Search Result
Results for "
Enzyme Inhibition
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-107030
-
-
-
- HY-124781
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
ML406 is a small molecule probe that shows anti-tubercular activity via M.tuberculosis BioA (DAPA synthase) enzyme inhibition with an IC50 of 30 nM. M.tuberculosis BioA is an enzyme involved in biotin biosynthesis in M.tuberculosis .
|
-
-
- HY-B0580A
-
|
(-)-Ketorolac
|
COX
|
Inflammation/Immunology
|
|
(S)-Ketorolac is a nonsteroidal anti-inflammatory agent. (S)-ketorolac exhibits potent COX1 and COX2 enzyme inhibition .
|
-
-
- HY-161514
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-15 (Compound 6c) is a selective inhibitor of Xanthine oxidase (XO) (IC50=0.13 μM). Xanthine oxidase-IN-15 inhibits XO catalysis by forming a stable interaction with the active site of XO. Xanthine oxidase-IN-15 is mainly used in the study of hyperuricemia and gout .
|
-
-
- HY-163495
-
-
-
- HY-121328
-
|
S-2852F
|
Parasite
|
Infection
Neurological Disease
|
|
Empenthrin (S-2852F) is a synthetic pyrethroid. Empenthrin can be used in insecticides. Empenthrin shows a clear species-specificity in the inhibitory effect on the Pentobarbital (PTB)-metabolizing enzyme(s). Empenthrin prolongs PTB induced-sleeping time in mice through an inhibition of the PTB-metabolizing enzyme(s) in the liver, an effect that does not occur in rats. Empenthrin shows a clear species-specificity in the inhibitory effect on the PTB-metabolizing enzyme(s) .
|
-
-
- HY-W243460
-
|
|
Biochemical Assay Reagents
|
Others
|
|
EDTA copper(II) disodium salt, 97% can be used to eliminate the inhibition of enzyme-catalyzed reactions caused by trace heavy metals.
|
-
-
- HY-133078
-
|
|
Others
|
Cancer
|
|
Thienyldecyl isothiocyanate is an analog of thienylbutyl isothiocyanate that, like many isothiocyanates, demonstrates antiproliferative activity against cancer cells presumably by modulation of xenobiotic-metabolizing enzymes, such as by inhibition of cytochrome P450, and/or by induction of phase II detoxifying enzymes.
|
-
-
- HY-124334
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
L-161240 is an antibiotic, which exhibits antibacterial activity against Escherichia coli, through inhibition of LpxC enzyme (Ki is 50 nM) .
|
-
-
- HY-N11780
-
|
|
HIV
|
Infection
|
|
Clavirolide L (Compound 3) is a dolabellane-type diterpenoid that can be isolated from Clavularia viridis. Clavirolide L shows significant inhibition against HIV-1 without RT enzyme inhibition and can be used for HIV infection research .
|
-
-
- HY-130199
-
|
Parellic acid
|
Others
|
Metabolic Disease
|
|
Psoromic acid is a potent and selective RabGGTase (Rab geranylgeranyl transferase) inhibitor with an IC50 value of 1.3 µM. Psoromic acid is an antioxidative agent. Psoromic acid exhibits a competitive type of HMGR inhibition and mixed type of ACE (angiotensin converting enzyme) inhibition .
|
-
-
- HY-N2074
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
Picrinine, an akuammiline alkaloid, is isolated from the leaves of Alstonia scholaris. Picrinine exhibits anti-inflammatory activity through inhibition of the 5-lipoxygenase enzyme .
|
-
-
- HY-100796
-
|
Vatensol
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Guanoclor is an antihypertensive compound. Guanoclor is an adrenergic neurone-blocking agent, which also interferes with noradrenaline synthesis by inhibition of the enzyme dopamine beta-hydroxylase .
|
-
-
- HY-119737
-
|
|
Acetolactate Synthase (ALS)
|
Metabolic Disease
|
|
Chlorsulfuron blocks the biosynthesis of the amino acids valine and isoleucine in plants. Chlorsulfuron completely alleviates herbicide-induced growth inhibition. The site of action of Chlorsulfuron is the enzyme acetolactate synthase .
|
-
-
- HY-126404
-
-
-
- HY-W001857
-
|
N-Hydroxyoctanamide; Caprylhydroxamic acid
|
Biochemical Assay Reagents
Bacterial
|
Others
|
|
Octanohydroxamic acid (N-Hydroxyoctanamide; Caprylhydroxamic acid) can be used as an extractant for alkaloids, which are used in pharmaceutical and natural product research. Octanohydroxamic acid may also be involved in the inhibition of certain enzymes, such as hydroxamate hydrolases.
|
-
-
- HY-144717
-
|
|
Phosphatase
|
Metabolic Disease
|
|
PTP1B-IN-18 is an orally active complete mixed type protein tyrosine phosphatase 1B (PTP1B) inhibitor with a Ki of 35.2 μM. PTP1B-IN-18 can be used for type 2 diabetes research .
|
-
-
- HY-147730
-
|
|
HDAC
|
Cancer
|
|
A variety of compounds were designed and synthesized by modifying cap groups. The enzyme inhibition test showed that compound 12C had broad-spectrum enzyme inhibitory activity, and compounds 9m and 9q were more inclined to inhibit HDAC6, showing a certain selective inhibitory activity among the representative subtypes.
|
-
-
- HY-148190
-
|
CGT-8012
|
Dipeptidyl Peptidase
|
Endocrinology
|
|
Sheng Gelieting (CGT-8012) is a dipeptidy peptidase-IV enzyme (DP-IV) inhibitor. Sheng Gelieting has great DP-IV inhibition activity with an IC50 value of 87 nM. Sheng Gelieting can be used for curing or preventing diseases relevant to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete .
|
-
-
- HY-12390
-
|
Lopramine
|
Others
|
Neurological Disease
|
|
Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties .
|
-
-
- HY-12390A
-
|
Lopramine hydrochloride
|
Others
|
Neurological Disease
|
|
Lofepramine (Lopramine) hydrochloride is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine hydrochloride stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine hydrochloride may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine hydrochloride has significant anxiolytic efficacy in addition to its antidepressant properties .
|
-
-
- HY-112179
-
|
|
Others
|
Inflammation/Immunology
|
|
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition .
|
-
-
- HY-76200S
-
|
UK-109496-d3
|
Fungal
|
Infection
|
|
Voriconazole-d3 is the deuterium labeled Voriconazole. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2].
|
-
-
- HY-148466
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
IGUANA-1 is a potent inhibitor of ALDH1B1, which is a mitochondrial enzyme that promotes colorectal and pancreatic cancer. IGUANA-1 has significant inhibition against cancer cells .
|
-
-
- HY-14829F
-
|
5-epi-Isofagomine
|
Glucosidase
|
Metabolic Disease
|
|
L-Afegostat (5-epi-Isofagomine) is a glycosidase inhibitor. L-Afegostat is an iminosugar that can be used for the synthesis of carbohydrates. L-Afegostat shows enzyme inhibition to β-Glucosidase with an Ki of 30 μM .
|
-
-
- HY-121275
-
|
|
Pyruvate Kinase
|
Cancer
|
|
Benserazide is a PKM2 inhibitor. Benserazide directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide can be used for the research of melanoma .
|
-
-
- HY-17543
-
|
|
Deubiquitinase
|
Cancer
|
|
ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
|
-
-
- HY-135534
-
|
|
Others
|
Others
|
|
Lysine 4-nitroanilide is an amino acid derivative used in studies of enzymology. Two major arylamidase activities were isolated from particle-free supernatant of rat heart by DEAE-Sephadex chromatography. Although both enzymes hydrolyze L-leucine 4-nitroanilide, only the peak II enzyme does so. A third, minor peak (Ia) contains the enzyme active primarily toward L-lysine 4-nitroanilide. The molecular weights of the enzymes in peaks I and II are approximately 257,000 and 105,000, respectively. The optimum pH for the peak I enzyme is approximately pH 7.0, while that for the peak II enzyme is between 7.0 and 8.0. Both enzymes are inhibited by puromycin, p-hydroxymercurybenzoate, catechol, and divalent metal ions. Addition of dithiothreitol stimulates both activities. Dialysis against catechol resulted in inhibition of both peak I and II enzymes, but dialysis against EDTA inhibited only the peak II enzyme.
|
-
-
- HY-B0690
-
-
-
- HY-W032848
-
|
Y-3642
|
COX
|
Inflammation/Immunology
|
|
Tinoridine (Y-3642) is an orally active non-steroidal anti-inflammatory agent with potent antiperoxidative ability and radical scavenger activity. Tinoridine acts function by inhibiting COX enzyme, involves in hepatotoxicity inhibition. .
|
-
-
- HY-118175
-
|
|
Others
|
Others
|
|
RG 14921, a compound structurally related to erbstatin, was investigated for its mechanism of inhibition of epidermal growth factor (EGF) receptor tyrosine kinase and CAMP-dependent kinase activity by kinetic analysis. Both compounds are slow-binding inhibitors of EGF receptor kinase. Erbstatin inhibits EGF receptor kinase as a partially competitive inhibitor relative to ATP and peptide substrates, suggesting that it binds at different positions in the enzyme's ATP- and peptide substrate-binding sites, thereby reducing the enzyme's binding affinity for both substrates. In contrast, the derivative RG 14921 inhibits EGF receptor kinase activity as a noncompetitive inhibitor relative to ATP and peptide substrates. Structurally related compounds exhibit different modes of inhibition, suggesting that the catalytic center of the receptor kinase domain may have a dynamic and possibly extended structure. Erbstatin and RG 14921 exerted similar effects on CAMP-dependent protein kinase activity. In this system, both compounds exhibited strong inhibition and acted in a competitive inhibition manner with ATP and a noncompetitive inhibition manner with peptide substrates.
|
-
-
- HY-B1543
-
-
-
- HY-N2010
-
-
-
- HY-120865
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
1,3-PBIT is a potent inhibitor of iNOS with a Ki of 47 nM compared to Ki values for eNOS and nNOS are 9 and 0.25 μM, respectively, for the purified human enzymes. Its inhibition in whole cells is greatly diminished, presumably to poor membrane permeability.
|
-
-
- HY-N0579
-
Fraxin
3 Publications Verification
Fraxoside
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Fraxin isolated from Cortex Fraxini, is a glucoside of fraxetin and reported to exert potent anti-oxidative stress action , anti-inflammatory and antimetastatic properties. Fraxin shows its antioxidative effect through inhibition of cyclo AMP phosphodiesterase enzyme .
|
-
-
- HY-P1998
-
|
|
Others
|
Others
|
|
Pepsinostreptin is an enzyme inhibitor with the activity of inhibiting pepsin. Pepsinostreptin can form a 1:1 complex with pepsin and significantly inhibit its activity. The activity of pepsinostreptin makes it have important application potential in the study of protease inhibition and related biological processes .
|
-
-
- HY-P2776
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hexokinase (ScHEX1) (EC 2.7.1.1) is a glycolytic enzyme hexokinase that is inhibited by n-acetylglucosamine. Inhibition of Hexokinase (ScHEX1) by n-acetylglucosamine leads to its separation from the mitochondrial outer membrane, resulting in activation of NLRP3 inflammasome .
|
-
-
- HY-119737R
-
|
|
Acetolactate Synthase (ALS)
|
Metabolic Disease
|
|
Chlorsulfuron (Standard) is the analytical standard of Chlorsulfuron. This product is intended for research and analytical applications. Chlorsulfuron blocks the biosynthesis of the amino acids valine and isoleucine in plants. Chlorsulfuron completely alleviates herbicide-induced growth inhibition. The site of action of Chlorsulfuron is the enzyme acetolactate synthase .
|
-
-
- HY-144738
-
|
|
Epoxide Hydrolase
FAAH
|
Inflammation/Immunology
|
|
Dual FAAH/sEH-IN-1 (compound 3) is a high affinity dual sEH (soluble epoxide hydrolase) and FAAH (fatty acid amide hydrolase) inhibitor, with IC50 values of 9.6 and 7 nM, respectively. Dual FAAH/sEH-IN-1 shows antinociception against the inflammatory phase .
|
-
-
- HY-12390S
-
|
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Lofepramine-d3 (Lopramine-d3) is the deuterium labeled Lofepramine. Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties[1].
|
-
-
- HY-P2818
-
|
Apase
|
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
|
Alkaline phosphatase, Bovine intestine (Apase) is a membrane-bound glycoprotein that catalyzes the hydrolysis of phosphate monoesters at alkaline pH. Alkaline phosphatase can be used in molecular biology and enzyme-free analysis. Inhibition of tissue nonspecific alkaline phosphatase can block intracellular lipid accumulation .
|
-
-
- HY-76200
-
|
UK-109496
|
Fungal
Bacterial
|
Infection
Cancer
|
|
Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes .
|
-
-
- HY-P1923
-
|
L-ASNase
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
L-Asparaginase (L-ASNase) is a deamidating enzyme that catalyses the hydrolysis of L-asparagine and L-glutamine, and can be used for the research of acute lymphoblastic leukemia. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis .
|
-
-
- HY-132987
-
|
ARX-1796; AV-006
|
Beta-lactamase
Bacterial
|
Infection
|
|
Avibactam tomilopil (ARX-1796, AV-006), an Avibactam proagent, is an orally bioavailable β-lactamase inhibitor. Avibactam has a spectrum of inhibition of class A and C β-lactamases, including ESBLs, AmpC and Klebsiella pneumoniae carbapenemase (KPC) enzymes .
|
-
-
- HY-76200B
-
|
UK-109496 camphorsulfonate
|
Fungal
Bacterial
|
Infection
Cancer
|
|
Voriconazole (UK-109496) camphorsulfonate is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole camphorsulfonate exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes .
|
-
-
- HY-160912
-
|
|
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 .
|
-
-
- HY-115312
-
|
|
Others
|
Others
|
|
Ro 18-5364 is an inhibitor of gastric (H? + K?)-ATPase, which has the effect of inhibiting the activity of the enzyme. Ro 18-5364 has a very strong inhibitory effect on gastric mucosal (H? + K?)-ATPase, and the inhibitory effect is more significant at low pH. At the same time, there is no selectivity difference between the two enantiomers of (H? + K?)-ATPase, and its inhibitory effect can be studied and verified by a variety of experimental methods, including inhibition of enzyme activity, proton transport, and studies on its binding.
|
-
-
- HY-157068
-
|
|
Ferroptosis
|
Cancer
|
|
icFSP1 is a potent ferroptosis suppressor protein-1 (FSP1) inhibitor. icFSP1 does not competitively inhibit FSP1 enzyme activity, but instead triggers subcellular relocalization of FSP1 from the membrane and FSP1 condensation before ferroptosis induction, in synergism with GPX4 inhibition .
|
-
-
- HY-131605
-
|
GCV-TP
|
Endogenous Metabolite
|
Cancer
|
|
Ganciclovir triphosphate (GCV-TP) is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate has an IC50 of 0.01 μM and has good antiviral effects against CMV strains from humans, monkeys, mice, and guinea pigs. Ganciclovir triphosphate has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
|
-
-
- HY-152252
-
|
|
Bacterial
Fungal
|
Infection
|
|
Antibacterial agent 133 (4l) is an antimicrobial agent that has shown anti-Candida activity, particularly through LMD enzyme inhibition. Antibacterial agent 133 shows MIC90 values of 1.95 μg/mL against Candida albicans ATCC 24433, Candida smoothis ATCC 90030 and Candida subtilis ATCC 22019 .
|
-
- HY-N0579R
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Fraxin (Standard) is the analytical standard of Fraxin. This product is intended for research and analytical applications. Fraxin isolated from Cortex Fraxini, is a glucoside of fraxetin and reported to exert potent anti-oxidative stress action , anti-inflammatory and antimetastatic properties. Fraxin shows its antioxidative effect through inhibition of cyclo AMP phosphodiesterase enzyme .
|
-
- HY-133116
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
|
-
- HY-147691
-
|
|
Glutathione Peroxidase
Potassium Channel
|
Inflammation/Immunology
|
|
MPO-IN-5 (compound 1) is a potent, irreversible MPO (myeloperoxidase) inhibitor. MPO-IN-5 inhibits MPO peroxidation and hERG binding, with IC50 values of 0.22 and 2.8 μM, respectively. MPO-IN-5 shows rapid kinetics of inhibition, with enzyme inactivation rate (kinact/Ki) of 23000 M −1s −1 .
|
-
- HY-W587663
-
|
|
Dihydrofolate reductase (DHFR)
|
Infection
|
|
4 '-DTMP is a DHFR inhibitor with Ki of 5.1 nM (DHFR WT) and 34.3 nM (DHFR L28R), respectively. 4 '-DTMP carries a polar modification that induces additional local interactions with the enzyme. In particular, the hairpin structure on the M20 ring is related to the internal communication of the DHFR. 4 '-DTMP has potential inhibition of E.coli .
|
-
- HY-N2010R
-
|
|
Bacterial
HIV
Reactive Oxygen Species
|
Infection
Cardiovascular Disease
Cancer
|
|
Methyl gallate (Standard) is the analytical standard of Methyl gallate. This product is intended for research and analytical applications. Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitory activities.
|
-
- HY-113600
-
|
|
Others
|
Others
|
|
H-0106 dihydrochloride is a ROCK inhibitor with potent intraocular pressure (IOP)-lowering activity. H-0106 dihydrochloride can effectively inhibit ROCK enzyme. H-0106 dihydrochloride demonstrated significant IOP-lowering effects in monkey eyes. Studies with H-0106 dihydrochloride suggest that there may not be a direct relationship between ROCK inhibition and IOP reduction .
|
-
- HY-146410
-
|
|
Angiotensin Receptor
|
Others
|
|
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
|
-
- HY-144718
-
|
|
Phosphatase
|
Metabolic Disease
|
|
PTP1B-IN-17 (Compound 45), a potential selective benzimidazole derivative, acts as a protein tyrosine phosphatase 1B (PTP1B) inhibitor with a Ki of 30.2 μM. PTP1B-IN-17 can be used for the research of type 2 diabetes.
|
-
- HY-144716
-
|
|
Phosphatase
|
Metabolic Disease
|
|
PTP1B-IN-19 (Compound 43), a potential selective benzimidazole derivative, acts as a protein tyrosine phosphatase 1B (PTP1B) inhibitor with a Ki of 23.3 μM. PTP1B-IN-19 can be used for the research of type 2 diabetes.
|
-
- HY-144713
-
|
|
Phosphatase
|
Metabolic Disease
|
|
PTP1B-IN-16 (Compound 46), a potential selective benzimidazole derivative, acts as a protein tyrosine phosphatase 1B (PTP1B) inhibitor with a Ki of 12.6 μM. PTP1B-IN-16 can be used for the research of type 2 diabetes.
|
-
- HY-16731
-
|
EVT 302; RG1577; RO4602522
|
Monoamine Oxidase
Reactive Oxygen Species
|
Neurological Disease
|
|
Sembragiline (EVT 302) is a potent, selective and reversible monoamine oxidase B (MAO-B) inhibitor. Sembragiline reduces the metabolism of dopamine and other amine neurotransmitters by inhibiting the activity of the MAO-B enzyme, thereby potentially increasing the concentration of these neurotransmitters in the brain. Inhibition of the MAO-B enzyme also reduces the formation of toxic reactive oxygen species (ROS) that play a role in the pathological process of AD. Sembragiline has good oral activity and blood-brain barrier permeability. Sembragiline can be used in studies of AD, especially in patients with AD who show increased MAO-B activity .
|
-
- HY-A0004
-
Decitabine
Maximum Cited Publications
99 Publications Verification
5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716
|
DNA Methyltransferase
Apoptosis
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity .
|
-
- HY-P2802
-
|
α-D-Glucosidase, Yeast
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase, Yeast (α-D-Glucosidase, Yeast), a carbohydrate hydrolyzing enzyme, catalyzes the liberation of α-glucose from the non-reducing end of the substrate. α-Glucosidase can facilitate the absorption of glucose by the small intestine. Inhibition of α-Glucosidase is an effective management of non-insulin-dependent diabetes mellitus (NIDDM) .
|
-
- HY-76200R
-
|
UK-109496 (Standard)
|
Fungal
Bacterial
|
Infection
Cancer
|
|
Voriconazole (Standard) is the analytical standard of Voriconazole. This product is intended for research and analytical applications. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes .
|
-
- HY-10572A
-
|
(R)-DMP 266; (R)-EFV; (R)-L-743726
|
Reverse Transcriptase
|
Infection
|
|
(R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .
|
-
- HY-116138
-
|
|
Others
|
Others
|
|
RG-14467 is an epidermal growth factor receptor tyrosine kinase inhibitor with activity that inhibits enzyme activity. RG-14467 has similar inhibition kinetics to Lavendustin-A, with a dissociation constant of 3.4μM for the initial rapidly formed complex and an overall dissociation constant estimated to be less than or equal to 30nM, and is a partially competitive inhibitor for ATP.
|
-
- HY-129923
-
|
|
Others
|
Neurological Disease
|
|
(R)-Omeprazole sodium is a gastric acid resistant compound with activity to inhibit gastric acid secretion. (R)-Omeprazole sodium is metabolized in vivo, and its metabolism is primarily affected by cytochrome P450 enzymes. The interaction between (R)-Omeprazole sodium and mannitol may affect its bioavailability in formulations. (R)-Omeprazole sodium exhibits reversible direct and metabolism-dependent inhibition of CYP2C19 .
|
-
- HY-117318
-
|
|
Phosphodiesterase (PDE)
|
Infection
|
|
PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. PDE12-IN-1 increases 2′,5′-linked adenylate polymers (2-5A) levels, and the pEC50 value is 7.7. PDE12-IN-1 shows antiviral activity .
|
-
- HY-130244
-
|
|
Beta-secretase
|
Neurological Disease
|
|
BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux .
|
-
- HY-145270
-
|
|
Others
|
Metabolic Disease
|
|
ELOVL1-IN-2 is an elongation of very long chain fatty acid 1 (ELOVL1) enzyme inhibitor, ELOVL1-IN-2 shows weak ELOVL1 inhibition (IC50=21 μM) and moderate potency in a primary cellular assay (HEK293 C26 IC50=6.7 μM) .
|
-
- HY-143897
-
|
|
Pim
Apoptosis
|
Cancer
|
|
PIM1-IN-3 (Compound HL8) is a potent inhibitor of PIM1. PIM1-IN-3 shows selective inhibition for the PIM-1 enzyme. PIM1-IN-3 induces apoptosis efficiently in Colo320 cells. PIM1-IN-3 has the potential for the research of cancer diseases .
|
-
- HY-143898
-
|
|
Pim
|
Cancer
|
|
PIM1-IN-4 (Compound 8) is a potent inhibitor of PIM1. PIM1-IN-4 reveals strong inhibition of five other enzymes, i.e., SGK-1, PKA, CaMK-1, GSK3β, and MSK1. PIM1-IN-4 has the potential for the research of cancer diseases .
|
-
- HY-W014316
-
|
|
Bacterial
Fungal
|
Infection
|
|
5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol .
|
-
- HY-162238
-
|
|
Parasite
|
Infection
|
|
OSM-S-106 is a pro-inhibitor and that inhibition of PfAsnRS occurs via enzyme-mediated production of an Asn-OSM-S-106 adduct. OSM-S-106 inhibits protein translation and activates the amino acid starvation response. OSM-S-106 exhibits selective activity against Plasmodium blood and liver stages and low intrinsic clearance by human microsomes .
|
-
- HY-W422288
-
|
(Rac)-Ketoconazol; (Rac)-R 41400
|
Fungal
Cytochrome P450
|
Infection
|
|
(Rac)-Ketoconazole ((Rac)-R 41400) is an antifungal imidazole compound with oral activity. (Rac)-Ketoconazole interferes with ergosterol synthesis by inhibiting cytochrome P450-dependent 14α-sterol demethylase (CYP51), a key enzyme on the fungal cell membrane, leading to membrane dysfunction and ultimately inhibition of fungal growth and reproduction. (Rac)-Ketoconazole is indicated for studies of fungal infections .
|
-
- HY-116804
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
|
-
- HY-158177
-
|
|
EGFR
|
Cancer
|
|
EGFR T790M/L858R-IN-6 (compound 53), a pyrimidine compound, is a potent EGFR T790M/L858R inhibitor. EGFR T790M/L858R-IN-6 shows 90.88% enzyme activity inhibition with 0.05 μM .
|
-
- HY-119726
-
|
APX001; E1211
|
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Fosmanogepix (APX001) is a broad-spectrum agent against invasive fungal infections. Fosmanogepix (APX001) targets the conserved Gwt1 enzyme required for the localization of glycosylphosphatidylinositol-anchored mannoproteins in fungi. This inhibition prevents the appropriate localization of cell wall mannoproteins, which compromises cell wall integrity, biofilm formation, germ tube formation, and fungal growth. Fosmanogepix (APX001) can be used for invasive fungal infections research .
|
-
- HY-149987
-
|
KHK-IN-3
|
Ketohexokinase
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
KHK-IN-3 (Example 1) is a ketohexokinase (KHK) inhibitor. KHK-IN-3 can be used in the study of kidney disease, nonalcoholic steatohepatitis (NASH), diabetes and heart failure. KHK is a rate-limiting enzyme and fructokinase involved in fructose metabolism. KHK catalyzes the phosphorylation of fructose to fructose-1-phosphate (FIP) at the expense of ATP. The lack of feedback inhibition of fructose metabolism triggers the accumulation of downstream intermediates such as lipogenesis, gluconeogenesis, and oxidative phosphorylation .
|
-
- HY-A0004R
-
|
5-Aza-2'-deoxycytidine (Standard); 5-AZA-CdR (Standard); NSC 127716 (Standard)
|
DNA Methyltransferase
Apoptosis
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Decitabine (Standard) is the analytical standard of Decitabine. This product is intended for research and analytical applications. Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity .
|
-
- HY-158368
-
|
|
Apoptosis
ROS Kinase
|
Cancer
|
|
PRDX1-IN-2 (compound 15) is a selective inhibitor of the antioxidant enzyme Peroxiredoxin 1 (PRDX1) (IC50=0.35 μM). PRDX1-IN-2 decreases the mitochondria membrane potential of SW620 cells, probably due to ROS induced by PRDX1 inhibition, leading to cell apoptosis. PRDX1-IN-2 can be used for colorectal cancer research .
|
-
- HY-119726A
-
|
APX001 (tautomerism); E1211 (tautomerism)
|
Fungal
|
Infection
Inflammation/Immunology
|
|
Fosmanogepix tautomerism (APX001 tautomerism) is a broad-spectrum and orally active anti-invasive fungal compound. Fosmanogepix tautomerism targets the conserved Gwt1 enzyme required for the localization of glycosylphosphatidylinositol-anchored mannoproteins in fungi, and inhibition prevents proper localization of cell wall mannoproteins, thereby impairing cell wall integrity, biofilm formation, germ tube formation, and fungal growth. Fosmanogepix tautomerism can be used to study invasive fungal infections .
|
-
- HY-118061
-
|
|
Others
|
Infection
|
|
VCC234718 is a molecule with mycobacterial growth inhibitory activity, specifically targeting Mycobacterium tuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
|
-
- HY-136818
-
|
|
Others
|
Endocrinology
|
|
DA 4643 (hydrochloride) is an H2 receptor antagonist with the chemical name 2-guanidino-4 (3-methylaminomethyleneiminophenyl) thiazole dihydrochloride. It has a weak interaction with cytochrome P-450 and has a less inhibitory effect on P-450 than cimetidine and tiotidine. DA 4643 (hydrochloride) is able to inhibit both enzymatic and non-enzymatic lipid peroxidation reactions. This inhibition may not be achieved by inhibiting agent metabolizing enzymes, but rather due to the antioxidant properties of the compound itself. Compared with other H2 receptor antagonists such as cimetidine, ranitidine and tiotidine, DA 4643 (hydrochloride) shows a unique effect in lipid peroxidation inhibition. These properties make DA 4643 (hydrochloride) a potential H2 receptor antagonist with multiple mechanisms of action.
|
-
- HY-117247
-
|
|
DNA/RNA Synthesis
|
Infection
|
|
5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor with inhibitory activity against other folate-related enzymes. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed mild growth inhibition against enterococci, lactic acid bacteria, and L1210 cells in culture. 5,6,7,8-Tetrahydro-8-deazahomofolic acid also showed weak inhibition against thymidylate synthase, dihydrofolate reductase, glycyl-ribonucleoside aminotransferase, and aminoimidazole-carboxyacyl-ribonucleoside aminotransferase. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed low substrate activity for thymidylate synthase .
|
-
- HY-N0385
-
|
|
AMPK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
Gomisin J is a small molecular weight lignan found in Schisandra chinensis and has been demonstrated to have vasodilatory activity . Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca 2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells. gomisin J has potential benefits in treating nonalcoholic fatty liver disease .
|
-
- HY-144381
-
|
|
Bacterial
|
Infection
|
|
Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 µM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents .
|
-
- HY-N2045
-
|
|
PI3K
Akt
Apoptosis
Cytochrome P450
|
Neurological Disease
|
|
Musk ketone is a widely used artificial fragrance. Musk ketone is also a cytochrome P450 enzyme inducer. Musk ketone shows mutagenic and comutagenic effects in Hep G2 cells and induces neural stem cell proliferation and differentiation in cerebral ischemia via activation of the PI3K/Akt signaling pathway. In the brain, musk ketone is neuroprotective against stroke injury through inhibition of cell apoptosis .
|
-
- HY-W011258
-
|
L-Tyrosyl-L-phenylalanine
|
Xanthine Oxidase
Angiotensin-converting Enzyme (ACE)
|
Inflammation/Immunology
Cancer
|
|
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells .
|
-
- HY-P2848A
-
|
|
Toll-like Receptor (TLR)
|
Infection
Metabolic Disease
|
|
Cholesterol oxidase, Rhodococcus sp. is a key enzyme in the cholesterol degradation process. It catalyzes the isomerization and oxidation of cholesterol mediated by the coenzyme FAD. Research indicates that cholesterol oxidase plays a crucial role in the pathogenicity of Mycobacterium tuberculosis by modulating the host macrophage immune response through inhibition of the Toll-like receptor 2 (TLR2) signaling pathway, thereby enhancing the survival of Mycobacterium tuberculosis. Cholesterol oxidase, from Rhodococcus sp., shows potential for research in the field of tuberculosis .
|
-
- HY-W195933
-
|
|
Others
|
|
|
6-Aminopyridine-3-thioamide is a compound with anti-tumor activity that can inhibit the activity of specific enzymes, thereby affecting cell proliferation and survival. 6-Aminopyridine-3-thioamide has also been studied for the inhibition of neurodegenerative diseases and has shown the potential to improve neurological function. The structural characteristics of 6-Aminopyridine-3-thioamide make it an important bioactive molecule in compound development.
|
-
- HY-111191
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment .
|
-
- HY-N0354
-
|
|
Virus Protease
Topoisomerase
Apoptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Anthraquinone is used as a precursor for dye formation and agrochemicals, existing in different organisms, such as bacteria, fungi, plants, and some animals. Anthraquinone has biological activities: anticancer, antiinflammatory, diuretic, antiarthritic, antifungal, antibacterial, antimalarial and antioxidant. Anthraquinone also plays an important role in the primary metabolism of plants by acting on the electron transport chain through the inhibition of energy transfer in the photosynthetic process. Anthraquinone can intercalates into DNA and inhibits the topoisomerase II (topo II) enzyme, resulting in cell death via Apoptosis .
|
-
- HY-161063
-
-
- HY-161064
-
|
|
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
DHFR-IN-15 (compound 34) is a dihydrofolate reductase (DHFR) inhibitor with potential anticancer activity. DHFR-IN-15 effectively binds to DHFR in cells, reducing DHFR levels to 10 nM .
|
-
- HY-W050154R
-
|
|
Parasite
Tyrosinase
NF-κB
CDK
|
Infection
Inflammation/Immunology
Cancer
|
|
Kojic acid (Standard) is the analytical standard of Kojic acid. This product is intended for research and analytical applications. Kojic acid is a substance produced by Aspergillus oryzae, with various biological activities including antitumor, insecticidal, antibacterial, antioxidant, and radioprotective effects. Kojic acid exhibits tyrosinase inhibition activity by capturing copper ions that bind to the active site of tyrosinase, preventing its activation. Tyrosinase is a key enzyme in the biosynthesis of melanin, so kojic acid can block melanin production. Additionally, kojic acid shows potential inhibition of NF-κB activity in human keratinocytes, which may also be related to the anti-melanogenic effect induced by kojic acid. Kojic acid is effective when administered orally and can also be absorbed transdermally. Nano-carrier systems prepared with kojic acid demonstrate effective delivery of anticancer drugs. Kojic acid holds promise for research in cancer, infectious diseases, and skin whitening among other fields .
|
-
- HY-N8161
-
|
Kaempferol 3,7-diglucoside
|
Glucosidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside), a flavonol, possesses enzyme inhibition property towards α-amylase, α-glucosidase and Acetylcholinesterase. Kaempferol-3,7-di-O-β-glucoside protects differentiating neuronal cells, SH-SY5Y from Amyloid β peptide-induced injury. Kaempferol-3,7-di-O-β-glucoside has the potential for Alzheimer's research .
|
-
- HY-147720
-
|
|
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.
|
-
- HY-114564
-
|
E5510
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Satigrel (E5510) is a potent inhibitor of platelet aggregation. Satigrel inhibits collagen- and arachidonic acid-induced platelet aggregation through preventing thromboxane A2 synthesis by selective inhibition of the target enzyme, PGHS1, which exists in platelets. Satigrel inhibits PGHS1 (IC50: 0.081 μM) and PGHS2 (IC50: 5.9 μM). Satigrel is against Type III PDE, Type V and Type II (IC50: 15.7 μM, 39.8 μM and 62.4 μM, respectively) .
|
-
- HY-161449
-
|
|
11β-HSD
|
Metabolic Disease
|
|
JTT-654 is an orally active, potent and selective11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. The IC50 of JTT-654 for 11β-HSD1 is 4.65, 0.97, and 0.74 nM in human, rat, and mouse recombinant enzymes, respectively. JTT-654 showed competitive inhibition against human recombinant enzyme. The IC50 value for human 11β-HSD2 is > 30 μM (human 11β-HSD2 is responsible for the reverse reaction against human 11β-HSD1). JTT-654 ameliorates insulin resistance and non-obese type 2 diabetes by inhibiting adipose tissue and liver 11β-HSD1 .
|
-
- HY-108347
-
|
|
P-glycoprotein
BCRP
|
Metabolic Disease
|
|
CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM) .
|
-
- HY-150260
-
|
|
Bacterial
|
Infection
|
|
SA09-Cu is a noncompetitive and potent NDM-1 inhibitor with an IC50 of 9.6 nM. SA09-Cu can convert NDM-1 into an inactive state by oxidizing the Zn(II)-thiolate site of the enzyme and avoids to be reduced by intracellular thiols of bacteria. SA09-Cu exhibits excellent inhibition against a series of clinical NDM-1-producing carbapenem-resistant Enterobacteriaceae (CRE) in restoring the Meropenem (HY-13678) effect, and slows down the development of carbapenem resistance .
|
-
- HY-122026
-
|
PF-367
|
GSK-3
|
Neurological Disease
|
|
PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay.?PF-04802367 shows desirable central nervous system (CNS)?properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50?values of 10.0 and 9.0 nM in mobility shift assays, respectively .
|
-
- HY-169217
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP3A4-IN-4 (compound Δ,Λ-3), a Ru(II)−Ir(III) Conjugate, is a photoactive inhibitor of the major human drug metabolizing enzyme CYP3A4. CYP3A4-IN-4 containing the [Ru(tpy)(Me2bpy)] photocaging group showed an IC50 of 2.2 μM for inhibition of microsomal CYP3A4 under light conditions (λirr=530 nm, tirr=15 min). CYP3A4-IN-4 shows the phototherapeutic index (PI) for of 5.4 .
|
-
- HY-D0837
-
|
Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene
|
Ser/Thr Protease
Thrombopoietin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease .
|
-
- HY-161649
-
|
|
Cytochrome P450
Aryl Hydrocarbon Receptor
|
Cancer
|
|
hCYP1B1-IN-2 (compound 3n) is a potent human cytochrome P450 1B1 enzyme hCYP1B1 inhibitor. hCYP1B1-IN-2 shows the extremely potent anti-hCYP1B1 activity (IC50=0.040 nM) and blocks AhR transcription activity. hCYP1B1-IN-2 potently inhibits hCYP1B1 via a mix inhibition manner, showing a Ki value of 21.71 pM .
|
-
- HY-W014316R
-
|
|
Bacterial
Fungal
|
Infection
|
|
5-Bromo-5-nitro-1,3-dioxane (Standard) is the analytical standard of 5-Bromo-5-nitro-1,3-dioxane. This product is intended for research and analytical applications. 5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol .
|
-
- HY-117807
-
|
|
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 .
|
-
- HY-D0837R
-
|
|
Ser/Thr Protease
Thrombopoietin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Imidazole (Standard) is the analytical standard of Imidazole. This product is intended for research and analytical applications. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease .
|
-
-
-
HY-L044
-
|
|
550 compounds
|
|
Nucleoside and nucleotide analogues are synthetic, chemically modified compounds that have been developed to mimic their physiological counterparts in order to exploit cellular metabolism and subsequently be incorporated into DNA and RNA to inhibit cellular division and viral replication. In addition to their incorporation into nucleic acids, nucleoside and nucleotide analogues can interact with and inhibit essential enzymes such as human and viral polymerases (that is, DNA-dependent DNA polymerases, RNA-dependent DNA polymerases or RNA-dependent RNA polymerases), kinases, ribonucleotide reductase, DNA methyltransferases, purine and pyrimidine nucleoside phosphorylase and thymidylate synthase. These actions of nucleoside and nucleotide analogues have potential therapeutic benefits — for example, in the inhibition of cancer cell growth, the inhibition of viral replication as well as other indications.
MCE offers a unique collection of 550 nucleotide compounds including nucleotide, nucleoside and their structural analogues. MCE Nucleotide Compound Library is a useful tool to discover anti-cancer and antiviral drugs for high throughput screening (HTS) and high content screening (HCS).
|
-
-
HY-L130
-
|
|
616 compounds
|
|
Non-steroidal anti-inflammatory drugs (NSAIDs) are members of a therapeutic drug class with potent anti-inflammatory, analgesic and antipyretic activity, and are among the most widely used drugs worldwide. The most prominent NSAIDs are aspirin, ibuprofen, and naproxen.
The main mechanism of action of NSAIDs is the inhibition of the enzyme cyclooxygenase (COX), based on which NSAIDs can be classified into two types: non-selective and COX-2 selective. Most NSAIDs are non-selective and inhibit both COX-1 and COX-2 activity.
MCE offers a unique collection of 616 non-steroidal compounds with identified anti-inflammatory activity. MCE non-steroidal anti-inflammatory library is a useful tool for the study of anti-inflammatory drugs and pharmacology.
|
-
-
HY-L067
-
|
|
688 compounds
|
|
Antibiotics are types of antimicrobial products used for the treatment and prevention of bacterial infections. Antibiotics can kill or inhibit bacterial growth. Although the target of an antibiotic is bacteria, some antibiotics also attack fungi and protozoans. However, antibiotics rarely have an effect on viruses. The major mechanism underlying antibiotics is the inhibition or regulation of enzymes involved in cell wall biosynthesis, nucleic acid metabolism and repair, protein synthesis, or disruption of membrane structure. Many of these cellular functions targeted by antibiotics are most active in multiplying cells. Since there is often overlap in these functions between prokaryotic bacterial cells and eukaryotic mammalian cells, it is not surprising that some antibiotics have also been found to be useful as anticancer agents.
MCE supplies a unique collection of 688 antibiotics, including penicillins, cephalosporins, tetracyclines, macrolides, etc. MCE Antibiotics Library is a useful tool for anti-bacterial or anti-cancer drugs discovery.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D0837
-
|
Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene
|
Cell Assay Reagents
|
|
Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease .
|
-
- HY-W699238
-
|
|
Cell Assay Reagents
|
|
S-(-)-Aminoglutethimide D-tartrate is an aromatase inhibitor with activity that blocks adrenal steroidogenesis. S-(-)-Aminoglutethimide D-tartrate can be used to inhibit steroid-related diseases. S-(-)-Aminoglutethimide D-tartrate is often used clinically to control certain types of cancer. S-(-)-Aminoglutethimide D-tartrate effectively reduces testosterone and estrogen levels through an enzyme inhibition mechanism.
|
-
- HY-D0837R
-
|
|
Cell Assay Reagents
|
|
Imidazole (Standard) is the analytical standard of Imidazole. This product is intended for research and analytical applications. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-W011258
-
|
L-Tyrosyl-L-phenylalanine
|
Xanthine Oxidase
Angiotensin-converting Enzyme (ACE)
|
Inflammation/Immunology
Cancer
|
|
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells .
|
-
- HY-P4594
-
|
|
Peptides
|
Others
|
|
Z-Phe-His-Leu is the substrate of plasma converting enzyme, with enhanced discriminating power at peak converting enzyme inhibition .
|
-
- HY-P10244F
-
|
|
Peptides
|
Infection
|
|
Biotin-YVAD-FMK is an inhibitor for vacuolar processing enzyme (VPE), with a 64% inhibition at 5 μM. Biotin-YVAD-FMK is an irreversible substrate for caspase 1 .
|
-
- HY-P10346
-
|
Smooth-Muscle Myosin Light-Chain Kinase (796-815)
|
Peptides
|
Cardiovascular Disease
Inflammation/Immunology
|
|
smMLCK peptide is a specific inhibitor of smooth muscle myosin light chain kinase (smMLCK). The smMLCK peptide mimics the substrate and competitively inhibits the binding of the actual substrate to the enzyme, thereby inhibiting the kinase activity. This inhibition prevents the phosphorylation of the myosin light chain, thus inhibiting muscle contraction .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-130199
-
-
-
- HY-N2074
-
-
-
- HY-N2010
-
-
-
- HY-N0579
-
-
-
- HY-P2818
-
-
-
- HY-76200
-
Voriconazole
Maximum Cited Publications
6 Publications Verification
UK-109496
|
Microorganisms
Source classification
|
Fungal
Bacterial
|
|
Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes .
|
-
-
- HY-N11780
-
-
-
- HY-P1998
-
-
-
- HY-N0579R
-
-
-
- HY-N2010R
-
-
-
- HY-76200R
-
|
UK-109496 (Standard)
|
Microorganisms
Source classification
|
Fungal
Bacterial
|
|
Voriconazole (Standard) is the analytical standard of Voriconazole. This product is intended for research and analytical applications. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes .
|
-
-
- HY-N0385
-
-
-
- HY-N0354
-
|
|
Seeds of Cassia tora Linn.
Quinones
Structural Classification
other families
Classification of Application Fields
Leguminosae
Anthraquinones
Source classification
Other Diseases
Plants
Disease Research Fields
|
Virus Protease
Topoisomerase
Apoptosis
|
|
Anthraquinone is used as a precursor for dye formation and agrochemicals, existing in different organisms, such as bacteria, fungi, plants, and some animals. Anthraquinone has biological activities: anticancer, antiinflammatory, diuretic, antiarthritic, antifungal, antibacterial, antimalarial and antioxidant. Anthraquinone also plays an important role in the primary metabolism of plants by acting on the electron transport chain through the inhibition of energy transfer in the photosynthetic process. Anthraquinone can intercalates into DNA and inhibits the topoisomerase II (topo II) enzyme, resulting in cell death via Apoptosis .
|
-
-
- HY-W050154R
-
|
|
Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Parasite
Tyrosinase
NF-κB
CDK
|
|
Kojic acid (Standard) is the analytical standard of Kojic acid. This product is intended for research and analytical applications. Kojic acid is a substance produced by Aspergillus oryzae, with various biological activities including antitumor, insecticidal, antibacterial, antioxidant, and radioprotective effects. Kojic acid exhibits tyrosinase inhibition activity by capturing copper ions that bind to the active site of tyrosinase, preventing its activation. Tyrosinase is a key enzyme in the biosynthesis of melanin, so kojic acid can block melanin production. Additionally, kojic acid shows potential inhibition of NF-κB activity in human keratinocytes, which may also be related to the anti-melanogenic effect induced by kojic acid. Kojic acid is effective when administered orally and can also be absorbed transdermally. Nano-carrier systems prepared with kojic acid demonstrate effective delivery of anticancer drugs. Kojic acid holds promise for research in cancer, infectious diseases, and skin whitening among other fields .
|
-
-
- HY-N8161
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-76200S
-
|
|
|
Voriconazole-d3 is the deuterium labeled Voriconazole. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2].
|
-
-
- HY-12390S
-
|
|
|
Lofepramine-d3 (Lopramine-d3) is the deuterium labeled Lofepramine. Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties[1].
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent:
