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Results for "Acyl transferase Inhibitors" in MCE Product Catalog:

123

Inhibitors & Agonists

1

Screening Libraries

1

Biochemical Assay Reagents

3

Peptides

40

Natural
Products

2

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-135955
    Levothyroxine acyl glucuronide

    Thyroxine Acyl-β-D-glucuronide

    Endogenous Metabolite Metabolic Disease
    Levothyroxine acyl glucuronide (Thyroxine Acyl-β-D-glucuronide), an endogenous metabolite, is the acyl glucuronide formation of thyroxine (T4).
  • HY-135956
    T3 Acyl glucuronide

    Endogenous Metabolite Metabolic Disease
    T3 Acyl glucuronide, an endogenous metabolite, is the acyl glucuronide formation of triiodothyronine (T3).
  • HY-136344
    Simvastatin Acyl-β-D-glucuronide

    Drug Metabolite Others
    Simvastatin Acyl-β-D-glucuronide is a metabolite of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
  • HY-50861
    AZD3988

    Acyltransferase Metabolic Disease
    AZD3988 is a diacylglycerol acyl transferase-1 (DGAT-1) inhibitor with IC50s of 6, 5, 11 nM for human, rat, mouse, respectively.
  • HY-113957
    MPI_5a

    HDAC Cancer
    MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM.
  • HY-N6706
    Enniatin complex

    Bacterial Acyltransferase Apoptosis Cancer Infection
    Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines .
  • HY-128350A
    FGTI-2734 mesylate

    Farnesyl Transferase Cancer
    FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.
  • HY-128350
    FGTI-2734

    Farnesyl Transferase Cancer
    FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.
  • 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-119738
    OSMI-1

    Acyltransferase Metabolic Disease
    OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC50 value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.
  • HY-113085
    3-Hydroxyhippuric acid

    Endogenous Metabolite Others
    3-Hydroxyhippuric acid is an acyl glycine. Acyl glycines are normally minor metabolites of fatty acids.
  • HY-113165
    Isobutyryl-L-carnitine

    Endogenous Metabolite Metabolic Disease
    Isobutyryl-L-carnitine is a product of the acyl-CoA dehydrogenases. Isobutyryl-L-carnitine is a member of the class of compounds known as acyl carnitines.
  • HY-118916
    FTI-2148

    Farnesyl Transferase Cancer
    FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
  • HY-118916A
    FTI-2148 diTFA

    Farnesyl Transferase Cancer
    FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
  • HY-112732B
    Sparfosic acid trisodium

    Others Cancer Metabolic Disease
    Sparfosic acid trisodium, is a potent inhibitor of aspartate transcarbamoyl transferase, with anti-tumor and antimetabolite activity. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis.
  • HY-113210
    Hydroxyphenylacetylglycine

    Endogenous Metabolite Metabolic Disease
    Hydroxyphenylacetylglycine is an acyl glycine, and an endogenous human metabolite.
  • HY-113353
    Nicotinuric acid

    Endogenous Metabolite Others
    Nicotinuric acid is an acyl glycine. Nicotinuric acid is a metabolite of nicotinic acid.
  • HY-32219
    T863

    Acyltransferase Metabolic Disease
    T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.
  • HY-108706
    KDM2A/7A-IN-1

    Histone Demethylase Cancer
    KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.
  • HY-N6994
    Isoasatone A

    Others Infection
    Isoasatone A is a natural product isolated from the plant Heterotropa takaoi M., with anti-insect activity. Isoasatone A againsts S. litura by acting on cytochrome P450 monoxygenases and glutathione transferases.
  • HY-16706
    Remodelin

    Histone Acetyltransferase Cancer
    Remodelin is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.
  • HY-16706A
    Remodelin hydrobromide

    Histone Acetyltransferase Cancer
    Remodelin hydrobromide is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.
  • HY-113367
    Suberylglycine

    Endogenous Metabolite Metabolic Disease
    Suberylglycine is an acyl glycine, which is a normally minor metabolite of fatty acid.
  • HY-N1424
    Glycoursodeoxycholic acid

    Ursodeoxycholylglycine

    Endogenous Metabolite Neurological Disease
    Glycoursodeoxycholic acid, a acyl glycine and a bile acid-glycine conjugate, is a metabolite of ursodeoxycholic acid.
  • HY-B0535
    Ethambutol

    Emb

    Bacterial Antibiotic Infection
    Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
  • HY-113232
    3-Methylcrotonylglycine

    Endogenous Metabolite Metabolic Disease
    3-Methylcrotonylglycine is an acyl glycine, a normal amino acid metabolite found in urine.
  • HY-115393A
    N-Heptanoyl-L-homoserine lactone

    Others
    N-Heptanoyl-L-homoserine lactone is a member of N-acyl-homoserine lactone family. N-acyl-homoserine lactones (AHL) regulate gene expression in gram-negative bacteria, such as Echerichia and Salmonella, and are involved in quorum sensing, cell to cell communication among bacteria.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-B0535A
    Ethambutol dihydrochloride

    Emb dihydrochloride

    Bacterial Antibiotic Infection
    Ethambutol dihydrochloride (Emb dihydrochloride) is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
  • HY-W015464
    N-Isovaleroylglycine

    Endogenous Metabolite Metabolic Disease
    N-Isovaleroylglycine is an acyl glycine and could be used as a biomarker for the predispositon for weight gain and obesity.
  • HY-124960
    CTPB

    Histone Acetyltransferase Cancer
    CTPB is a good activator of p300 histone acetyl transferase (HAT) enzyme.
  • HY-B0027
    Valnemulin Hydrochloride

    Bacterial Antibiotic Others
    Valnemulin hydrochloride is a pleuromutilin antibiotic which inhibits protein synthesis in bacteria by binding the peptidyl transferase enzyme in the 50s ribosomal subunit.
  • HY-114361
    OSMI-4

    Others Metabolic Disease
    OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor, with an EC50 of 3 μM in cells.
  • HY-16111
    BMS-214662

    Farnesyl Transferase Cancer
    BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.
  • HY-17374
    Benfotiamine

    S-Benzoylthiamine O-monophosphate

    Reactive Oxygen Species Neurological Disease
    Benfotiamine is a synthetic S-acyl derivative of thiamine (vitamin B1); an antioxidant dietary supplement.
  • HY-112174
    UDP-GlcNAc Disodium Salt

    UDP-α-D-N-Acetylglucosamine Disodium Salt

    Others Metabolic Disease
    UDP-GlcNAc Disodium Salt (UDP-α-D-N-Acetylglucosamine Disodium Salt) is a donor substrate of O-GlcNAc transferase (OGT).
  • HY-111530
    GSTO1-IN-1

    Gutathione S-transferase Cancer
    GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50 of 31 nM.
  • HY-111417
    GSK2973980A

    Acyltransferase Metabolic Disease
    GSK2973980A is a potent and selective Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitor with an IC50 of 3 nM.
  • HY-16437
    RP-64477

    Acyltransferase Cardiovascular Disease
    RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).
  • HY-15873
    FTI 276

    Farnesyl Transferase Cancer
    FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 and 0.5 nM for Plasmodium falciparum and human.
  • HY-19183
    E-5324

    Acyltransferase Metabolic Disease
    E-5324 is potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with IC50s of 44 to 190 nM.
  • HY-101627
    YM17E

    Acyltransferase Metabolic Disease
    YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
  • HY-W014787
    Decanedioic acid

    Endogenous Metabolite Metabolic Disease
    Decanedioic acid, a normal urinary acid, is found to be associated with carnitine-acylcarnitine translocase deficiency and medium chain acyl-CoA dehydrogenase deficiency.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-F0004
    β-Nicotinamide mononucleotide

    β-NM; NMN

    Endogenous Metabolite Others
    β-nicotinamide mononucleotide (β-NM) is an intermediate in NAD+ biosynthesis produced from nicotinamide (NAM) and phosphoribosyl pyrophosphate (PRPP) by nicotinamide phosphoribosyl transferase enzyme with no toxicity.
  • HY-15873A
    FTI 276 TFA

    Farnesyl Transferase Cancer
    FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 nM and 0.5 nM for Plasmodium falciparum and human, respectively.
  • HY-U00430
    MGAT2-IN-2

    Acyltransferase Metabolic Disease
    MGAT2-IN-2 is a potent and selective acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC50 of 3.4 nM.
  • HY-W016562
    Hippuric acid

    2-Benzamidoacetic acid

    Endogenous Metabolite Metabolic Disease
    Hippuric Acid (2-Benzamidoacetic acid), an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
  • HY-15872
    FTI-277

    Farnesyl Transferase Cancer
    FTI-277 is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.
  • HY-100737
    ML349

    Phospholipase Cancer
    ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
  • HY-122078
    FR-190809

    Acyltransferase Metabolic Disease
    FR-190809 is a potent, nonadrenotoxic, orally efficacious acyl-CoA:cholesterol O-acyltransferase (ACAT) inhibitor, with an IC50 of 45 nM.
  • HY-N6739
    Beauvericin

    Acyltransferase Infection Cardiovascular Disease
    Beauvericin is a Fusarium mycotoxin. Beauvericin inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 3 μM in an enzyme assay using rat liver microsomes.
  • HY-100400A
    K-604 dihydrochloride

    Acyltransferase Cardiovascular Disease
    K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45±0.06 μM.
  • HY-B1337
    Choline chloride

    Others Others
    Choline chloride is an organic compound and a quaternary ammonium salt, an acyl group acceptor and choline acetyltransferase substrate, also is an important additive in feed especially for chickens where it accelerates growth.
  • HY-N6702
    Enniatin A

    Acyltransferase Infection Cardiovascular Disease
    Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using rat liver microsomes.
  • HY-113166
    Dodecanoylcarnitine

    Endogenous Metabolite Metabolic Disease
    Dodecanoylcarnitine is present in fatty acid oxidation disorders such as long-chain acyl CoA dehydrogenase deficiency, carnitine palmitoyltransferase I/II deficiency, and is also associated with celiac disease.
  • HY-W015240
    N-Acetyl-L-glutamic acid

    Endogenous Metabolite Metabolic Disease
    N-Acetyl-L-glutamic acid, a N-acyl-L-amino acid, is a component of animal cell culturing media. N-Acetyl-L-glutamic acid is a metabolite of Saccharomyces cerevisiae and human.
  • HY-13215
    Avasimibe

    CI-1011; PD-148515

    Acyltransferase Cancer
    Avasimibe is an oral inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT) with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively.
  • HY-15197
    ABT-046

    Acyltransferase Metabolic Disease
    ABT-046 is a potent, selective, and orally efficacious acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC50= 8 nM).
  • 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-112534
    GSTO-IN-2

    Gutathione S-transferase Cancer
    GSTO-IN-2 is a glutathione S-transferase inhibitor with IC50s of 3.6, 16.3, and 1.4 μM for GSTA2, GSTM1, and GSTP1-1.
  • 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-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-13057
    O6BTG-octylglucoside

    Glucose-conjugated MGMT inhibitor

    DNA Methyltransferase Cancer
    O6BTG-octylglucoside is a potent O 6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
  • HY-128918
    SIS17

    HDAC Others
    SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
  • 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-113801
    N-(3-Oxooctanoyl)-DL-homoserine lactone

    (Rac)-3-oxo-C8-HSL

    Others Metabolic Disease
    N-(3-Oxooctanoyl)-DL-homoserine lacton is a member of N-Acyl homoserine lactone (AHL) from gram-negative bacteria, with stereochemistry-dependent growth regulatory activity for roots .
  • HY-W017522
    Adipic acid

    Endogenous Metabolite Metabolic Disease
    Adipic acid is found to be associated with HMG-CoA lyase deficiency, carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency, and medium Chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism.
  • HY-12628
    GNE-618

    Nampt Cancer
    GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.
  • HY-N1963
    Curzerene

    Gutathione S-transferase Cancer
    Curzerene is a sesquiterpene is isolated from the rhizome of Curculigo orchioides Gaertn with anti-cancer activity. Curzerene inhibits glutathione S-transferase A1 (GSTA1) mRNA and protein expression. Curzerene induces cell apoptosis.
  • HY-17511
    Potassium oxonate

    Potassium azaorotate; Potassium otastat

    Others Metabolic Disease
    Potassium oxonate is an inhibitor of uricase, inhibits the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate catalyzed by pyrimidine phosphoribosyl-transferase in a different manner from allopurinol in cell-free extracts and intact cells in vitro.
  • HY-15872A
    FTI-277 hydrochloride

    Farnesyl Transferase Apoptosis Influenza Virus Cancer Infection
    FTI-277 hydrochloride is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 hydrochloride can inhibits hepatitis delta virus (HDV) infection.
  • HY-15136
    Lonafarnib

    Sch66336

    Farnesyl Transferase Autophagy Influenza Virus Cancer Infection
    Lonafarnib is an orally bioavailable farnesyl protein transferase (FPTase) inhibitor for H-ras, K-ras and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib has anti-hepatitis delta virus (HDV) activities.
  • HY-111903
    Levomecol

    Bacterial Infection
    Levomecol (Chloramphenicol), made up of Chloramphenicol, Methyluracil, is a broad-spectrum antibiotic that is derived from the bacterium Streptomyces venezuelae. Levomecol (Chloramphenicol)) stops bacterial growth by binding to the bacterial ribosome (blocking peptidyl transferase) and inhibiting protein synthesis.
  • HY-N1282
    Seneciphylline

    Gutathione S-transferase Cytochrome P450 Cancer
    Seneciphylline is a toxic pyrrolizidine alkaloid in Senecio plants. Seneciphylline significantly increases the activities of epoxide hydrase and glutathione-S-transferase but causes reduction of cytochrome P-450 and related monooxygenase activities.
  • HY-136615
    5-Hydroxydecanoate sodium

    Potassium Channel Neurological Disease
    5-Hydroxydecanoate sodium is a selective ATP-sensitive K + (KATP) channel blocker (IC50 of ~30 μM). 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity.
  • HY-16482
    Teglicar

    Endogenous Metabolite Metabolic Disease
    Teglicar is a selective and reversible inhibitor of liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1). Teglicar reduces ketogenesis and glucose production, decreases gluconeogenesis and improves glucose homeostasis. Teglicar has a potential antihyperglycemic propert.
  • HY-N7384
    Vitamin B15

    Pangamic Acid

    Others Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Vitamin B15 (Pangamic Acid) is a natural, ubiquitously in plant seeds substance and can used be as an agent stimulating cellular respiration. Vitamin B15 contains D-gluconodimethyl amino acetic acid. Vitamin B15 is also a immune-correcting agent. Vitamin B15 can be used for wide range of diseases.
  • HY-13634B
    TLK117

    TER117

    Gutathione S-transferase Cancer Inflammation/Immunology
    TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.
  • HY-N1916
    Coniferyl ferulate

    Gutathione S-transferase P-glycoprotein Cancer
    Coniferyl ferulate, a strong inhibitor of glutathione S-transferase (GST) isolated from Radix Angelicae sinensis, reverses multidrug resistance and downregulates P-glycoprotein. Coniferyl ferulate shows strong inhibition of human placental GST with an IC50 of 0.3 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-136409
    N-Decanoyl-L-homoserine lactone

    Bacterial
    N-Decanoyl-L-homoserine lactone is a member of N-acyl-homoserine lactone family. N-Acylhomoserine lactones (AHL) regulate gene expression in Gram-negative bacteria, such as Echerichia and Salmonella, and are involved in quorum sensing, cell to cell communication among bacteria.
  • HY-N4193
    Glabrol

    Acyltransferase Cardiovascular Disease
    Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 24.6 μM for rat liver microsomal ACAT activity.
  • HY-135784
    OSMI-2

    Acyltransferase Metabolic Disease
    OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.
  • HY-18982
    Anisomycin

    Flagecidin; Wuningmeisu C

    DNA/RNA Synthesis JNK Bacterial Apoptosis Antibiotic Cancer Infection
    Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system. Anisomycin is a JNK activator, which increases phospho-JNK. Anisomycin is a bacterial antibiotic isolated from Streptomyces griseolus.
  • HY-100399
    Nevanimibe

    PD-132301; ATR-101

    Acyltransferase Apoptosis Cancer
    Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer.
  • HY-113089
    Epsilon-(gamma-glutamyl)-lysine

    H-Glu(H-Lys-OH)-OH; γ-Glu-ε-Lys

    Others Metabolic Disease
    Epsilon-(gamma-glutamyl)-lysine is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration.
  • HY-117832
    Pyripyropene A

    Acyltransferase Infection Inflammation/Immunology Cardiovascular Disease
    Pyripyropene A is a potent and selective sterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2) inhibitor, with an IC50 of 0.07 µM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo.
  • HY-100399A
    Nevanimibe hydrochloride

    PD-132301 hydrochloride; ATR101 hydrochloride

    Acyltransferase Apoptosis Cancer
    Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.
  • HY-126329
    AZD9898

    Gutathione S-transferase Inflammation/Immunology
    AZD9898 is an orally active leukotriene-C4 synthetase (LTC4S, glutathione S-transferase II) inhibitor, with an IC50 of 0.28 nM. AZD9898 mitigates the GABA binding and hepatic toxicity signal. AZD9898 has the potential to treat asthma.
  • HY-135785
    OSMI-3

    Acyltransferase Metabolic Disease
    OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells.
  • HY-N3806
    Enniatin B

    Acyltransferase ERK Cancer Infection Cardiovascular Disease
    Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes. Enniatins B decreases the activation of ERK (p44/p42).
  • 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-108341
    PF-06424439

    Acyltransferase Metabolic Disease
    PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
  • HY-129123
    ML318

    Antibiotic Infection
    ML318 is a biaryl nitrile inhibitor of PvdQ acylase with an IC50 of 20 nM by binding in the acyl-binding site. ML318 inhibits P. aeruginosa (PAO1) with an IC50 of 19 μM. ML318 prevents pyoverdine production and limits the growth of P. aeruginosa under iron-limiting conditions.
  • HY-N6707
    Triacsin C

    WS 1228A; FR 900190

    Others Infection
    Triacsin C (WS 1228A), a natural intracellular long-chain acyl-CoA synthetases (ACSL) inhibitor, is from Streptomyces aureofaciens. Triacsin C inhibits TAG accumulation into lipid droplets (LD) by suppressing ACSL activity. Triacsin C is found to be highly effective against rotavirus replication.
  • HY-108341A
    PF-06424439 methanesulfonate

    Acyltransferase Metabolic Disease
    PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
  • HY-B1599
    Chloramphenicol palmitate

    Bacterial Infection
    Chloramphenicol palmitate is an orally active broad spectrum antibiotic and has a broad spectrum of activity against gram positive and gram negative bacteria. Chloramphenicol palmitate inhibits bacterial protein synthesis by blocking the peptidyl transferase step. Chloramphenicol palmitate can be used as bacterial selection agent in transformed cells containing chloramphenicol resistance genes.
  • HY-135425
    10,12-Tricosadiynoic acid

    Acyltransferase Metabolic Disease
    10,12-Tricosadiynoic acid is a highly specific, selective, high affinity and orally active acyl-CoA oxidase-1 (ACOX1) inhibitor. 10,12-Tricosadiynoic acid can treat high fat diet- or obesity-induced metabolic diseases by improving mitochondrial lipid and ROS metabolism.
  • 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-123087
    N-(3-Hydroxytetradecanoyl)-DL-homoserine lactone

    N-(3-oxodecanoyl)-homoserine lactone

    Bacterial Infection
    N-(3-Hydroxytetradecanoyl)-DL-homoserine lactone (N-(3-oxodecanoyl)-homoserine lactone) is a member of N-Acyl homoserine lactone (AHL) from V. alginolyticus strains. N-(3-Hydroxytetradecanoyl)-DL-homoserine lactone is used for biofilm formation and has antibacterial activity.
  • HY-106783
    Polymyxin B nonapeptide

    Bacterial Antibiotic Infection
    Polymyxin B nonapeptide is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue. Polymyxin B nonapeptide is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes.
  • HY-13634
    Ezatiostat hydrochloride

    TER199; TLK199 hydrochloride

    Gutathione S-transferase Apoptosis Cancer
    Ezatiostat hydrochloride (TER199; TLK199 hydrochloride) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat hydrochloride leads to JNK activation by inhibiting GSTP1. Ezatiostat hydrochloride stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat hydrochloride has the potential for myelodysplastic syndrome (MDS) treatment.
  • HY-106783A
    Polymyxin B nonapeptide TFA

    Bacterial Infection
    Polymyxin B nonapeptide TFA is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue. Polymyxin B nonapeptide TFA is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes.
  • HY-13634A
    Ezatiostat

    TER199(free base); TLK199

    Gutathione S-transferase Apoptosis Cancer
    Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment.
  • HY-16908A
    Lefamulin acetate

    BC-3781 acetate

    Bacterial Antibiotic Infection
    Lefamulin acetate (BC-3781 acetate) is an orally active antibiotic for community-acquired bacterial pneumonia (CABP) treatment. Lefamulin acetate (BC-3781 acetate) is the first semi-synthetic pleuromutilin for systemic treatment of bacterial infections in humans. Lefamulin acetate (BC-3781 acetate) inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome, preventing the binding of transfer RNA for peptide transfer.
  • HY-B2246
    L-Carnitine hydrochloride

    (R)-Carnitine hydrochloride

    Endogenous Metabolite Metabolic Disease
    L-Carnitine hydrochloride ((R)-Carnitine hydrochloride), a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine hydrochloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine hydrochloride is an antioxidant. L-Carnitine hydrochloride can ameliorate metabolic imbalances in many inborn errors of metabolism.
  • 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-B1640
    Ethacrynic acid

    Gutathione S-transferase NF-κB Calcium Channel Cancer Inflammation/Immunology
    Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-122643
    NITD-916

    Bacterial Infection
    NITD-916, a 4-hydroxy-2-pyridone derivative, is an orally active and highly lipophilic mycobacterial enoyl reductase InhA inhibitor with an IC50 of 570 nM. NITD-916 forms a ternary complex with InhA and NADH to block access to the fatty acyl substrate binding pocket. NITD-916 has potent anti-tuberculosis effects.
  • HY-136282
    OGT-IN-2

    Others
    OGT-IN-2 is a O-GlcNAc transferase (OGT) inhibitor with an IC50 of 53 μM. OGT-IN-2 reduces proliferation and viability of prostate cancer cells in vitro. OGT-IN-2 depletes intracellular alanine and decreases glucose consumption by cancer cells. OGT-IN-2 decreases markers of ER stress and apoptosis in pregnant diabetic mice and reduces neural tube defects in embryos from diabetic mice.
  • 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-135318
    NBDHEX

    Glutathione Peroxidase Apoptosis Autophagy Cancer
    NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
  • HY-N6798
    Myriocin

    HCV Antibiotic Infection
    Myriocin, a fungal metabolite isolated from Myriococcum albomyces, Isaria sinclairi and Mycelia sterilia, is a potent inhibitor of serine-palmitoyl-transferase (SPT) and a key enzyme in de novo synthesis of sphingolipids. Myriocin strongly suppresses replication of both the subgenomic HCV-1b replicon and the JFH-1 strain of genotype 2a infectious HCV, with an IC50 of 3.5 µg/mL for inhibiting HCV infection.
  • HY-127146
    Platensimycin

    Antibiotic Bacterial
    Platensimycin is an antibiotic produced by S. platensis that inhibits gram-positive bacteria by selectively inhibiting cellular lipid biosynthesis (IC50=0.1 μM). Platensimycin targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s=48 nM and 160 nM for S.aureus and E.coli enzymes, respectively). Platensimycin is a promising agent for overcoming antibiotic resistance.
  • HY-108538
    Ethacrynic acid D5

    Gutathione S-transferase NF-κB Calcium Channel Inflammation/Immunology
    Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • 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-N6711
    Equisetin

    HIV Integrase Infection
    Equisetin is an N-methylserine-derived acyl tetramic acid isolated from a terrestrial fungus Fusarium equiseti NRRL 5537. Equisetin is a tetramate-containing natural product with antibiotic and cytotoxic activity. Equisetin inhibits the growth of Gram-positive bacteria and HIV-1 integrase activity but shows no activity against Gram-negative bacteria. Equisetin is a Quorum-sensing inhibitor (QSI) that attenuates QS-regulated virulence phenotypes in P. aeruginosa without affecting the growth of bacterias, serves as a leading compound for the treatment of P. aeruginosa infections.
  • 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-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.