Search Result
Results for "
flux
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
7
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-136068
-
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Antibiotic
Bacterial
Autophagy
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Infection
Cancer
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DCAP is a broad-spectrum antibiotic targeting the membranes of both Gram-positive and Gram-negative bacteria. DCAP blocks autophagy at the late stages by preventing autophagolysosome maturation and interrupting the autophagic flux .
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- HY-120620
-
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Others
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Others
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BMS-195270 is a small molecule that inhibits Carbachol (HY-B1208)-evoked tonicity of isolated rat bladder strips. BMS-195270 inhibits calcium flux .
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-
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- HY-17508
-
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Bacterial
Cytochrome P450
Autophagy
Antibiotic
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Infection
Cancer
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Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
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- HY-114865
-
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RGS Protein
Calcium Channel
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Neurological Disease
|
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BMS-192364 is targeting the Gα-RGS interaction to produce an inactive Gα-RGS complex. BMS-192364 reduces urinary bladder contraction and exert RGS-agonist properties by increasing the action of GAPs on Gq proteins. BMS-192364 inhibits calcium flux .
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-
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- HY-115570
-
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GW108X
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Kinesin
ULK
Autophagy
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Cancer
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GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK .
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-
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- HY-W111589F
-
-
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- HY-121366
-
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RU-15525
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Calcium Channel
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Others
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Kadethrin is a synthetic pyrethroid that acts as an insecticide. Kadethrin can affect the binding of [3H] full-histamine toxin ([3H]H12-HTX) to the nicotinic acetylcholine (Ach) receptor/channel binding sites, and it inhibits the Ca 2+ flux through the receptor ion channels .
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-
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- HY-111274
-
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Indometacin farnesil
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COX
Autophagy
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Inflammation/Immunology
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Indomethacin farnesil is an orally active proagent of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes .
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- HY-E70008
-
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Sirtuin
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Inflammation/Immunology
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Lumbokinase attenuates myocardial ischemia-reperfusion (I-R) injury through the activation of Sirt1 signaling, and thus enhances autophagic flux and reduces I-R-induced oxidative damage, inflammation and apoptosis .
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- HY-118758
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γ-Kainic acid-glutamic acid
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Sodium Channel
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Neurological Disease
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γ-Kainylglutamic acid (γ-Kainic acid-glutamic acid), a dipeptide derived from kainic and L-Glutamic acids, is a selective antagonist of amino acid induced neuroexcitation with anticonvulsant properties. γ-Kainylglutamic acid inhibits the stimulation of Na + fluxes induced in brain slices by the neuroexcitant N-methyl-D-aspartic acid. γ-Kainylglutamic acid is also effective in protecting mice from picrotoxin-induced convulsions with an EC50 value of 0.17 μmol .
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- HY-14397S
-
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Indometacin-d4
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Isotope-Labeled Compounds
COX
Autophagy
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Inflammation/Immunology
Cancer
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Indomethacin-d4 is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
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- HY-112683
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ASCT
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Cancer
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V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells .
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- HY-112683A
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ASCT
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Cancer
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V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells .
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- HY-110282
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Oxidative Phosphorylation
Mitochondrial Metabolism
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Metabolic Disease
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S3QEL-2, a suppressor of superoxide production from mitochondrial complex III, potently and selectively suppresses site IIIQo superoxide production (IC50=1.7 μM). S3QEL-2 does not affect oxidative phosphorylation, and normal electron flux. S3QEL-2 inhibits HIF-1α accumulation .
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- HY-146401
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CXCR
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Cancer
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CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice .
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- HY-148129
-
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TRP Channel
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Cardiovascular Disease
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TRPC6-IN-3 (compound 17) is a potent, orally active transient receptor potential C6 ion channel (TRPC6) inhibitor. TRPC6-IN-3 modulates not only intracellular calcium concentration, but also membrane potential by modulating the flux of cations including calcium and sodium ions. TRPC6-IN-3 can be used in research of respiratory system .
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- HY-P99190
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BMS-936557; MDX-1100
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CXCR
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Inflammation/Immunology
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Eldelumab (BMS-936557) is a human anti-CXCL10 (IP-10) monoclonal antibody (IgG1 type). Eldelumab selectively binds to CXCL10 and blocks CXCL10-induced calcium flux and cell migration. Eldelumab can be used in studies of autoimmune and auto-inflammatory diseases such as rheumatoid arthritis, ulcerative colitis and crohn's disease .
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- HY-124582
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NEO214
1 Publications Verification
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Autophagy
mTOR
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Cancer
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NEO214 is an autophagy inhibitor and a covalent conjugate of the PDE4 inhibitor Rolipram (HY-16900) and perillyl alcohol (HY-N7000). It has anti-cancer activity and blood-brain barrier (BBB) permeability. Over sex. NEO214 prevents autophagy-lysosome fusion, thereby blocking autophagic flux and triggering glioma cell death. The process involves mTOR activation, andTFEB(Transcription Factor EB) aggregation. NEO214 inhibitionMacroautophagy/autophagy in glioblastoma cells has the potential to overcome chemotherapy resistance in glioblastoma .
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- HY-15568
-
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P2X Receptor
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Neurological Disease
Inflammation/Immunology
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A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux .
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- HY-15568A
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P2X Receptor
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Neurological Disease
Inflammation/Immunology
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A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux .
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- HY-15297
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OPC-8212
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Phosphodiesterase (PDE)
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Infection
Cardiovascular Disease
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Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research .
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- HY-125836
-
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CCR
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Endocrinology
Cancer
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CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.
CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively .
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- HY-B1243
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Sodium Channel
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Neurological Disease
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Propoxycaine hydrochloride inhibits voltage-gated sodium channels, and thereby inhibits the ionic flux required for the initiation and conduction of impulses. Propoxycaine hydrochloride application can lead to a loss of sensation.
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- HY-100582
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Ribitol
1 Publications Verification
Adonitol; Adonite
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Endogenous Metabolite
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Others
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Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol.
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- HY-124759
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CCR
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Inflammation/Immunology
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CCR1 antagonist 9 is a potent and selective CCR1 antagonist with an IC50 of 6.8 nM in calcium flux assay .
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- HY-120588
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- HY-112818
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-
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- HY-161743
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AUTOTACs
Autophagy
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Cancer
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PBA-1105 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 increases the autophagic flux of Ub-conjugated aggregates .
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- HY-161744
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AUTOTACs
Autophagy
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Cancer
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PBA-1106 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1106 increases the autophagic flux of Ub-conjugated aggregates .
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- HY-116082
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Dopamine Receptor
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Neurological Disease
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CP 226269 is a potent dopamine D4 receptor agonist that induces calcium flux with EC50 of 32.0 nM. CP 226269 can be used in the research of schizophrenia and other related diseases .
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- HY-129111
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EACC
3 Publications Verification
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Autophagy
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Infection
Neurological Disease
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EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion .
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- HY-150757
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Autophagy
Apoptosis
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Cancer
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Autophagy-IN-2 (Compound 7h) is an autophagic flux inhibitor. Autophagy-IN-2 induces cancer cell apoptosis and can be used for triple-negative breast cancer research .
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- HY-110200
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m-Phenylenediacrylic acid; m-Benzenediacrylic acid
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Aquaporin
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Metabolic Disease
Cancer
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TC AQP1 1 (m-Phenylenediacrylic acid) is a potent AQP1 inhibitor. TC AQP1 1 inhibits AQP1-mediated water flux in oocytes, with an IC50 of 8 μM .
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- HY-125746
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Fluorescent Dye
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Others
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BODIPY-cholesterol is an intrinsically lipophilic, and cell-permeable analog of cholesterol with a fluorescent BODIPY group. BODIPY-cholesterol can be used to monitor sterol uptake and inter-organelle sterol flux in cells. (Excitation/Emission: 505/515 nm) .
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- HY-100582S1
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Adonitol-2-13C; Adonite-2-13C
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Isotope-Labeled Compounds
Endogenous Metabolite
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Others
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Ribitol-2- 13C is the 13C labeled Ribitol. Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol
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- HY-100582S2
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Adonitol-3-13C; Adonite-3-13C
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Isotope-Labeled Compounds
Endogenous Metabolite
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Others
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Ribitol-3- 13C is the 13C labeled Ribitol. Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol
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- HY-100582S3
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Adonitol-5-13C; Adonite-5-13C
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Isotope-Labeled Compounds
Endogenous Metabolite
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Others
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Ribitol-5- 13C is the 13C labeled Ribitol. Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol
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- HY-135891
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CCR
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Neurological Disease
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AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
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- HY-100582S
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Adonitol-1-13C; Adonite-1-13C
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Isotope-Labeled Compounds
Endogenous Metabolite
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Others
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Ribitol-1- 13C is the 13C labeled Ribitol. Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol .
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- HY-19548
-
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Arginase
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Endocrinology
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BEC, an arginine analogue, is a slow-binding competitive inhibitor of the binuclear manganese metalloenzyme arginase. BEC enhances substrate flux to NO synthase, thereby enhancing NO-dependent smooth muscle relaxation in the corpus cavernosum, and enhances penile erection .
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- HY-16039
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LPL Receptor
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Inflammation/Immunology
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AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
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- HY-N5123
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Others
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Others
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α-L-Rhamnose is a terminal residue of steviol glycosides Dulcoside A and Dulcoside B. α-L-Rhamnose recognizing lectin site of human dermal fibroblasts functions as a signal transducer: modulation of Ca 2+ fluxes and gene expression .
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- HY-115493
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CXCR
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Others
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TIQ-15 is a potent CXCR4 antagonist with an IC50 value of 6 nM for CXCR4 Ca 2+ flux. TIQ-15 inhibits CYP450 2D6 with an IC50 value of 0.32 μM .
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- HY-W083373A
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Bacterial
Autophagy
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Cancer
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3,4-Dimethoxychalcone is a Caloric restriction mimetics (CRMs). 3,4-Dimethoxychalcone induces the deacetylation of cytoplasmic proteins and stimulates autophagy flux. 3,4-Dimethoxychalcone can be used for cardiac and cancer diseases research .
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- HY-15991
-
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AZD1722; RDX5791
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Na+/H+ Exchanger (NHE)
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Metabolic Disease
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Tenapanor (AZD1722) is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor has the potential for the research of hyperphosphatemia .
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- HY-15991A
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AZD1722 hydrochloride; RDX5791 hydrochloride
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Na+/H+ Exchanger (NHE)
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Metabolic Disease
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Tenapanor (AZD1722) hydrochloride is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor hydrochloride reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor hydrochloride has the potential for the research of hyperphosphatemia .
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- HY-103706
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ROC-325
1 Publications Verification
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Autophagy
Apoptosis
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Cancer
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ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis .
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- HY-161619
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-
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- HY-P3041
-
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Calcium Channel
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Endocrinology
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Chromostatin bovine is a chromogranin A (CGA) derivative peptide, which inhibits postassium or carbamoylcholine induced catecholamine release with an ID50 of 5 nM. Chromostatin bovine reduces calcium flux, enhances the desensitization process of the cholinergic-evoked secretory response and modulates the endocrine response associated with catecholamine .
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- HY-112711
-
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Atg4
Autophagy
Cathepsin
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Cancer
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LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 µM and a Kd of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo .
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- HY-15084B
-
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MK-801
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iGluR
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Neurological Disease
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Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
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- HY-101908
-
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CCR
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Inflammation/Immunology
Endocrinology
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BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM) .
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- HY-115570A
-
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(Z/E)-GW108X
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Kinesin
ULK
Autophagy
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Cancer
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(Z/E)-GW406108X is a mixture of different configurations of GW406108X (HY-115570). GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM .
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- HY-15415
-
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Na+/Ca2+ Exchanger
Autophagy
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Cancer
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KB-R7943 mesylate is a widely used inhibitor of the reverse Na +/Ca 2+ exchanger (NCXrev) with IC50 of 5.7±2.1 μM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.
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- HY-D0713
-
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Monocarboxylate Transporter
Mitochondrial Metabolism
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Cancer
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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 .
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- HY-131349
-
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CCR
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Cancer
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CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity .
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- HY-131349A
-
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CCR
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Metabolic Disease
Cancer
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CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity .
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- HY-50694
-
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ICA-17043
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Potassium Channel
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Others
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Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca 2+-activated K + channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca 2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM .
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- HY-161745
-
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AUTOTACs
p62
Autophagy
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Cancer
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PBA-1105b is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105b increases the autophagic flux of Ub-conjugated aggregates. PBA-1105b is a drastically longer PEG-based linker than PBA-1105 .
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- HY-143312D
-
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GLP Receptor
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Metabolic Disease
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(R)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R .
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- HY-161740
-
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AUTOTACs
Estrogen Receptor/ERR
Autophagy
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Cancer
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PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC) that induces p62 self-oligomerization and degradation of estrogen receptor ERβ (DC50:~2 nM, HEK293T). PHTPP-1304 also induces the formation of p62 +ERβ + puncta that are affected by autophagic flux in a dose-dependent manner .
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- HY-14397S1
-
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COX
Autophagy
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Inflammation/Immunology
Cancer
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Indomethacin-d4 Methyl Ester is the deuterium labeled Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
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- HY-129555
-
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Bacterial
HSV
Antibiotic
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Infection
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Surfactin is a potent cyclic lipopeptide biosurfactants consists of four isomers (Surfactin A, B, C and D), which mediates flux of mono-and divalent cations, such as calcium, across lipid bilayer membranes. Surfactin can act as an antimicrobial adjuvant with anti-bacterial, anti-fungal, antimycoplasma and hemolytic effects . Surfactin also has antiviral activity against a variety of enveloped viruses .
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- HY-143312B
-
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GLP Receptor
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Metabolic Disease
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(R)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R .
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- HY-134964
-
-
- HY-P3710
-
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Calcium Channel
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Others
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Ser-Ala-alloresact is a sperm activating peptide (SAP). The peptides released from eggs of marine invertebrates play a central role in fertilization .
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- HY-W031727
-
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Parasite
Toll-like Receptor (TLR)
SARS-CoV
Autophagy
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Infection
Cancer
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Hydroxychloroquine (HCQ) is a synthetic oral antimalarial drug that can be used in the study of malaria and autoimmune diseases such as systemic lupus erythematosus and rheumatoid arthritis. Hydroxychloroquine is a potent autophagic flux inhibitor with antiviral activity (such as SARS-CoV-2 virus) that inhibits Toll-like receptor 7/9 (TLR7/9) signaling .
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- HY-P10408
-
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EGFR
MMP
Calcium Channel
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Infection
Inflammation/Immunology
|
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Candidalysin is a cytolytic peptide toxin, which is initially isolated from Candida albicans and exhibits virulent and avirulent characters. Candidalysin activates epithelial cell signaling pathways by interacting with the epithelial growth factor receptor (EGFR) of host cells, activates matrix metalloproteinase (MMP) and calcium flux, resulting in inflammatory responses and recruitment of immune cells. Candidalysin exhibits cytotoxicity by dealing membran damage to host cells .
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- HY-150636
-
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Autophagy
Apoptosis
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Cancer
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Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
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- HY-118233
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M 17055
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Chloride Channel
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Neurological Disease
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Alilusem potassium is a diuretic. In anesthetized dogs undergoing water diuresis, Alilusem potassium effectively decreased free water clearance and increased Na+ and Cl- levels in excreted urine. When combined with Furosemide (HY-B0135) or Hydrochlorothiazid, Alilusem potassium further inhibited free water clearance. Alilusem potassium inhibited the lumen-positive transepithelial voltage and lumen-to-cistern Cl- flux in isolated rabbit cortical thick ascending limbs of Henle .
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- HY-155994
-
|
|
PIKfyve
Autophagy
PROTACs
|
Cancer
|
|
PIK5-12d is a PROTAC PIKfyve degrader (DC50: 1.48 nM). PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagic flux in multiple prostate cancer cells. PIK5-12d inhibits prostate cancer cell proliferation. PIK5-12d has anti-tumor activity .
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-
- HY-P1682
-
|
POL6326
|
CXCR
Arrestin
|
Cancer
|
|
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
-
- HY-107678
-
|
WAY-317538
|
nAChR
|
Neurological Disease
|
|
SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca 2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research .
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-
- HY-117982
-
|
|
GnRH Receptor
ERK
|
Endocrinology
|
|
SKI2496 is an orally active GnRH receptor antagonist (IC50: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca 2+ flux with an IC50 value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC50 value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders .
|
-
- HY-13699
-
|
|
GnRH Receptor
PERK
|
Others
|
|
NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca 2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases .
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-
- HY-17508S1
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Clarithromycin-d3is the deuterium labeledClarithromycin(HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
|
-
- HY-162147
-
|
|
mTOR
Autophagy
|
Inflammation/Immunology
|
|
Nur77 modulator 3 (9e) can bind to Nur77 and inhibit TGF-β1-induced α-SMA and COLA1 expression in a Nur77-dependent manner. Nur77 modulator 3 induces Nur77 expression and enhances autophagic flux by inhibiting the mTORC1 signaling pathway in vitro and in vivo. Nur77 modulator 3 blocks the progression of hepatic fibrosis .
|
-
- HY-P1682A
-
|
POL6326 TFA
|
CXCR
Arrestin
|
Cancer
|
|
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
-
- HY-143312C
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
(S)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
|
-
- HY-143312E
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
(S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 hydrochloride is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
|
-
- HY-118830
-
|
DK-PGD2; 15-Oxo-13,14-dihydro-PGD2; 13,14-Dihydro-15-keto-PGD2
|
Prostaglandin Receptor
|
Endocrinology
|
|
13, 14-Dihydro-15-keto prostaglandin D2 (DK-PGD2) is a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway. 13, 14-Dihydro-15-keto prostaglandin D2 is a selective agonist for the DP2 receptor. 13, 14-Dihydro-15-keto prostaglandin D2 can inhibit ion flux in canine colonic mucosa preparation .
|
-
- HY-100991
-
|
ZK 39106; LSU-65
|
GABA Receptor
|
Neurological Disease
|
|
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex .
|
-
- HY-12927
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
|
-
- HY-W011209
-
|
Riboprine
|
Autophagy
Endogenous Metabolite
|
Cancer
|
|
N6-Isopentenyladenosine (Riboprine), an RNA modification found in cytokinins, which regulate plant growth/differentiation, and a subset of tRNAs, where it improves the efficiency and accuracy of translation. N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with an interesting anti-melanoma activity .
|
-
- HY-W753806
-
|
UK 33274 hydrochloride
|
Others
|
Cardiovascular Disease
|
|
Doxazosin hydrochloride (UK 33274 hydrochloride) is a compound used to inhibit hypertension and prostate hyperplasia, with activity that inhibits postsynaptic α1-adrenoceptors on vascular smooth muscle. Doxazosin hydrochloride can cause vasodilation, thereby reducing peripheral vascular resistance. Doxazosin hydrochloride was found to inhibit the proliferation and migration of hepatic stellate cells in a mouse liver fibrosis model. Doxazosin hydrochloride regulates fibrosis, autophagy, and apoptosis of hepatic stellate cells by activating the PI3K/Akt/mTOR signaling pathway. Doxazosin hydrochloride also blocks autophagic flux and induces apoptosis of hepatic stellate cells .
|
-
- HY-164682
-
|
|
Others
|
Infection
|
|
AMD 3329 octahydrobromide is a potent and selective anti-HIV-1 and HIV-2 compound with activity to inhibit viral replication. AMD 3329 blocks viral invasion by binding to the chemokine receptor CXCR4. AMD 3329 exhibits EC50 values as low as 0.8 and 1.6 nM when inhibiting HIV-1 and HIV-2 replication, showing better antiviral efficacy than AMD3100. AMD 3329 significantly inhibits the binding of specific CXCR4 monoclonal antibodies and the Ca(2+) flux induced by SDF-1alpha. AMD 3329 is also able to effectively interfere with virus-induced syncytium formation, with an EC50 value of 12 nM .
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-
- HY-W748509
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrial membrane depolarization .
|
-
- HY-117219
-
|
|
Others
|
Metabolic Disease
|
|
SKF 104976 is a 3,2-carboxylic acid derivative with potent 14-alpha-demethylase (14 alpha DM) inhibitory activity. SKF 104976 inhibited 14 alpha DM activity by 50% at 2 nM in Hep G2 cell extracts. SKF 104976 inhibited the incorporation of [14C]acetate into cholesterol in intact cells at similar concentrations, accompanied by accumulation of lanosterol, and resulted in a 40-70% decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity. SKF 104976 did not affect the uptake and degradation of low-density lipoprotein in Hep G2 cells, indicating that HMGR and low-density lipoprotein receptor activities are not coordinately regulated under these conditions. The inhibitory effect of SKF 104976 on HMGR activity remained unchanged even when the flux of carbon units in the sterol synthesis pathway was reduced by 80%. SKF 104976 did not inhibit HMGR activity under conditions where sterol synthesis was almost completely blocked by lovastatin .
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| Cat. No. |
Product Name |
Type |
-
- HY-125746
-
|
|
Fluorescent Dyes/Probes
|
|
BODIPY-cholesterol is an intrinsically lipophilic, and cell-permeable analog of cholesterol with a fluorescent BODIPY group. BODIPY-cholesterol can be used to monitor sterol uptake and inter-organelle sterol flux in cells. (Excitation/Emission: 505/515 nm) .
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| Cat. No. |
Product Name |
Type |
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10408
-
|
|
EGFR
MMP
Calcium Channel
|
Infection
Inflammation/Immunology
|
|
Candidalysin is a cytolytic peptide toxin, which is initially isolated from Candida albicans and exhibits virulent and avirulent characters. Candidalysin activates epithelial cell signaling pathways by interacting with the epithelial growth factor receptor (EGFR) of host cells, activates matrix metalloproteinase (MMP) and calcium flux, resulting in inflammatory responses and recruitment of immune cells. Candidalysin exhibits cytotoxicity by dealing membran damage to host cells .
|
-
- HY-P1682A
-
|
POL6326 TFA
|
CXCR
Arrestin
|
Cancer
|
|
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
-
- HY-P3041
-
|
|
Calcium Channel
|
Endocrinology
|
|
Chromostatin bovine is a chromogranin A (CGA) derivative peptide, which inhibits postassium or carbamoylcholine induced catecholamine release with an ID50 of 5 nM. Chromostatin bovine reduces calcium flux, enhances the desensitization process of the cholinergic-evoked secretory response and modulates the endocrine response associated with catecholamine .
|
-
- HY-P3710
-
|
|
Calcium Channel
|
Others
|
|
Ser-Ala-alloresact is a sperm activating peptide (SAP). The peptides released from eggs of marine invertebrates play a central role in fertilization .
|
-
- HY-P1682
-
|
POL6326
|
CXCR
Arrestin
|
Cancer
|
|
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99190
-
|
BMS-936557; MDX-1100
|
CXCR
|
Inflammation/Immunology
|
|
Eldelumab (BMS-936557) is a human anti-CXCL10 (IP-10) monoclonal antibody (IgG1 type). Eldelumab selectively binds to CXCL10 and blocks CXCL10-induced calcium flux and cell migration. Eldelumab can be used in studies of autoimmune and auto-inflammatory diseases such as rheumatoid arthritis, ulcerative colitis and crohn's disease .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-100582S
-
|
|
|
Ribitol-1- 13C is the 13C labeled Ribitol. Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol .
|
-
-
- HY-14397S1
-
|
|
|
Indomethacin-d4 Methyl Ester is the deuterium labeled Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
|
-
-
- HY-14397S
-
|
|
|
Indomethacin-d4 is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
|
-
-
- HY-100582S1
-
|
|
Ribitol-2- 13C is the 13C labeled Ribitol. Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol
|
-
-
- HY-100582S2
-
|
|
Ribitol-3- 13C is the 13C labeled Ribitol. Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol
|
-
-
- HY-100582S3
-
|
|
Ribitol-5- 13C is the 13C labeled Ribitol. Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol
|
-
-
- HY-17508S1
-
|
|
|
Clarithromycin-d3is the deuterium labeledClarithromycin(HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
|
-
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