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Pathways Recommended: Metabolic Enzyme/Protease
Results for "

enzyme models

" in MedChemExpress (MCE) Product Catalog:

22

Inhibitors & Agonists

1

Biochemical Assay Reagents

1

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-135470
    Nifurpirinol

    P-7138

    		 Antibiotic Bacterial Infection
    Nifurpirinol (P-7138) is a nitroaromatic antibiotic and acts as a novel substrate for the bacterial nitroreductase (NTR) enzyme. Nifurpirinol is a more potent proagent compared to Metronidazole to trigger cell-ablation in nitroreductase expressing transgenic models .
    Nifurpirinol
  • HY-138830
    TAK-418

    		Histone Demethylase Neurological Disease
    TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models .
    TAK-418
  • HY-163346
    TPEG-P

    		Others Metabolic Disease
    TPEG-P is an enzyme-activated intramolecular hydrogen bond (IMHB) enhanced probe, developed for ALP detection in cells and mice models of DILI .
    TPEG-P
  • HY-160912
    ELOVL6-IN-5

    		ELOVL Cancer
    ELOVL6-IN-5 (compound B) is an inhibitor of the elongase enzyme of long-chain fatty acid family 6 (ELOVL6). ELOVL6 is a rate-limiting enzyme for the elongation of saturated and monounsaturated long-chain fatty acids and is an effective target for inhibiting diabetes. ELOVL6-IN-5 reduces hepatic fatty acid levels in a mouse model of diet-induced obesity (DIO). However, ELOVL6 inhibition by ELOVL6-IN-5 did not improve insulin resistance .
    ELOVL6-IN-5
  • HY-157521
    AANAT-IN-1

    		Acyltransferase Endocrinology
    AANAT-IN-1 (compound 30) is a potent inhibitor (IC50: 10μM) of aralkylamine N-acetyltransferase (AANAT). AANAT is responsible for the synthesis of melatonin, which is involved in disorders such as seasonal affective disorder (SAD) in which melatonin levels are abnormally high .
    AANAT-IN-1
  • HY-101494
    Temuterkib
    Maximum Cited Publications
    24 Publications Verification

    LY3214996

    		 ERK Cancer
    Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.
    Temuterkib
  • HY-114196
    Aclimostat

    ZGN-1061

    		 MetAP Metabolic Disease
    Aclimostat (ZGN-1061) is a potent inhibitor of the MetAP2 enzyme and displays favorable efficacy and safety in preclinical studies. ZGN-1061 produced similar efficacy as beloranib for weight loss, improvements in metabolic parameters in a mouse model of obesity and insulin resistance, and concordant changes in gene transcription in HepG2 cells .
    Aclimostat
  • HY-163069
    Antitubercular agent-43

    		Bacterial Infection
    Antitubercular agent-43 (compound A11) is an orally active and potent antitubercular agent. Antitubercular agent-43 shows highly metabolic stability against human and mouse cytochrome P450 enzymes. Antitubercular agent-43 exhibits bactericidal efficacy in acute TB infection mouse model .
    Antitubercular agent-43
  • HY-W150340
    β-Lactose

    		Galectin Biochemical Assay Reagents Cancer
    β-Lactose is a disaccharide commonly found in milk and dairy products. It consists of two monosaccharides, glucose and galactose, linked by β-glycosidic bonds. β-Lactose has various applications in the food industry, especially as a sweetener and bulking agent. Furthermore, it can be used as a substrate for enzymes involved in lactose metabolism and as a model compound for studying carbohydrate-protein interactions.
    β-Lactose
  • HY-NP009
    α-Lactalbumin

    		Biochemical Assay Reagents Others
    α-Lactalbumin is a Ca 2+-binding protein. α-Lactalbumin has a single strong Ca 2+-binding site and for this reason it frequently serves as a simple model Ca 2+-binding protein. α-Lactalbumin is a component of lactose synthase, an enzyme system, which consists of galactosyltransferase (GT) and α-Lactalbumin .
    α-Lactalbumin
  • HY-146974
    PDE4-IN-9

    		Phosphodiesterase (PDE) Inflammation/Immunology
    PDE4-IN-9 (Compound 5j) is a potent inhibitor of PDE4. PDE4-IN-9 exhibits lower IC50 value (1.4 μM) against PDE4 than parent rolipram (2.0 μM) in in vitro enzyme assay. PDE4-IN-9 also displays good in vivo activity in animal models of asthma/COPD and sepsis induced by LPS .
    PDE4-IN-9
  • HY-16911
    AFN-1252
    5+ Cited Publications

    API-1252; Debio 1452

    		 Bacterial Antibiotic Infection
    AFN-1252 is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 exhibits typical MIC90 values of ⩽0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith .
    AFN-1252
  • HY-155726
    Cy-FBP/SBPase-IN-1

    		Others Others
    Cy-FBP/SBPase-IN-1 (compound S5) is a Cy-FBP/SBPase inhibitor, which is an important regulatory enzyme in cyanobacterial photosynthesis. Thus Cy-FBP/SBPase-IN-1 inhibits Calvin cycle and photosystem, and decreases photosynthetic efficiency in cyanobacterial photosynthesis. Cy-FBP/SBPase-IN-1 potently inhibits the growth of cyanobacteria, as well as Synechocystis sp.PCC6803. Cy-FBP/SBPase-IN-1 shows safety profile in human-derived cells and zebrafish models .
    Cy-FBP/SBPase-IN-1
  • HY-12501A
    ITI-214
    3 Publications Verification

    		 Phosphodiesterase (PDE) Neurological Disease
    ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions .
    ITI-214
  • HY-146755
    TIY-7

    		Trk Receptor Cancer
    TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
    TIY-7
  • HY-147720
    γ-Secretase modulator 11

    		γ-secretase Neurological Disease
    5-{8-[(3,4'- difluoro [1,1'- biphenyl]-4-yl) methoxy] - 2-methylimidazo [1,2-a] pyridin-3-yl}-n-methylpyridin-2-formamide (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.
    γ-Secretase modulator 11
  • HY-12501
    ITI-214 free base

    		Phosphodiesterase (PDE) Neurological Disease
    ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions .
    ITI-214 free base
  • HY-155732
    NPD-2975

    		Parasite Infection
    NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively .
    NPD-2975
  • HY-N6972
    Cepharanthine
    3 Publications Verification

    		 SARS-CoV Cytochrome P450 Apoptosis Parasite Infection Inflammation/Immunology Cancer
    Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
    Cepharanthine
  • HY-W352344
    2'-Deoxy-L-adenosine

    		HBV Infection
    2'-Deoxy-L-adenosine is an orally active synthon for modified oligodeoxyribonucleotides. 2'-Deoxy-L-adenosine is a potent, specific and selective inhibitor of the replication of hepatitis B virus (HBV) as well as the closely related duck and woodchuck hepatitis viruses (WHV) .
    2'-Deoxy-L-adenosine
  • HY-151093
    IDO2-IN-1
    1 Publications Verification

    		 Indoleamine 2,3-Dioxygenase (IDO) Inflammation/Immunology
    IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC50 value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research .
    IDO2-IN-1
  • HY-161483
    CBP/p300 ligand 3

    		Epigenetic Reader Domain Histone Acetyltransferase Neurological Disease Cancer
    CBP/p300 ligand 3 is a target protein ligand of CBPD-268 (HY-161369). CBP and p300 are two proteins with histone acetyltransferase (HAT) activity, and CBP and p300 play key roles in regulating biological processes such as gene expression, cell proliferation, differentiation and DNA repair. Through its acetyltransferase activity, CBP/p300 can acetylate histones and other proteins, thereby regulating chromatin structure and gene expression. CBP/p300 ligand 3 regulates the function of CBP/p300 by binding to a specific domain of the CBP/p300 protein (the bromine domain or HAT domain), inhibiting its enzyme activity or altering its interactions with other proteins (transcription factors). CBP/p300 ligand 3 can be used in cancer, neurodegenerative diseases and other disease models associated with abnormal CBP/p300 function .
    CBP/p300 ligand 3

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