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time-dependent inhibitor

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47

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1

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5

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3

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1

Click Chemistry

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-U00197
    Tilmacoxib

    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-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-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-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-108341
    PF-06424439
    Maximum Cited Publications
    13 Publications Verification

    		 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-158309
    hOAT-IN-1

    		Aminotransferases (Transaminases) Cancer
    hOAT-IN-1 (compound 5) is a mechanical inhibitor of human ornithine aminotransferase (hOAT). hOAT-IN-1 as a time-dependent inhibitor can form tightly bound PLP inhibitor adduct with hOAT. hOAT-IN-1 can result IN tight occupation of the active site of hOAT. hOAT-IN-1 can be used in the study of lung cell carcinoma .
    hOAT-IN-1
  • HY-144689
    BChE-IN-3

    		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-106855
    Almokalant

    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-143468
    MEK-IN-5

    		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-P4302
    Z-FK-ck

    Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone

    		 Cathepsin Cardiovascular Disease
    Z-FK-ck (Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone) is a potent and selective gingipain-K-specific inhibitor. Z-FK-ck prolongs plasma thrombin time (TT) in a dose- and time-dependent manner .
    Z-FK-ck
  • HY-170962
    SDUY817

    		Neprilysin Aminopeptidase Neurological Disease
    SDUY817 is a dual APN/NEP inhibitor, with IC50 values of 0.29 μM for APN and 7.4 μM for NEP. SDUY817 exerts analgesic effects in a concentration- and time-dependent manner, and can be used for research in the field of neuropathic pain disorders .
    SDUY817
  • HY-B0363
    Nimesulide
    5+ Cited Publications

    R805

    		 COX Inflammation/Immunology Cancer
    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-108341A
    PF-06424439 methanesulfonate
    Maximum Cited Publications
    13 Publications Verification

    		 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-18642A
    (R)-CYP3cide

    (R)-PF-4981517

    		 Cytochrome P450 Others
    (R)-CYP3cide ((R)-PF-4981517) is the R-isomer of CYP3cide (HY-18642). CYP3cide is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4) .
    (R)-CYP3cide
  • HY-133862
    SCH-202676

    		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-110012
    SCH-202676 hydrobromide

    		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-N0220R
    Dauricine (Standard)

    		Oxidative Phosphorylation NF-κB Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Dauricine (Standard) is the analytical standard of Dauricine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-172091
    CZY43

    		EGFR Cancer
    CZY43 is a HER3 degrader. CZY43 can effectively induce HER3 degradation in a dose- and time-dependent manner in breast cancer SKBR3 cells. CZY43 potently inhibits HER3-dependent signaling and cancer cell growth and outperforms Bosutinib (HY-10158) .
    CZY43
  • HY-115750
    Nω-allyl-L-arginine

    		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-B0363R
    Nimesulide (Standard)

    		COX Inflammation/Immunology Cancer
    Nimesulide (Standard) is the analytical standard of Nimesulide. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0363S
    Nimesulide D5

    		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-19323A
    (S)-Ceralasertib
    2 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-B0363S1
    Nimesulide-13C6

    R805-13C6

    		 Isotope-Labeled Compounds COX Inflammation/Immunology Cancer
    Nimesulide- 13C6 (R805- 13C6) is 13C 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.
    Nimesulide-13C6
  • HY-108704
    CT-721

    		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-16718
    Dagrocorat

    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-16718A
    Dagrocorat hydrochloride

    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-100740A
    Lanabecestat hydrochloride

    AZD-3293 hydrochloride; LY3314814 hydrochloride

    		 Beta-secretase Neurological Disease
    Lanabecestat (AZD-3293) hydrochloride is a potent BACE1 inhibitor that has been investigated for its potential as a modifying treatment for Alzheimer's disease. Lanabecestat (hydrochloride) demonstrated significant dose- and time-dependent reductions in concentrations of amyloid beta peptides in plasma, cerebrospinal fluid, and brain. Lanabecestat (hydrochloride) was also shown to produce reductions in Aβ neuritic plaque burden without demonstrating clinical benefits or slowing the progression of Alzheimer's disease pathophysiology.
    Lanabecestat hydrochloride
  • HY-151285
    JAK-2/3-IN-3

    		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-N13739
    Taraxinic acid

    		Tyrosinase Cancer
    Taraxinic acid can be found in the roots of Taraxacum flavostylum and Taraxacum lucidum. It is a Tyrosinase inhibitor that dose-dependently inhibits Tyrosinase activity, showing approximately 54.5% inhibition at a concentration of 50 μg/mL. Taraxinic acid has an IC50 of 83.2 μM against melanoma cells A375 and HTB140, and an IC50 of 60.4 μM against melanoma cells WM793, with activity being both dose- and time-dependent. Taraxinic acid holds promise for research in the field of anticancer therapy .
    Taraxinic acid
  • HY-117540
    ZLD10A

    		Histone Methyltransferase Cancer
    ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .
    ZLD10A
  • HY-N7854
    Anacardic acid diene

    Anacardic acid 15:2

    		 Bacterial Infection
    Anacardic acid diene is a polyunsaturated form of anacardic acid (HY-N2020) that has been found in cashew nut shell liquid. It has antibacterial activity against methicillin resistant S. aureus (MRSA) and S. mutans (MICs=12.5 and 6.25 μg/mL, respectively). Anacardic acid diene has schistosomicidal activity against adult S. mansoni worms when used at a concentration of 100 μM. It also inhibits soybean lipoxygenase-1 in a time-dependent manner.
    Anacardic acid diene
  • HY-18642
    CYP3cide

    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-168072
    GP130-IN-1

    		Interleukin Related Apoptosis Autophagy Cancer
    GP130-IN-1 (compound 49) is a potent GP130 inhibitor with significant in vitro antitumor activity and higher selectivity than Bazedoxifene (HY-A0031). GP130-IN-1 induces ultrastructural changes in cells, causing cell cycle arrest in the G0/G1 phase in a time-dependent manner and triggering apoptosis and autophagy. GP130-IN-1 can be used in the study of triple-negative breast cancer .
    GP130-IN-1
  • HY-135334S
    ACP-5862-d4

    		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-W012896
    2-Thiohydantoin

    		Biochemical Assay Reagents 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
    MAO-B-IN-9

    		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-155811
    DQP-997-74

    		iGluR 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
    ArnicolideC

    		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-162464
    MPD2

    		PROTACs SARS-CoV Infection
    MPD2 is a Cereblon-binding ligand-based PROTAC that degrades MPro, the main protease of SARS-CoV-2. MPD2 effectively reduced MPro protein levels in 293T cells in a time-dependent manner (DC50=296 nM). MPD2 exhibited potent antiviral activity against multiple SARS-CoV-2 strains and had enhanced potency against Nirmatrelvir (HY-138687) resistant strains. MPD2 provides a new direction for antiviral drug development against SARS-CoV-2 and other emerging coronavirus pathogens (Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker (HY-W275882)；Red: SARS-CoV-2 MPro Inhibitor MP18 (HY-158763)) .
    MPD2
  • HY-N10188
    Nidurufin

    		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
    5+ Cited Publications

    		 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-150576
    c-Met-IN-13

    		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-139664A
    (R)-GSK-3685032

    		DNA Methyltransferase Cancer
    (R)-GSK-3685032 is the R-enantiomer of GSK-3685032. 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 .
    (R)-GSK-3685032
  • HY-146312
    AChE/BChE/MAO-B-IN-1

    		Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    AChE/BChE/MAO-B-IN-1 (Compound 10) is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC50 values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity .
    AChE/BChE/MAO-B-IN-1
  • HY-W587743
    N1-Acetyl-5-methoxykynuramine hydrochloride

    AMK hydrochloride

    		 Prostaglandin Receptor PGE synthase COX Reactive Oxygen Species Neurological Disease Metabolic Disease
    N1-Acetyl-5-methoxykynuramine (AMK) hydrochloride is an active metabolite of the neurohormone melatonin (HY-B0075). N1-Acetyl-5-methoxykynuramine hydrochloride (200 µM) effectively scavenges singlet oxygen (ROS).1 It also inhibits the production of prostaglandin E2 (PGE2) and prostaglandin D2 (PGD2) induced by epinephrine and arachidonic acid in a concentration- and time-dependent manner, and suppresses the increase in COX-2 levels induced by LPS (HY-D1056) in RAW 264.7 macrophages at a concentration of 500 µM. In a mouse model of Parkinson's disease induced by MPTP (HY-15608), N1-Acetyl-5-methoxykynuramine hydrochloride (20 mg/kg) reduces the increase in lipid peroxidation in the cytosol and mitochondria of the substantia nigra and striatum. N1-Acetyl-5-methoxykynuramine hydrochloride can be used in research on metabolic and neurological diseases
    N1-Acetyl-5-methoxykynuramine hydrochloride
  • HY-139664B
    (S)-GSK-3685032

    		DNA Methyltransferase Cancer
    (S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. 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 .
    (S)-GSK-3685032

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