2. Search Result
Search Result
Pathways Recommended: Metabolic Enzyme/Protease
Results for "

enzyme models

" in MedChemExpress (MCE) Product Catalog:

40

Inhibitors & Agonists

1

Biochemical Assay Reagents

1

Peptides

2

Natural
Products

1

Oligonucleotides

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-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-101494
    Temuterkib
    Maximum Cited Publications
    27 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-163346
    TPEG-P

    		Biochemical Assay Reagents 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-W055845
    4-Methylbenzamide oxime

    		Biochemical Assay Reagents Others
    4-Methylbenzamide oxime is a model of benzamide oxime and can be used as a substrate for mitochondrial amidoxime reducing component (mARC) catalytic enzyme reduction .
    4-Methylbenzamide oxime
  • HY-A0113
    Cilazaprilat

    Ro 31-3113

    		 Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Cilazaprilat is an inhibitor of angiotensin-converting enzyme (ACE; IC50=0.7 nM for the rat enzyme) and an active metabolite of Cilazapril (HY-A0043). It decreases creatine kinase release in primary neonatal rat cardiac myocytes in an in vitro model of ischemia-reperfusion injury induced by hypoxia and reoxygenation when used at a concentration of 10 μM.3 Intra-arterial administration of cilazaprilat (3 μg/kg per minute) increases coronary blood flow and fractional shortening in a dog model of coronary hypoperfusion-induced myocardial ischemia.
    Cilazaprilat
  • HY-122604
    PF-DcpSi

    		DNA/RNA Synthesis Neurological Disease
    PF-DcpSi is a mRNA decapping scavenger enzyme (DcpS) inhibitor (IC50: 0.11 nM). PF-DcpSi (30 mg/kg,i.p.) ameliorates the disease phenotype in a mice model of spinal muscular atrophy (SMA) .
    PF-DcpSi
  • 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-120663
    KRCA-0713

    		Anaplastic lymphoma kinase (ALK) Cancer
    KRCA-0713 is an ALK inhibitor with anti-ALK activity. KRCA-0713 showed promising anti-ALK activity in enzyme and cell-based experiments. KRCA-0713 was shown to effectively inhibit ALK-driven tumor growth in H3122 xenograft model studies, similar to the effect of ceritinib .
    KRCA-0713
  • 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-14923
    Ilepatril

    AVE 7688

    		 Angiotensin-converting Enzyme (ACE) Metabolic Disease
    Ilepatril, a dual inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase, has inhibitory effects in the type 2 diabetic nephropathy model in obese Zucker diabetic fatty (ZDF) rats. Ilepatril significantly reduced albuminuria in a dose-dependent manner and may be a strategy distinct from metabolic control to inhibit type 2 diabetic nephropathy .
    Ilepatril
  • HY-18112
    AZ-4217

    		Beta-secretase Neurological Disease
    AZ-4217 is an inhibitor for β-site amyloid precursor protein cleavage enzyme 1 (BACE1), with IC50 of 160 pM in human SH-SY5Y cells. AZ-4217 reduces amyloid deposition in Tg2576 mouse models, and is used for Alzheimer’s Disease research .
    AZ-4217
  • 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-120482
    CHM-1-P-Na

    		Others Others
    CHM-1-P-Na is a sodium monophosphate salt of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one, which can be converted into CHM-1, a compound with a unique anti-tumor mechanism, in vitro and in vivo, and has excellent anti-tumor activity in tumor models and clear pharmacological effects on related enzymes.
    CHM-1-P-Na
  • 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-116945
    Diphenamid

    		Endogenous Metabolite Others
    Diphenamid is a chemical compound that exhibits herbicide activity. Diphenamid acts by inhibiting the enzyme acetyl-CoA carboxylase. Diphenamid has shown resistance as a model for mimicking organic pollutants in wastewater treatment processes, especially in the presence of multiple anions. The degradation of diphenamid is significantly affected by certain inorganic ions, such as chromium (VI) and nitrogen oxides. Diphenamid shows changes in toxicity with longer treatment times, and the results of toxicity tests on selected algae indicate higher toxicity at 240 minutes of treatment .
    Diphenamid
  • HY-168300
    Antiangiogenic agent 7

    		Reactive Oxygen Species Apoptosis Inflammation/Immunology Cancer
    Antiangiogenic agent 7 (Compound 1) can induce cell apoptosis, increase Reactive Oxygen Species, and inhibit the intracellular enzyme thioredoxin reductase. Antiangiogenic agent 7 has anti-cancer activity, with an IC50 of 0.08-3.5 μM against cervical cancer cells HeLa, prostate cancer cells PC-3, and non-small cell lung cancer A549. Antiangiogenic agent 7 inhibits tumor growth in mouse xenograft models .
    Antiangiogenic agent 7
  • 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-116264
    CatB-IN-1

    		Ser/Thr Protease Cancer
    CatB-IN-1 is an enzyme inhibitor with significant inhibitory activity against tumor invasion. CatB-IN-1 may reduce the invasiveness of tumor cells by regulating intracellular protein metabolism. CatB-IN-1 demonstrates effective anti-invasive ability in cell models and can significantly reduce the invasive ability of MCF-10A neoT cells. The structure-activity relationship study of CatB-IN-1 shows that its design can target multiple functions of cat hepsin B .
    CatB-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-19109
    RG-7152

    		Others Others
    RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that can induce peroxisomal β-oxidation and peroxisome bifunctional enzymes (PBEs) in hepatocytes in various animal models. It has been shown to significantly increase PBE levels and β-oxidation activity in rat and mouse liver homogenates, while smaller effects were observed in guinea pigs and monkeys and no effect in dogs. In vitro studies have also shown that it can induce PBEs comparable to clofibric acid, indicating its potential as a peroxisome proliferator .
    RG-7152
  • HY-114622
    AFN-1252 tosylate

    API-1252 tosylate; Debio 1452 tosylate

    		 Bacterial Antibiotic Infection
    AFN-1252 (API-1252) tosylate is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 tosylate exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 tosylate exhibits typical MIC90 values of ?0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 tosylate is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith .
    AFN-1252 tosylate
  • 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-112142A
    (Rac)-AB-423

    DVR-23

    		 HBV Inflammation/Immunology
    (Rac)-AB-423 (DVR-23) is an anti-HBV candidate compound with promising anti-HBV activity. (Rac)-AB-423 showed no induction of CYP1A2, CYP3A4, or CYP2B6 enzyme activity at high concentrations. (Rac)-AB-423 exhibited desirable pharmacokinetic properties, enabling good systemic exposure and high oral bioavailability. (Rac)-AB-423 achieved more than 2 log viral load reduction in the hydrodynamic injection (HDI) HBV mouse model .
    (Rac)-AB-423
  • 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-15048
    GPI 15427

    		PARP Inflammation/Immunology
    GPI 15427 is a potent inhibitor of the enzyme poly (ADP-ribose) polymerase-1 (PARP-1), which plays a harmful role during inflammation. In a rat model of gut injury and inflammation, including splanchnic artery occlusion (SAO) shock and dinitrobenzene sulfonic acid (DNBS)-induced colitis, GPI 15427 demonstrated strong anti-inflammatory effects. It reduced inflammatory cell infiltration, histological injury, and delayed clinical signs of inflammation. GPI 15427 also diminished the accumulation of poly (ADP-ribose) in the ileum and colon of treated rats. These results suggest GPI 15427 could be useful for treating intestinal ischemia and inflammation .
    GPI 15427
  • HY-149127
    Rosolutamide

    ASC-JM17; ALZ-003

    		 Keap1-Nrf2 Androgen Receptor HSP Mitophagy Metabolic Disease
    Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby activating the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels .
    Rosolutamide
  • HY-117807
    A-176120

    		Ras Cancer
    A-176120 is a potent inhibitor of farnesyltransferase, crucial for Ras protein farnesylation in cancer cells. It exhibits high selectivity for farnesyltransferase (IC50 1.2 ± 0.3 nM) over related enzymes like geranylgeranyltransferases and squalene synthase. Inhibition of Ras processing in H-ras and K-ras mutated cells demonstrates its efficacy in blocking Ras-mediated signaling. A-176120 shows anti-angiogenic effects by inhibiting vascular endothelial growth factor (VEGF) secretion and disrupting capillary formation in endothelial cells. In vivo studies reveal its ability to reduce tumor growth in Ras-transformed cells and enhance survival in animal models. These findings highlight A-176120 as a promising FPP analogue with potent anti-tumor and anti-angiogenic properties .
    A-176120
  • HY-P10819
    S9-CMC1 TFA

    		Histone Demethylase Apoptosis Cancer
    S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
    S9-CMC1 TFA
  • 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-N6972
    Cepharanthine
    4 Publications Verification

    		 Autophagy 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-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-N6972R
    Cepharanthine (Standard)

    		Autophagy SARS-CoV Cytochrome P450 Apoptosis Parasite Infection Inflammation/Immunology Cancer
    Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. 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 (Standard)
  • 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

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: