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Results for "All sglt2 Inhibitors" in MCE Product Catalog:

126

Inhibitors & Agonists

114

Screening Libraries

2

Dye Reagents

1

Biochemical Assay Reagents

7

Peptides

8

MCE Kits

1

Inhibitory Antibodies

31

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-10451S
    Canagliflozin D4

    SGLT Cancer Metabolic Disease
    Canagliflozin D4 is a deuterium labeled Canagliflozin. Canagliflozin is a selective SGLT2 inhibitor.
  • HY-10450S
    Dapagliflozin D5

    BMS-512148 D5

    SGLT Cancer Metabolic Disease
    Dapagliflozin D5 (BMS-512148 D5) is a deuterium labeled Dapagliflozin. Dapagliflozin is a competitive SGLT2 inhibitor.
  • HY-15409
    Empagliflozin

    BI 10773

    SGLT Metabolic Disease
    Empagliflozin is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2.
  • HY-17604
    Bexagliflozin

    EGT1442; EGT0001442; THR-1442

    SGLT Metabolic Disease
    Bexagliflozin is a potent and selective SGLT2 inhibitor with IC50 value of 5.6 μM /2 nM in SGLT1 /SGLT2 respectively.
  • HY-14902
    Tofogliflozin

    CSG452

    SGLT Metabolic Disease
    Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.
  • HY-109092
    Licogliflozin

    LIK066

    SGLT Metabolic Disease Inflammation/Immunology
    Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor.
  • HY-15461
    Ertugliflozin

    PF-04971729

    SGLT Metabolic Disease
    Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2. Has the potential for the treatment of type 2 diabetes mellitus.
  • HY-109018
    Velagliflozin

    SGLT Metabolic Disease
    Velagliflozin is an orally available sodium-glucose cotransporter 2 (SGLT2) inhibitor, with anti-diabetic activity.
  • HY-15516
    Sotagliflozin

    LX-4211; LP-802034

    SGLT Metabolic Disease
    Sotagliflozin (LX-4211) is a potent dual SGLT2/1 inhibitor. Antidiabetic agents.
  • HY-15461A
    Ertugliflozin L-pyroglutamic acid

    PF-04971729 L-pyroglutamic acid

    SGLT Metabolic Disease
    Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2. Has the potential for the treatment of type 2 diabetes mellitus.
  • HY-13413
    Tofogliflozin (hydrate)

    CSG-452 hydrate

    SGLT Reactive Oxygen Species Metabolic Disease
    Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells.
  • HY-101782
    HSK0935

    HSK-0935; HSK 0935

    SGLT Metabolic Disease
    HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic activities.
  • HY-14894
    Ipragliflozin

    ASP1941

    SGLT Metabolic Disease
    Ipragliflozin (ASP1941) is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
  • HY-14894A
    Ipragliflozin L-Proline

    SGLT Metabolic Disease
    Ipragliflozin (L-Proline) is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
  • HY-I0383
    Canagliflozin hemihydrate

    JNJ 28431754 hemihydrate

    SGLT Cancer Metabolic Disease
    Canagliflozin hemihydrate (JNJ28431754 hemihydrate) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.
  • HY-10451
    Canagliflozin

    JNJ 28431754

    SGLT Metabolic Disease Cancer
    Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.
  • HY-123797
    KGA-2727

    SGLT Metabolic Disease
    KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 has antidiabetic efficacy.
  • HY-10450
    Dapagliflozin

    BMS-512148

    SGLT Metabolic Disease Cancer
    Dapagliflozin (BMS-512148), a new type of drug used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine. Dapagliflozin induces HIF1 expression and attenuates renal IR injury.
  • HY-101122
    LX2761

    SGLT Metabolic Disease
    LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract.
  • HY-17638
    Mizagliflozin

    DSP-3235 free base; KGA-3235 free base; GSK-1614235 free base

    SGLT Metabolic Disease
    Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic drug that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.
  • HY-14945
    Remogliflozin etabonate

    GSK189075

    SGLT Metabolic Disease
    Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a prodrug based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.
  • HY-N0142
    Phloretin

    NSC 407292; RJC 02792

    SGLT Endogenous Metabolite Metabolic Disease Cancer
    Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Prunus mandshurica, has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively.Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation.
  • HY-10450A
    Dapagliflozin ((2S)-1,2-propanediol, hydrate)

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

    SGLT Cancer Metabolic Disease
    Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of drug used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine. Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury.
  • HY-D0987
    Stains-All

    Others Others
    Stains-All is a cationic carbocyanine dye.
  • HY-W004500
    All-trans-retinal

    Endogenous Metabolite Others
    All-trans-retinal is a one of the major vitamin A metabolites in the retina. In physiological conditions, all-trans-RAL is regenerated to the visual chromophore, 11-cis-retinal.
  • HY-N7495
    all-trans-Anhydro Retinol

    Anhydrovitamin A

    Endogenous Metabolite Metabolic Disease
    all-trans-Anhydro Retinol (Anhydrovitamin A) is a metabolite of Vitamin A. all-trans-Anhydro Retinol is used in synthetic multivitamin preparations.
  • HY-107494A
    all-trans-4-Oxoretinoic acid

    All-trans 4-Keto Retinoic Acid

    Endogenous Metabolite Metabolic Disease
    all-trans-4-Oxoretinoic acid, an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-136175
    SNDX-5613

    Epigenetic Reader Domain Cancer
    SNDX-5613 is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).
  • HY-A0143
    Dihomo-γ-linolenic acid

    All-cis-8,11,14-Eicosatrienoic acid

    Endogenous Metabolite Cancer Inflammation/Immunology Cardiovascular Disease
    Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system.
  • HY-N2302
    Fucoxanthin

    All-trans-Fucoxanthin

    Others Cancer Metabolic Disease Inflammation/Immunology
    Fucoxanthin is a marine carotenoid and shows anti-obesity, anti-diabetic, anti-oxidant, anti-inflammatory and anticancer activities.
  • HY-130640
    (S,R,S)-AHPC-Me-C7 ester

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-Me-C7 ester is a E3 ligase ligand-linker conjugate used to synthesise BCL-XL PROTAC degraders.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-B1960
    Canthaxanthin

    E 161g; All-trans-Canthaxanthin

    Reactive Oxygen Species Cancer Inflammation/Immunology
    Canthaxanthin is a red-orange carotenoid with various biological activities, such as antioxidant, antitumor properties.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-D0889
    Glycylglycine

    Endogenous Metabolite Metabolic Disease
    Glycylglycine is the simplest of all peptides and could function as a gamma-glutamyl acceptor.
  • HY-13022
    CC-401 hydrochloride

    CC401 HCl

    JNK Cancer
    CC-401 hydrochloride is a potent inhibitor of all three forms of JNK with Ki of 25 to 50 nM.
  • HY-13022A
    CC-401

    JNK Cancer
    CC-401 is a potent inhibitor of all three forms of JNK with Ki of 25 to 50 nM.
  • HY-P9906
    Bevacizumab

    Anti-Human VEGF, Humanized Antibody

    VEGFR Cancer
    Bevacizumab, a humanized monoclonal antibody, specifically binds to all VEGF-A isoforms with high affinity.
  • HY-113159
    Docosapentaenoic acid 22n-3

    Endogenous Metabolite Metabolic Disease
    Docosapentaenoic acid (22n-3) is a component of phospholipids found in all animal cell membranes.
  • HY-W017770
    Ademetionine disulfate tosylate

    Others Neurological Disease
    Ademetionine disulfate tosylate is the principal biological methyl donor synthesized in all mammalian cells but most abundantly in the liver.
  • HY-19373
    RWJ-445167

    3DP-10017

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

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-14531
    Talarozole

    R115866

    RAR/RXR Cytochrome P450 Autophagy Inflammation/Immunology
    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
  • HY-107383
    Tetrahydrobiopterin

    Sapropterin

    NO Synthase Endogenous Metabolite Inflammation/Immunology
    Tetrahydrobiopterin is a cofactor of the aromatic amino acid hydroxylases enzymes and also acts as an essential cofactor for all nitric oxide synthase (NOS) isoforms.
  • HY-121324
    Prometryn

    Others Others
    Prometryn could improves the control of all weed species and increased lint yield compared with the systems.
  • HY-12808
    STF-118804

    Nampt Apoptosis Cancer
    STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.
  • HY-B1216
    Oxeladin citrate

    Others Inflammation/Immunology
    Oxeladin citrate is a cough suppressant, is a highly potent and effective drug used to treat all types of cough of various etiologies.
  • HY-14817
    Indeglitazar

    PPM 204

    PPAR Metabolic Disease
    Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ.
  • HY-N2318
    Podocarpic acid

    TRP Channel Neurological Disease
    Podocarpic acid is a natural product, which has the best all-round positive effect and acts as a novel TRPA1 activator.
  • HY-Y0258
    Benzocaine

    Sodium Channel Neurological Disease
    Benzocaine shares a common receptor with all othe rLAs in the voltage-gated Na + channel, with an IC50 of 0.8 mM tested with a potential of +30 mV.
  • HY-12640
    Pyrantel pamoate

    Pyrantel embonate

    Parasite Antibiotic Infection
    Pyrantel pamoate is a deworming agent in the treatment of hookworms (all species) and roundworms in domesticated animal; acts as a depolarizing neuromuscular blocking agent.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

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

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-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.
  • 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-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-14802
    Talarozole R enantiomer

    (R)-Talarozole

    Cytochrome P450 Cancer
    Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.
  • HY-113325
    NADP

    Endogenous Metabolite Others
    NADP is nicotinamide adenine dinucleotide phosphate, acting as a key cofactor for electron transfer in the metabolism of all organisms, being alternately oxidized (NADP +) and reduced (NADPH).
  • HY-B0216
    Ethynyl Estradiol

    17α-Ethynylestradiol; Ethynylestradiol

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
  • HY-N0913
    Manninotriose

    Others Others
    Manninotriose is a novel and important player in the RFO(Raffinose family oligosaccharides) metabolism of red dead deadnettle; potential to improve the side effects of MTX for ALL treatment.
  • HY-P1486
    Angiotensinogen (1-14), human

    Endogenous Metabolite Cardiovascular Disease
    Angiotensinogen (1-14), human is a fragment of the renin substrate angiotensinogen. Angiotensinogen is naturally occurring substrate for renin and a precursor for all angiotensin peptides.
  • HY-101541
    Docosahexaenoic Acid methyl ester

    Methyl docosahexaenoate; All cis-DHA methyl ester

    Others Neurological Disease
    Docosahexaenoic Acid methyl ester is a methylated docosahexaenoic acid analog which can be intercalated into membrane phospholipids without being oxidized or hydrolyzed.
  • HY-P1486A
    Angiotensinogen (1-14), human TFA

    Endogenous Metabolite Cardiovascular Disease
    Angiotensinogen (1-14), human TFA is a fragment of the renin substrate angiotensinogen. Angiotensinogen is naturally occurring substrate for renin and a precursor for all angiotensin peptides.
  • HY-U00189
    Sch412348

    Adenosine Receptor Neurological Disease
    Sch412348 is a potent competitive antagonist of the human adenosine A2A receptor (Ki=0.6 nM) and has >1000-fold selectivity over all other adenosine receptors.
  • HY-15981
    Omarigliptin

    MK-3102

    Dipeptidyl Peptidase Metabolic Disease
    Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all proteases tested (IC50 > 67 μM).
  • HY-135813
    LtaS-IN-1

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

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-W004260
    Arachidic acid

    Icosanoic acid

    Endogenous Metabolite Others
    Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue.
  • HY-112542
    Nemadectin

    CL-287088; LL-F28249 α

    Parasite Antibiotic Infection
    Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity.
  • HY-16911
    AFN-1252

    API-1252; Debio 1452

    Bacterial Antibiotic Infection
    AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ≤0.12 μg/ml.
  • HY-12866
    Larotrectinib

    LOXO-101; ARRY-470

    Trk Receptor Apoptosis Cancer
    Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
  • HY-14608
    (S)-Glutamic acid

    (+)-L-Glutamic acid

    Endogenous Metabolite iGluR Ferroptosis Apoptosis Neurological Disease
    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  • HY-14608A
    L-Glutamic acid monosodium salt

    Monosodium glutamate

    iGluR Apoptosis Ferroptosis Neurological Disease
    L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  • HY-18732A
    L-NMMA acetate

    Tilarginine acetate; Methylarginine acetate

    NO Synthase Cardiovascular Disease
    L-NMMA acetate is a nitric oxide synthase inhibitor of all NOS isoforms including NOS1, NOS2, and NOS3. The Ki values for nNOS (rat), eNOS (human), and iNOS (mouse) are approximately 0.18, 0.4, and 6 µM, respectively.
  • HY-101918
    DS-1040 Tosylate

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

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-136522
    S2116

    Histone Demethylase Apoptosis Cancer
    S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
  • HY-128607
    Mcl1-IN-9

    Bcl-2 Family Cancer
    Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.
  • HY-111778
    EHMT2-IN-1

    Histone Methyltransferase Cancer
    EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer.
  • HY-111904
    EHMT2-IN-2

    Histone Methyltransferase Cancer
    EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer.
  • HY-N3841
    ε-​Viniferin

    epsilon-Viniferin

    Cytochrome P450 Inflammation/Immunology
    ε-Viniferin, the dimer of Resveratrol and isolated from Vitis vinifera, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant capacity.
  • HY-21088
    3-Amino-2-piperidinone

    Cyclo-ornithine

    Endogenous Metabolite Metabolic Disease
    3-aminopiperidine-2-one is a metabolite from all living organisms. 3-aminopiperidine-2-one is a delta-lactam that is 2-piperidone substituted at position 3 by an amino group.
  • HY-N0086
    N6-Methyladenosine

    6-Methyladenosine; N-Methyladenosine

    Endogenous Metabolite Influenza Virus Infection
    N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities.
  • HY-13271
    Tubastatin A Hydrochloride

    Tubastatin A HCl; TSA HCl

    HDAC Autophagy Apoptosis Cancer
    Tubastatin A (Hydrochloride) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
  • HY-13271A
    Tubastatin A

    HDAC Autophagy Apoptosis Cancer
    Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
  • HY-12866A
    Larotrectinib sulfate

    LOXO-101 sulfate; ARRY-470 sulfate

    Trk Receptor Apoptosis Cancer
    Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
  • HY-136523
    S2157

    Histone Demethylase Apoptosis Cancer
    S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-P1783
    M2e, human

    Influenza Virus Infection
    M2e, human, consisting of the 23 extracellular residues of M2 (the third integral membrane protein of influenza A), has been remarkably conserved in all human influenza A, which is a valid and versatile vaccine candidate to protect against any strain of human influenza A.
  • HY-128602
    c-Kit-IN-2

    c-Kit Cancer
    c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively.
  • HY-11012
    TDZD-8

    GSK-3β Inhibitor I; NP 01139

    GSK-3 Cancer
    TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
  • HY-111791
    ACY-1083

    HDAC Cancer
    ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.
  • HY-N1372
    (R)-Fangchinoline

    Thalrugosine; Thaligine

    Bacterial Antibiotic Cancer Infection Inflammation/Immunology Cardiovascular Disease
    (R)-Fangchinoline (Thalrugosine), a alkaloids from genus Stephania,exhibits antimicrobial and hypotensive activity. The roots and stems of several plants from genus Stephania are all used as traditional Chinese medicine and have been used for treatment of fever, diarrhea, dyspepsia and urinary disease.
  • HY-120548
    KBU2046

    Others Cancer
    KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-P1783A
    M2e, human TFA

    Influenza Virus Infection
    M2e, human TFA, consisting of the 23 extracellular residues of M2 (the third integral membrane protein of influenza A), has been remarkably conserved in all human influenza A. M2e, human TFA is a valid and versatile vaccine candidate to protect against any strain of human influenza A.
  • HY-P2315
    Human β-defensin-1

    HβD-1

    Antibiotic Bacterial Infection
    Human β-defensin-1 (HβD-1) is a cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by all epithelial surfaces, but also by circulatory cells and cells of the reproductive tract. Human β-defensin-1 has antimicrobial activities against a broad-sperm bacteria.
  • HY-115475
    SW-100

    HDAC Neurological Disease
    SW-100, a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays a significantly improved ability to cross the blood-brain-barrier.
  • HY-118743
    KMN-80

    Prostaglandin Receptor Metabolic Disease
    KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors.
  • HY-P1852
    TIP 39, Tuberoinfundibular Neuropeptide

    Adenylate Cyclase Neurological Disease
    TIP 39, Tuberoinfundibular Neuropeptide is a neuropeptide and parathyroid hormone 2 receptor (PTH2R) agonist. TIP 39 is highly conserved among species. TIP39 from all species activates adenylyl cyclase and elevates intracellular calcium levels through parathyroid hormone 2 receptor (PTH2R).
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-100765
    BI-0252

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.
  • HY-N2181
    Acetylshikonin

    Cytochrome P450 AChE Cancer Inflammation/Immunology
    Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity. Acetylshikonin is a non-selective cytochrome P450 inhibitor against all P450s (IC50 values range from 1.4-4.0 μM). Acetylshikonin is an AChE inhibitor and exhibits potent antiapoptosis activity.
  • HY-N7539
    Cognac oil

    Others Metabolic Disease
    Cognac oil, mainly found in wine lees, has unique fatty acid profiles, including Palmitic acid (59.26%), Linoleic acid (11.92%), Myristic acid (8.97%), Oleic acid (8.3%) and other fatty acids. Cognac oil leads to a general increase in the permeation of R6G (Rhodamine 6G) across all the membranes.
  • HY-120508
    Pivanex

    AN-9; Pivalyloxymethyl butyrate

    HDAC Bcr-Abl Apoptosis Cancer Inflammation/Immunology
    Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates bcr-abl protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties.
  • HY-114286
    PXS-5153A

    Monoamine Oxidase Inflammation/Immunology
    PXS-5153A is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A could reduce crosslinks and ameliorates fibrosis.
  • HY-N7054
    Volemitol

    D-Volemitol

    Others Metabolic Disease
    Volemitol (D-Volemitol) is a seven-carbon sugar alcohol that fulfills several important physiological functions in certain species of the genus Primula. Volemitol is the major nonstructural carbohydrate in leaves of all stages of development. Volemitol functions as a photosynthetic product, phloem translocate (phloem-mobile), and storage carbohydrate. Volemitol biosynthesis proceeds by a novel, NADPH-dependent, ketose reductase (sedoheptulose reductase).
  • HY-100233
    IQ-1S free acid

    JNK Cancer Inflammation/Immunology
    IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
  • HY-114286A
    PXS-5153A monohydrochloride

    Monoamine Oxidase Inflammation/Immunology
    PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride could reduce crosslinks and ameliorates fibrosis.
  • HY-N7434
    N-Nitrosodiethylamine

    DNA/RNA Synthesis
    N-Nitrosodiethylamine is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
  • HY-12076
    BMS 777607

    BMS 817378

    c-Met/HGFR TAM Receptor Cancer
    BMS 777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
  • HY-N6022
    Byakangelicin

    Others Metabolic Disease
    Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.
  • HY-120323
    DRI-C21045

    TNF Receptor Inflammation/Immunology
    DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 µM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 µM and 4.5 µM, respectively.
  • HY-108584
    Flindokalner

    BMS-204352

    Potassium Channel Neurological Disease
    Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
  • HY-112724
    SHR0302

    JAK Apoptosis Cancer Inflammation/Immunology
    SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects.
  • HY-112831
    BI-409306

    Phosphodiesterase (PDE) Neurological Disease
    BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); BI-409306 can be used in the research of memory enhancement in CNS disorders.
  • HY-128851
    Coenzyme A

    Endogenous Metabolite Cancer Neurological Disease
    Coenzyme A is is an obligatory cofactor in all living cells synthesised from pantothenate (Vitamin B5), adenosine triphosphate (ATP) and cysteine. Covalent binding of Coenzyme A to Peroxiredoxin 5 (Prdx5) results in complete inhibition of its peroxidase activity, which is reversed by reduction with DTT.Coenzyme A and its thioester derivatives are key players in major catabolic and anabolic pathways and the regulation of gene expression. Many human pathologies, including cancer, diabetes and neurodegeneration, have been associated with abnormal biosynthesis and homeostasis of CoA and its derivatives.
  • HY-110105
    NS8593 hydrochloride

    Potassium Channel Neurological Disease
    NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
  • HY-19336
    BAZ2-ICR

    Epigenetic Reader Domain Cancer
    BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-120878
    CXCR2-IN-2

    CXCR Inflammation/Immunology
    CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
  • HY-19975
    RN-1734

    TRP Channel Neurological Disease
    RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM). RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells.
  • HY-121744
    PS10

    PDHK Inflammation/Immunology
    PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
  • HY-10015
    PAP-1

    5-(4-Phenoxybutoxy)psoralen

    Potassium Channel Inflammation/Immunology
    PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects.
  • HY-108596
    BL-1249

    Potassium Channel Inflammation/Immunology
    BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM).
  • HY-120944
    BAY-7598

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