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Results for "5 alpha Reductase Inhibitors" in MCE Product Catalog:

534

Inhibitors & Agonists

2

Screening Libraries

13

Peptides

2

Inhibitory Antibodies

122

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-113960
    ERRα antagonist-1

    Estrogen Receptor/ERR Cancer
    ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
  • HY-19949
    HIF-2α-IN-1

    HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay.
  • HY-101491
    SR-18292

    PGC-1α Autophagy Metabolic Disease
    SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
  • HY-113038
    D-α-Hydroxyglutaric acid

    (R)-2-Hydroxypentanedioic acid

    Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    D-α-Hydroxyglutaric acid ((R)-2-Hydroxypentanedioic acid) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling.
  • HY-110266
    GN44028

    HIF/HIF Prolyl-Hydroxylase Cancer
    GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.
  • HY-111507
    PDGFRα kinase inhibitor 1

    PDGFR Cancer
    PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
  • HY-15438
    SB 415286

    GSK-3 Apoptosis Metabolic Disease
    SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
  • HY-114423
    p38α inhibitor 1

    p38 MAPK Autophagy Inflammation/Immunology
    p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.
  • HY-18874
    p38-α MAPK-IN-1

    p38 MAPK Autophagy Others
    p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
  • HY-111387
    IDF-11774

    HIF/HIF Prolyl-Hydroxylase Cancer
    IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.
  • HY-13671
    LW6

    HIF-1α inhibitor; LW8

    HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
  • HY-14929A
    Migalastat hydrochloride

    GR181413A

    Others Others
    Migalastat hydrochloride (GR181413A) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
  • HY-18371
    TC-S 7009

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ≫ 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression.
  • HY-100542
    D-α-Hydroxyglutaric acid disodium

    Disodium (R)-2-hydroxyglutarate

    Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling.
  • HY-112535
    α-2,3-sialyltransferase-IN-1

    Lith-O-Asp analog

    Others Cancer Inflammation/Immunology
    α-2,3-sialyltransferase-IN-1 (Lith-O-Asp analog) is a noncompetitive α-2,3-sialyltransferase inhibitor with an IC50 of 6 μM.
  • HY-18370
    HIF-2α-IN-3

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent.
  • HY-U00459
    GSK2850163

    IRE1 Cancer
    GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
  • HY-U00459B
    GSK2850163 hydrochloride

    IRE1 Cancer
    GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
  • HY-N4327
    Eurycomalactone

    NF-κB Infection Inflammation/Immunology
    Eurycomalactone is a natural product found in Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor, with an IC50 of 0.5 μM. Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα/β and IκBα.
  • HY-100735
    C 87

    TNF Receptor Inflammation/Immunology
    C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
  • HY-W019838
    D-Erythro-dihydrosphingosine

    Endogenous Metabolite Phospholipase Cancer
    D-Erythro-dihydrosphingosin directly inhibits cytosolic phospholipase A2α (cPLA2α) activity.
  • HY-107782
    Picrotin

    Others Neurological Disease
    Picrotin is an inhibitor of glycine receptors (GlyRs) which blocks α2 GlyR, α1 GlyR and α3 GlyR.
  • HY-12836A
    IFN alpha-IFNAR-IN-1 hydrochloride

    IFNAR Inflammation/Immunology
    IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM).
  • HY-N3002
    α-Arbutin

    4-Hydroxyphenyl α-D-glucopyranoside

    Tyrosinase Metabolic Disease
    α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is emerging as popular and effective skin whiteners, acting as tyrosinase inhibitor.
  • HY-107532
    N-Nonyldeoxynojirimycin

    NN-DNJ; Nonyl-DNJ

    Glucosidase Metabolic Disease
    N-Nonyldeoxynojirimycin (NN-DNJ) is a potent inhibitor of alpha-glucosidase and alpha-1,6-glucosidase (IC50s, 0.42, 8.4 μM, respectively), inhibits glycogen breakdown.
  • HY-U00376
    5α-reductase-IN-1

    Others Metabolic Disease
    5α-reductase-IN-1 is an inhibitor of 5α-reductase, used for the research of patterned alopecia in combination with minoxidil.
  • HY-125840
    PT2977

    MK-6482

    HIF/HIF Prolyl-Hydroxylase Cancer
    PT2977 (MK-6482) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. PT2977, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. PT2977 is a potential treatment for clear cell renal cell carcinoma (ccRCC).
  • HY-123076
    Pifithrin-α, p-Nitro, Cyclic

    PFN-α

    MDM-2/p53 Neurological Disease
    Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
  • HY-10801
    CAY10650

    Phospholipase Inflammation/Immunology
    CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC 50 value of 12 nM.
  • HY-B0141A
    Alpha-Estradiol

    Alfatradiol; Epiestradiol; Epiestrol

    5 alpha Reductase Endogenous Metabolite Inflammation/Immunology
    Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
  • HY-N0242
    Fraxinellone

    PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT Cancer Inflammation/Immunology
    Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.
  • HY-113212
    Ursocholic acid

    Endogenous Metabolite Metabolic Disease
    Ursocholic acid, a bile acid found predominantly in bile of mammals, is transformed into deoxycholic acid by the intestinal microflora in mice. Ursodeoxycholic acid is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α.
  • HY-12867
    PT-2385

    HIF/HIF Prolyl-Hydroxylase Cancer
    PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.
  • HY-17537
    APY29

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-107371
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde

    NSC95682

    IRE1 Cancer
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1α inhibitor with an IC50 of 0.08 μM, extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5.
  • HY-112275
    TNF-α-IN-1

    TNF Receptor Cancer Inflammation/Immunology
    TNF-α-IN-1 is a TNF-α inhibitor extracted from patent US20030096841A1, compound example I-7.
  • HY-B0942
    Benzethonium chloride

    nAChR Neurological Disease
    Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
  • HY-112910
    Grp94 Inhibitor-1

    HSP Cancer Infection
    Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
  • HY-12688
    Succinyl phosphonate

    Others Others
    Succinyl phosphonate is an inhibitor of the α-ketoglutarate dehydrogenase.
  • HY-U00313
    Tropodifene

    Tropaphen

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Tropodifene (Tropaphen) is an α-Adrenergic receptor inhibitor.
  • 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-50855B
    Silmitasertib sodium salt

    CX-4945 sodium salt

    Casein Kinase Autophagy Cancer
    Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
  • HY-11087
    SD 0006

    SD-06

    p38 MAPK Autophagy Inflammation/Immunology
    SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC50 of 110 nM for p38α.
  • HY-19763
    BEBT-908

    PI3Kα inhibitor 1

    PI3K Cancer
    BEBT-908 (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .
  • HY-U00090
    N-Methylmoranoline

    MOR 14; N-Methyl-1-deoxynojirimycin; N-Methylmoranolin

    Glucosidase Metabolic Disease
    N-Methylmoranoline (MOR 14) is an α-glucosidase inhibitor.
  • HY-N1064
    Xanthoplanine

    nAChR Neurological Disease
    Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
  • HY-124957
    α-NETA

    Apoptosis Cancer
    α-NETA is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM. α-NETA is a potent chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM). α-NETA has anti-cancer activity.
  • HY-N0255
    alpha-Hederin

    α-Hederin

    Apoptosis Others
    alpha-Hederin (α-Hederin) is a water-soluble pentacyclic triterpenoid saponin, possessing several biological properties such as antispasmodic, moliscicidic, anthelmithic and inhibiting cell proliferation,
  • HY-121172
    1,4-DPCA

    HIF/HIF Prolyl-Hydroxylase Cancer
    1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
  • HY-129453
    BOP sodium

    Integrin Inflammation/Immunology
    BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins.
  • HY-19332
    Kifunensine

    FR-900494

    Others Inflammation/Immunology
    Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD.
  • HY-125713
    Ganoderic acid Y

    Glucosidase Enterovirus Infection
    Ganoderic acid Y is a α-glucosidase inhibitor with an IC50 of 170 μM for yeast α-glucosidase. Ganoderic acid Y inhibits enterovirus 71 (EV71) replication through blocking EV71 uncoating.
  • HY-50855
    Silmitasertib

    CX-4945

    Casein Kinase Autophagy Cancer
    Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
  • HY-133807A
    (Rac)-Benpyrine

    TNF Receptor Inflammation/Immunology
    (Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
  • HY-130264
    HIF-2α-IN-2

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA).
  • HY-15893
    DMOG

    Dimethyloxallyl Glycine

    HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
  • HY-15969
    Sal003

    Phosphatase Apoptosis Cancer
    Sal003 is a potent, specific and cell-permeable inhibitor of the eukaryotic translation initiation factor 2α (eIF2α) phosphatase. Sal003 is a derivative of salubrinal.
  • HY-10257
    BAY 11-7085

    BAY 11-7083

    NF-κB Ferroptosis Apoptosis Cancer
    BAY 11-7085 (BAY 11-7083) is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.
  • HY-10401
    VX-702

    p38 MAPK Autophagy Inflammation/Immunology
    VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.
  • HY-14975
    R1487 Hydrochloride

    p38 MAPK Autophagy Cancer
    R1487 (Hydrochloride) is highly potent and highly selective inhibitors of p38α.
  • HY-12285
    Serabelisib

    MLN1117; INK1117; TAK-117

    PI3K Cancer
    Serabelisib (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.
  • HY-107406
    Antimycin A1

    Mitochondrial Metabolism Cancer
    Antimycin A1 is a specific electron transfer inhibitor of ubiquinol-cytochrome c oxidoreductase. Antimycin A1 inhibits angiogenesis through decrease in VEGF production caused by inhibition of HIF-1α activation.
  • HY-16187
    EL-102

    HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability.
  • HY-19707
    4μ8C

    IRE1 Inhibitor III

    IRE1 Metabolic Disease
    4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
  • HY-B0379A
    Adiphenine hydrochloride

    nAChR Neurological Disease
    Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride can be used as a local anesthetic.
  • HY-U00179
    CDC801

    Phosphodiesterase (PDE) TNF Receptor Cancer
    CDC801 is a potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α) inhibitor with IC50 of 1.1 μM and 2.5 μM, respectively.
  • HY-114368
    Kira8

    AMG-18

    IRE1 Inflammation/Immunology
    Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  • HY-15484
    Pifithrin-α hydrobromide

    Pifithrin hydrobromide; PFTα hydrobromide

    MDM-2/p53 Aryl Hydrocarbon Receptor Ferroptosis Cancer
    Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.
  • HY-14126
    BIO-1211

    Integrin Inflammation/Immunology
    BIO-1211 is a highly selective and orally active α4β1 (VLA-4) inhibitor, with IC50 values of 4 nM and 2 μM for α4β1 and α4β7, respectively.
  • HY-107641
    α-Cyano-4-hydroxycinnamic acid

    α-Cyano-4-hydroxycinnamate

    Monocarboxylate Transporter Metabolic Disease
    α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications.
  • HY-N0877
    Bufalin

    Na+/K+ ATPase Cancer
    Bufalin is an active component isolated from Chan Su, acts as a potent Na +/K +-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.
  • HY-10231
    PX-478

    HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.
  • HY-70073
    Zaurategrast

    CT7758

    Integrin Inflammation/Immunology
    Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor.
  • HY-19710
    MKC3946

    IRE1 Cancer
    MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
  • HY-N0466
    Rebaudioside A

    Endogenous Metabolite Glucosidase Others
    Rebaudioside A is a steviol glycoside, α-glucosidase inhibitor with IC50 of 35.01 μg/ml.
  • HY-13261
    A66

    PI3K Cancer
    A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
  • HY-19717
    DCVC

    S-[(1E)-1,2-dichloroethenyl]--L-cysteine

    TNF Receptor
    DCVC inhibits pathogen-stimulated TNF-α in human extra placental membranes in vitro.
  • HY-10328
    Neflamapimod

    VX-745

    p38 MAPK Autophagy Inflammation/Immunology
    Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
  • HY-12012
    SB 216763

    GSK-3 Autophagy Neurological Disease Cancer
    SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.
  • HY-N0374
    Licochalcone C

    Glucosidase Metabolic Disease
    Licochalcone C could inhibit α-glucosidase, with IC50s of <100 nM and 92.43 μM for α-glucosidase and protein tyrosine phosphatase 1B (PTP1B), respectively.
  • HY-N3115
    Palbinone

    Others Inflammation/Immunology
    Palbinone is a terpenoid isolated from the roots of Paeonia albiflora Pallas, potently inhibits 3α-hydroxysteroid dehydrogenase (3α-HSD), with an IC50 of 46 nM. Anti-inflammatory activity.
  • HY-P1420
    TAT-cyclo-CLLFVY

    HIF/HIF Prolyl-Hydroxylase
    TAT-cyclo-CLLFVY is a selective HIF-1 dimerization inhibitor. TAT-cyclo-CLLFVY blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50=1.3 μM). TAT-cyclo-CLLFVY inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. TAT-cyclo-CLLFVY also reduces tubularization of hypoxic HUVECs.
  • HY-129113
    α-​Chaconine

    COX Inflammation/Immunology
    α-Chaconine, isolated from a Solanum tuberosum L. cv Jayoung, inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
  • HY-136347
    3α-Hydroxy pravastatin sodium

    HMG-CoA Reductase (HMGCR) Drug Metabolite Cardiovascular Disease
    3α-Hydroxy pravastatin sodium is the major metabolite of Pravastatin. Pravastatin is a competitive HMG-CoA reductase inhibitor.
  • HY-16194
    Emiglitate

    BAY o 1248

    Others Metabolic Disease
    Emiglitate (BAY o 1248) is a potent, selective and competitive inhibitor of α-glucoside hydrolase.
  • HY-N0492
    α-Lipoic Acid

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

    NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.
  • HY-N2566
    Euscaphic acid

    DNA/RNA Synthesis PI3K Apoptosis Cancer
    Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.
  • HY-111255
    SPD304

    TNF Receptor Cancer
    SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.
  • HY-116446
    Pironetin

    Microtubule/Tubulin Cancer
    Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity.
  • HY-108697A
    (Rac)-PT2399

    HIF/HIF Prolyl-Hydroxylase Cancer
    (Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM.
  • HY-U00037
    Ecopladib

    PLA 725

    Phospholipase Inflammation/Immunology
    Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
  • HY-12399
    MKC9989

    IRE1 Cancer
    MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
  • HY-13281
    PIK-75 hydrochloride

    DNA-PK PI3K Apoptosis Cancer
    PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis.
  • HY-U00266
    Cefetrizole

    Glucosidase Infection Metabolic Disease
    Ceftezole is an α-Glucosidase inhibitor with an IC50 and a Ki of 2.1 μM and 0.578 μM, respectively.
  • HY-13864
    PF-4989216

    PI3K Apoptosis Cancer
    PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.
  • HY-101272
    GDC-0326

    PI3K Cancer
    GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
  • HY-16294
    LY2090314

    GSK-3 Cancer
    LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
  • HY-N6968
    α-Humulene

    Humulene; α-Caryophyllene

    NO Synthase COX Inflammation/Immunology
    α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 µg/mL). α-Humulene inhibits COX-2 and iNOS expression.
  • HY-135674
    SR-318

    p38 MAPK TNF Receptor Cancer Inflammation/Immunology
    SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.
  • HY-13229
    BOC-D-FMK

    Caspase Cancer
    Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
  • HY-10403
    PH-797804

    p38 MAPK Autophagy Inflammation/Immunology Cancer
    PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC50=26 nM and Ki=5.8 nM for p38α; Ki=40 nM for p38β) and does not inhibit JNK2.
  • HY-100740C
    (1α,1'S,4β)-Lanabecestat

    (1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814

    Beta-secretase Neurological Disease
    (1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) is a Beta site APP Cleaving Enzymel (BACE1) inhibitor extracted from patent WO2012087237A1, compound 20a, has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively.
  • HY-115463
    EB-3D

    AMPK Apoptosis Cancer
    EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
  • HY-15761
    AZD2858

    GSK-3 Neurological Disease
    AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
  • HY-108431
    MN58b

    Apoptosis Cancer
    MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity.
  • HY-U00458
    K-80003

    TX-803

    Akt Cancer
    K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
  • HY-100337
    WWL70

    MAGL Neurological Disease
    WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 70 nM.
  • HY-16937
    ISA-2011B

    Others Cancer
    ISA-2011B is a PIP5K1α inhibitor with promising anticancer effects .
  • HY-135385
    Dihydro Dutasteride

    Drug Metabolite Inflammation/Immunology
    Dihydro Dutasteride is a metabolite of Dutasteride. Dutasteride is a potent inhibitor of both 5 alpha-reductase isozymes.
  • HY-120111
    MW-150

    MW01-18-150SRM

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-12825
    BHPI

    Estrogen Receptor/ERR Cancer
    BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
  • HY-103248
    Toyocamycin

    Vengicide

    IRE1 Fungal Antibiotic Cancer Infection
    Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM. Toyocamycin (Vengicide) induces apoptosis. Toyocamycin (Vengicide) shows no effect on IRE1α auto-phosphorylation.
  • HY-108645
    AL 8697

    p38 MAPK Autophagy Inflammation/Immunology
    AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity.
  • HY-110193
    SPP-86

    RET Cancer
    SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
  • HY-N4121
    Isocurcumenol

    Estrogen Receptor/ERR Apoptosis
    Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively.
  • HY-101068
    TOFA

    RMI14514; MDL14514

    Acetyl-CoA Carboxylase Cancer
    TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).
  • HY-N6722
    Swainsonine

    Tridolgosir

    Bacterial Antibiotic Cancer Infection
    Swainsonine is an alkaloid isolated from Astragalus, acts as an inhibitor of α-mannosidase, with anti-tumor activity.
  • HY-U00206
    D2343

    Adrenergic Receptor Endocrinology
    D2343 is a β2-adrenoceptor agonist and also is an α1- adrenoceptor inhibitor.
  • HY-101562
    GDC-0077

    RG6114

    PI3K Apoptosis Cancer
    GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα.
  • HY-119307
    Apratastat

    MMP TNF Receptor Cancer
    Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively.
  • HY-128677
    NCC007

    Casein Kinase Neurological Disease
    NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.
  • HY-13453
    BAY 11-7082

    BAY 11-7821

    IKK Deubiquitinase Autophagy Apoptosis Cancer Inflammation/Immunology
    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
  • HY-19931
    COH29

    RNR Inhibitor COH29

    DNA/RNA Synthesis Cancer
    COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
  • HY-B0194A
    Tizanidine hydrochloride

    Adrenergic Receptor Cancer Neurological Disease Endocrinology
    Tizanidine hydrochloride is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
  • HY-100947
    VH-298

    Ligand for E3 Ligase Others
    VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology.
  • HY-B0194
    Tizanidine

    Adrenergic Receptor Neurological Disease Endocrinology Cancer
    Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
  • HY-117771A
    DO34 analog

    Others Metabolic Disease
    DO34 analog is a triazole DAGL(α) inhibitor extracted from patent WO2017096315 A1, compound 100.
  • HY-111055
    BIP-135

    GSK-3 Neurological Disease
    BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.
  • HY-110398
    5,6,7-Trimethoxyflavone

    Baicalein trimethyl ether

    p38 MAPK Inflammation/Immunology Cancer
    5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera.
  • HY-19383
    Ertiprotafib

    PTP 112

    Phosphatase IKK PPAR Metabolic Disease
    Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
  • HY-128463
    N-tert-Butyl-α-phenylnitrone

    COX Reactive Oxygen Species Metabolic Disease Inflammation/Immunology Neurological Disease
    N-tert-Butyl-α-phenylnitrone is a nitrone-based free radical scavenger that forms nitroxide spin adducts. N-tert-Butyl-α-phenylnitrone inhibits COX2 catalytic activity. N-tert-Butyl-α-phenylnitrone has potent ROS scavenging, anti-inflammatory, neuroprotective, anti-aging and anti-diabetic activities, and can penetrate the blood-brain barrier.
  • HY-13635A
    Finasteride acetate

    MK-906 acetate

    5 alpha Reductase Cancer
    Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
  • HY-13635
    Finasteride

    MK-906

    5 alpha Reductase Cancer
    Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
  • HY-128420
    Lobeline sulfate

    α-Lobeline sulfate; L-Lobeline sulfate

    Endogenous Metabolite Neurological Disease
    Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) is a nonstimulant medication that can alter dopamine uptake in brain. Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) inhibits nicotine-induced hyperactivity and is effective in smoking cessation.
  • HY-P9926
    Dupilumab

    REGN-668; SAR-231893

    Interleukin Related Inflammation/Immunology
    Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis.
  • HY-19610
    α-Amanitin

    α-Amatoxin

    DNA/RNA Synthesis ADC Cytotoxin Cancer
    α-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.
  • HY-N0472
    Geraniin

    TNF Receptor Cancer Metabolic Disease Inflammation/Immunology
    Geraniin is a TNF-α releasing inhibitor with numerous activities including anticancer, anti-inflammatory, and anti-hyperglycemic activities, with an IC50 of 43 μM.
  • HY-12050
    CP-673451

    PDGFR Cancer
    CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.
  • HY-U00460
    3,6-DMAD hydrochloride

    IRE1 Cancer
    3,6-DMAD hydrochloride is a inhibitor of the IRE1α-XBP1 pathway of the unfolded protein response.
  • HY-16596
    CNX-1351

    PI3K Cancer
    CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
  • HY-100470
    NSC781406

    PI3K mTOR Cancer
    NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
  • HY-U00459A
    GSK2850163 (S enantiomer)

    Others Others
    GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.
  • HY-U00125
    CGP-53153

    5 alpha Reductase Endocrinology
    CGP-53153 is a steroidal inhibitor of 5 alpha reductase with IC50s of 36 and 262 nM in rat and human prostatic tissue, respectively.
  • HY-128942
    MAC glucuronide α-hydroxy lactone-linked SN-38

    Drug-Linker Conjugates for ADC Cancer
    MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 99 and 105 ng/mL, respectively.
  • HY-N6962
    α-Spinasterol

    TRP Channel COX Infection Neurological Disease
    α-Spinasterol, isolated from Spinacia oleracea, has antibacterial activity. α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.
  • HY-N0328
    alpha-Mangostin

    α-Mangostin

    Reactive Oxygen Species Apoptosis Bacterial Fungal Virus Protease Cancer
    alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
  • HY-12407
    ZK168281

    VD/VDR Metabolic Disease
    ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.
  • HY-15486
    Salubrinal

    Phosphatase HSV Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.
  • HY-114454
    INH14

    IKK Cancer Inflammation/Immunology
    INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.
  • HY-P1259
    PR-39

    Proteasome Bacterial Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-120111A
    MW-150 hydrochloride

    MW01-18-150SRM hydrochloride

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-N0613
    Sauchinone

    NF-κB Inflammation/Immunology
    Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity.
  • HY-13076
    CHIR-98014

    GSK-3 Metabolic Disease
    CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.
  • HY-108606
    PI-828

    PI3K Casein Kinase Cancer
    PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.
  • HY-112619
    TES-991

    Others Metabolic Disease
    TES-991 is a potent and selective human α‑Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) inhibitor, with an IC50 of 3 nM.
  • HY-N3962
    Glycyrrhisoflavone

    Glucosidase Metabolic Disease
    Glycyrrhisoflavone, an active prenylflavonoid, mainly derived from the extract of the roots of Glycyrrhiza uralensis Fisch.. Glycyrrhisoflavone inhibits α-glucosidase.
  • HY-16715
    Acumapimod

    p38 MAPK Autophagy Inflammation/Immunology
    Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.
  • HY-12019
    SGX-523

    c-Met/HGFR Cancer
    SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α.
  • HY-112716
    N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride

    Others Cancer
    N-alpha-Tosyl-L-lysine chloromethyl ketone (TLCK), a trypsin like protease inhibitor, sensitizes HeLa cells to Fas-mediated cell death.
  • HY-N3625
    Coronalolic acid

    Coronalonic acid

    NF-κB Inflammation/Immunology
    Coronalolic acid, extract from the apical bud of Gardenia sootepenesis Hutch, inhibits TNF-α-induced NF-κB activity and NO production.
  • HY-N0835
    (20S)-Protopanaxatriol

    20(S)-APPT; g-PPT

    Glucocorticoid Receptor Estrogen Receptor/ERR LXR Apoptosis Cardiovascular Disease Endocrinology
    (20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor.
  • HY-13228
    YM-201636

    PIKfyve PI3K Autophagy Influenza Virus Cancer Infection
    YM-201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. YM-201636 also inhibits p110α with an IC50 of 3.3 μM. YM-201636 inhibits retroviral replication.
  • HY-P1259A
    PR-39 TFA

    Proteasome Bacterial Inflammation/Immunology
    PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-16134A
    Celgosivir hydrochloride

    MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride

    Glucosidase HCV HIV Infection
    Celgosivir hydrochloride (MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
  • HY-16134
    Celgosivir

    MBI 3253; MDL 28574; MX3253

    Glucosidase HCV HIV Infection
    Celgosivir (MBI 3253; MDL 28574; MX3253) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
  • HY-10626
    T0901317

    LXR FXR ROR Apoptosis Cancer Metabolic Disease Cardiovascular Disease
    T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
  • HY-13468
    KW-2478

    HSP Cancer
    KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
  • HY-125833
    Alpha-Naphthoflavone

    Aromatase Cancer
    Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively.
  • HY-G0008
    Mebeverine metabolite O-desmethyl Mebeverine alcohol

    O-desmethyl Mebeverine alcohol

    Adrenergic Receptor Drug Metabolite Metabolic Disease
    Mebeverine metabolite O-desmethyl Mebeverine alcohol is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
  • HY-13535A
    ATN-161 trifluoroacetate salt

    ATN-161 TFA salt

    Integrin Cancer
    ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
  • HY-101028
    ZINC13466751

    HIF/HIF Prolyl-Hydroxylase Cancer Cardiovascular Disease
    ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 µM.
  • HY-15845
    STF-083010

    IRE1 Cancer
    STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
  • HY-112182
    UM-164

    DAS-DFGO-II

    Src p38 MAPK Autophagy Cancer
    UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
  • HY-15704
    LH846

    Casein Kinase Cancer
    LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
  • HY-14622
    Necrostatin 2

    RIP kinase Cancer
    Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM. Necrostatin 2 is also a RIPK1 inhibitor.
  • HY-135902A
    Synucleozid hydrochloride

    NSC 377363 hydrochloride

    DNA/RNA Synthesis Neurological Disease
    Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
  • HY-110261
    GS143

    IKK E1/E2/E3 Enzyme NF-κB Inflammation/Immunology
    GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCF βTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and tran­scrip­tion of tar­get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.
  • HY-N1881
    4',5-Dihydroxyflavone

    Lipoxygenase Glucosidase Others
    4',5-Dihydroxyflavone is a soybean LOX-1 and yeast α-Glucosidase inhibitor, with an Ki of 102.6 μM for soybean LOX-1 and an IC50 of 66 μM for yeast α-glucosidase. LOX-1 isshort for Lectin-like oxidized low-density lipoprotein receptor-1.
  • HY-14282
    Lanoconazole

    Fungal Infection Inflammation/Immunology
    Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis.
  • HY-121638A
    (5Z,2E)-CU-3

    Apoptosis Cancer
    (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
  • HY-N2022
    Castanospermine

    Glucosidase Cancer
    Castanospermine inhibits all forms of α- and β-glucosidases, especially glucosidase l (required for glucoprotein processing by transfer of mannose and glucose from asparagine-linked lipids).
  • HY-135386
    5β-​Dutasteride

    Drug Metabolite Inflammation/Immunology
    5β-Dutasteride is the S configuration of Dutasteride. 5β-Dutasteride is a potent inhibitor of both 5 alpha-reductase isozymes.
  • HY-N0358
    1,4-Dicaffeoylquinic acid

    1,4-DCQA

    Others Inflammation/Immunology
    1,4-Dicaffeoylquinic acid (1,4-DCQA) is a phenylpropanoid from Xanthii fructus, inhibits LPS-stimulated TNF-α production.
  • HY-N1470
    Plantagoside

    Others Metabolic Disease
    Plantagoside, isolated from the seeds of Plantago asiatica, is a specific and non-competitive inhibitor for jack bean α-mannosidase, with an IC50 of 5 μM.
  • HY-100339
    GSK583

    RIP kinase Endocrinology
    GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM.
  • HY-N1425
    Tiliroside

    Others Metabolic Disease
    Tiliroside, a glycosidic flavonoid, possesses anti-diabetic activities. Tiliroside is a noncompetitive inhibitor of α-amylase with a Ki value of 84.2  μM. Tiliroside inhibits carbohydrate digestion and glucose absorption in the gastrointestinal tract.
  • HY-15466
    CH5132799

    PI3K Cancer
    CH5132799 is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
  • HY-12743A
    K-7174 dihydrochloride

    Others Inflammation/Immunology
    K-7174 dihydrochloride is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
  • HY-129571
    BioE-1115

    Ser/Thr Protease Casein Kinase Metabolic Disease
    BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC50 of ~4 nM. BioE-1115 is also a potent casein kinase inhibitor with an IC50 of ~10 μM.
  • HY-12030
    PIK-90

    PI3K DNA-PK Cancer
    PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
  • HY-13862
    AZD1080

    GSK-3 Neurological Disease
    AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
  • HY-12743
    K-7174

    Others Inflammation/Immunology
    K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
  • HY-15453
    Devimistat

    CPI-613

    Apoptosis Cancer
    Devimistat (CPI-613) is a lipoic acid analog that inhibits pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts mitochondrial metabolism and shows strong antitumor activity.
  • HY-N6602
    α-Solanine

    Apoptosis Cancer
    α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in potatoes, has been observed to inhibit growth and induce apoptosis in cancer cells.
  • HY-10395
    PD173955

    Bcr-Abl Src Apoptosis Cancer
    PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.
  • HY-102040
    Hispidol

    (Z)-Hispidol

    TNF Receptor Inflammation/Immunology
    Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 µM.
  • HY-111365
    TES-1025

    Others Metabolic Disease
    TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13 nM.
  • HY-15846
    CPI-203

    Epigenetic Reader Domain Apoptosis Cancer
    CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).
  • HY-N0629
    Maslinic acid

    Crategolic acid; 2α-Hydroxyoleanolic acid

    NF-κB Bacterial HIV Inflammation/Immunology Cancer
    Maslinic acid can inhibit the DNA-binding activity of NF-κB p65 and abolish the phosphorylation of IκB-α, which is required for p65 activation.
  • HY-122464
    (±)-Jasmonic acid

    Others
    (±)-Jasmonic acid is a plant growth regulator and a derivative of α-linolenic acid. (±)-Jasmonic acid decreases chlorophyll levels in green and etiolated barley leaf segments and inhibits elongation of rice seedlings.
  • HY-10172
    IMD-0354

    IKK2 Inhibitor V

    IKK Cancer
    IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
  • HY-10580
    GSK 3 Inhibitor IX

    6-Bromoindirubin-3'-oxime; BIO; MLS 2052

    GSK-3 CDK Apoptosis Cancer
    GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
  • HY-12338
    ON 146040

    PI3K Bcr-Abl Cancer
    ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
  • HY-116830
    BRD0705

    GSK-3 Cancer
    BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research.
  • HY-107531
    A 1070722

    GSK-3 Cancer
    A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain.
  • HY-14649
    Retinoic acid

    Vitamin A acid; all-trans-Retinoic acid; ATRA

    RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
  • HY-120215
    KT203

    MAGL Metabolic Disease
    KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells.
  • HY-19776
    3α-Aminocholestane

    Phosphatase Cancer
    3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.
  • HY-120177
    KT182

    MAGL Others
    KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.
  • HY-N0694
    Schisantherin A

    Gomisin-C; Schizantherin-A; Wuweizi ester-A

    NF-κB Inflammation/Immunology
    Schisantherin A is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
  • HY-13743
    Roquinimex

    Linomide; FCF89; ABR212616

    TNF Receptor Inflammation/Immunology
    Roquinimex (Linomide; PNU212616; ABR212616) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity; inhibits angiogenesis and reduces the secretion of TNF alpha.
  • HY-126052
    Gnetol

    COX Tyrosinase HDAC Cancer Metabolic Disease
    Gnetol is a phenolic compound isolated from the root of Gnetum ula Brongn. Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities.
  • HY-128598
    MD2-TLR4-IN-1

    Toll-like Receptor (TLR) Cancer Inflammation/Immunology
    MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
  • HY-119940
    MC180295

    (rel)-MC180295

    CDK Cancer
    MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect.
  • HY-12511
    SKF-86002

    p38 MAPK Autophagy Apoptosis Inflammation/Immunology
    SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM).
  • HY-N0014
    Icariin

    Ieariline

    Phosphodiesterase (PDE) PPAR Autophagy Inflammation/Immunology Cardiovascular Disease Cancer
    Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
  • HY-11105
    Pilaralisib analogue

    XL147 analogue

    PI3K Apoptosis Cancer
    Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.
  • HY-10215
    Luminespib

    VER-52296; AUY922; NVP-AUY922

    HSP Autophagy Apoptosis Cancer
    Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
  • HY-12869
    AZD-8835

    PI3K Cancer
    AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively.
  • HY-117771
    DO34

    Others Metabolic Disease
    DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC50 for DAGLβ.
  • HY-14316A
    Tebanicline dihydrochloride

    Ebanicline dihydrochloride; ABT-594 dihydrochloride

    nAChR Neurological Disease
    Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
  • HY-13689
    Go 6983

    Gö 6983; Goe 6983

    PKC Cancer
    Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
  • HY-12340
    ETP-46321

    PI3K Cancer
    ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
  • HY-12437
    BDP5290

    ROCK Cancer
    BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
  • HY-N7637
    Tubuloside B

    Others Cancer
    Tubuloside B, one of the phenylethanoids isolated from the stems of Cistanche salsa, inhibits TNFα-induced apoptosis. Tubuloside B possesses antioxidative effects.
  • HY-B2006
    Fenvalerate

    Phosphatase Bacterial Infection
    Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide.
  • HY-A0077
    Perphenazine

    5-HT Receptor Adrenergic Receptor Dopamine Receptor Histamine Receptor Neurological Disease Endocrinology
    Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
  • HY-14282A
    (Z)-Lanoconazole

    Fungal Infection Inflammation/Immunology
    (Z)-Lanoconazole is the Z configuration of Lanoconazole. Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis.
  • HY-135590
    Raloxifene 4-Monomethyl Ether

    Estrogen Receptor/ERR
    Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6.
  • HY-135584
    Raloxifene 6-Monomethyl Ether

    Estrogen Receptor/ERR
    Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 250 nM and a pIC50 of 6.6.
  • HY-12085
    Apremilast

    CC-10004

    Phosphodiesterase (PDE) Apoptosis TNF Receptor Inflammation/Immunology
    Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
  • HY-10255A
    Sunitinib

    SU 11248

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-N2270
    Chicanine

    p38 MAPK ERK IKK Inflammation/Immunology
    Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity.
  • HY-13469
    Debio 0932

    CUDC-305

    HSP Cancer
    Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively.
  • HY-101438
    Darbufelone

    CI-1004

    Prostaglandin Receptor Leukotriene Receptor Inflammation/Immunology Endocrinology
    Darbufelone is a dual inhibitor of cellular PGF and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50= 0.19 μM) but is much less potent with PGHS-1 (IC50=20 μM).
  • HY-N1987
    Cucurbitacin IIb

    Apoptosis Inflammation/Immunology
    Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α.
  • 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-32018
    Cot inhibitor-2

    MAP3K Cancer
    Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
  • HY-101438A
    Darbufelone mesylate

    CI-1004 mesylate

    Prostaglandin Receptor Leukotriene Receptor Inflammation/Immunology Endocrinology
    Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
  • HY-10527
    Telatinib

    Bay 57-9352

    c-Kit PDGFR VEGFR Cancer
    Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
  • HY-10402
    Losmapimod

    GSK-AHAB; GW856553X; SB856553

    p38 MAPK Autophagy Inflammation/Immunology Cancer
    Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
  • HY-12299
    WH-4-023

    Dual LCK/SRC inhibitor

    Src Cancer
    WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
  • HY-N1200
    Stigmasterol glucoside

    5 alpha Reductase Inflammation/Immunology
    Stigmasterol glucoside is a sterol isolated from P. urinaria with high antioxidant and anti-inflammatory activities, act as an inhibitor of 5α-reductase with an IC50 of 27.2 µM.
  • HY-19708
    KIRA6

    IRE1 Cancer Metabolic Disease Inflammation/Immunology
    KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 µM. KIRA6 can trigger an apoptotic response.
  • HY-10291
    Tarenflurbil

    (R)-Flurbiprofen; MPC7869

    RAR/RXR Autophagy Inflammation/Immunology Neurological Disease
    Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [ 3H]9-cis-RA to RXRα LBD with IC50 of 75 μM.
  • HY-100315
    Tyrosine kinase-IN-1

    VEGFR PDGFR FGFR Cardiovascular Disease
    Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
  • HY-10255
    Sunitinib Malate

    SU 11248 Malate

    PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-10683
    PKI-402

    PI3K mTOR Cancer
    PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
  • HY-16903
    PKC-IN-1

    PKC Inflammation/Immunology
    PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
  • HY-12774
    IC261

    Casein Kinase Apoptosis Cancer
    IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
  • HY-13514
    TG 100713

    PI3K Cancer
    TG 100713 is an inhibitor of PI3K, with IC50s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively.
  • HY-13493
    AC710

    PDGFR c-Kit FLT3 Cancer
    AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
  • HY-17044
    Duvelisib

    IPI-145; INK1197

    PI3K Cancer
    Duvelisib is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
  • HY-15190
    NVP-HSP990

    HSP-990

    HSP Apoptosis Cancer
    NVP-HSP990 is a potent and selective Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, 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-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-N1949
    Homoplantaginin

    TNF Receptor NF-κB Inflammation/Immunology
    Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.
  • HY-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-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-135680
    I-OMe-Tyrphostin AG 538

    I-OMe-AG 538

    IGF-1R Cancer Metabolic Disease
    I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
  • HY-10320
    Doramapimod

    BIRB 796

    p38 MAPK Raf Autophagy Inflammation/Immunology Cancer
    Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM.
  • HY-15174
    Dactolisib Tosylate

    BEZ235 Tosylate; NVP-BEZ 235 Tosylate

    PI3K mTOR Autophagy Cancer
    Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
  • HY-70013
    Abiraterone

    CB-7598

    Cytochrome P450 Cancer
    Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
  • HY-12046
    PIK-93

    PI4K PI3K Virus Protease Cancer
    PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
  • HY-W009783
    1-Deoxymannojirimycin hydrochloride

    HIV Influenza Virus Infection
    1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity.
  • HY-100398
    PF-04979064

    PI3K mTOR Cancer
    PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
  • HY-N7095
    Ceftezole

    CTZ

    Bacterial Antibiotic Infection
    Ceftezole (CTZ) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole (CTZ) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.
  • HY-100207
    CP21R7

    CP21

    GSK-3 Cancer
    CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.
  • HY-15356
    BIO-acetoxime

    BIA

    GSK-3 Apoptosis HSV Infection Inflammation/Immunology Neurological Disease
    BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity.
  • HY-N7096
    Ceftezole sodium

    CTZ sodium

    Bacterial Antibiotic Infection
    Ceftezole sodium (CTZ sodium) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole sodium (CTZ sodium) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.
  • HY-B0089
    Acarbose

    BAY g 5421

    Glucosidase Metabolic Disease
    Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin.
  • HY-12837
    EN460

    Others Others
    EN460 is a small molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1); interacts selectively(IC50=1.9 uM) with the reduced, active form of ERO1α and prevents its reoxidation.
  • HY-N4095
    Brevifolincarboxylic acid

    Aryl Hydrocarbon Receptor Glucosidase Metabolic Disease Inflammation/Immunology
    Brevifolincarboxylic acid is extracted from Polygonum capitatum, has inhibitory effect on the aryl hydrocarbon receptor (AhR). Brevifolincarboxylic acid is an α-glucosidase inhibitor with an IC50 of 323.46 μM.
  • HY-124876
    SynuClean-D

    SC-D

    Others Neurological Disease
    SynuClean-D (SC-D) is an inhibitor of α-synuclein aggregation, disrupts mature amyloid fibrils, prevents fibril propagation, and abolishes the degeneration of dopaminergic neurons in an animal model of Parkinson’s disease.
  • HY-14305A
    BMS-582949 hydrochloride

    p38 MAPK Autophagy Inflammation/Immunology
    BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.
  • HY-10342
    Enzastaurin

    LY317615

    PKC Autophagy Apoptosis Cancer
    Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
  • HY-13812
    QNZ

    EVP4593

    NF-κB TNF Receptor Inflammation/Immunology Neurological Disease
    QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel.
  • HY-13982
    JSH-23

    NF-κB Cancer Metabolic Disease Inflammation/Immunology
    JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
  • HY-W015445
    SD-169

    p38 MAPK Metabolic Disease
    SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
  • HY-107589A
    BIO5192 hydrate

    Integrin Inflammation/Immunology
    BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
  • HY-116830B
    BRD5648

    (R)-BRD0705

    Others Cancer
    BRD5648 ((R)-BRD0705) is an inactive (R)-enantiomer of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).
  • HY-P0224
    N-Formyl-Met-Leu-Phe

    fMLP; N-Formyl-MLF

    TNF Receptor Inflammation/Immunology
    N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.
  • HY-135307
    SSF-109

    Huanjunzuo

    Fungal Infection
    SSF-109 is a broad-spectrum fungicide which has protective activity against plant disease. SSF-109 inhibits the biosynthesis of ergosterol at the 14α-demethylation step in Botrytis cinerea.
  • HY-124108
    Eicosatetraynoic acid

    ETYA

    COX PPAR Others
    Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM.
  • HY-100779
    Rimacalib

    SMP 114

    CaMK Autophagy Metabolic Disease
    Rimacalib (SMP 114) is a Ca 2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.
  • HY-N0042
    Ginsenoside Rc

    Panaxoside Rc

    GABA Receptor TNF Receptor Interleukin Related Cancer Inflammation/Immunology Neurological Disease
    Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
  • HY-17406
    Tolcapone

    Ro 40-7592

    COMT Amyloid-β Neurological Disease
    Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
  • HY-100544
    FLLL32

    STAT JAK Apoptosis Cancer
    FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
  • HY-15244
    Alpelisib

    BYL-719

    PI3K Cancer
    Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.
  • HY-P2657
    Verucopeptin

    HIF/HIF Prolyl-Hydroxylase Proton Pump Endogenous Metabolite Cancer
    Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
  • HY-121750
    CCG-222740

    Ras ROCK Cancer
    CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
  • HY-12034
    WYE-354

    mTOR Autophagy Apoptosis Cancer
    WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2.
  • HY-11068
    SB 239063

    p38 MAPK Autophagy Inflammation/Immunology
    SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD.
  • HY-110282
    S3QEL-2

    Mitochondrial Metabolism Metabolic Disease
    S3QEL-2, a suppressor of superoxide production from mitochondrial complex III, potently and selectively suppresses site IIIQo superoxide production (IC50=1.7 μM). S3QEL-2 does not affect oxidative phosphorylation, and normal electron flux. S3QEL-2 inhibits HIF-1α accumulation.
  • HY-B0135A
    Furosemide sodium

    NKCC Cancer Metabolic Disease
    Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
  • HY-B0135
    Furosemide

    NKCC Metabolic Disease Cancer
    Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
  • HY-N2110
    Phellopterin

    Others Inflammation/Immunology
    Phellopterin is a natural product isolated from P. trifoliata. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
  • HY-N0906
    Ginsenoside Rk3

    NF-κB Inflammation/Immunology Cardiovascular Disease
    Ginsenoside Rk3 is present in the roots Panax notoginseng herbs. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 14.24±1.30 μM in HepG2 cells.
  • HY-N3431
    Kaempferol-7-O-rhamnoside

    Glucosidase Metabolic Disease
    Kaempferol-7-O-rhamnoside, isolated from Chimonanthus nitens Oliv. Leaves, is a potent α-glucosidase activity inhibitor. Kaempferol-7-O-rhamnoside has the potential for diabetes.
  • HY-13223
    Crenolanib

    CP-868596

    FLT3 PDGFR Autophagy Cancer
    Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
  • HY-B0089A
    Acarbose sulfate

    Bay-g 5421 sulfate

    Glucosidase Metabolic Disease
    Acarbose (BAY g 5421) sulfate, antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose sulfate can potentiate the hypoglycemic effects of sulfonylureas or insulin.
  • HY-P1453A
    CMD178 TFA

    STAT Inflammation/Immunology
    CMD178 (TFA) is a lead peptide that consistently reduces the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 (TFA) also is an inhibitor of STAT5 and inhibits Tregcells development.
  • HY-N0191
    Andrographolide

    Andrographis

    NF-κB SARS-CoV Influenza Virus Autophagy Cancer Infection Inflammation/Immunology
    Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
  • HY-N2350
    Cynaropicrin

    MMP NF-κB TNF Receptor Cancer
    Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
  • HY-122521
    Sootepin D

    NF-κB Inflammation/Immunology
    Sootepin D (compound 6), a triterpene from the apical bud of Gardenia sootepensis, inhibits TNF-α-induced NF-κB activity with an IC50 of 8.3μM. Sootepin D has anti-inflammatory activity.
  • HY-10721
    PF-AKT400

    AKT protein kinase inhibitor

    Akt Cancer
    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
  • HY-50094
    Pictilisib

    GDC-0941

    PI3K Autophagy Apoptosis Cancer
    Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
  • HY-12036
    GSK1059615

    PI3K mTOR Apoptosis Cancer
    GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
  • HY-P1872
    OV-1, sheep

    Bacterial Infection
    OV-1, sheep is an alpha-helical antimicrobial ovispirin peptide derived from SMAP29 peptide (sheep), which inhibits several antibiotic-resistant bacterial strains including mucoid and nonmucoid Pseudomonas aeruginosa.
  • HY-135808
    BIZ 114

    NF-κB Inflammation/Immunology
    BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases.
  • HY-N1940
    β-Anhydroicaritin

    Interleukin Related TNF Receptor MMP Inflammation/Immunology
    β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties[1]inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
  • HY-N0722
    Neochlorogenic acid

    trans-5-O-Caffeoylquinic acid

    NF-κB Interleukin Related TNF Receptor COX Inflammation/Immunology Cancer
    Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and IL-1β. Neochlorogenic acid suppresses iNOS and COX-2 protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.
  • HY-15506
    TAK-593

    PDGFR VEGFR Cancer
    TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
  • HY-13049
    Cediranib maleate

    AZD-2171 maleate

    VEGFR Autophagy PDGFR Cancer
    Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  • HY-N2821
    (+)-Afzelechin

    Glucosidase Metabolic Disease
    (+)-Afzelechin, isolated from rhizomes of Bergenia ligulata, is an alpha-glucosidase activity inhibitor with an ID50 (50% inhibition dose) value of 0.13 mM. (+)-Afzelechin can delay the absorption of carbohydrates in food to suppress postprandial hyperglycemia and hyperinsulinemia.
  • HY-P1106
    K41498

    CRFR Cardiovascular Disease
    K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 can be used for hypotension study.
  • HY-114263
    NXT629

    PPAR Cancer
    NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.
  • HY-108847
    Etanercept

    TNF Receptor Inflammation/Immunology
    Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
  • HY-107597
    SU3327

    JNK Metabolic Disease Inflammation/Immunology
    SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase.
  • HY-103489
    PI-273

    PI4K Apoptosis Cancer
    PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.
  • HY-100211
    TAPI-2

    TNF Protease Inhibitor 2

    MMP SARS-CoV Cancer
    TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.
  • HY-W010041
    Scyllo-Inositol

    Amyloid-β Endogenous Metabolite Neurological Disease
    Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and loweres amyloid plaques in an Alzheimer's disease mouse model.
  • HY-N0822
    Shikonin

    C.I. 75535; Isoarnebin 4

    Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV Cancer
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis.
  • HY-114009
    AKR1C1-IN-1

    Others Neurological Disease
    AKR1C1-IN-1 is a potent and selective inhibitor of human 20α-hydroxysteroid dehydrogenase (AKR1C1), with a Ki value of 4 nM for AKR1C1.
  • HY-10205
    Cediranib

    AZD2171

    VEGFR Autophagy PDGFR Cancer
    Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  • HY-126114
    Lupeol acetate

    Others Inflammation/Immunology
    Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.
  • HY-20180
    Pictilisib dimethanesulfonate

    GDC-0941 dimethanesulfonate; GDC-0941 2 MeSO3H salt

    PI3K Autophagy Apoptosis Cancer
    Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
  • HY-16782
    Pexmetinib

    ARRY-614

    p38 MAPK Autophagy Cancer
    Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
  • HY-N6073
    Soyasapogenol A

    Others Inflammation/Immunology
    Soyasapogenol A, a triterpene compound, isolated from the roots of Abrus cantoniensis. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model.
  • HY-12047
    Ponatinib

    AP24534

    Bcr-Abl PDGFR VEGFR FGFR Src Autophagy Cancer
    Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-N7377
    Butyl isobutyl phthalate

    Glucosidase Metabolic Disease
    Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM. Butyl isobutyl phthalate shows a hypoglycemic effect and has the potential for diabetes treatment.
  • HY-101457
    JZP-430

    MAGL Metabolic Disease
    JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).
  • HY-B0006A
    Carvedilol phosphate hemihydrate

    BM 14190 phosphate hemihydrate

    Adrenergic Receptor Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is a non-selective β/α-1 blocker. Carvedilol phosphate hemihydrate inhibits lipid peroxidation with an IC50 of 5 μM. Carvedilol phosphate hemihydrate is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol phosphate hemihydrate is an autophagy inducer that inhibits the NLRP3 inflammasome.
  • HY-D0162
    Malachite green oxalate

    IKK NF-κB Apoptosis Cancer
    Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo.
  • HY-17514
    Itraconazole

    R51211

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects.
  • HY-N6733
    Aphidicolin

    DNA/RNA Synthesis HSV Apoptosis Antibiotic Infection Inflammation/Immunology
    Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering with the activity of DNA polymerase. Aphidicolin is an antibiotic produced by the mold Cephalosporium aphidicola. Aphidicolin is a potent inhibitor of cellular deoxyribonucleic acid synthesis and inhibits the growth of herpes simplex virus. Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line.
  • HY-15271A
    WYE-687 dihydrochloride

    mTOR PI3K Cancer
    WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
  • HY-15310
    Ivermectin

    MK-933

    Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. 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). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
  • HY-P1106A
    K41498 TFA

    CFTR Cardiovascular Disease
    K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 TFA can be used for hypotension study.
  • HY-N0604
    Ginsenoside Rh1

    Prosapogenin A2; Sanchinoside B2; Sanchinoside Rh1

    PPAR TNF Receptor Interleukin Related Endogenous Metabolite Inflammation/Immunology
    Ginsenoside Rh1 (Prosapogenin A2; Sanchinoside B2; Sanchinoside Rh1) is isolated from the root of Panax Ginseng. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
  • HY-N0029
    Forsythoside B

    TNF Receptor NF-κB Inflammation/Immunology
    Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
  • HY-124607
    (R)-BRD3731

    GSK-3 Neurological Disease
    (R)-BRD3731 is a GSK3 inhibitor extracted from patent US20160375006A1, compound example 273, has IC50s of 1.05 and 6.7 μM for GSK3β and GSK3α, respectively.
  • HY-14860A
    1-Deoxynojirimycin hydrochloride

    Duvoglustat hydrochloride

    Glucosidase PI3K Bacterial Antibiotic Infection Metabolic Disease
    1-Deoxynojirimycin hydrochloride (Duvoglustat hydrochloride) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin hydrochloride suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin hydrochloride possesses antihyperglycemic, anti-obesity, and antiviral features.
  • HY-14860
    1-Deoxynojirimycin

    Duvoglustat

    Glucosidase PI3K Metabolic Disease
    1-Deoxynojirimycin (Duvoglustat) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin possesses antihyperglycemic, anti-obesity, and antiviral features.
  • HY-101146
    SF2523

    PI3K Epigenetic Reader Domain DNA-PK Cancer
    SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
  • HY-15509A
    Semapimod tetrahydrochloride

    CNI-1493; CPSI-2364 tetrahydrochloride

    TNF Receptor Interleukin Related p38 MAPK Inflammation/Immunology
    Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.
  • HY-13894
    Tyrphostin AG1296

    AG1296

    PDGFR c-Kit FLT3 Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
  • HY-P1189
    Echistatin

    Integrin Metabolic Disease Inflammation/Immunology
    Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
  • HY-B0006
    Carvedilol

    BM 14190

    Adrenergic Receptor Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
  • HY-17406S
    Tolcapone D7

    Ro 40-7592 D7

    COMT Amyloid-β Neurological Disease
    Tolcapone D7 (Ro 40-7592 D7) is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
  • HY-108264
    TCS 21311

    NIBR3049

    JAK PKC GSK-3 Cancer
    TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.
  • HY-70063
    Buparlisib

    BKM120; NVP-BKM120

    PI3K Apoptosis Cancer
    Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
  • HY-N0907
    Ginsenoside Rg6

    NF-κB Apoptosis Cancer Inflammation/Immunology
    Ginsenoside Rg6 is the component isolated from notoginseng. Ginsenoside Rg6 inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 29.34±2.22 μM in HepG2 cells. Ginsenoside Rg6 also exhibits apoptosis-inducing effect.
  • HY-N7433
    4,6-O-Ethylidene-α-D-glucose

    Ethylidene-glucose

    GLUT Endogenous Metabolite Metabolic Disease
    4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport.
  • HY-13728
    Plevitrexed

    ZD 9331; BGC9331

    Thymidylate Synthase Cancer
    Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical.
  • HY-B0760
    Fenofibric acid

    FNF acid

    PPAR COX Metabolic Disease
    Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
  • HY-12688A
    Succinyl phosphonate trisodium salt

    Endogenous Metabolite Reactive Oxygen Species Cancer Metabolic Disease Neurological Disease
    Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
  • HY-14590
    Kaempferol

    Kempferol; Robigenin

    Estrogen Receptor/ERR Autophagy Mitophagy Apoptosis HIV Parasite Endogenous Metabolite Cancer
    Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.
  • HY-W013636
    2-Ketoglutaric acid

    alpha-Ketoglutaric acid

    Tyrosinase Endogenous Metabolite Others
    2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM).
  • HY-12987
    Pimozide

    R6238

    Dopamine Receptor Adrenergic Receptor STAT Cancer Neurological Disease Endocrinology
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-10204
    OSI-930

    c-Fms c-Kit VEGFR Apoptosis Cancer
    OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.
  • HY-N7599
    Chrysophanol triglucoside

    Phosphatase Glucosidase Metabolic Disease
    Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research.
  • HY-15177
    PF-04691502

    PI3K mTOR Autophagy Cancer
    PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with Kis of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.
  • HY-B0258
    Gemfibrozil

    CI-719

    PPAR Cytochrome P450 Metabolic Disease Cardiovascular Disease
    Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering drug; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
  • HY-N1956
    Rubiadin-1-methyl ether

    NF-κB Metabolic Disease
    Rubiadin-1-methyl ether is a natural anthraquinone isolated from Morinda officinalis How, and inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65.
  • HY-14415
    SR8278

    Others Metabolic Disease
    SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm.
  • HY-N6857
    Armepavine

    NF-κB Inflammation/Immunology
    Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades.
  • HY-107427
    PF-3644022

    MAPKAPK2 (MK2) p38 MAPK Inflammation/Immunology
    PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
  • HY-130240
    GCN2-IN-6

    Eukaryotic Initiation Factor (eIF) Cancer
    GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells).
  • HY-19805
    STO-609

    CaMK AMPK Autophagy Metabolic Disease
    STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
  • HY-P1189A
    Echistatin TFA

    Integrin Metabolic Disease Inflammation/Immunology
    Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
  • HY-111745
    Tyk2-IN-5

    JAK Inflammation/Immunology
    Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model.
  • HY-B1367
    Carbenoxolone disodium

    Gap Junction Protein Infection Inflammation/Immunology
    Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation.
  • HY-N2574
    Gitogenin

    Glucosidase Metabolic Disease
    Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms.
  • HY-15785
    TAS-116

    HSP Cancer
    TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
  • HY-123037
    Triadimefon

    Fungal
    Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis.
  • HY-W013636A
    2-Ketoglutaric acid Sodium

    alpha-Ketoglutaric acid Sodium

    Tyrosinase Endogenous Metabolite Metabolic Disease
    2-Ketoglutaric acid Sodium (Alpha-Ketoglutaric acid Sodium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM).
  • HY-133680
    β-Tocopherol

    Tyrosinase Metabolic Disease
    β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol.
  • HY-107222
    Lysionotin

    Others Inflammation/Immunology
    Lysionotin is a flavonoid isolated from few flower lysionotus herbs. Lysionotin efficiently inhibit α-Toxin (a pore-forming protein) expression and shows significant protection against S. aureus in vitro and in vivo. Lysionotin has the potential for the treatment of S. aureus induced pneumonia.
  • HY-10343
    Sotrastaurin

    AEB071

    PKC Inflammation/Immunology Cancer
    Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.
  • HY-N1990
    Gypenoside XLIX

    PPAR Inflammation/Immunology Cardiovascular Disease
    Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
  • HY-124607B
    BRD3731

    GSK-3 Neurological Disease
    BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 can be used for the research of a mood disorder, post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorder.
  • HY-120272
    SMAP-2

    DT-1154

    Phosphatase Cancer
    SMAP-2 (DT-1154) is an orally bioavailable phosphatase 2A (PP2A) activator which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A. SMAP-2 (DT-1154) inhibits the growth of KRAS-mutant lung cancers .
  • HY-15245
    GSK2636771

    PI3K Cancer
    GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
  • HY-101569
    LXS196

    PKC Cancer
    LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. LXS196 has the potential for uveal melanoma research.
  • HY-125263
    OP-1074

    Estrogen Receptor/ERR Cancer
    OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
  • HY-N0316
    Mollugin

    Others Cancer
    Mollugin is a major bioactive component isolated from Rubia cordifolia L.. Mollugin has an anti-cancer therapeutic effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 via the p38-Smad signaling pathway .
  • HY-121538
    CUDA

    Epoxide Hydrolase PPAR Cardiovascular Disease
    CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
  • HY-10230
    Midostaurin

    PKC412; CGP 41251

    PKC Cancer
    Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
  • HY-12330
    AZD8186

    PI3K Cancer
    AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC5050=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
  • HY-113756A
    Latanoprost acid

    Prostaglandin Receptor Inflammation/Immunology
    Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.
  • HY-13241
    Ralimetinib dimesylate

    LY2228820 dimesylate

    p38 MAPK Autophagy Apoptosis Cancer Inflammation/Immunology
    Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
  • HY-13335
    PKCβ inhibitor 1

    PKC Apoptosis Cancer
    PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
  • HY-107390A
    AX-024 hydrochloride

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-107390
    AX-024

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-N1356
    Reticuline

    JAK STAT NF-κB Inflammation/Immunology
    Reticuline, isolated from Litsea cubeba, shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3.
  • HY-131081
    γ-Amanitin

    DNA/RNA Synthesis ADC Cytotoxin Cancer
    γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin (HY-19610) and β-Amanitin (HY-125586).
  • HY-N6775
    Sonolisib

    PX-866

    PI3K Cancer
    Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.
  • HY-12185
    BRD7389

    Ribosomal S6 Kinase (RSK) Cancer Metabolic Disease
    BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells.
  • HY-120110
    IOX4

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Neurological Disease
    IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2.
  • HY-12235
    PI-3065

    PI3K Inflammation/Immunology Cancer
    PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.
  • HY-107139
    JNJ-10229570

    Melanocortin Receptor Endocrinology
    JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
  • HY-114855
    BT2

    Bcl-2 Family Metabolic Disease
    BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM.
  • 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-50905
    Dovitinib

    CHIR-258; TKI258

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
  • HY-112613
    UCB9608

    PI4K Inflammation/Immunology
    UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent.
  • HY-N0041
    Ginsenoside Rb3

    Gypenoside IV

    NF-κB COX NO Synthase Cancer Inflammation/Immunology
    Ginsenoside Rb3 is extracted from steamed Panax notoginseng. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
  • HY-N0633
    Muscone

    Interleukin Related TNF Receptor NF-κB NOD-like Receptor (NLR) Inflammation/Immunology Cardiovascular Disease
    Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate.
  • HY-19306
    SB-267268

    Integrin Cancer
    SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
  • HY-100513A
    Dehydroaltenusin

    Apoptosis DNA/RNA Synthesis Cancer
    Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM). Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.
  • HY-N0515
    Ophiopogonin D

    PPAR NF-κB Calcium Channel Inflammation/Immunology Cardiovascular Disease
    Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
  • HY-112461A
    NF449 octasodium

    P2X Receptor Cardiovascular Disease
    NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs.
  • HY-10571A
    Delavirdine mesylate

    U 90152 mesylate; BHAP-U 90152 mesylate

    HIV Reverse Transcriptase Infection
    Delavirdine (U 90152; BHAP-U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
  • HY-10571
    Delavirdine

    U 90152; BHAP-U 90152

    HIV Reverse Transcriptase Infection
    Delavirdine (U 90152; BHAP-U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
  • HY-114414
    HDACs/mTOR Inhibitor 1

    HDAC mTOR Apoptosis Cancer
    HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo.
  • HY-109068
    Parsaclisib

    INCB050465

    PI3K Cancer
    Parsaclisib (INCB050465) is a potent and selective PI3Kδ inhibitor, with an IC50 of 1 nM at 1 mM ATP, and shows appr 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.
  • HY-19962
    Paxalisib

    GDC-0084

    PI3K mTOR Cancer
    Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
  • HY-107526
    NFPS

    GlyT Neurological Disease
    NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively. NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion.
  • HY-10406
    Talmapimod

    SCIO-469

    p38 MAPK Cancer
    Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
  • HY-10207
    Dovitinib lactate

    CHIR-258 lactate; TKI-258 lactate

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
  • HY-126307
    Urolithin B

    NF-κB JNK ERK Akt AMPK Endogenous Metabolite Inflammation/Immunology
    Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
  • HY-15180
    Buparlisib Hydrochloride

    BKM120 Hydrochloride; NVP-BKM120 Hydrochloride

    PI3K Apoptosis Cancer
    Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
  • HY-16526
    Pilaralisib

    XL-147; SAR245408

    PI3K Cancer
    Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
  • HY-50904
    Nintedanib

    BIBF 1120

    PDGFR VEGFR FGFR Cancer
    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
  • HY-12868
    Bimiralisib

    PQR309

    PI3K mTOR Cancer
    Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
  • HY-10456
    TAK-715

    p38 MAPK Casein Kinase Inflammation/Immunology
    TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.
  • HY-110177
    SP-100030

    NF-κB Inflammation/Immunology
    SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA).
  • HY-103463
    SA57

    FAAH MAGL Neurological Disease
    SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases.
  • HY-129624A
    Bisindolylmaleimide VIII acetate

    Ro 31-7549 acetate; Bis VIII acetate

    PKC Apoptosis Cancer Inflammation/Immunology
    Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
  • HY-N7626
    Eleutherol

    Fungal Glucosidase Infection
    Eleutherol is a naphthalene isolated from E. americana with antifungal activities. Eleutherol is against yeasts Candida albicans, C. tropicalis, Saccharomyces cerevisiae and Cryptococcus neoformans with MIC values between 7.8 µg/mL and 250 µg/mL. Eleutherol inhibits α-glucosidase function with an IC50>1.00 mM.
  • HY-130252
    YQ128

    NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology
    YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity.
  • HY-11106
    Nintedanib esylate

    BIBF 1120 esylate

    PDGFR VEGFR FGFR Cancer
    Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
  • HY-10681
    Gedatolisib

    PKI-587; PF-05212384

    PI3K mTOR Cancer
    Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 is equally effective in both complexes of mTOR, mTORC1 and mTORC2.
  • HY-18754
    FR 167653 free base

    p38 MAPK Autophagy Endocrinology
    FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
  • HY-133897
    (Rac)-Indoximod

    1-Methyl-DL-tryptophan; (Rac)-NLG-8189

    Indoleamine 2,3-Dioxygenase (IDO) Cancer Inflammation/Immunology
    (Rac)-Indoximod (1-Methyl-DL-tryptophan) is an indoleamine 2,3-dioxygenase (IDO) inhibitor. Co-treatment with IFN-γ and (Rac)-Indoximod markedly reduces the activity of human cardiac myofibroblasts (hCMs) expressing α-SMA and induces apoptosis through up-regulating the IRF-1, Fas, and FasL genes.
  • HY-10987A
    ENMD-2076

    Aurora Kinase FLT3 VEGFR FGFR PDGFR Src Apoptosis Cancer
    ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
  • HY-112443
    AZD3458

    PI3K Cancer Metabolic Disease Inflammation/Immunology
    AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively.
  • HY-111424
    BDP9066

    Ras Cancer
    BDP9066 is a potent and selective myotonic dystrophy-related Cdc42-binding kinase MRCK inhibitor with an IC50 of 64 nM for MRCKβ in SCC12 cells, Ki values of 0.0136 nM and 0.0233 nM for MRCKα/β in house determinations, respectively. BDP9066 has therapeutic effect on skin cancer by reducing substrate phosphorylation.
  • HY-15505
    RWJ-67657

    JNJ 3026582

    p38 MAPK Cancer Inflammation/Immunology Cardiovascular Disease
    RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity.
  • HY-N6704
    Enniatin A1

    ERK Apoptosis Cancer
    Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes.
  • HY-13898
    Taselisib

    GDC-0032; RG-7604

    PI3K Cancer
    Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
  • HY-14166
    MK-886

    L 663536

    FLAP Leukotriene Receptor PPAR Apoptosis Cancer
    MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.
  • HY-113952
    Actinonin

    (-)-Actinonin

    Aminopeptidase Bacterial MMP Apoptosis Antibiotic Cancer Infection
    Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.
  • HY-111508
    PI3K/mTOR Inhibitor-2

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.
  • HY-16438
    RRx-001

    Apoptosis Parasite Cancer Infection Inflammation/Immunology
    RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.
  • HY-13531
    AS-604850

    PI3K Cancer
    AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively.
  • HY-10209A
    Masitinib mesylate

    AB-1010 mesylate

    c-Kit PDGFR Src FGFR Apoptosis Cancer
    Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.
  • HY-P1280
    Margatoxin

    Potassium Channel Neurological Disease
    Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research.
  • HY-19269
    FK706

    Elastase Inflammation/Immunology
    FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect.
  • HY-10230S
    Midostaurin-D5

    PKC412-D5; CGP 41251-D5

    Others Cancer
    Midostaurin-D5 (PKC412-D5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
  • HY-101762
    TyK2-IN-2

    JAK Phosphodiesterase (PDE) Inflammation/Immunology
    TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC50 of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases.
  • HY-10209
    Masitinib

    AB1010

    c-Kit PDGFR Src FGFR FAK Apoptosis Cancer
    Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.
  • HY-N7510
    12-O-Methylcarnosic acid

    12-Methoxycarnosic acid

    5 alpha Reductase Cancer Infection
    12-O-Methylcarnosic acid (12-Methoxycarnosic acid), a diterpene carnosic acid isolated from the acetone extract of Salvia microphylla, is an active constituent of 5α-reductase inhibition with an IC50 value of 61.7 μM. 12-O-Methylcarnosic acid inhibits proliferation in LNCaP cells. 12-O-Methylcarnosic acid has antioxidant, anti-cancer and antimicrobial activity.
  • HY-N7056
    4'-Hydroxychalcone

    Proteasome Cancer Inflammation/Immunology
    4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.
  • HY-N7683
    Prunetin 5-O-β-D-glucopyranoside

    Glucosidase Metabolic Disease
    Prunetin 5-O-β-D-glucopyranoside is an isoflavone isolated from extracts of Potentilla astracanica. Prunetin 5-O-β-D-glucopyranoside is a potent and uncompetitive inhibitor of α-glucosidase, with an IC50 of 56.05 μg/mL. Prunetin 5-O-β-D-glucopyranoside can be used for the research of type-2 diabetes.
  • HY-18754A
    FR 167653

    FR 167653 sulfate

    p38 MAPK Autophagy Endocrinology
    FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
  • HY-10295
    SB 202190

    p38 MAPK Autophagy Apoptosis Ferroptosis Cancer Neurological Disease
    SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits.
  • HY-10811
    GNE-493

    PI3K mTOR Cancer
    GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
  • HY-10987
    ENMD-2076 Tartrate

    Aurora Kinase FLT3 VEGFR FGFR Src PDGFR Apoptosis Cancer
    ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
  • HY-15900
    Voxtalisib

    XL765; SAR245409

    PI3K mTOR Cancer
    Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.
  • HY-N2278
    Kushenol A

    Leachianone E

    Tyrosinase Glucosidase Cancer
    Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively. Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase. Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging.
  • HY-50673
    Dactolisib

    BEZ235; NVP-BEZ235

    PI3K mTOR Autophagy Cancer
    Dactolisib (BEZ235) is a dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
  • HY-10115
    PI-103

    PI3K mTOR DNA-PK Autophagy Apoptosis Cancer
    PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.
  • HY-N3807
    Enniatin B1

    Acyltransferase ERK NF-κB Cancer Infection Cardiovascular Disease
    Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
  • HY-120179A
    LP-922761 hydrate

    Others Neurological Disease
    LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
  • HY-10115A
    PI-103 Hydrochloride

    PI3K mTOR DNA-PK Autophagy Apoptosis Cancer
    PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.
  • HY-120179
    LP-922761

    Others Neurological Disease
    LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
  • 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-13334
    BGT226 maleate

    NVP-BGT226 maleate

    PI3K mTOR Autophagy Apoptosis Cancer
    BGT226 maleate (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.
  • HY-107818
    4-Hydroxychalcone

    NF-κB Inflammation/Immunology Cardiovascular Disease
    4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice.
  • HY-10405
    Pamapimod

    Ro4402257; R1503

    p38 MAPK Autophagy Inflammation/Immunology
    Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.
  • HY-126047B
    (R)-(+)-Anatabine

    NF-κB Amyloid-β nAChR Inflammation/Immunology Neurological Disease
    (R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
  • HY-A0036
    Bazedoxifene acetate

    TSE-424 acetate

    Estrogen Receptor/ERR Cancer
    Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-N0043
    Ginsenoside Rd

    Gypenoside VIII

    NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease Cancer
    Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
  • HY-A0031
    Bazedoxifene

    TSE-424

    Estrogen Receptor/ERR Cancer
    Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-12987S
    Pimozide D4

    R6238 D4

    Dopamine Receptor Adrenergic Receptor STAT Cancer Endocrinology Neurological Disease
    Pimozide D4 (R6238 D4) is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-10206
    Amuvatinib

    MP470; HPK 56

    c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Apoptosis Cancer
    Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
  • HY-N0173
    Cinchonidine

    α-Quinidine

    Serotonin Transporter Parasite Infection
    Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
  • HY-A0031A
    Bazedoxifene hydrochloride

    TSE-424 hydrochloride

    Estrogen Receptor/ERR Cancer
    Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-17356
    Fenofibrate

    PPAR Cytochrome P450 Autophagy Cardiovascular Disease Cancer
    Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
  • HY-122537A
    Arotinolol

    Adrenergic Receptor 5-HT Receptor Cardiovascular Disease
    Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
  • HY-117800
    BJE6-106

    B106

    PKC Apoptosis Cancer Inflammation/Immunology
    BJE6-106 (B106) is a potent, selective 3 rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM). BJE6-106 (B106) induces caspase-dependent apoptosis. BJE6-106 (B106) possesses tumor-specific effect.
  • HY-B0850
    Difenoconazole

    Fungal
    Difenoconazole is a broad-spectrum triazole fungicide 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. Difenoconazole inhibits the growth of F. graminearum isolates in vitro (EC50s = 1.69-19.6 mg/L for mycelial growth). Difenoconazole also inhibits growth of A. sonali, F. fulva, B. cinerea, and R. solani (EC50s = 0.131 mg/L, 0.069 mg/L, 0.297 mg/L, and 0.252 mg/L, respectively).
  • HY-13866
    Ro 31-8220 mesylate

    Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate

    PKC Neurological Disease Cardiovascular Disease Cancer
    Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
  • HY-108601A
    Ro 32-0432 hydrochloride

    PKC Inflammation/Immunology Neurological Disease
    Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
  • HY-13866A
    Ro 31-8220

    Bisindolylmaleimide IX

    PKC Neurological Disease Cardiovascular Disease
    Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
  • HY-103637A
    Vimirogant hydrochloride

    VTP-43742 hydrochloride

    ROR Inflammation/Immunology
    Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research.
  • HY-19918A
    Anatabine dicitrate

    NF-κB Amyloid-β nAChR Inflammation/Immunology Neurological Disease
    Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
  • HY-124151
    Adenosine-2'-monophosphate

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

    Adenosine Receptor Endogenous Metabolite Neurological Disease
    Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
  • HY-10195B
    Ruboxistaurin hydrochloride

    LY 333531 hydrochloride

    PKC Metabolic Disease
    Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is a selective and ATP-competitive PKCβ inhibitor with IC50s of 4.7 nM and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin hydrochlorid shows less potent inhibition on PKCη (IC50, 52 nM), PKCα (IC50, 360 nM), PKCγ (IC50, 300 nM), PKCδ (IC50, 250 nM), and has no effect on PKCζ (IC50, >100 μM).
  • HY-16585
    VS-5584

    SB2343

    PI3K mTOR Cancer
    VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC50s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as mTORC1.
  • HY-N2535
    Coniferaldehyde

    Ferulaldehyde

    Others Inflammation/Immunology
    Coniferaldehyde (Ferulaldehyde), isolated from the ethanol extract of Vitex rotundifolia fruits, is an effective inducer of heme oxygenase-1 (HO-1). Coniferaldehyde exerts anti-inflammatory properties in response to LPS. Coniferaldehyde inhibits LPS-induced apoptosis through the PKCα/β II/Nrf-2/HO-1 dependent pathway in RAW264.7 macrophage cells.
  • HY-100490B
    Rilmenidine phosphate

    Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy Cardiovascular Disease
    Rilmenidine phosphate, an antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate is also an alpha 2-adrenoceptor agonist. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
  • HY-13440
    AMG 511

    PI3K Cancer
    AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.
  • HY-107417
    Hypothemycin

    VEGFR MEK FLT3 PDGFR ERK Cancer
    Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.
  • HY-10297
    Omipalisib

    GSK2126458; GSK458

    PI3K mTOR Autophagy Cancer
    Omipalisib (GSK2126458) is an orally active and highly selective inhibitor of PI3K with Kis of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. Omipalisib has anti-cancer activity.
  • HY-10108
    LY294002

    PI3K Casein Kinase DNA-PK Autophagy Apoptosis Cancer Infection
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
  • HY-12513
    Samotolisib

    LY3023414

    PI3K DNA-PK mTOR Autophagy Cancer
    Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations.
  • HY-N0811
    Anemarsaponin B

    NO Synthase COX NF-κB Inflammation/Immunology
    Anemarsaponin B is a steroidal saponin isolated from the rhizomes of A. asphodeloides (Liliaceae). Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
  • HY-10256A
    SB 203580 hydrochloride

    RWJ 64809 hydrochloride

    p38 MAPK Autophagy Mitophagy Inflammation/Immunology Cancer
    SB 203580 hydrochloride (RWJ 64809 hydrochloride) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy and mitophagy activator.
  • HY-124662
    IHVR-19029

    Glucosidase Infection
    IHVR-19029 is a potent endoplasmic reticulum (ER) α-glucosidases I and II inhibitor, with an IC50 of 0.48 μM for ER a-glucosidase I. IHVR-19029 efficiently blocks the replication of several hemorrhagic fever viruses, such as Dengue virus (DENV), Ebola virus (EBOV) and Rift Valley fever virus. The combination of IHVR-19029 with Favipiravir (HY-14768) improves the antiviral efficacy.
  • HY-113466
    4-Hydroxynonenal

    4-HNE

    Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite Cancer Neurological Disease Cardiovascular Disease
    4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
  • HY-106387
    Dexanabinol

    HU-211

    NF-κB TNF Receptor Interleukin Related Neurological Disease
    Dexanabinol (HU-211) is an artificially synthesized cannabinoid derivative and lacks cannabimimetic effects. Dexanabinol exhibits not only the antioxidant and neuroprotective activities in brain but also anti-inflammatory activity by inhibiting NF-κB and decreasing cytokines such as TNFα and interleukin-6, which could ensure the integrity of BBB and reduce cell apoptosis and death. Dexanabinol is widely used in head injury or stroke treatment and has been shown to be safe in animals and humans.
  • HY-100490
    Rilmenidine

    Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy Cardiovascular Disease
    Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
  • HY-103045
    CMPD101

    PKC ROCK Cardiovascular Disease
    CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
  • HY-18980
    Rottlerin

    Mallotoxin; NSC 56346; NSC 94525

    PKC Autophagy Apoptosis Infection Cancer
    Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation.
  • HY-N2056
    11-​Keto-​beta-​boswellic acid

    11-Keto-β-boswellic acid

    Lipoxygenase Leukotriene Receptor NF-κB Cancer
    11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.
  • HY-N6979
    Crustecdysone

    20-Hydroxyecdysone

    Caspase Autophagy Endogenous Metabolite Cardiovascular Disease
    Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Cyanotis arachnoides C.B.Clarke which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP. Crustecdysone exhibits regulatory or protective roles in the cardiovascular system. Crustecdysone is an active metabolite of Ecdysone (α-Ecdysone; HY-N0179)
  • HY-W011266
    JNJ-10198409

    PDGFR Cancer
    JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM).
  • HY-N0619
    Mulberroside A

    TNF Receptor Interleukin Related Tyrosinase Inflammation/Immunology
    Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
  • HY-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-10256
    SB 203580

    RWJ 64809

    p38 MAPK Autophagy Mitophagy Inflammation/Immunology Cancer
    SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.
  • HY-19744
    T6167923

    MyD88 Inflammation/Immunology
    T6167923 is a potent and selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with an 50 of 2.7  μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.
  • HY-14913
    Apricitabine

    SPD754; AVX754

    Nucleoside Antimetabolite/Analog HIV DNA/RNA Synthesis Infection
    Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2].
  • HY-N0226
    Epiberberine

    AChE Beta-secretase Metabolic Disease Neurological Disease
    Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease. Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberinecan be used for the research of diabetic disease.
  • HY-N0226A
    Epiberberine chloride

    AChE Beta-secretase Reactive Oxygen Species Metabolic Disease Neurological Disease
    Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberine has the potential effect in the research of diabetic disease.
  • HY-32329
    Setiptiline

    Org-8282

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
  • HY-19357
    E3330

    APX-3330

    DNA/RNA Synthesis Cancer
    E3330 (APX-3330) is a direct, orally active and selective AP endonuclease 1 (APE1; REF-1) inhibitor, which suppresses NF-κB DNA-binding activity. E3330 (APX-3330) blocks TNF-α-induced activation of IL-8 production in liver cancer cell lines. E3330 (APX-3330) shows anticancer properties, such as inhibition of cancer cell growth and migration.
  • HY-N3945
    Glaucine

    O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396

    Phosphodiesterase (PDE) Calcium Channel Adrenergic Receptor Dopamine Receptor Influenza Virus Infection Inflammation/Immunology
    Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca 2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities.
  • HY-15648F
    GSK-J4 hydrochloride

    Histone Demethylase Cancer
    GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1.
  • HY-N0617
    Sanggenon C

    NF-κB Cancer Inflammation/Immunology Cardiovascular Disease
    Sanggenon C is a flavanone Diels-Alder adduct compound, which is isolated from the root bark of Morus cathayana. Sanggenon C exerts protective effects against cardiac hypertrophy and fibrosis via suppression of the calcineurin/NFAT2 pathway. Sanggenon C inhibits inducible nitric oxide synthase expression in RAW264.7 cells, and tumor necrosis factor-α-stimulated cell adhesion and vascular cell adhesion molecule-1 expression, by suppressing NF-κB activity. Sanggenon C possesses antioxidant, anti-inflammatory activities and inhibits Pancreatic lipase (PL) with the an IC50 of 3.00 μM.
  • HY-13522
    Fimepinostat

    CUDC-907

    PI3K HDAC Apoptosis Cancer
    Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
  • HY-B0498
    Bindarit

    AF2838

    CCR Inflammation/Immunology Neurological Disease Cancer Endocrinology
    Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity.
  • HY-19974
    TAK-220

    CCR HIV Infection Endocrinology
    TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
  • 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-108359
    Alsterpaullone

    9-Nitropaullone; NSC 705701

    CDK GSK-3 Cancer
    Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders.
  • 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-13246
    Apitolisib

    GDC-0980; GNE 390; RG 7422

    PI3K mTOR Apoptosis Cancer
    Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
  • HY-15346
    Copanlisib

    BAY 80-6946

    PI3K Cancer
    Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.
  • HY-15346A
    Copanlisib dihydrochloride

    BAY 80-6946 dihydrochloride

    PI3K Cancer
    Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity.
  • HY-113953
    Z-Asp-CH2-DCB

    Caspase Inflammation/Immunology
    Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.
  • HY-15648B
    GSK-J4

    Histone Demethylase Apoptosis Cancer
    GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
  • HY-N5072
    Desmethylglycitein

    4',6,7-Trihydroxyisoflavone

    CDK PI3K PKC Cancer
    Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
  • 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.