Search Result
Results for "
transport inhibitor
" in MedChemExpress (MCE) Product Catalog:
10
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-110101
-
-
-
- HY-108322
-
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Others
|
Cardiovascular Disease
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NBTGR (p-Nitrobenzylthioguanosine) is a potent inhibitor of nucleoside transport; inhibits adenosine uptake with a Ki of 70 nM.
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-
-
- HY-101091
-
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Apoptosis
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Cancer
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Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
|
-
-
- HY-132182
-
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Others
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Cancer
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HPA-12 is an intracellular ceramide transport protein inhibitor .
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-
-
- HY-122473
-
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SGLT
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Metabolic Disease
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fluoro-Dapagliflozin, a structural analog of Dapagliflozin, is a selective SGLT2 inhibitor with Ki values of 5.3 nM and 330 nM for SGLT2 and SGLT1, respectively. fluoro-Dapagliflozin blocks glucose transport and glucose-coupled currents .
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-
-
- HY-138142
-
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Others
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Metabolic Disease
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Euphol acetate is a triterpene that can be isolated from Euphorbia broteri. Euphol acetate is an inhibitor of hepatic transport proteins organic anion-transporting polypeptide 1/3 (OATP1B1/3) .
|
-
-
- HY-N0832
-
-
-
- HY-B2119
-
Tauroglycocholic acid sodium salt
|
Biochemical Assay Reagents
|
Endocrinology
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Sodium tauroglycocholate is an inhibitor of the biliary acid transporting system of the hepatocyte and also a surfactant used as a chemical permeation enhancer.
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-
-
- HY-115366
-
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Others
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Neurological Disease
|
Soluflazine is a nucleoside transport inhibitor with anticonvulsant action. Soluflazine can be used as an antiepileptic agent .
|
-
-
- HY-20558
-
-
-
- HY-157536
-
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Bacterial
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Infection
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SMT-738 is a small-molecule inhibitor of bacterial lipoprotein transport targeting Enterobacteriaceae .
|
-
-
- HY-N2522
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Gummiferin dipotassium
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Others
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Others
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Carboxyatractyloside dipotassium is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport .
|
-
-
- HY-B0590B
-
(+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine
|
Monoamine Transporter
|
Cancer
|
(+)-Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.
|
-
-
- HY-B0937
-
|
Parasite
|
Infection
|
Amprolium, an anticoccidial drug used in poultry, is a thiamine-like agent that inhibits thiamine transport in coccidia by inhibiting thiamine absorption and carbohydrate synthesis.
|
-
-
- HY-U00049
-
-
-
- HY-113329
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Taurocyamine
|
Endogenous Metabolite
|
Metabolic Disease
|
Guanidinoethyl sulfonate (Taurocyamine), a transport antagonist of taurine, induces much urinary taurine excretion with a resulting decrease in the tissue taurine content and readily produces taurine-deficient fetal rats in pregnant rats . Guanidinoethyl sulfonate, a structural analogue of taurine, acts as a competitive inhibitor of taurine transport .
|
-
-
- HY-107433
-
-
-
- HY-147429A
-
Abx MCP TFA; RG6006 TFA
|
Antibiotic
Bacterial
|
Infection
|
Zosurabalpin TFA is a tethered macrocyclic peptide antibiotic, acting specifically on A. baumannii. Zosurabalpin TFA inhibits lipopolysaccharide-transport .
|
-
-
- HY-W337358
-
|
Others
|
Neurological Disease
|
N-(3-Hydroxyphenyl)-arachidonoyl amide (Compound 23) is an anandamide transport inhibitor with an IC50 of 21.3 μM .
|
-
-
- HY-N6701
-
|
Arp2/3 Complex
|
Cancer
|
Dihydrocytochalasin B (H2CB) is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport . Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis . Dihydrocytochalasin B (H2CB) inhibits active calcium transport and causes a Ca 2+increase in the mucosal scrapings .
|
-
-
- HY-B1756
-
-
-
- HY-120338
-
-
-
- HY-N11913
-
|
Biochemical Assay Reagents
|
Others
|
Siderin is a Photosystem II inhibitor that effectively inhibits ATP synthesis and chloroplast electron transport during photosynthesis in isolated spinach. Siderin can be used in the study of plant photosynthesis .
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-
-
- HY-19062
-
-
-
- HY-130055
-
HQNO
1 Publications Verification
|
Mitochondrial Metabolism
|
Infection
|
HQNO, secreted by P. aeruginosa, is a potent electron transport chain inhibitor with a Kd of 64 nM for complex III . HQNO is a potent inhibitor of mitochondrial NDH-2 in many species .
|
-
-
- HY-116788
-
|
Bacterial
|
Infection
|
Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata, an analog of spiro-indoline-thadiazole, shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM .
|
-
-
- HY-114197
-
-
-
- HY-W142117
-
|
Fluorescent Dye
|
Others
|
H-Asp(AMC)-OH, a amino acid derivative, is a fluorescent dye. H-Asp(AMC)-OH dose not inhibit glycine transport at a concentration of 0.25 mM .
|
-
-
- HY-121214
-
|
Mitochondrial Metabolism
|
Infection
|
Amisulbrom is a sulfonamide fungicide used to control oomycete diseases. Amisulbrom biochemically inhibits the cytochrome-bc1 complex of the mitochondrial electron transport system .
|
-
-
- HY-113995
-
AH5183
|
mAChR
|
Neurological Disease
|
(-)-Vesamicol (AH5183) is an inhibitor of acetylcholine transport into synaptic vesicles, with the IC50 of 75 nM . (-)-Vesamicol can be used for release and recycling of synaptic vesicles study .
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-
-
- HY-W012572
-
|
Mitochondrial Metabolism
|
Metabolic Disease
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D-Histidine is an enantiomer of L-histidine (HY-N0832). L-Histidine is an essential amino acid for infants. L-Histidine is an inhibitor of mitochondrial glutamine transport .
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-
-
- HY-B1848
-
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Others
|
Others
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Hexazinone is a nonselective herbicide from the triazine family. Hexazinone binds to the D-1 quinone protein of the electron transport chain in photosystem II to inhibit the photosynthesis .
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-
-
- HY-B1849
-
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Others
|
Infection
|
Hexazinone is a nonselective herbicide from the triazine family. Hexazinone binds to the D-1 quinone protein of the electron transport chain in photosystem II to inhibit the photosynthesis .
|
-
-
- HY-124617
-
|
Others
|
Inflammation/Immunology
Cancer
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AMXT1501 is a novel inhibitor of the polyamine transport system. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells .
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-
-
- HY-N10094
-
|
Others
|
Others
|
Maculosidine is a furoquinoline alkaloid that can be isolated from Balfourodendron riedelianum. Maculosidine inhibits ATP synthesis, basal, phosphorylating and uncoupled electron transport in plants. Maculosidine inhibits Hill reaction on spinach chloroplasts .
|
-
-
- HY-W179181
-
|
GLUT
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Metabolic Disease
|
MSNBA is a specific inhibitor of GLUT5 fructose transport in proteoliposomes. MSNBA competitively inhibits GLUT5 fructose uptake with a KI of 3.2±0.4?μM in MCF7 cells .
|
-
-
- HY-N0832S
-
-
-
- HY-W754708
-
|
LXR
Na+/K+ ATPase
|
Cardiovascular Disease
|
Ouabagenin is a naturally occurring LXR ligand with LXR selective agonist activity. Ouabagenin acts as an EC 3.6.3.9 (Na(+)/K(+)- transport ATPase) inhibitor .
|
-
-
- HY-100957
-
|
|
|
Dilazep dihydrochloride is an inhibitor of adenosine uptake. Dilazep dihydrochloride has cerebral and coronary vasodilating action through enhancement of effect of adenosine. Dilazep dihydrochloride also inhibits the ischemic damage, platelet aggregation, and membrane transport of nucleosides .
|
-
-
- HY-111321
-
-
-
- HY-100322
-
|
Chloride Channel
|
Cardiovascular Disease
|
H100 is a Cl - transport inhibitor, with partial effects against both the NaK2Cl cotransporter and the Band 3 anion exchanger, but no effect against KCl cotransporter, in human erythrocytes.
|
-
-
- HY-111548
-
|
Others
|
Others
|
Spastazoline is a selective spastin (a microtubule-severing AAA protein) inhibitor, with an IC50 of 99 nM for Human spastin. Spastazoline can be used for cell division- and intracellular vesicle transport-related research .
|
-
-
- HY-112177
-
|
Fungal
Mitochondrial Metabolism
Antibiotic
|
Infection
|
Myxothiazol, an antifungal antibiotic, is a mitochondrial electron transport chain complex III (bc1 complex) inhibitor. Myxothiazol inhibits the growth of many yeasts and fungi at concentrations between 0.01 and 3 μg/ml .
|
-
-
- HY-130004
-
|
Antibiotic
Bacterial
|
Infection
|
MsbA-IN-6 is a potent inhibitor of MsbA. MsbA-IN-6 is an antibiotic. Gram-negative ATP-binding cassette (ABC) transporter MsbA, an essential inner membrane protein, transports lipopolysaccharide from the inner leaflet to the periplasmic face of the inner membrane. MsbA-IN-6 kills Escherichia coli through inhibition of its ATPase and transport activity, with no loss of activity against clinical multidrug-resistant strains .
|
-
-
- HY-W008566
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Norharman; β-Carboline
|
Monoamine Oxidase
Endogenous Metabolite
|
Infection
Neurological Disease
Cancer
|
Norharmane (Norharman), a β-carboline alkaloid, is a potent and reversible monoamine oxidase inhibitor, with IC50 values of 6.5 and 4.7 μM for MAO-A and MAO-B, respectively. Norharmane causes antidepressant responses. Norharmane is also a prospective anti-cancer photosensitizer. Norharmane alters polar auxin transport (PAT) by inhibiting PIN2, PIN3 and PIN7 transport proteins, thus causing a significant inhibitory effect on the growth of Arabidopsis thaliana seedlings .
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-
-
- HY-124789
-
|
Bacterial
Antibiotic
|
Infection
|
TBT1 is a first-generation inhibitor of the MsbA transporter. TBT1 is an LPS transport inhibitor and MsbA ATPase stimulator in strains from the Acinetobacter genus. TBT1 stimulated ATPase activity with an EC50 of 13 µM .
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-
-
- HY-121088
-
|
Others
|
Cardiovascular Disease
Others
|
Ceefourin 2 is a potent and highly selective inhibitor of MRP4. Ceefourin 2 inhibits the transport of MRP4 substrates but is not selective for other ABC transporters. Ceefourin 2 shows lower cytotoxicity and higher microsomal and acid stability .
|
-
-
- HY-162396
-
|
P-glycoprotein
|
Cancer
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P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .
|
-
-
- HY-17513
-
BAY314666; BAY-MKH 3586
|
Others
|
Others
|
Amicarbazone(BAY-MKH3586; BAY314666) is a potent inhibitor of photosynthetic electron transport via binding to the Qb domain of photosystem II (PSII); herbicide with a broad spectrum of weed control.
|
-
-
- HY-135336A
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(S)-(-)-Verapamil hydrochloride
|
Leukotriene Receptor
Calcium Channel
Apoptosis
|
Cancer
|
(S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells .
|
-
- HY-N9362
-
|
Antibiotic
|
Infection
|
Emodinanthrone, an anthraquinone, is a sprecursor of Emodin (HY-14393) with antibiotic activity. Emodinanthrone inhibits respiration-driven solute transport at micromolar concentrations in membrane vesicles of Escherichia coli .
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- HY-N1462
-
|
|
|
Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart .
|
-
- HY-N6782
-
-
- 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-10822
-
BGC 945; ONX-0801
|
Thymidylate Synthase
|
Others
|
Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L .
|
-
- HY-128424
-
|
Others
|
Metabolic Disease
|
4'-Deoxyphlorizin is an inhibitor of the glucose transport system. 4'-Deoxyphlorizi has good phlorizin hydrolase inhibitory activity with the Km value of 0.59 nM and the Ki value of 0.33 nM, respectively .
|
-
- HY-N9429
-
|
Others
|
Metabolic Disease
|
6-Deoxy-D-glucose is an inhibitor of glucose oxidation. 6-Deoxy-D-glucose is a structural homomorph of D-glucose, and can be used for study of D-glucose transport .
|
-
- HY-135336
-
(R)-(+)-Verapamil hydrochloride
|
P-glycoprotein
Apoptosis
|
Cancer
|
(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents .
|
-
- HY-10824
-
PT523
|
Antifolate
Dihydrofolate reductase (DHFR)
|
Cancer
|
Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth .
|
-
- HY-P3711
-
|
Na+/K+ ATPase
|
Others
|
SPAI-1 is a specific inhibitor for monovalent cation transporting ATPases. SPAI-1 is a peptide isolated from porcine duodenum, inhibits Na +, K +-ATPase and H +, K +-ATPase in vitro, stimulates Mg 2+-ATPase .
|
-
- HY-N6684
-
Vomitoxin
|
Others
|
Metabolic Disease
|
Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .
|
-
- HY-B1813A
-
(±)-AH5183 hydrochloride
|
Sigma Receptor
|
Neurological Disease
|
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively .
|
-
- HY-W009823
-
|
Chloride Channel
|
Others
|
Phenyl benzoate is a benzoate ester obtained by the formal condensation of phenol with benzoic acid. Phenyl benzoate is a chloride transport blocker, inhibits Cl --dependent Glu accumulation into vesicles. Phenyl benzoate can be used as preservative in cosmetic products .
|
-
- HY-N1502
-
Gummiferin tripotassium
|
|
|
Carboxyatractyloside (Gummiferin) tripotassium is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport from the inner mitochondria to the inner mitochondria. Carboxyatractyloside tripotassium can be used for the study of cellular energy metabolism and mitochondrial biology .
|
-
- HY-146391
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases agent transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells .
|
-
- HY-D0843S
-
NEM-d5
|
Cathepsin
Deubiquitinase
|
Others
|
N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2]. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor[3].
|
-
- HY-119984
-
|
Others
|
Others
|
DNP-INT is a potent photosynthetic electron transport chain (PETC) inhibitor. DNP-INT competently inhibits the oxidation of plastid quinoline by binding to the Q0 site of Cyt-b6f (Kd=1.4 nM), thereby inhibiting electron transfer in plants .
|
-
- HY-142444
-
|
AP-1
|
Metabolic Disease
|
SSAO/VAP-1 inhibitor 1 is a potent inhibitor of SSAO/VAP-1. SSAO/VAP-1 promotes the transfer of Glucose transport 4 (GLUT 4) from adipocytes to the cell membrane, thereby regulating glucose transport. In endothelial cells, SSAO/VAP-1 can mediate the adhesion and exudation of leukocytes and endothelial cells, and participate in inflammatory responses. SSAO/VAP-1 inhibitor 1 has the potential for the research of inflammation and/or inflammation-related disease or diabetes and/or diabetes-related disease (extracted from patent WO2021102774A1, compound E3) .
|
-
- HY-101867
-
AU1235
2 Publications Verification
|
Bacterial
|
Infection
Cancer
|
AU1235, an adamantyl urea, is a potent MmpL3 inhibitor. The Mycobacterium tuberculosis protein MmpL3 performs an essential role in cell wall synthesis, since it effects the transport of trehalose monomycolates across the inner membrane .
|
-
- HY-112730
-
PEO-IAA
5 Publications Verification
2-(1H-Indol-3-yl)-4-oxo-4-phenyl-butyric acid
|
Others
|
Others
|
PEO-IAA is an indole-3-acetic acid (IAA) antagonist. PEO-IAA is an auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs).
|
-
- HY-103504
-
|
GABA Receptor
|
Neurological Disease
|
(S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant agent .
|
-
- HY-112847
-
Sulfo-N-succinimidyl oleate
|
Mitophagy
|
Inflammation/Immunology
|
Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate binds the CD36 receptor on the surface of microglia. Anti-inflammatory effect .
|
-
- HY-112847A
-
Sulfo-N-succinimidyl oleate sodium
|
Mitophagy
|
Inflammation/Immunology
|
Sulfosuccinimidyl oleate sodium (Sulfo-N-succinimidyl oleate sodium) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate sodium is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate sodium binds the CD36 receptor on the surface of microglia. Anti-inflammatory effect .
|
-
- HY-N0832S1A
-
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
L-Histidine- 13C6, 15N3 hydrochloride is the 13C and 15N labled L-Histidine (HY-N0832). L-Histidine is an essential amino acid for infants. L-Histidine is an inhibitor of mitochondrial glutamine transport.
|
-
- HY-156408
-
|
LPL Receptor
|
Inflammation/Immunology
|
Spns2-IN-1 is a potent inhibitor of Spns2-dependent S1P transport (Spns2), with IC50 of 1.4±0.3 μM that plays an important role in immune response .
|
-
- HY-162369
-
|
P-glycoprotein
|
Cancer
|
PID-9 is a P-glycoprotein inhibitor. PID-9 has multidrug resistance (MDR) reversal activity (IC50 = 0.1338 μM) and low toxicity. PID-9 inhibits the transport function of P-gp without downregulating P-gp expression .
|
-
- HY-D0713
-
7ACC2
5 Publications Verification
|
Monocarboxylate Transporter
Mitochondrial Metabolism
|
Cancer
|
7ACC2 is a potent monocarboxylate transporter (MCT) inhibitor with an IC50 of 11 nM for inhibition of [ 14C]-lactate influx. 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport. 7ACC2 is an anticancer agent through inhibition of lactate flux .
|
-
- HY-N10272
-
|
Fungal
Bacterial
|
Infection
|
Avenaciolide is an antifungal bis-γ-lactone found in Aspergillus avenaceus. Avenaciolide has also antibacterial action. Avenaciolide is a specific inhibitor of glutamate transport in rat liver mitochondria. Avenaciolide interferes with the ability of ADP to stimulate the rate of glutamate oxidation .
|
-
- HY-B1849S
-
|
Isotope-Labeled Compounds
|
Infection
|
Hexazinone-d6 is the deuterium labeled Hexazinone[1]. Hexazinone is a nonselective herbicide from the triazine family. Hexazinone binds to the D-1 quinone protein of the electron transport chain in photosystem II to inhibit the photosynthesis[2].
|
-
- HY-N0832S1
-
-
- HY-B0817
-
|
|
|
Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: rat liver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function .
|
-
- HY-121123
-
2-Aminoadamantane-2-carboxylic acid
|
Aminopeptidase
|
Cancer
|
Adamantanine (2-Aminoadamantane-2-carboxylic acid) inhibits the transport of methionine (Ki is 0.76 mM) and leucine into Ehrlich ascites carcinoma cells. Adamantanine inhibits proliferation of P388 lymphocytic leukemia cells with an IC50 of >1 mM. Adamantanine inhibits the leucine aminopeptidase with an I/S0.5 of 10.5 .
|
-
- HY-100928
-
|
|
|
YS 035 hydrochloride is a Ca 2+ antagonist on cellular uptake and mitochondrial efflux of calcium ions. YS 035 hydrochloride inhibits Ca 2+ uptake by muscle cells and inhibits Na +/Ca 2+ exchange (Ki=28 µM). YS 035 hydrochloride is a useful tool for research on the mitochondrial Ca 2+ transport .
|
-
- HY-141700
-
|
FATP
|
Metabolic Disease
|
FATP1-IN-2 (compound 12a), an arylpiperazine derivative, is an orally active fatty acid transport protein 1 (FATP1) inhibitor (human IC50=0.43 μM, mouse IC50=0.39 μM) .
|
-
- HY-123158
-
SAN 835H
|
Others
|
Others
|
Diflufenzopyr (SAN 835H) is an auxin transport inhibitor. Diflufenzopyr can enhance the activity of auxin herbicides, such as quinclorac (HY-B0871) and picloram (HY-B2034), and of the synthetic auxin, 1-naphthaleneacetic acid (HY-18570) .
|
-
- HY-W854295
-
PtdIns-(1,2-dioctanoyl) (sodium)
|
P-glycoprotein
|
Cancer
|
Phosphatidylinositol-1,2-dioctanoyl sodium significantly inhibits transmembrane P-gp transport in a reproducible, cell line-independent, and substrate-independent manner. Phosphatidylinositol-1,2-dioctanoyl sodium plays an important role in signal transduction and cell movement .
|
-
- HY-155863
-
|
Others
|
Inflammation/Immunology
|
AJ2-71 is a SLCl5A4 inhibitor. AJ2-71 inhibits IFN-α production. AJ2-71 blocks SLC15A4-mediated MDP transport. AJ2-71 can be used for research of inflammation .
|
-
- HY-B0133
-
Pimaricin
|
Fungal
Endogenous Metabolite
Antibiotic
Bacterial
|
Infection
|
Natamycin (Pimaricin) is a macrolide antibiotic agent produced by several Streptomyces strains. Natamycin inhibits the growth of fungi via inhibition of amino acid and glucose transport across the plasma membrane. Natamycin is a food preservative, an antifungal agent in agriculture, and is widely used for fungal keratitis research .
|
-
- HY-N7433
-
Ethylidene-glucose
|
GLUT
Endogenous Metabolite
|
Metabolic Disease
|
4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport .
|
-
- HY-135336AS
-
(S)-(-)-Verapamil-d7 hydrochloride
|
Isotope-Labeled Compounds
Leukotriene Receptor
Calcium Channel
Apoptosis
|
Cancer
|
(S)-Verapamil-d7 (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1][2].
|
-
- HY-155849
-
|
Pyruvate Kinase
|
Cancer
|
Pkm2-in-4 (compound 5C) is a selective inhibitor of PKM2 (IC50=0.35 μM), which regulates pyruvate-dependent respiration and induces mitochondrial H202 production rate and electron transport system coupling .
|
-
- HY-123742
-
|
Others
|
Metabolic Disease
|
Estradiol 3-sulfate 17-glucuronide potassium is metabolite of estradiol. Estradiol 3-sulfate 17-glucuronide potassium inhibits multidrug resistance protein (MRP) mediated 17β -Estradiol 17-(β -D-Glucuronide) transport with a Ki of 22 μM .
|
-
- HY-101453
-
|
|
|
Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma .
|
-
- HY-120103
-
|
Sodium Channel
|
Metabolic Disease
|
PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used for the research of regulating glucose metabolism and lipid metabolism .
|
-
- HY-119770
-
SDZ-HDL 376
|
Others
|
Cardiovascular Disease
|
HDL376 is a scavenger receptor class B type I (SR-BI) inhibitor. HDL376 directly inhibits SR-BI-mediated lipid transport in cells and in liposomes reconstituted with purified SR-BI (IC50 = 0.22 μM). HDL376 can be used for the research of atherosclerotic coronary artery disease .
|
-
- HY-W077242
-
|
DNA/RNA Synthesis
|
Cancer
|
1,4-Anthraquinone is a potent anticancer agent. 1,4-Anthraquinone blocks nucleoside transport, inhibits macromolecule synthesis, induces DNA fragmentation, and decreases the growth and viability of cancer cells. 1,4-Anthraquinone can be used to research anti-leukemia .
|
-
- HY-16592
-
Brefeldin A
Maximum Cited Publications
62 Publications Verification
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
Bacterial
|
Infection
Cancer
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus . Brefeldin A is also an autophagy and mitophagy inhibitor . Brefeldin A is a CRISPR/Cas9 activator . Brefeldin A inhibits HSV-1 and has anti-cancer activity .
|
-
- HY-D0843
-
NEM
|
|
|
N-Ethylmaleimide (NEM) derives from maleic acid, it can alkylates free sulfhydryl. N-Ethylmaleimide is an irreversible cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide inhibits prolyl endopeptidase with an IC50 value of 6.3 μM. N-Ethylmaleimide can be used to modify cysteine residues in proteins and peptides .
|
-
- HY-N3513
-
Kuwanon C
|
Others
|
Cardiovascular Disease
|
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
|
-
- HY-B1837A
-
beta-Cyfluthrin
|
Calcium Channel
|
Neurological Disease
|
β-Cyfluthrin (beta-Cyfluthrin) is a type II synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibiting Ca 2+ ATPase involved in calcium transport .
|
-
- HY-135336S
-
(R)-(+)-Verapamil-d7 hydrochloride
|
Isotope-Labeled Compounds
P-glycoprotein
Apoptosis
|
Cancer
|
(R)-Verapamil-d7 (hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents[1][2].
|
-
- HY-116042
-
|
Adenosine Receptor
|
Cardiovascular Disease
|
FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium .
|
-
- HY-N7119
-
|
Others
|
Inflammation/Immunology
|
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity . Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function .
|
-
- HY-101388
-
|
|
|
AM404, an inhibitor of endocannabinoid reuptake, blocks anandamide transport with IC50 values in the low micromolar range . AM404 is able to relax rat isolated hepatic arteries contracted with Phenylephrine, with a pEC50 value of 7.4 (corresponding to an EC50 of 0.04 µM). Neuroprotective Effect .
|
-
- HY-126362
-
|
Glucosidase
|
Others
|
ML266 is glucocerebrosidase (GCase) molecule chaperone with IC50 of 2.5 µM. ML266 binds to GCase and transports of the mutant protein to the lysosome, and resume the activity of GCase. ML266 dose not inhibit the GCase enzyme’s action. ML266 has the potential for the research of gaucher disease .
|
-
- HY-124617A
-
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells . Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines .
|
-
- HY-N6715
-
|
Influenza Virus
Bacterial
|
Infection
|
Tenuazonic acid, belonging to tetramic acids that are the largest family of natural products, is a putative nonhost-selective mycotoxin isolated from Alternaria alternate . Tenuazonic acid blocks electron transport beyond primary quinone acceptor (QA) by interacting with D1 protein and it is a broad-spectrum and effective photosystem II (PSII) inhibitor .
|
-
- HY-W019868
-
|
Others
|
Others
|
1-O-Hexadecyl-2-O-acetyl-sn-glycerol is an alkyl acylglycerol that may activate the amino acid transport activity of the A-system and stimulate the absorption of methylaminoisobutyric acid (MeAIB). MeAIB inhibits mTOR phosphorylation, which may affect intestinal amino acid absorption and signal transduction .
|
-
- HY-N11854
-
|
Others
|
Others
|
Brassicanate A sulfoxide has herbicidal activity. Brassicanate A sulfoxide inhibits the biosynthesis of essential amino acids in plants. Brassicanate A sulfoxide binds to dihydroxyacid dehydratase (DHAD), hydroxymethylpyruvate dioxygenase (HPPD), acetolactate synthase (ALS), PYL family proteins and transport inhibitor response 1 (TIR1), and reduces their activity. Brassicanate A sulfoxide can be isolated from Brassica oleracea .
|
-
- HY-138559
-
|
Mitochondrial Metabolism
|
Neurological Disease
|
GW604714X is a potent inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X is a highly specific mitochondrial pyruvate carrier (MPC) inhibitor with a Ki <0.1 nM. GW604714X also inhibits L-lactate transport by the plasma membrane monocarboxylate transporter (MCT1), but at concentrations more than 4 orders of magnitude greater than the MPC .
|
-
- HY-118207
-
|
GABA Receptor
|
Cancer
|
LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively .
|
-
- HY-B0853
-
|
|
|
Paclobutrazol is a triazole-containing plant growth retardant that is known to inhibit the biosynthesis of gibberellins. Paclobutrazol also has antifungal activities. Paclobutrazol, transported acropetally in plants, can also suppress the synthesis of abscisic acid and induce chilling tolerance in plants. Paclobutrazol is typically used to support research on the role of gibberellins in plant biology .
|
-
- HY-116425
-
Alanap 1
|
Others
|
Others
|
N-1-Naphthylphthalamic acid (Alanap 1) is a modulator of polar auxin transport that competes with auxin (indole-3-acetic acid, IAA) for membrane binding sites. N-1-Naphthylphthalamic acid also disrupts maize leaf initiation, KNOX protein regulation, and leaf margin formation .
|
-
- HY-W003836
-
7-Methoxy-NAA
|
Others
|
Others
|
7-Methyl-1-naphthyl acetic acid is a potent
inhibitor of auxin action in plants. 7-Methyl-1-naphthyl acetic acid inhibits
AUX1, PIN, and ABCB protein-mediated auxin transport expressed in yeast.
7-Methyl-1-naphthyl acetic acid can be used in auxin dependent development
.
|
-
- HY-141699
-
|
Others
|
Metabolic Disease
|
FATP1-IN-1 (compound 5k) is a fatty acid transport protein 1 (FATP1) inhibitor. FATP1-IN-1 is an inhibition of recombinant human or mouse acyl-CoA synthetase activity of FATP1, with the IC50 values of 0.046 μM or 0.60 μM, respectively .
|
-
- HY-145894
-
|
Others
|
Others
|
NaPi2b-IN-2 (compound 5) is a potent inhibitor of sodium-dependent transport protein 2b (SLC34A2, NaPi2b), with an IC50 of 38 nM for human NaPi2b. NaPi2b-IN-2 can be used for the research of hyperphosphatemia .
|
-
- HY-156242
-
|
Apoptosis
|
Cancer
|
BQZ-485 is a a potent GDI2 inhibitor through the interaction with Tyr245. BQZ-485 disrupts the intrinsic GDI2-Rab1A interaction, thereby abolishing vesicular transport from the endoplasmic reticulum (ER) to the Golgi apparatus and initiating subsequent paraptosis events .
|
-
- HY-B0817S
-
|
Parasite
|
Infection
|
Pyridaben-d13 is the deuterium labeled Pyridaben[1]. Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: rat liver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function[2][3].
|
-
- HY-B1246
-
|
Bacterial
Proton Pump
|
Infection
|
Thonzonium bromide is an antibacterial agent that is structurally similar to Farnesol (HY-Y0248A). Thonzonium bromide is also a monocationic surface-active agent, which inhibits RANKL-induced osteoclast formation and bone resorption in vitro and prevents LPS-induced bone loss in vivo. Thonzonium bromide inhibits proton transport in a dose-dependent manner (EC50=69 μM) .
|
-
- HY-114936
-
AR-054
|
Bacterial
ADC Cytotoxin
Antibiotic
Mitochondrial Metabolism
|
Infection
Neurological Disease
Cancer
|
Piericidin A (AR-054) is a natural mitochondrial NADH-ubiquinone oxidoreductase (complex I) inhibitor. Piericidin A is a potent neurotoxin and inhibits mitochondrial respiration by disrupting the electron transport system through its action on NADH-ubiquinone reductase. Piericidin A is also a potential quorum-sensing inhibitor that suppresses the expression of the virulence genes of Erwinia carotovora subsp. atroseptica (Eca). Piericidin A is an ADC cytotoxin and has anti-bacterial, anticancer, insecticidal activity .
|
-
- HY-145597
-
|
GLUT
|
Metabolic Disease
Cancer
|
KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death .
|
-
- HY-126222
-
|
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
MitoTam bromide, hydrobromide, a Tamoxifen derivative , is an electron transport chain (ETC) inhibitor. MitoTam bromide, hydrobromide reduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology . MitoTam bromide, hydrobromide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells .
|
-
- HY-125283
-
|
Mitochondrial Metabolism
|
Metabolic Disease
|
IM176OUT05 is a high solubility biguanide. IM176OUT05 activates stem cell metabolism, promotes hair regrowth and increases stemness induction and maintenance during the pluripotent stem cell generation process. IM176OUT0 inhibits mitochondrial electron transport chain (ETC) activity with an IC50 of 3.2 μM .
|
-
- HY-10465
-
BMS-790052 dihydrochloride; EBP 883 dihydrochloride
|
HCV
|
Infection
|
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
|
-
- HY-10466
-
BMS-790052; EBP 883
|
HCV
|
Infection
|
Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
|
-
- HY-142957
-
|
Others
|
Others
|
NaPi2b-IN-1 is a potent and orally active inhibitor of sodium-dependent phosphate transport protein 2b (NaPi2b) with an IC50 of 64 nM. NaPi2b is primarily expressed in the small intestine, lungs, and testes and plays an important role in phosphate homeostasis. NaPi2b-IN-1 has the potential for the research of hyperphosphatemia .
|
-
- HY-N1839
-
|
Apoptosis
Glucosidase
|
Cancer
|
3-Hydroxybakuchiol can be isolated from Otholobium mexicanum J. W. Grimes. 3-Hydroxybakuchiol is an electron transport chain (ETC) inhibitor. 3-Hydroxybakuchiol has antitumor activity, and induces tumor cell apoptosis. 3-Hydroxybakuchiol also has moderate inhibitory activity against α-glucosidase (IC50: 345 μM) .
|
-
- HY-126222A
-
|
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
MitoTam iodide, hydriodide is a Tamoxifen derivative , an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology .
MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells . MitoTam iodide, hydriodide causes apoptosis .
|
-
- HY-111956
-
|
Fluorescent Dye
|
Cancer
|
D-Ala-Lys-AMCA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA can be used for characterizing PEPT1-specific substrates or inhibitors .
|
-
- HY-111956B
-
|
Fluorescent Dye
|
Cancer
|
D-Ala-Lys-AMCA hydrochloride is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA hydrochloride may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA hydrochloride can be used for characterizing PEPT1-specific substrates or inhibitors .
|
-
- HY-W008344
-
|
Nucleoside Antimetabolite/Analog
|
Others
|
2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes .
|
-
- HY-146429
-
|
Others
|
Metabolic Disease
|
NaPi2b-IN-3 (compound 5) is a potent sodium-dependent transport protein 2b (SLC34A2, NaPi2b) inhibitor with IC50s of 71 nM and 28 nM for human NaPi2b and rat NaPi2b, respectively. NaPi2b-IN-3 can be used for researching hyperphosphatemia .
|
-
- HY-146241
-
|
EAAT
ASCT
|
Cancer
|
SN40 is a potent amino acid transport (AAT) inhibitor with Kis of 7.29 μM, 2.42 μM, 2.94 μM, 5.55 μM, 24.43 μM and 5.55 μM for rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN40 can be used for researching anticancer .
|
-
- HY-W037817
-
Dimethyl glutamate
|
Potassium Channel
Bacterial
|
Infection
Metabolic Disease
|
Dimethyl L-glutamate (Dimethyl glutamate), a membrane-permeable analog of Glutamate, can stimulate insulin release induced by Glucose. Dimethyl L-glutamate suppresses the KATP channel activities. Dimethyl L-glutamate inhibits E. gracilis growth and causes abnormal cell division. Dimethyl L-glutamate can be used in the research of diabetes, glucose transport, phosphorylation, and further metabolism .
|
-
- HY-146241B
-
|
Others
|
Others
|
SN40 hydrochloride is a potent amino acid transport (AAT) inhibitor with Kis of 7.29 μM, 2.42 μM, 2.94 μM, 5.55 μM, 24.43 μM and 5.55 μM for rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN40 hydrochloride can be used for researching anticancer .
|
-
- HY-111956A
-
|
Fluorescent Dye
|
Cancer
|
D-Ala-Lys-AMCA TFA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA TFA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA TFA can be used for characterizing PEPT1-specific substrates or inhibitors .
|
-
- HY-B1837AR
-
beta-Cyfluthrin (Standard)
|
Calcium Channel
|
Neurological Disease
|
β-Cyfluthrin (Standard) is the analytical standard of β-Cyfluthrin. This product is intended for research and analytical applications. β-Cyfluthrin (beta-Cyfluthrin) is a type II synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibiting Ca 2+ ATPase involved in calcium transport .
|
-
- HY-122416
-
Lonchocarpol A; Senegalensin
|
BCRP
|
Metabolic Disease
Cancer
|
6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin .
|
-
- HY-10466S
-
BMS-790052-d6; EBP 883-d6
|
Isotope-Labeled Compounds
HCV
|
Infection
|
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
|
-
- HY-10466S2
-
BMS-790052-d16; EBP 883-d16
|
Isotope-Labeled Compounds
HCV
|
Infection
|
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
|
-
- HY-125469
-
PF-04895162
|
Potassium Channel
|
Neurological Disease
|
ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects .
|
-
- HY-146242
-
|
EAAT
ASCT
|
Cancer
|
SN05 is a potent amino acid transport (AAT) inhibitor with Kis of 2.77 μM, 0.73 μM, 0.87 μM, 3.7 μM, 7.25 μM, 7.23 μM and 2.22 μM for human ASCT1, rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN05 can be used for researching anticancer .
|
-
- HY-108464A
-
|
Sodium Channel
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
|
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM . Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay . Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway . Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease .
|
-
- HY-101561
-
BLU-285
|
c-Kit
PDGFR
|
Cancer
|
Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
|
-
- HY-156237
-
|
Autophagy
|
Others
|
Beclin1-ATG14L interaction inhibitor 1 (com 19) is a selective Beclin1-ATG14L interaction inhibitor. This protein interaction mechanism specifically targets complex I of the lipid kinase VPS34 without affecting complex II. Because the integrity of VPS34 complex II depends on the Beclin 1-UVRAG interaction. Beclin1-ATG14L interaction inhibitor 1 can disrupt the formation of VPS34 complex I and inhibit autophagy, but does not affect complex II-related vesicle transport .
|
-
- HY-116716
-
|
MicroRNA
|
Cancer
|
PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development .
|
-
- HY-119101
-
|
CCR
Potassium Channel
P-glycoprotein
|
Inflammation/Immunology
|
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis .
|
-
- HY-107522
-
|
EAAT
|
Neurological Disease
|
DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively .
|
-
- HY-107522B
-
|
EAAT
|
Neurological Disease
|
DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA ammonium blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively .
|
-
- HY-19995
-
GSK 137647
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response .
|
-
- HY-N0668
-
|
GLUT
Amylases
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Rubusoside is a diterpene glycoside that is also a sweetener and solubilizer with anti-angiogenic, anti-cancer, anti-obesity, anti-allergic and anti-asthmatic effects. Rubusoside attenuates airway hyperresponsiveness and reduces inflammatory cells in bronchoalveolar lavage fluid (BALF), reducing OVA (HY-W250978)-induced airway inflammation. Rubusoside also prevents palmitic acid-induced lipotoxicity in pancreatic INS-1 cells, reduces the transport of human glucose transporters GLUT-1 and fructose GLUT-5, and inhibits NF-κB and α-amylase (α-amylase) .
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- HY-103216A
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Adrenergic Receptor
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Neurological Disease
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RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport .
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Cat. No. |
Product Name |
Type |
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- HY-W142117
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- HY-111956B
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Fluorescent Dyes/Probes
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D-Ala-Lys-AMCA hydrochloride is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA hydrochloride may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA hydrochloride can be used for characterizing PEPT1-specific substrates or inhibitors .
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- HY-111956
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Fluorescent Dyes/Probes
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D-Ala-Lys-AMCA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA can be used for characterizing PEPT1-specific substrates or inhibitors .
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- HY-111956A
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Fluorescent Dyes/Probes
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D-Ala-Lys-AMCA TFA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA TFA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA TFA can be used for characterizing PEPT1-specific substrates or inhibitors .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-W142117
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Fluorescent Dye
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Others
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H-Asp(AMC)-OH, a amino acid derivative, is a fluorescent dye. H-Asp(AMC)-OH dose not inhibit glycine transport at a concentration of 0.25 mM .
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- HY-100801A
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Peptides
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Others
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DL-threo-3-Hydroxyaspartic acid is a glutamate uptake inhibitor that can block glutamate transport in cannulated sprague dawley rat .
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- HY-162396
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P-glycoprotein
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Cancer
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P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .
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- HY-118534
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BRN-2209058
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Peptides
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Endocrinology
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Cyclobutyrol is a potent choleretic agent. Cyclobutyrol also inhibits biliary lipid secretion. Cyclobutyrol induces choleretic is unrelated to bile acids. Cyclobutyrol and bile acids do not compete for the hepatobiliar transport mechanisms[1]
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- HY-P3711
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Na+/K+ ATPase
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Others
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SPAI-1 is a specific inhibitor for monovalent cation transporting ATPases. SPAI-1 is a peptide isolated from porcine duodenum, inhibits Na +, K +-ATPase and H +, K +-ATPase in vitro, stimulates Mg 2+-ATPase .
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- HY-111956
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Fluorescent Dye
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Cancer
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D-Ala-Lys-AMCA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA can be used for characterizing PEPT1-specific substrates or inhibitors .
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-
- HY-111956B
-
|
Fluorescent Dye
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Cancer
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D-Ala-Lys-AMCA hydrochloride is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA hydrochloride may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA hydrochloride can be used for characterizing PEPT1-specific substrates or inhibitors .
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- HY-W037817
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Dimethyl glutamate
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Potassium Channel
Bacterial
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Infection
Metabolic Disease
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Dimethyl L-glutamate (Dimethyl glutamate), a membrane-permeable analog of Glutamate, can stimulate insulin release induced by Glucose. Dimethyl L-glutamate suppresses the KATP channel activities. Dimethyl L-glutamate inhibits E. gracilis growth and causes abnormal cell division. Dimethyl L-glutamate can be used in the research of diabetes, glucose transport, phosphorylation, and further metabolism .
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- HY-111956A
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Fluorescent Dye
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Cancer
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D-Ala-Lys-AMCA TFA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA TFA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA TFA can be used for characterizing PEPT1-specific substrates or inhibitors .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-D0843S
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N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2]. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor[3].
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- HY-B1849S
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Hexazinone-d6 is the deuterium labeled Hexazinone[1]. Hexazinone is a nonselective herbicide from the triazine family. Hexazinone binds to the D-1 quinone protein of the electron transport chain in photosystem II to inhibit the photosynthesis[2].
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- HY-N0832S
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L-Histidine- 15N3 is the 15N-labeled L-Histidine. L-Histidine is an essential amino acid for infants. L-Histidine is an inhibitor of mitochondrial glutamine transport.
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- HY-N0832S1A
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L-Histidine- 13C6, 15N3 hydrochloride is the 13C and 15N labled L-Histidine (HY-N0832). L-Histidine is an essential amino acid for infants. L-Histidine is an inhibitor of mitochondrial glutamine transport.
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- HY-N0832S1
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L-Histidine- 13C6, 15N3 is 13C and 15N-labeled L-Histidine (HY-N0832). L-Histidine is an essential amino acid for infants. L-Histidine is an inhibitor of mitochondrial glutamine transport.
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- HY-135336AS
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(S)-Verapamil-d7 (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1][2].
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-
- HY-135336S
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(R)-Verapamil-d7 (hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents[1][2].
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- HY-B0817S
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Pyridaben-d13 is the deuterium labeled Pyridaben[1]. Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: rat liver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function[2][3].
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-
- HY-10466S
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Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
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- HY-10466S2
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Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
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Cat. No. |
Product Name |
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Classification |
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- HY-10822
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BGC 945; ONX-0801
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Alkynes
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Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L .
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