Lasalocid sodium

    Lasalocid-A sodium; Ionophore X-537A sodium; Antibiotic X-537A sodium

    Bacterial Autophagy Cancer Infection
    Lasalocid sodium (Lasalocid-A sodium) treatment led to an increase in cell wall thickness, whilst the quantity and sugar composition of the cell wall remained unchanged in BY-2 cells.
  • HY-14864
    Mapracorat

    ZK-245186; BOL-303242X

    Glucocorticoid Receptor Endocrinology
    Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
  • 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-N5025
    Bullatine A

    P2X Receptor Cancer Inflammation/Immunology
    Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed.
  • HY-112705
    VU0529331

    Potassium Channel Neurological Disease
    VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
  • HY-104070
    LG-100064

    RAR/RXR Autophagy Cancer
    LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.
  • HY-110237
    BX430

    P2X Receptor Calcium Channel Cardiovascular Disease
    BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
  • HY-130118
    MRGPRX1 agonist 1

    Others Neurological Disease
    MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1), with an EC50 of 50 nM, and is inactive on MRGPRC11. Analgesic effect.
  • HY-16963
    GW627368

    Prostaglandin Receptor Inflammation/Immunology Endocrinology Cancer
    GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor with additional human TP receptor affinity, with pKi values of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively.
  • HY-107500
    UVI 3003

    RAR/RXR Autophagy Others
    UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
  • HY-108525
    Fluorobexarotene

    RAR/RXR Cancer
    Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.
  • HY-111996
    Kv3 modulator 1

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 has the potential for inflammatory pain treatment.
  • HY-12434
    INT-767

    FXR GPCR19 Autophagy Cancer
    INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively.
  • HY-14171S
    Bexarotene D4

    LGD1069 D4

    RAR/RXR Autophagy Cancer
    Bexarotene D4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
  • HY-10402
    Losmapimod

    GSK-AHAB; GW856553X; SB856553

    p38 MAPK Autophagy Inflammation/Immunology Cancer
    Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
  • HY-70050A
    Alosetron

    GR 68755; GR 68755X

    5-HT Receptor Neurological Disease
    Alosetron (GR 68755) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
  • HY-14864A
    (S)-Mapracorat

    (S)-ZK-245186; (S)-BOL-303242X

    Glucocorticoid Receptor Endocrinology
    (S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
  • HY-101044
    PPADS tetrasodium

    P2X Receptor Na+/Ca2+ Exchanger Neurological Disease
    PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca²⁺exchanger in guinea pig airway smooth muscle.
  • HY-13264
    Degrasyn

    WP1130

    Deubiquitinase Bcr-Abl Apoptosis Autophagy Cancer
    Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
  • HY-P7061A
    ALX 40-4C Trifluoroacetate

    CXCR Infection Endocrinology
    ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
  • HY-P7061
    ALX 40-4C

    CXCR Infection Endocrinology
    ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
  • HY-100469
    LXRβ agonist-2

    LXR Cardiovascular Disease
    LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis.
  • HY-N2450
    Sulforaphene

    Apoptosis EGFR ERK NF-κB Cancer
    Sulforaphene, isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals.
  • HY-13290
    KN-62

    CaMK P2X Receptor Autophagy Metabolic Disease Cancer
    KN-62 is a selective and potent inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with IC50 of 0.9 μM, KN-62 also displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
  • HY-103244
    CITCO

    Apoptosis Cancer
    CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors.
  • HY-110249
    CINPA1

    Others Metabolic Disease
    CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.
  • HY-N2078
    Yamogenin

    Neodiosgenin

    LXR Metabolic Disease
    Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes.
  • HY-70050C
    Alosetron Hydrochloride

    GR 68755C; GR 68755 (Hydrochloride); GR 68755X (Hydrochloride)

    5-HT Receptor Neurological Disease
    Alosetron Hydrochloride (GR 68755 Hydrochloride) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
  • HY-16305
    Maribavir

    1263W94; BW1263W94; GW257406X

    CMV Infection
    Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM. Maribavir has potent antiviral activity against HCMV and Epstein-Barr virus (EBV).
  • HY-70050AS
    Alosetron D3

    GR 68755 D3; GR 68755X D3

    5-HT Receptor Neurological Disease
    Alosetron D3 (GR 68755 D3) is a deuterium labeled Alosetron. Alosetron is a serotonin 5HT3-receptor antagonist.
  • HY-P0172A
    ATI-2341 TFA

    CXCR Cancer Inflammation/Immunology Endocrinology
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
  • HY-15971A
    AMD 3465

    GENZ-644494

    CXCR HIV Infection Endocrinology
    AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-15310
    Ivermectin

    MK-933

    Parasite HIV Integrase Mitophagy Autophagy Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite medication used in humans most commonly to treat nematode infections such as onchocerciasis, as well as scabies and lice. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs).
  • HY-109513
    Ioxilan

    Others Others
    Ioxilan is a low-osmolar, nonionic and tri-iodinated diagnostic contrast agent. Ioxilan is also an X-ray contrast agent for excretory urography and contrast enhanced computed tomographic (CECT) imaging of the head and body. Intravascular injection results in opacification of vessels in the path of flow of the contrast medium, permitting radiographic visualization of the internal structures of the human body until significant hemodilution occurs.
  • HY-13821
    Epoxomicin

    BU-4061T

    Proteasome Apoptosis Cancer Inflammation/Immunology
    Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
  • HY-P0172
    ATI-2341

    CXCR Inflammation/Immunology Endocrinology Cancer
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
  • HY-15371
    Forskolin

    Coleonol; Colforsin

    Adenylate Cyclase FXR Autophagy Cancer Endocrinology Metabolic Disease Inflammation/Immunology
    Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
  • HY-15971
    AMD 3465 hexahydrobromide

    GENZ-644494 hexahydrobromide

    CXCR HIV Infection Endocrinology
    AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-109067
    Opiranserin

    GlyT 5-HT Receptor P2X Receptor Neurological Disease
    Opiranserin, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.
  • HY-125996
    NR1H4 activator 1

    FXR Inflammation/Immunology
    NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.
  • HY-80002
    BMX-IN-1

    BMX kinase inhibitor

    Btk BMX Kinase Cancer
    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
  • 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 DTT-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-16561
    Resveratrol

    trans-Resveratrol; SRT501

    IKK Autophagy Mitophagy Apoptosis Sirtuin Inflammation/Immunology Cancer
    Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor.
  • HY-100277
    Mifobate

    SR-202

    PPAR Metabolic Disease
    Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects.
  • HY-70050B
    Alosetron ((Z)-2-butenedioate)

    GR 68755 ((Z)-2-butenedioate); GR 68755X ((Z)-2-butenedioate)

    5-HT Receptor Neurological Disease
    Alosetron (Z)-2-butenedioate (GR 68755 (Z)-2-butenedioate) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
  • HY-113259
    7α-Hydroxy-4-cholesten-3-one

    Endogenous Metabolite Metabolic Disease
    7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane X receptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1.
  • HY-100008
    Peretinoin

    NIK333

    RAR/RXR SPHK Autophagy HCV Cancer Infection
    Peretinoin is an oral acyclic retinoid retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM.
  • HY-107738
    Guggulsterone

    Z/E-Guggulsterone

    Apoptosis JNK Akt Caspase FXR Autophagy Cancer
    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.