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time-dependent

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54

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1

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1

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4

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8

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4

Isotope-Labeled Compounds

2

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-125348

    Drug Metabolite Cancer
    6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion–transporting polypeptides 1B1/SLCO1B1 (OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer .
    6α-Hydroxy paclitaxel
  • HY-P3089A

    Potassium Channel Others
    Dendrotoxin K TFA is a Kv1.1 channel blocker. Dendrotoxin K TFA determines glutamate release in CA3 neurons in a time-dependent manner through the control of the presynaptic spike waveform .
    Dendrotoxin K TFA
  • HY-16718

    PF-00251802

    Glucocorticoid Receptor Cytochrome P450 Inflammation/Immunology Endocrinology
    Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
    Dagrocorat
  • HY-P3089

    Potassium Channel Others
    Dendrotoxin K is a Kv1.1 channel blocker. Dendrotoxin K determines glutamate release in CA3 neurons in a time-dependent manner through the control of the presynaptic spike waveform .
    Dendrotoxin K
  • HY-144689

    Cholinesterase (ChE) Neurological Disease
    BChE-IN-3 (compound 45a) is a potent, selective, time-dependent and pseudoirreversible BChE inhibitor, with an IC50 of 56.9 nM. BChE-IN-3 also shows marginal and reversible (not time-dependent) inhibition of AChE .
    BChE-IN-3
  • HY-16718A

    PF-00251802 hydrochloride

    Glucocorticoid Receptor Cytochrome P450 Inflammation/Immunology Endocrinology
    Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
    Dagrocorat hydrochloride
  • HY-121144

    Refosporen

    Bacterial Antibiotic Infection
    Cefazedone (Refosporen), a first-generation cephalosporin, is a time-dependent antibiotic with activity against Gram-positive and Gram-negative bacteria .
    Cefazedone
  • HY-U00197

    JTE522; JTP19605; RWJ57504

    COX Inflammation/Immunology
    Tilmacoxib (JTE522) is a highly selective, time-dependent and irreversible human COX-2 inhibitor with an IC50 of 85 nM in an enzyme assay.
    Tilmacoxib
  • HY-106855

    H 234​/09

    Potassium Channel Cardiovascular Disease
    Almokalant is a class III antiarrhythmic agent, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K + current.
    Almokalant
  • HY-19832
    SC66
    5 Publications Verification

    Akt Apoptosis Cancer
    SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.
    SC66
  • HY-N0220
    Dauricine
    2 Publications Verification

    Oxidative Phosphorylation NF-κB Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Dauricine, a bisbenzylisoquinoline alkaloid in Menispermum dauricum, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer .
    Dauricine
  • HY-15648C
    GSK-J5
    1 Publications Verification

    Histone Demethylase Parasite Cancer
    GSK-J5 is a potent inhibitor of Schistosome and worm. GSK-J5 increases schistosomula mortality and adult worm motility and mortality, as well as egg oviposition, in a dose- and time-dependent manner .
    GSK-J5
  • HY-100686

    GABA Receptor Neurological Disease
    U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.
    U93631
  • HY-143468

    Apoptosis MEK Cancer
    MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells .
    MEK-IN-5
  • HY-D1527

    Fluorescent Dye Others
    N-(3-Fluoranthyl)maleimide is a thiol fluorescent probe with a lifetime of 20 nsec. N-(3-Fluoranthyl)maleimide has a maximum excitation wavelength of 370 nm and can be used to study the time-dependent processes of biopolymers .
    N-(3-Fluoranthenyl)maleimide
  • HY-125348S

    Isotope-Labeled Compounds Cancer
    6α-Hydroxy Paclitaxel-d5 is the deuterium labeled 6α-Hydroxy paclitaxel. 6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion–transporting polypeptides 1B1/SLCO1B1 (OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer[1].
    6α-Hydroxy Paclitaxel-d5
  • HY-134508

    Others Others
    C24-Ceramide is a sphingolipid that can be used for the lipid membranes composed. C24-Ceramide induces time-dependent changes in membrane properties. C24-Ceramide induces membrane reorganization .
    C24-Ceramide
  • HY-B0363
    Nimesulide
    5+ Cited Publications

    R805

    COX Inflammation/Immunology
    Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
    Nimesulide
  • HY-108341

    Acyltransferase Metabolic Disease
    PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
    PF-06424439
  • HY-133862

    Influenza Virus G protein-coupled Bile Acid Receptor 1 Adenosine Receptor Infection
    SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 µM .
    SCH-202676
  • HY-108341A
    PF-06424439 methanesulfonate
    5+ Cited Publications

    Acyltransferase Metabolic Disease
    PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
    PF-06424439 methanesulfonate
  • HY-149036

    Ferroptosis Endogenous Metabolite Reactive Oxygen Species Cancer
    PAA5 is a methide carbon-centered polynuclear Au(I) cluster. PAA5 can release Au(I) causing Pro-oxidant response and accelerated ferroptosis. PAA5 increases the expression of pH2AX in a time-dependent manner. PAA5 has anticancer activity .
    PAA5
  • HY-110012

    Adenosine Receptor Infection
    SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 μM .
    SCH-202676 hydrobromide
  • HY-N1214A

    (E/Z)-Super Squalene; (E/Z)-AddaVax

    Apoptosis Cancer
    (E/Z)-Squalene ((E/Z)-Super Squalene; (E/Z)-AddaVax) is a triterpenic compound. (E/Z)-Squalene accumulates and reduces liver cholesterol and triglycerides in the liver. (E/Z)-Squalen regulates the production of intracellular active oxidants (ROS) and induces apoptosis and necrosis in a concentration-and time-dependent manner .
    (E/Z)-Squalene
  • HY-12519
    Oltipraz
    Maximum Cited Publications
    13 Publications Verification

    RP 35972; NSC 347901

    HIF/HIF Prolyl-Hydroxylase HIV Keap1-Nrf2 Parasite Cancer
    Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
    Oltipraz
  • HY-N8481

    3,6-DHF

    Apoptosis Cancer
    3,6-Dihydroxyflavone is an anti-cancer agent. 3,6-Dihydroxyflavone dose- and time-dependently decreases cell viability and induces apoptosis by activating caspase cascade, cleaving poly (ADP-ribose) polymerase (PARP). 3,6-Dihydroxyflavone increases intracellular oxidative stress and lipid peroxidation .
    3,6-Dihydroxyflavone
  • HY-115750

    NO Synthase Neurological Disease
    Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O .
    Nω-allyl-L-arginine
  • HY-B0363S

    COX Inflammation/Immunology
    Nimesulide-d5 is a deuterium labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties[1][2].
    Nimesulide D5
  • HY-143883

    Akt Cancer
    MS143 is a potent AKT degrader (DC50=46 nM and GI50=0.8 µM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth .
    MS143
  • HY-N6843
    Arnicolide D
    1 Publications Verification

    Caspase PI3K Akt mTOR STAT Cancer
    Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner .
    Arnicolide D
  • HY-157788

    PROTACs Reactive Oxygen Species Ferroptosis Glutathione Peroxidase Cancer
    ZX703 (compound 5I) is a PROTAC that significantly degrades GPX4 in a dose- and time-dependent manner through the ubiquitin-proteasome and autophagy-lysosome pathways (DC50=0.315 µM). ZX703 induces ferroptosis by inducing Reactive Oxygen Species (ROS) accumulation in cells. ZX703 can be used for cancer research .
    ZX703
  • HY-108704

    Bcr-Abl Cancer
    CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities . CT-721 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CT-721
  • HY-19323A
    (S)-Ceralasertib
    1 Publications Verification

    (S)-AZD6738

    ATM/ATR Cancer
    (S)-Ceralasertib ((S)-AZD6738) is extracted from patent WO2011154737A1, Compound II, exhibits an IC50 of 2.578 nM . (S)-Ceralasertib is a potent and selective sulfoximine morpholinopyrimidine ATR inhibitor with excellent preclinical physicochemical and pharmacokinetic (PK) characteristics. (S)-Ceralasertib is developed improving aqueous solubility and eliminates CYP3A4 time-dependent inhibition .
    (S)-Ceralasertib
  • HY-135334
    ACP-5862
    1 Publications Verification

    Drug Metabolite Btk Cytochrome P450 Cancer
    ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM .
    ACP-5862
  • HY-12519S

    RP 35972-d3; NSC 347901-d3

    Isotope-Labeled Compounds HIF/HIF Prolyl-Hydroxylase HIV Keap1-Nrf2 Cancer
    Oltipraz-d3 is the deuterium labeled Oltipraz. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
    Oltipraz-d3
  • HY-134508A

    Others Others
    C24-Ceramide (d18:1/24:0) is a sphingolipid that can be used for the lipid membranes composed. C24-Ceramide (d18:1/24:0) induces time-dependent changes in membrane properties. C24-Ceramide (d18:1/24:0) induces membrane reorganization .
    C24-Ceramide (d18:1/24:0)
  • HY-18642

    PF-4981517

    Cytochrome P450 Others
    CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on agent metabolism .
    CYP3cide
  • HY-151285

    Apoptosis JAK Inflammation/Immunology Cancer
    JAK-2-/3-IN-3 (compound ST4j) is a potent JAK2/3 inhibitor with IC50s of 13.00 and 14.86 nM for JAK2 and JAK3, respectively. JAK-2-/3-IN-3 inhibits autophosphorylation of JAK2 and induces apoptosis in a dose- and time-dependent manner. JAK-2-/3-IN-3 can be used in studies of lymph derived diseases and leukemia .
    JAK-2/3-IN-3
  • HY-135334S

    Isotope-Labeled Compounds Drug Metabolite Btk Cytochrome P450 Cancer
    ACP-5862-d4 is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM[1][2].
    ACP-5862-d4
  • HY-13438
    AZD3839 free base
    1 Publications Verification

    Beta-secretase Cancer
    AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease .
    AZD3839 free base
  • HY-W012896

    Others Others
    2-Thiohydantoin acts as an inhibitor for the corrosion of mild steel in 0.1 M HCl and its inhibition efficiency is both concentration and immersion time dependent .
    2-Thiohydantoin
  • HY-146314

    Monoamine Oxidase Amyloid-β Neurological Disease
    MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MAO-B-IN-9
  • HY-N1410

    Triacetylresveratrol, an acetylated analog of Resveratrol. Triacetylresveratrol decreases the phosphorylation of STAT3 and NF-κB in a dose- and time- dependent manner in PANC-1 and BxPC-3 cells. Anticancer effects .
    Triacetylresveratrol
  • HY-155811

    Others Neurological Disease
    DQP-997-74 (compound 2i) is a selective inhibitor of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC50: 0.069 μM and 0.035 μM), with blood-brain barrier penetrability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases .
    DQP-997-74
  • HY-N6842

    Others Infection Cancer
    ArnicolideC is a sesquiterpene lactone isolated Centipeda minima . ArnicolideC exertes a cytotoxic effect on the panel of Nasopharyngeal carcinoma (NPC) cells, significantly inhibiting cell growth in a dose- and time- dependent manner. ArnicolideC also exhibits inhibitory effects on NPC proliferation .
    ArnicolideC
  • HY-N10188

    Others Cancer
    Nidurufin is a potent cell cycle inhibitor with antitumor activity.Nidurufin induces in vitro cell cycle arrest at G2/M transition in the K562 cell line in a concentration and time dependent manner(IC50=12.6 μM) .
    Nidurufin
  • HY-139664
    GSK-3685032
    3 Publications Verification

    DNA Methyltransferase Cancer
    GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
    GSK-3685032
  • HY-149035

    Others Cancer
    PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model .
    PAA4
  • HY-150576

    c-Met/HGFR Cancer
    c-Met-IN-13 is a potent c-Met inhibitor with an IC50 value of 2.43 nM. c-Met-IN-13 shows excellent cytotoxicity for cancer cells. c-Met-IN-13 shows antiproliferative activity in a concentration- and time- dependent manner. c-Met-IN-13 has the potential for the research of cancer .
    c-Met-IN-13
  • HY-117570

    PDI Neurological Disease
    KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family . KSC-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    KSC-34

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