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2 3a Inhibitors

" in MedChemExpress (MCE) Product Catalog:

40

Inhibitors & Agonists

1

Inhibitory Antibodies

2

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10029
    Nutlin-3a
    Maximum Cited Publications
    34 Publications Verification

    Rebemadlin

    		 MDM-2/p53 E1/E2/E3 Enzyme Autophagy Apoptosis Cancer
    Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas .
    Nutlin-3a
  • HY-18899
    Nec-3a

    Nec-3a is a Necrostatin-3 analogue. Nec-3a is a RIP1 inhibitor (IC50: 0.44 μM). Nec-3a inhibits the autophosphorylation activity of the RIP1 kinase domain .
    Nec-3a
  • HY-106312A
    Enviroxime

    LY122772

    		 Enterovirus Infection
    Enviroxime (LY122772) is an antiviral compound that inhibits the replication of rhinoviruses and enteroviruses. Enviroxime blocks the replication of plus-strand viral RNA by targeting the viral 3A coding region. Enviroxime can be a useful tool for investigating the natural function of the 3A protein .
    Enviroxime
  • HY-157537
    α-Amylase-IN-5

    		Amylases Metabolic Disease
    α-Amylase-IN-5 (compound 3a) is a α-amylase inhibitor, with an IC50 of 18.8 mM .
    α-Amylase-IN-5
  • HY-149479
    Quorum Sensing-IN-3

    		Bacterial Infection
    QS-IN-1 (Compound 3a) is a quorum sensing inhibitor against pseudomonas aeruginosa. QS-IN-1 inhibits biofilm formation .
    Quorum Sensing-IN-3
  • HY-157090
    AChE/MAO-B-IN-6

    		Monoamine Oxidase Cholinesterase (ChE) Neurological Disease
    AChE/MAO-B-IN-6 (compound 3a) is a dual inhibitor of AChE and h-MAO-B with potential to inhibit Alzheimer's disease .
    AChE/MAO-B-IN-6
  • HY-161293
    p38-α MAPK-IN-6

    		p38 MAPK Cancer
    p38-α MAPK-IN-6 (compound 3a) is a p38α mitogen-activated protein kinase inhibitor .
    p38-α MAPK-IN-6
  • HY-17464
    Cilostazol
    3 Publications Verification

    OPC 13013

    		 Phosphodiesterase (PDE) Autophagy Cardiovascular Disease Cancer
    Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
    Cilostazol
  • HY-151136
    DY-46-2

    		DNA Methyltransferase Cancer
    DY-46-2 is a high potency and selectivity novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor with an IC50 value of 0.39 μM .
    DY-46-2
  • HY-146163
    Topoisomerase II inhibitor 7

    		Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis .
    Topoisomerase II <em>inhibitor</em> 7
  • HY-115981
    NS5A-IN-2

    		HCV Protease Infection
    NS5A-IN-2 (Compound 33) is a potent inhibitor of NS5A. NS5A-IN-2 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good metabolic stability . NS5A-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    NS5A-IN-2
  • HY-126144
    GSK-3β inhibitor 1
    2 Publications Verification

    		 GSK-3 Metabolic Disease
    GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM .
    GSK-3β <em>inhibitor</em> 1
  • HY-10493
    Cobicistat
    5+ Cited Publications

    GS-9350

    		 Cytochrome P450 HIV Infection Cancer
    Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.
    Cobicistat
  • HY-17464S
    Cilostazol-d11

    		Isotope-Labeled Compounds Phosphodiesterase (PDE) Autophagy Cardiovascular Disease Cancer
    Cilostazol-d11 is the deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].
    Cilostazol-d11
  • HY-17464S1
    Cilostazol-d4

    OPC-13013-d4

    		 Isotope-Labeled Compounds Phosphodiesterase (PDE) Autophagy Cardiovascular Disease Cancer
    Cilostazol-d4 is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].
    Cilostazol-d4
  • HY-N6748
    Roquefortine C

    		P-glycoprotein Cytochrome P450 Bacterial Endogenous Metabolite Infection Cancer
    Roquefortine C, a fungal cyclopeptide isolated from Penicillium roquefortii, activates P-gp and also inhibits P450-3A and other haemoproteins. Roquefortine C has bacteriostatic activities against Gram-positive bacteria .
    Roquefortine C
  • HY-W028690
    DNMDP
    3 Publications Verification

    		 Phosphodiesterase (PDE) Cancer
    DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity .
    DNMDP
  • HY-151445
    ZIKV-IN-2

    		DNA Methyltransferase Virus Protease Flavivirus Infection
    ZIKV-IN-2 (compound 3a) is a potent ZIKV NS5 methyl transferase (MTase) inhibitor with an IC50 value of 38.86 μM. ZIKV-IN-2 inhibits ZIKV replication and infection. ZIKV-IN-2 can be used in research of Zika virus (ZIKV) .
    ZIKV-IN-2
  • HY-115982
    NS5A-IN-3

    		HCV Protease Infection
    NS5A-IN-3 (Compound 15) is a potent inhibitor of NS5A. NS5A-IN-3 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good metabolic stability. NS5A-IN-3 exhibits a higher resistance barrier than daclatasvir against genotype 1b . NS5A-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    NS5A-IN-3
  • HY-W009689
    TbPTR1 inhibitor 2

    		Parasite Infection
    TbPTR1 inhibitor 2 (Compound 3a) is a PTR1 enzyme inhibitor, with IC50s of 34.2 and 32.9 μM for TbPTR1 and LmPTR1. TbPTR1 inhibitor 2 has anti-parasitic activity against T. brucei (IC50: 34.2 μM) .
    TbPTR1 <em>inhibitor</em> 2
  • HY-15335
    Nutlin-3b

    		MDM-2/p53 E1/E2/E3 Enzyme Cancer
    Nutlin-3b is a p53/MDM2 inhibitor with an IC50 of 13.6 μM. Nutlin-3b is 150 times less potent in binding to MDM2 than Nutlin-3a .
    Nutlin-3b
  • HY-10568
    TC-E 5005

    		Phosphodiesterase (PDE) Metabolic Disease
    TC-E 5005 is a potent and selective PDE10A inhibitor with IC50 values of 7.28, 239, 779, 919, 3,100, and 3,700 nM for PDE10A, 2A, 11A, 5A, 7B and 3A, respectively. TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate .
    TC-E 5005
  • HY-147885
    HCV-IN-41

    		HCV Infection
    HCV-IN-41 (compound 4) is a highly potent hepatitis C virus (HCV) inhibitor with an EC50 value of 0.006762 nM, 5.183 nM, 1.365 nM and 142.2 nM for HCV genotype 1b, 2a, 3a and 4a, respectively. HCV-IN-41 reduces HCV RNA replication .
    HCV-IN-41
  • HY-N12209
    Neohelmanthicin A

    		Others Cancer
    Neohelmanthicin A (compound 3A) is a phenylpropanoid compound with antitumor activity. The IC50s of Neohelmanthicin A for inhibiting leukemia cell line EL4, breast cancer cell line S180 and breast cancer cell line MCF7 are 0.13 μM, 7 μM and 23 μM respectively .
    Neohelmanthicin A
  • HY-155610
    VEGFR-2-IN-32

    		VEGFR Cancer
    VEGFR-2-IN-32 (Comp 3a) is an inhibitor of VEGFR-2 with an IC50 of 8.93 nM. VEGFR-2-IN-32 has cytotoxic activity against PC-3 cells with an IC50 of 1.22 μM. VEGFR-2-IN-32 can be used for anti-prostate cancer research .
    VEGFR-2-IN-32
  • HY-10493S
    Cobicistat-d8

    GS-9350-d8

    		 Isotope-Labeled Compounds HIV Cytochrome P450 Infection
    Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules .
    Cobicistat-d8
  • HY-142686
    SGK1-IN-3

    		SGK Inflammation/Immunology
    SGK1-IN-3 (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 has the potential for the research of osteoarthritis .
    SGK1-IN-3
  • HY-155979
    SARS-CoV-2 3CLpro-IN-16

    		SARS-CoV Infection
    SARS-CoV-2 3CLpro-IN-16 (Compound 3a) is a covalent SARS-CoV-2 3CLpro inhibitor (IC50s: 2.124 μM). SARS-CoV-2 3CLpro-IN-16 binds to the active site and forms a covalent bond with Cys145 of 3CLpro .
    SARS-CoV-2 3CLpro-IN-16
  • HY-149305
    PptT-IN-4

    		Bacterial Potassium Channel Calcium Channel Sodium Channel Infection
    PptT-IN-4 (Compound 3a) is a PptT inhibitor (IC50: 0.71 μM). PptT-IN-4 inhibits Mtb H37Rv with a MIC value of 42 μM. PptT-IN-4 also inhibits hERG, hCav1.2, and hNav1.5 channels with IC50s of 11 μM, 8.1 μM, 6.9 μM respectively .
    PptT-IN-4
  • HY-19840
    Voxilaprevir

    GS-9857

    		 HCV Protease Infection
    Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity . Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively . Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research .
    Voxilaprevir
  • HY-126144A
    (E/Z)-GSK-3β inhibitor 1

    		GSK-3 Metabolic Disease
    (E/Z)-GSK-3β inhibitor 1 is a racemic compound of (E)-GSK-3β inhibitor 1 and (Z)-GSK-3β inhibitor 1 isomers. GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM .
    (E/Z)-GSK-3β <em>inhibitor</em> 1
  • HY-133180
    YW1128

    		Wnt β-catenin Metabolic Disease
    YW1128 (compound 3a) is a potent Wnt/β-Catenin inhibitor. YW1128 induces the proteasome degradation of β-catenin and subsequent inhibits the Wnt/β-catenin signaling in cells. YW1128 significantly decreases hepatic lipid accumulation. YW1128 improves glucose tolerance of high fat diet-fed mice without noticeable toxicity. YW1128 down regulates the genes involved in the glucose and fatty acid anabolism .
    YW1128
  • HY-15745A
    PSI-7409 tetrasodium
    5+ Cited Publications

    		 HCV Infection
    PSI-7409 tetrasodium is an active 5'-triphosphate metabolite of sofosbuvir (PSI-7977), inhibiting HCV NS5B polymerases, with IC50s of 1.6, 2.8, 0.7 and 2.6 μM for GT 1b_Con1, GT 2a_JFH1, GT 3a, and GT 4a NS5B polymerases, respectively.
    PSI-7409 tetrasodium
  • HY-117026
    LKY-047

    		Cytochrome P450 Metabolic Disease Inflammation/Immunology
    LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
    LKY-047
  • HY-12594
    Paritaprevir
    10+ Cited Publications

    ABT-450; Veruprevir

    		 HCV Protease HCV SARS-CoV Infection
    Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor) .
    Paritaprevir
  • HY-12594A
    Paritaprevir dihydrate

    ABT-450 dihydrate; Veruprevir dihydrate

    		 HCV Protease HCV SARS-CoV Infection
    Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor) .
    Paritaprevir dihydrate
  • HY-125182
    SMCypI C31

    		HCV Infection
    SMCypI C31 is a non-peptidic cyclophilin inhibitor with potent peptidyl-prolyl cis/trans isomerases (PPIase) inhibitory activity (IC50 of 0.1 µM). SMCypI C31 shows pangenotype anti-HCV activity with EC50s ranging from 1.20 to 7.76 μM for genotype 1a, 1b, 2a, 3a, and 5a HCV subgenomic replicons (HCV-SGRs) and chimeric genotype 2a/4a HCV-SGRs. SMCypI C31 disrupts the cyclophilin A-NS5A interaction .
    SMCypI C31
  • HY-146253
    CDK1/2/4-IN-1

    		CDK Apoptosis Bcl-2 Family Caspase Cancer
    CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research .
    CDK1/2/4-IN-1
  • HY-10238
    Danoprevir
    15+ Cited Publications

    ITMN-191; R7227; RO5190591; RG7227

    		 HCV Protease HCV SARS-CoV Infection
    Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC50 of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC50 higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC50s=0.2-0.4 nM) as well as 2b and 3a (IC50s=1.6, 3.5 nM) . Danoprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 0.05 μM .
    Danoprevir
  • HY-146294
    COX-2/5-LOX-IN-1

    		COX Inflammation/Immunology
    COX-2/5-LOX-IN-1 (compound 3a) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-1 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-1 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-1 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 12.13, 0.4 and 4.96 μM, respectively .
    COX-2/5-LOX-IN-1

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