Search Result
Results for "
glycoprotein substrate
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0777
-
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CL301423
|
Antibiotic
BCRP
P-glycoprotein
Parasite
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Infection
Neurological Disease
|
|
Moxidectin (CL301423) is an orally active and brain-penetrant macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
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- HY-N11287A
-
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Endogenous Metabolite
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Others
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UDP-xylose disodium is an endogenous sugar nucleotide and a catalytic substrate of UDP-xylose disodium synthase (UXS). UDP-xylose disodium is a sugar donor for the synthesis of glycoproteins, polysaccharides, various metabolites and oligosaccharides in plants, vertebrates and fungi, and participates in the synthesis of proteoglycans as a glycosyl donor. UDP-xylose disodium participates in the regulation of the synthesis of extracellular matrix components and can be used to study the mechanism of proteoglycan biosynthesis in glycobiology and related diseases (such as connective tissue diseases)[1][2].
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- HY-107903
-
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Thyroglobulin from bovine
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Biochemical Assay Reagents
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Cancer
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Thyroglobulin is a 660 kDa, dimeric glycoprotein produced by the follicular cells of the thyroid and used entirely within the thyroid gland. Thyroglobulin acts as a substrate for the synthesis of the thyroid hormones thyroxine (T4) and triiodothyronine (T3), as well as the storage of the inactive forms of thyroid hormone and iodine within the follicular lumen of a thyroid follicle. Thyroglobulin activates Akt kinase activity in FRTL-5 thyroid cell .
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- HY-107212
-
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Parasite
Chloride Channel
P-glycoprotein
Bacterial
|
Infection
|
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Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM .
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- HY-17367
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-
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- HY-14895
-
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CM346
|
Parasite
Monoamine Oxidase
Sigma Receptor
P-glycoprotein
|
Infection
Cardiovascular Disease
Neurological Disease
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Fabomotizole (CM346) is an insecticide with anxiolytic, antianxiety, and neuroprotective activities and a substrate of p-glycoprotein. Fabomotizole inhibits the ST-segment depression induced by isoproterenol in a rat model of acute subendocardial ischemia. Fabomotizole also inhibits Giardia lamblia and has the potential to inhibit giardiasis. Fabomotizole also targets Sigma1R, NRH:quinone reductase 2 (NQO2), and MAO-A to exert anxiolytic effects .
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-
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- HY-108286
-
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Cordanum
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Adrenergic Receptor
|
Cardiovascular Disease
|
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Talinolol (Cordanum) is a long-acting, cardioselective β1-adrenergic receptor blocker. Talinolol exhibits cardioprotective and antihypertensive activities. Talinolol is also a well-known and frequently used probe substrate for P-glycoprotein (P-gp) activity .
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- HY-N2453
-
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PPAR
NF-κB
P-glycoprotein
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Inflammation/Immunology
Cancer
|
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Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .
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- HY-G0017
-
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Norimatinib; Imatinib metabolite N-Desmethyl imatinib; CGP 74588
|
Drug Metabolite
P-glycoprotein
Apoptosis
|
Neurological Disease
Cancer
|
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N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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- HY-17367A
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- HY-W039897
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α-Methyl-D-mannoside
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Environmental Pollutants
Bacterial
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Infection
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Methyl α-D-mannopyranoside (α-Methyl-D-mannoside) is a methyl glycoside derivative and conformational stabilizer of α-D-mannopyranose. The glycosidic bond conformation of Methyl α-D-mannopyranoside is significantly affected by the environment. In aqueous solution, Methyl α-D-mannopyranoside stabilizes into a trans conformation via intermolecular hydrogen bonds; in the gas phase, however, steric interactions drive Methyl α-D-mannopyranoside to prefer a clockwise gauche conformation. Methyl α-D-mannopyranoside also serves as a major component of secondary cell wall polymers in some bacteria and an active precursor site for virus-targeted glycoproteins. Methyl α-D-mannopyranoside acts as an acceptor substrate for alternansucrase, mediating the transfer of D-glucopyranosyl groups to generate a variety of glycosylated oligosaccharide products, with methyl α-D-glucopyranosyl-(1→6)-α-D-mannopyranoside as the main component. Methyl α-D-mannopyranoside is applicable to studies on bacterial pathogenic mechanisms associated with mannose-specific fimbrial lectins .
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- HY-P3008
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-
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- HY-A0279A
-
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Mikamycin B; Mikamycin IA
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Bacterial
Antibiotic
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Infection
|
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Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus .
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- HY-N11287
-
|
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Endogenous Metabolite
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Others
|
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UDP-xylose is an endogenous sugar nucleotide and a catalytic substrate of UDP-xylose synthase (UXS). UDP-xylose is a sugar donor for the synthesis of glycoproteins, polysaccharides, various metabolites and oligosaccharides in plants, vertebrates and fungi, and participates in the synthesis of proteoglycans as a glycosyl donor. UDP-xylose participates in the regulation of the synthesis of extracellular matrix components and can be used to study the mechanism of proteoglycan biosynthesis in glycobiology and related diseases (such as connective tissue diseases)[1][2].
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- HY-142686A
-
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SGK
CDK
P-glycoprotein
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Inflammation/Immunology
|
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SGK1-IN-3 hydrochloride (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC50 of <1 nM against hSGK1. SGK1-IN-3 hydrochloride blocks the activity of CDK family members. SGK1-IN-3 hydrochloride serves as a P-glycoprotein substrate. SGK1-IN-3 can be used for the research of osteoarthritis .
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- HY-16191
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
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- HY-B0777S
-
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CL-301423-d3
|
Isotope-Labeled Compounds
BCRP
Parasite
Antibiotic
P-glycoprotein
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Infection
|
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Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
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- HY-G0017S
-
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Norimatinib-d8; Imatinib metabolite N-Desmethyl imatinib-d8; CGP 74588-d8
|
Isotope-Labeled Compounds
Drug Metabolite
P-glycoprotein
Apoptosis
|
Neurological Disease
Cancer
|
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N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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- HY-173162
-
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P-glycoprotein
Potassium Channel
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Cardiovascular Disease
Cancer
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GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome .
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- HY-128038
-
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Opioid Receptor
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Neurological Disease
|
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N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein .
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- HY-E70039
-
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Others
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Others
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alpha-2-3,6,8-Sialidosidase (SpNanA) catalyses hydrolysis of alpha-(2->3)-, alpha-(2->6)-, alpha-(2->8)- glycosidic linkages of terminal sialic acid residues in oligosaccharides, glycoproteins, glycolipids, colominic acid and synthetic substrates .
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- HY-142686
-
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SGK
P-glycoprotein
CDK
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Inflammation/Immunology
|
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SGK1-IN-3 (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC50 of <1 nM against hSGK1. SGK1-IN-3 blocks the activity of CDK family members. SGK1-IN-3 is a P-glycoprotein substrate. SGK1-IN-3 can be used for research on osteoarthritis .
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- HY-148596
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UDP-N-Acetyl-D-glucosamine; Uridine diphospho-N-acetylglucosamine; UDP-N-acetylglucosamine
|
Endogenous Metabolite
P2Y Receptor
Drug Intermediate
Glycosyltransferase
|
Infection
|
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UDP-GlcNAc (UDP-N-Acetyl-D-glucosamine) is an important component and precursor of bacterial peptidoglycan. UDP-GlcNAc is a nucleotide sugar used by Glycosyltransferases to synthesize glycoproteins, glycosaminoglycans, glycolipids, and glycoRNA. UDP-GlcNAc also serves as the donor substrate for forming O-GlcNAc, a dynamic intracellular protein modification involved in diverse signaling and disease processes. UDP-GlcNAc is the sugar nucleotide donor for the synthesis of O-GlcNAc modified proteins. UDP-GlcNAc also acts as a full agonist of the P2Y14 receptor and inhibits the formation of cAMP. UDP-GlcNAc can be used in studies related to bacterial infections .
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- HY-E70054
-
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Others
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Others
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beta-1,3-Galactosyltransferase (WbgO) (CgtB) acts on N-glycan substrates. beta-1,3-Galactosyltransferase (WbgO) catalyzes the formation of type 1 chains on oligosaccharide, glycopeptide, and glycoprotein substrates, including itself .
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- HY-W001601
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iGluR
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Neurological Disease
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Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease .
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- HY-17367S4
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- HY-123793
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- HY-17367S2
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-
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- HY-P10282
-
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CaMK
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Neurological Disease
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Synapsin I-(3-13), a substrate for CaMK1, is a glycoprotein. Synapsin I is a phosphoprotein that coats the cytoplasmic side of synaptic vesicles and regulates their trafficking within nerve terminals .
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- HY-107212R
-
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Reference Standards
Parasite
Chloride Channel
P-glycoprotein
Bacterial
|
Infection
|
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Selamectin (Standard) is the analytical standard of Selamectin. This product is intended for research and analytical applications. Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM .
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- HY-N3197
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(+)-Neostenine
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P-glycoprotein
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Cancer
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Neostenine is a stenine-type Stemona alkaloid, with antitussive activity. Neostenine is also a substrate of P-glycoprotein with high absorptive permeability in Caco-2 monolayer model. Neostenine also shows oral activity for intestinal application .
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- HY-A0279AR
-
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Mikamycin B (Standard); Mikamycin IA (Standard)
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Reference Standards
Bacterial
Antibiotic
|
Infection
|
|
Pristinamycin IA (Standard) is the analytical standard of Pristinamycin IA. This product is intended for research and analytical applications. Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus[1].
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- HY-108286S
-
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Isotope-Labeled Compounds
Adrenergic Receptor
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Cardiovascular Disease
|
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(Rac)-Talinolol-d5 is the racemate of Talinolol. Talinolol (Cordanum) is a long-acting, cardioselective β1-adrenergic receptor blocker. Talinolol exhibits cardioprotective and antihypertensive activities. Talinolol is also a well-known and frequently used probe substrate for P-glycoprotein (P-gp) activity .
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- HY-170569
-
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Dipeptidyl Peptidase
Cytochrome P450
P-glycoprotein
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Metabolic Disease
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Cetagliptin is an orally active inhibitor for dipeptidyl peptidase 4 (DPP-4) and CYP2D6 (IC50 of 6 µM). Cetagliptin is a substrate for P-glycoprotein. Cetagliptin reduces the GLP-1 degradation, maintains the level of postprandial blood sugar, and can be used in type 2 diabetes mellitus research .
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- HY-13646B
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HM30181 hydrochloride; HM30181A hydrochloride
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P-glycoprotein
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Others
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Encequidar hydrochloride (HM30181 hydrochloride) is an oral P-glycoprotein (P-gp) inhibitor with the activity of enhancing the oral bioavailability of P-gp substrate drugs. Encequidar shows the highest potency among various MDR1 inhibitors, with IC50=0.63nM. Encequidar effectively blocks the transepithelial transport of paclitaxel in MDCK monolayer cells, with IC50=35.4nM .
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- HY-W001601A
-
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iGluR
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Neurological Disease
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Budipine hydrochloride is an anti-parkinson agent. Budipine hydrochloride also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine hydrochloride also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine hydrochloride can be used for the research of CNS disorders include Parkinson disease .
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-
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- HY-B0777R
-
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CL301423 (Standard)
|
Antibiotic
BCRP
P-glycoprotein
Parasite
Reference Standards
|
Infection
|
|
Moxidectin (Standard) is the analytical standard of Moxidectin. This product is intended for research and analytical applications. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
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-
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- HY-123934
-
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P-glycoprotein
|
Neurological Disease
|
|
VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .
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- HY-17367S3
-
-
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- HY-W001601R
-
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Reference Standards
iGluR
|
Neurological Disease
|
|
Budipine (Standard) is the analytical standard of Budipine. This product is intended for research and analytical applications. Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease .
|
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- HY-17367AR
-
|
BMS-232632 sulfate (Standard)
|
Reference Standards
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
Endogenous Metabolite
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Infection
Cancer
|
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Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of
3.49 μM .
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-
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- HY-G0017A
-
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Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate; CGP 74588 mesylate
|
Drug Metabolite
P-glycoprotein
Apoptosis
|
Neurological Disease
Cancer
|
|
N-Desmethyl imatinib mesylate (Norimatinib mesylate) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib mesylate binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib mesylate induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib mesylate exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib mesylate can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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- HY-N2453R
-
|
|
Reference Standards
PPAR
NF-κB
P-glycoprotein
|
Inflammation/Immunology
Cancer
|
|
Convallatoxin (Standard) is the analytical standard of Convallatoxin. This product is intended for research and analytical applications. Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .
|
-
-
- HY-17367R
-
|
BMS-232632 (Standard)
|
Reference Standards
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
Endogenous Metabolite
|
Infection
Cancer
|
|
Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .
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- HY-17367S5
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-
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- HY-G0017S1
-
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Norimatinib-d4; Imatinib metabolite N-Desmethyl imatinib-d4; CGP 74588-d4
|
Isotope-Labeled Compounds
Drug Metabolite
P-glycoprotein
Apoptosis
|
Neurological Disease
Cancer
|
|
N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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- HY-10289
-
|
RO-4876904
|
Dipeptidyl Peptidase
GLP Receptor
P-glycoprotein
|
Metabolic Disease
|
|
Carmegliptin (RO-4876904) is an orally active and potent DPP IV inhibitor with a human DPP IV IC50 of 6.8 nM. Carmegliptin binds to the S1 pocket of DPP IV, blocks the degradation of GLP 1, potentiates endogenous GLP 1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin acts as a substrate for human P glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin can be used for the research of type 2 diabetes, non insulin dependent diabetes mellitus .
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- HY-E70568
-
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Ser/Thr Protease
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Others
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Protease (O-glycan Cleaving) is recombinantly expressed from E.coli and contains a His tag. Protease (O-glycan Cleaving) is an O-glycan-dependent protease that digests proteins carrying mucin-type O-glycans, including sialylated substrates, glycosylated Ser and Thr residues at the N terminus. Protease (O-glycan Cleaving) digests a variety of O-glycan structures, including sialylated glycosylated core 1 and core 2 structures and Tn antigen. Protease (O-glycan Cleaving) does not digest terminally modified serine or threonine residues, nor does it digest N-glycosylation sites on glycoproteins.
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-
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- HY-G0017R
-
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Norimatinib (Standard); Imatinib metabolite N-Desmethyl imatinib (Standard); CGP 74588 (Standard)
|
Reference Standards
Drug Metabolite
P-glycoprotein
Apoptosis
|
Others
|
|
N‑Desmethyl imatinib (Standard) is the analytical standard of N‑Desmethyl imatinib (Norimatinib) (HY-G0017R). This product is intended for research and analytical applications. N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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-
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- HY-138074
-
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5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
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Parasite
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Infection
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Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
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- HY-129046J
-
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Endonuclease
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Metabolic Disease
|
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RNase B Glycoprotein Standard is a substrate containing PNGase F and can be used to determine PNGase F activity. RNase B Glycoprotein Standard can be used as a glycoprotein standard.
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-
- HY-181804
-
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BCRP
P-glycoprotein
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Cancer
|
|
MRS8288 is a ABCG2 and P-glycoprotein inhibitor, with an IC50 of 0.96 μM against ABCG2 and an IC50 of 1.39 μM against P-glycoprotein. MRS8288 inhibits the ATPase activity of ABCG2 and P-glycoprotein, and suppresses ABCG2-mediated substrate transport. MRS8288 is applicable for cancer research .
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-
- HY-180935
-
|
|
Drug Derivative
P-glycoprotein
|
Cancer
|
|
Doxorubamine is a Doxorubicin (HY-15142A) derivative. Doxorubamine is a poor substrate of P-glycoprotein. Doxorubamine efficiently kills agent-sensitive ovarian cancer .
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-
- HY-P2869J
-
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|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
β-Galactosidase, Kluyveromyces lactis is a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. SubstRates of different β-galactosidases include ganglioside GM1, lactosylceramides, lactose, and various glycoproteins.
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-
- HY-E70890
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|
|
Glycosidase
|
Metabolic Disease
|
|
β-Galactosidase Mutein, E. coli is a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. Substrates of different β-galactosidases include ganglioside GM1, lactosylceramides, lactose, and various glycoproteins.
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- HY-E71027
-
|
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Biochemical Assay Reagents
|
Metabolic Disease
|
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β-Galactosidase-biotin labeled, Escherichia coli is a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. SubstRates of different β-galactosidases include ganglioside GM1, lactosylceramides, lactose, and various glycoproteins.
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- HY-E71299
-
|
|
Glycosidase
|
Others
|
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β-Galactosidase 42A, Bifidobacterium longum (EC 3.2.1.23) is a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. Substrates of different β-galactosidases include ganglioside GM1, lactosylceramides, lactose, and various glycoproteins.
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- HY-E71299B
-
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Glycosidase
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Others
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β-Galactosidase 42A, Thermotoga maritima (EC 3.2.1.23) is a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. Substrates of different β-galactosidases include ganglioside GM1, lactosylceramides, lactose, and various glycoproteins.
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- HY-E71297
-
|
|
Glycosidase
|
Others
|
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β-Galactosidase 2A, Bacteroides thetaiotaomicron (EC 3.2.1.23) is a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. Substrates of different β-galactosidases include ganglioside GM1, lactosylceramides, lactose, and various glycoproteins.
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- HY-E71296
-
|
|
Glycosidase
|
Others
|
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β-Galactosidase 1A, Sulfolobus solfataricus (EC 3.2.1.23) is a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. Substrates of different β-galactosidases include ganglioside GM1, lactosylceramides, lactose, and various glycoproteins.
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- HY-E71299A
-
|
|
Glycosidase
|
Others
|
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β-Galactosidase 42A, Caldicellulosiruptor saccharolyticus (EC 3.2.1.23) is a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. Substrates of different β-galactosidases include ganglioside GM1, lactosylceramides, lactose, and various glycoproteins.
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-
- HY-E71298
-
|
|
Glycosidase
|
Others
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β-Galactosidase 2B, Bacteroides thetaiotaomicron (EC 3.2.1.23) is a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. Substrates of different β-galactosidases include ganglioside GM1, lactosylceramides, lactose, and various glycoproteins.
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- HY-E71025
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|
Biochemical Assay Reagents
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Metabolic Disease
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β 1-4,6-Galactosidase, Jack bean (EC 3.2.1.23) is a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. Substrates of different β-galactosidases include ganglioside GM1, lactosylceramides, lactose, and various glycoproteins.
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- HY-174454
-
|
|
P-glycoprotein
|
Infection
|
|
Antitrypanosomal agent 24 is a benzothiazole amidoxime with strong and selective antitrypanosomal activity (IC50 = 0.92 μM). Antitrypanosomal agent 24 is a substrate of the P-glycoprotein efflux pump. Antitrypanosomal agent 24 has high membrane permeability and good metabolic stability. Antitrypanosomal agent 24 binds to DNA/RNA by intercalation .
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- HY-108286R
-
|
Cordanum (Standard)
|
Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Talinolol (Standard) is the analytical standard of Talinolol (HY-108286). This product is intended for research and analytical applications. Talinolol (Cordanum) is a long-acting, cardioselective β1-adrenergic receptor blocker. Talinolol exhibits cardioprotective and antihypertensive activities. Talinolol is also a well-known and frequently used probe substrate for P-glycoprotein (P-gp) activity .
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-
- HY-182440
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AZD3783 is an orally active, blood-brain barrier-penetrant 5-HT1B receptor antagonist. AZD3783 reverses agonist-induced hypothermia, inhibits separation-induced vocalizations in guinea pig pups, and acts as a moderately permeable glycoprotein substrate with moderate clearance. AZD3783 inhibits hERG channel activity. AZD3783 is applicable for research on depression, anxiety disorders, and other psychiatric diseases associated with serotonergic neurotransmission .
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-
- HY-165444
-
|
NGD-913
|
GABA Receptor
|
Neurological Disease
|
|
CP-615003 is a potent and subtype-selective partial agonist of GABAA receptor (GABAA receptor) (Ki = 1.1 μM). CP-615003 is mainly converted into the active metabolite CP-900725 through oxidative deamination in monkeys and humans, and the latter also has GABAA receptor affinity. CP-615003 is a substrate of P-glycoprotein (P-gp/MDR1), resulting in severe limitation of its penetration into the central nervous system (CNS). CP-615003 can be used for the study of CNS-related indications .
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-
- HY-10289A
-
|
RO-4876904 hydrochloride
|
Dipeptidyl Peptidase
GLP Receptor
P-glycoprotein
|
Metabolic Disease
|
|
Carmegliptin hydrochloride (RO-4876904 hydrochloride) is an orally active and potent DPP‑IV inhibitor with a human DPP‑IV IC50 of 6.8 nM. Carmegliptin hydrochloride binds to the S1 pocket of DPP‑IV, blocks the degradation of GLP‑1, potentiates endogenous GLP‑1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin hydrochloride acts as a substrate for human P‑glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin hydrochloride can be used for the research of type 2 diabetes, non‑insulin‑dependent diabetes mellitus .
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-
- HY-N17304
-
|
|
Drug Derivative
P-glycoprotein
|
Cancer
|
|
10S,13aR-Antofine N-oxide is a phenanthroindolizidine N-oxide alkaloid and cytotoxic agent found in Cynanchum vincetoxicum. 10S,13aR-Antofine N-oxide exerts cytotoxic effects in drug-sensitive (KB-3-1, IC50 = 0.11 μM) and multi-drug-resistant (KB-V1, IC50 = 0.16 μM) carcinoma cells. 10S, 13aR-Antofine N-oxide acts as a poor substrate for the P-glycoprotein (P-170) efflux pump. 10S,13aR-Antofine N-oxide can be used for the research of cancers .
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-
- HY-182383
-
|
|
CDK
Apoptosis
|
Cancer
|
|
VMY-1-101 is a fluorescent cyclin-dependent kinase (CDK) inhibitor, with an excitation of 410 nm and emission of 512 nm. VMY-1-101 competitively inhibits ATP binding to CDKs. VMY-1-101 induces G2/M cell cycle arrest in human breast cancer cells. VMY-1-101 induces modest apoptosis in human breast cancer cells. VMY-1-101 blocks proliferation of human breast cancer cells, including multidrug resistance-positive cells, and is not a substrate for p-glycoprotein. VMY-1-101 localizes to the cytoplasm of human breast cancer cells. VMY-1-101 shows increased binding to human breast cancer tissue compared to fluorophore alone. VMY-1-101 can be used for the research of breast cancer .
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-
- HY-120247
-
|
|
Vasopressin Receptor
P-glycoprotein
|
Others
|
|
TASP0434299 (Compound 10) is a radiolabeled ligand for the vasopressin V1b receptor. TASP0434299 exhibits high binding affinity for human and murine V1B receptors, with IC50 values of 0.526 nM and 0.641 nM, respectively, and shows potent antagonistic activity against the human V1B receptor with an IC50 of 0.639 nM. TASP0434299 is a substrate for human and rhesus monkey P-glycoprotein, resulting in low brain uptake in rhesus monkeys. TASP0434299 binds to V1B receptors in rat and monkey pituitary tissues in a saturable and specific manner both in vitro and in vivo. When radiolabeled with tritium or 11C, TASP0434299 serves as a prototype V1B receptor radiotracer to visualize V1B receptor in the pituitary gland of anesthetized monkeys via positron emission tomography .
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-
| Cat. No. |
Product Name |
Type |
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- HY-107903
-
|
Thyroglobulin from bovine
|
Biochemical Assay Reagents
|
|
Thyroglobulin is a 660 kDa, dimeric glycoprotein produced by the follicular cells of the thyroid and used entirely within the thyroid gland. Thyroglobulin acts as a substrate for the synthesis of the thyroid hormones thyroxine (T4) and triiodothyronine (T3), as well as the storage of the inactive forms of thyroid hormone and iodine within the follicular lumen of a thyroid follicle. Thyroglobulin activates Akt kinase activity in FRTL-5 thyroid cell .
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-
- HY-P3008
-
|
|
Biochemical Assay Reagents
|
|
Submandibular mucin is a high molecular weight glycoprotein that is used as a substrate for the viral enzyme neuraminidase .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P3008
-
-
- HY-P10282
-
|
|
CaMK
|
Neurological Disease
|
|
Synapsin I-(3-13), a substrate for CaMK1, is a glycoprotein. Synapsin I is a phosphoprotein that coats the cytoplasmic side of synaptic vesicles and regulates their trafficking within nerve terminals .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N11287A
-
|
|
Natural Products
Classification of Application Fields
Other Diseases
Endogenous metabolite
Disease Research Fields
Source Classification
|
Endogenous Metabolite
|
|
UDP-xylose disodium is an endogenous sugar nucleotide and a catalytic substrate of UDP-xylose disodium synthase (UXS). UDP-xylose disodium is a sugar donor for the synthesis of glycoproteins, polysaccharides, various metabolites and oligosaccharides in plants, vertebrates and fungi, and participates in the synthesis of proteoglycans as a glycosyl donor. UDP-xylose disodium participates in the regulation of the synthesis of extracellular matrix components and can be used to study the mechanism of proteoglycan biosynthesis in glycobiology and related diseases (such as connective tissue diseases)[1][2].
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-
-
- HY-17367
-
-
-
- HY-N2453
-
-
-
- HY-17367A
-
-
-
- HY-A0279A
-
-
-
- HY-N11287
-
|
|
Alkaloids
Microorganisms
Other Alkaloids
Source Classification
|
Endogenous Metabolite
|
|
UDP-xylose is an endogenous sugar nucleotide and a catalytic substrate of UDP-xylose synthase (UXS). UDP-xylose is a sugar donor for the synthesis of glycoproteins, polysaccharides, various metabolites and oligosaccharides in plants, vertebrates and fungi, and participates in the synthesis of proteoglycans as a glycosyl donor. UDP-xylose participates in the regulation of the synthesis of extracellular matrix components and can be used to study the mechanism of proteoglycan biosynthesis in glycobiology and related diseases (such as connective tissue diseases)[1][2].
|
-
-
- HY-148596
-
|
UDP-N-Acetyl-D-glucosamine; Uridine diphospho-N-acetylglucosamine; UDP-N-acetylglucosamine
|
Human Gut Microbiota Metabolites
Microorganisms
Endogenous metabolite
Source Classification
|
Endogenous Metabolite
P2Y Receptor
Drug Intermediate
Glycosyltransferase
|
|
UDP-GlcNAc (UDP-N-Acetyl-D-glucosamine) is an important component and precursor of bacterial peptidoglycan. UDP-GlcNAc is a nucleotide sugar used by Glycosyltransferases to synthesize glycoproteins, glycosaminoglycans, glycolipids, and glycoRNA. UDP-GlcNAc also serves as the donor substrate for forming O-GlcNAc, a dynamic intracellular protein modification involved in diverse signaling and disease processes. UDP-GlcNAc is the sugar nucleotide donor for the synthesis of O-GlcNAc modified proteins. UDP-GlcNAc also acts as a full agonist of the P2Y14 receptor and inhibits the formation of cAMP. UDP-GlcNAc can be used in studies related to bacterial infections .
|
-
-
- HY-N3197
-
-
-
- HY-A0279AR
-
-
-
- HY-17367AR
-
-
-
- HY-N2453R
-
|
|
Structural Classification
Ranunculaceae
Adonis amurensis Regel et Radde
Plants
Steroids
|
Reference Standards
PPAR
NF-κB
P-glycoprotein
|
|
Convallatoxin (Standard) is the analytical standard of Convallatoxin. This product is intended for research and analytical applications. Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .
|
-
-
- HY-17367R
-
-
-
- HY-N17304
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0777S
-
|
|
|
Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
-
- HY-G0017S
-
|
|
|
N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
|
-
-
- HY-17367S4
-
|
|
|
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
|
-
-
- HY-17367S2
-
|
|
|
Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
|
-
-
- HY-108286S
-
|
|
|
(Rac)-Talinolol-d5 is the racemate of Talinolol. Talinolol (Cordanum) is a long-acting, cardioselective β1-adrenergic receptor blocker. Talinolol exhibits cardioprotective and antihypertensive activities. Talinolol is also a well-known and frequently used probe substrate for P-glycoprotein (P-gp) activity .
|
-
-
- HY-17367S3
-
|
|
|
Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
|
-
-
- HY-17367S5
-
|
|
|
Atazanavir-d24 (BMS-232632-d24) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .
|
-
-
- HY-G0017S1
-
|
|
|
N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
|
-
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