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Targets Recommended: MAPKAPK2 (MK2) Pyk2 LRRK2 Bcl-2 Family EAAT2 P2X Receptor P2Y Receptor Arp2/3 Complex Keap1-Nrf2 EBI2/GPR183 MDM-2/p53 Na+/Ca2+ Exchanger Indoleamine 2,3-Dioxygenase (IDO) FAK E1/E2/E3 Enzyme GPR109A Itk CRAC Channel Calcium Channel BCRP MEK Ack1 sFRP-1

Results for "2 3a Inhibitors" in MCE Product Catalog:

35

Inhibitors & Agonists

5

Peptides

1

Inhibitory Antibodies

1

Natural
Products

5

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-P1505A
    C3a (70-77) TFA

    Complement 3a (70-77) (TFA)

    		 Complement System Inflammation/Immunology
    C3a (70-77) TFA (Complement 3a (70-77) TFA) is an octapeptide corresponding to the COOH terminus of C3a, exhibits the specificity and 1 to 2% biologic activities of C3a.
  • HY-10029
    Nutlin-3a

    		MDM-2/p53 E1/E2/E3 Enzyme Autophagy Apoptosis Cancer
    Nutlin-3a, 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.
  • HY-P1505
    C3a 70-77

    Complement 3a (70-77)

    		 Complement System Inflammation/Immunology
    C3a (70-77) is an octapeptide corresponding to the COOH terminus of C3a, exhibits the specificity and 1 to 2% biologic activities of C3a.
  • HY-P9805
    Anti-MERS-3A1 mAb

    MERS-3a1; MERS Antibody-3a1

    		 SARS-CoV Infection
    Anti-MERS-3A1 mAb (MERS-3A1) is a human monoclonal IgG1 antibody with the high binding affinity produced in CHO cells. Anti-MERS-3A1 mAb bocks the binding of MERS-CoV spike protein to DPP4 receptor.
  • HY-114267
    Cbz-B3A

    		mTOR Others
    Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
  • HY-12692
    DO3A tert-Butyl ester

    DO3a tert-butyl; DO3a-t-Bu-ester

    		 Others Others
    DOTA tert-Butyl ester is a benxyl derivative of the cyclic tosamide; can be nitrated directly; is more convenient to incorporate the nitro group after deprotection lithium aluminum hydride.
  • HY-17464
    Cilostazol

    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.
  • HY-15978
    P7C3-A20

    		Others Neurological Disease
    P7C3-A20 is a derivative of P7C3 with potent proneurogenic and neuroprotective activity. P7C3-A20 exerts an antidepressant-like effect. P7C3-A20 can cross the blood-brain barrier and therefore has the potential for brain injury treatment.
  • HY-126144
    GSK-3β inhibitor 1

    		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.
  • HY-10493
    Cobicistat

    GS-9350

    		 Cytochrome P450 HIV Infection
    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.
  • HY-N6748
    Roquefortine C

    		P-glycoprotein Cytochrome P450 Bacterial Cancer Infection
    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.
  • HY-W028690
    DNMDP

    		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.
  • 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.
  • HY-B0933
    Gadoteridol

    SQ-32692; Gd-HP-DO3a

    		 Others Others
    Gadoteridol is a gadolinium-based MRI contrast agent, used in the imaging of the central nervous system.
  • HY-15745A
    PSI-7409 tetrasodium

    		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.
  • HY-U00439
    Protein kinase inhibitors 1

    		DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-P1345
    TLQP-21

    		Complement System Endocrinology Neurological Disease
    TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.
  • HY-P1345A
    TLQP-21 TFA

    		Complement System Endocrinology Neurological Disease
    TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.
  • HY-10238
    Danoprevir

    ITMN-191; R7227; RO5190591; RG7227

    		 HCV Protease HCV 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).
  • HY-131005
    Ehp inhibitor 2

    		Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-121879
    SHP836

    		Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-124806
    TTP-8307

    		Enterovirus DNA/RNA Synthesis HCV Infection
    TTP-8307 is a potent inhibitor of the replication of several rhino- and enteroviruses. TTP-8307 inhibits coxsackievirus B3 (CVB3; EC50=1.2 μM) and poliovirus by interfering with the synthesis of viral RNA. TTP-8307 exerts antiviral activity through oxysterol-binding protein (OSBP).
  • HY-19373
    RWJ-445167

    3DP-10017

    		 Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    		Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    		 DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    		 Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-135813
    LtaS-IN-1

    		Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    		PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-101918
    DS-1040 Tosylate

    		Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    		GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-15583
    Auristatin F

    		Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-122470
    Stampidine

    		Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-11007
    GNF-2

    		Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-122872
    MKK7-COV-9

    		p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-120944
    BAY-7598

    		MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.

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