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6983

Inhibitors & Agonists

11

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33

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38

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3

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61

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48

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38

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18758
    IN-1130
    1 Publications Verification

    		 TGF-β Receptor Inflammation/Immunology Cancer
    IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis .
    IN-1130
  • HY-145846
    iNOs-IN-1
    1 Publications Verification

    		 NO Synthase Interleukin Related Inflammation/Immunology
    iNOs-IN-1 (YPW) is a potent inducible nitric oxide synthase (iNOS) inhibitor. iNOs-IN-1 can significantly inhibit the expression of IL-6 and iNOS, as well as reduce LPS-induced NO generation with dose-dependent manner in mouse macrophages. Anti-inflammatory effects .
    iNOs-IN-1
  • HY-161945
    IN-RNA-IN-2

    		HIV HIV Integrase Infection
    IN-RNA-IN-2 (compound 1a) is an inhibitor (IC50=70 nM) of the interaction between HIV-1 integrase and the viral RNA genome. IN-RNA-IN-2 exerts its anti-HIV activity by inhibiting the viral replication process .
    IN-RNA-IN-2
  • HY-130119
    Integrin-IN-2

    		Integrin Cancer
    Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively .
    Integrin-IN-2
  • HY-147047
    InhA-IN-2

    		Bacterial Infection
    InhA-IN-2 (Compound 23) is a Mycobacterium tuberculosis InhA (an enoyl ACP-reductase) inhibitor with an IC50 of 0.31 μM .
    InhA-IN-2
  • HY-146309
    iNOS-IN-2

    		NO Synthase Inflammation/Immunology
    iNOS-IN-2 (Compound 53) is a potent down-regulator of inducible nitric oxide synthase (iNOS) protein. iNOS-IN-2 effectively inhibits the NO production (IC50=6.4 μM). iNOS-IN-2 has a potential therapeutic effect on chronic inflammation .
    iNOS-IN-2
  • HY-150588
    InhA-IN-3

    		Bacterial Infection
    InhA-IN-3 (Compound TU12) is a Mycobacterium tuberculosis InhA (an enoyl ACP-reductase) inhibitor with an IC50 of 17.7 μM .
    InhA-IN-3
  • HY-150589
    InhA-IN-4

    		Bacterial Infection
    InhA-IN-4 (TU14) is a Mycobacterium tuberculosis InhA (an enoyl ACP-reductase) inhibitor with an IC50 of 15.6 μM .
    InhA-IN-4
  • HY-150055
    iNOs-IN-3

    		NO Synthase Inflammation/Immunology
    iNOs-IN-3 (Compound 2d) is an orally active nitric oxide synthase (iNOS) inhibitor (IC50=3.342 µM). iNOs-IN-3 shows anti-inflammatory activity and can be used in LPS-induced acute lung injury (ALI) research .
    iNOs-IN-3
  • HY-120884
    InhA-IN-5

    		Bacterial Infection
    InhA-IN-5 (compound 1) is a potent Mycobacterial tuberculosis (Mtb) trans-2-enoyl-acyl carrier protein reductase (InhA) inhibitor .
    InhA-IN-5
  • HY-P10150
    IN-2-LF

    		Bacterial Infection
    IN-2-LF is an inhibitor of lethal factor. IN-2-LF also inhibits furin with an IC50 of 2 μM. IN-2-LF enhances protection against anthrax lethal toxin when in combination with D6R .
    IN-2-LF
  • HY-160648
    InhA-IN-6

    		Bacterial Infection
    InhA-IN-6 (compound 8) is InhA inhibitor with the IC50 of 90 nM .
    InhA-IN-6
  • HY-160678
    InhA-IN-7

    		Bacterial Infection
    InhA-IN-7 (Compound 11) is a Triclocan (HY-B1119) derivative with inhibitory activity towards enoyl-acyl carrier protein reductase (InhA) with an IC50 of 96 nM. InhA-IN-7 inhibits proliferations of Mycobacterium tuberculosis wildtype and mutant strains with MICs ranging from 19 to 75 μM .
    InhA-IN-7
  • HY-169104
    InhA-IN-8

    		Bacterial Infection
    InhA-IN-8 (compound 6c) is an orally active inhibitor of Mycobacterium tuberculosis InhA (enoyl ACP reductase). InhA-IN-8 has good inhibitory activity against Mtb UalRv (MIC = 0.5-1 μg/mL). InhA-IN-8 can be used in research on acute tuberculosis model mice .
    InhA-IN-8
  • HY-168096
    iNOs-IN-5

    		NO Synthase Apoptosis Cardiovascular Disease Neurological Disease
    iNOs-IN-5 (Compound BN-4) is an inhibitor for iNOS with an IC50 of 0.1707 μM, and reduces NO levels in LPS (HT-D1056)-induced RAW264.7 cells. iNOs-IN-5 reduces the hypoxic injury stimulated ROS and lactate dehydrogenase expression, and exhibits anti-necrosis and anti-apoptosis efficacy. iNOs-IN-5 exhibits anti-cerebral ischemia and neuroprotective activities in SD rat models. iNOs-IN-5 is blood-brain barrier penetrable .
    iNOs-IN-5
  • HY-143492
    Influenza virus-IN-1

    		Influenza Virus Inflammation/Immunology
    Influenza virus-IN-1 (compound 14) is a potent influenza A virus inhibitor with an EC50 of 2.46 µM and CC50 of >200 µM. Influenza virus-IN-1 shows a concentration dependent inhibition activity for PAN endonuclease with EC50 of 312.36 nM. Influenza virus-IN-1 shows shows anti-influenza A virus activities .
    Influenza virus-IN-1
  • HY-143493
    Influenza virus-IN-2

    		Influenza Virus Inflammation/Immunology
    Influenza virus-IN-2 (compound 19) is a potent influenza virus inhibitor with an EC50 of 2.58 µM and CC50 of 150.85 µM. Influenza virus-IN-2 shows a concentration dependent inhibition activity for PAN endonuclease with EC50 of 489.39 nM. Influenza virus-IN-2 shows shows anti-influenza A virus activities .
    Influenza virus-IN-2
  • HY-146000
    Influenza virus-IN-3

    		Influenza Virus Inflammation/Immunology
    Influenza virus-IN-3 (compound 9) is a potent and selective influenza virus inhibitor with IC50s of 0.88, 0.10, 5.5, 0.51 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-3 shows antiviral and NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-3 shows low cytotoxicity with an CC50 of >200 µM .
    Influenza virus-IN-3
  • HY-146001
    Influenza virus-IN-4

    		Influenza Virus Inflammation/Immunology
    Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice .
    Influenza virus-IN-4
  • HY-146147
    Influenza virus-IN-5

    		Influenza Virus Infection
    Influenza virus-IN-5 (Compound 5f) is an inhibitor of influenza virus hemagglutinin (HA) with an EC50 of 1 nM against influenza A/H3N2 virus .
    Influenza virus-IN-5
  • HY-152078
    Influenza virus-IN-6

    		Influenza Virus Infection
    Influenza virus-IN-6 (Compound 35) is a potent influenza N-terminal domain of the polymerase acidic protein subunit (PAN) endonuclease inhibitor with an IC50 of 0.20 μM .
    Influenza virus-IN-6
  • HY-153570
    Influenza virus-IN-7

    		Influenza Virus Infection
    Influenza virus-IN-7 (Example 16) is an orally active cap-dependent endonuclease inhibitor that can be used for the research of influenza viral infectious diseases .
    Influenza virus-IN-7
  • HY-155476
    Influenza virus-IN-8

    		Influenza Virus Infection
    Influenza virus-IN-8 (compound A4) is an inhibitor of influenza virus (Influenza Virus) that induces viral nucleoprotein (NP) aggregation and prevents its nuclear accumulation. Influenza virus-IN-8 has broad-spectrum anti-influenza activity and can inhibit the replication and transcription of influenza A virus. Influenza virus-IN-8 also inhibits Oseltamivir (HY-13317)-resistant H1N1/pdm09 strains .
    Influenza virus-IN-8
  • HY-162805
    iNOS/TopoI-IN-1

    		NO Synthase Topoisomerase Apoptosis NF-κB Inflammation/Immunology Cancer
    iNOS/TopoI-IN-1 (compound AuL9) is a multi-target hybrid molecule with anti-tumor, anti-inflammatory and antioxidant activities. iNOS/TopoI-IN-1 inhibits the growth of breast cancer cells MCF-7 and MDA MB-231 in vitro with IC50 of 3.5 μM and 6.3 μM, respectively, and induces DNA damage and apoptosis of breast cancer cells by inhibiting human topoisomerase I (TopoI) (Ki=2.72 μM). In addition, NOS/TopoI-IN-1 inhibits the expression of iNOS by inhibiting the activation of NF-kB (Ki=1.49 μM) .
    iNOS/TopoI-IN-1
  • HY-131179
    Influenza A virus-IN-1

    		Influenza Virus Infection
    Influenza A virus-IN-1 is a dihydropyrrolidones derivative and is a potent inhibitor against wide subtypes of influenza A virus (IAV) with IC50 values from 3.11 μM to 7.13 μM. Influenza A virus-IN-1 efficiently inhibits replication of IAV, up-regulates the expression of key antiviral cytokines IFN-β and antiviral protein MxA .
    Influenza A virus-IN-1
  • HY-146004
    Influenza A virus-IN-4

    		Influenza Virus Infection
    Influenza A virus-IN-4 (compound 23b), an Oseltamivir derivative, is a potent inhibitor of neuraminidase. Influenza A virus-IN-4 exerts powerful inhibitions on influenza viruses .
    Influenza A virus-IN-4
  • HY-146167
    iNOS/PGE2-IN-1

    		NO Synthase Inflammation/Immunology
    iNOS/PGE2-IN-1 (compound 4a), an iNOS/PGE2 inhibitor, is a potent anti-inflammatory agent. iNOS/PGE2-IN-1 can inhibit LPS-induced NO production. iNOS/PGE2-IN-1 possesses low ulcerogenic liabilities .
    iNOS/PGE2-IN-1
  • HY-122844
    Ifebemtinib
    1 Publications Verification

    BI-853520; in-10018

    		 FAK Cancer
    Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1?nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900?nM and 1040?nM, respectively .
    Ifebemtinib
  • HY-161513
    iNOS/COX-2-IN-1

    		COX NO Synthase Inflammation/Immunology
    iNOS/COX-2-IN-1 (Compound 12e) is an inhibitor of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). iNOS/COX-2-IN-1 inhibits the NF-κB and MAPKs signaling pathways and thus exerts anti-inflammatory effects .
    iNOS/COX-2-IN-1
  • HY-162492
    Influenza A virus-IN-14

    		Influenza Virus Infection
    Influenza A virus-IN-14 (Compound 37) is an inhibitor for influenza virus type A (IAV), which inhibits H1N1 with an EC50 of 23 nM. Influenza A virus-IN-14 exhibits low cytotoxicity with CC50 of more than 100 μM. Influenza A virus-IN-14 inhibits cytopathic effect and improves the survival rates of cell Calu3. Influenza A virus-IN-14 exhibits synergistic activity with the neuraminidase inhibitor Oseltamivir (HY-13317). Influenza A virus-IN-14 exhibits poor pharmacokinetic properties in CD-1 mouse .
    Influenza A virus-IN-14
  • HY-159564
    iNOS/COX-2-IN-3

    		COX NO Synthase Inflammation/Immunology
    iNOS/COX-2-IN-3 (compound 7d) is a dual inhibitor of iNOS and COX-2, with potential anti-inflammatory activity against LPS (HY-D1056)-induced RAW 264.7 cells (IC50=3.48 μM). iNOS/COX-2-IN-3 has good plasma stability, oral activity and gastric safety, and its inhibitory activity on iNOS and COX-2 expression is 5.43-fold and 2.37-fold that of Indomethacin (HY-14397), respectively .
    iNOS/COX-2-IN-3
  • HY-122844A
    Ifebemtinib hydrochloride

    BI-853520 hydrochloride; in-10018 hydrochloride

    		 FAK Cancer
    Ifebemtinib (BI-853520) hydrochloride is an orally active and potent focal adhesion kinase (FAK) inhibitor (IC50 = 1 nM for recombinant FAK). Ifebemtinib hydrochloride exhibits antiproliferative activity against cancer cells .
    Ifebemtinib hydrochloride
  • HY-170646
    Influenza A virus-IN-15

    		Influenza Virus Infection
    Influenza A virus-IN-15 (Compound 9b), a quinoline derivative, is a broad-spectrum inhibitor of influenza A viruses with acceptable cytotoxicity (IC 50: 0.88-6.33 μM). Influenza A virus-IN-15 can inhibit the transcription and replication of viral RNA and is used in research for its antiviral effects against influenza A viruses (IAV) .
    Influenza A virus-IN-15
  • HY-149034
    Influenza A virus-IN-8

    S5

    		 Influenza Virus Infection Cancer
    Influenza A virus-IN-8 (S5) is a macrocyclic peptide with no cytotoxic. Influenza A virus-IN-8 is also a potent Influenza A Virus (IAV) inhibitor (with sufficient protease stability) with IC50s of 6.7 and 6.6 nM for H1 and H5 variants, respectively. Influenza A virus-IN-8 shows good affinitiescan to H1 variants, binds to a conserved region in the HA stem with a Kd of 1.0 nM .
    Influenza A virus-IN-8
  • HY-134884
    INCB086550

    PD-1/PD-L1-in-8

    		 PD-1/PD-L1 Cancer
    INCB086550 is a potent, oral, small-molecule PD-L1 inhibitor with IC50s value of 3.1, 4.9 and 1.9 nM for human, cynomolgus, and rat, respectively. INCB086550 promotes the dimerization of cell-surface PD-L1 and induces PD-L1 entry into Golgi vesicles then traffick to the nucleus. INCB086550 can be used for multiple cancers research .
    INCB086550
  • HY-R04609A
    In Vivo Rgma Rat Pre-designed siRNA Set A-1

    		Small Interfering RNA (siRNA) Cancer
    In Vivo Rgma Rat Pre-designed siRNA Set A-1 is a siRNA product designed for the Rgma (Rat) gene and can be used for in vivo experiments in rats.
    In Vivo Rgma Rat Pre-designed siRNA Set A-1
    In Vivo Rgma Rat Pre-designed siRNA Set A-1
  • HY-R04609B
    In Vivo Rgma Rat Pre-designed siRNA Set A-2‍

    		Small Interfering RNA (siRNA) Cancer
    In Vivo Rgma Rat Pre-designed siRNA Set A-2‍ is a siRNA product designed for the Rgma (Rat) gene and can be used for in vivo experiments in rats.
    In Vivo Rgma Rat Pre-designed siRNA Set A-2‍
    In Vivo Rgma Rat Pre-designed siRNA Set A-2‍
  • HY-R04609C
    In Vivo Rgma Rat Pre-designed siRNA Set A-3

    		Small Interfering RNA (siRNA) Cancer
    In Vivo Rgma Rat Pre-designed siRNA Set A-3 is a siRNA product designed for the Rgma (Rat) gene and can be used for in vivo experiments in rats.
    In Vivo Rgma Rat Pre-designed siRNA Set A-3
    In Vivo Rgma Rat Pre-designed siRNA Set A-3
  • HY-160623
    INS018 055

    TNIK&MAP4K4-in-2

    		 MAP4K Cancer
    INS018 055 (compound 112) is a TNIK and MAP4K4 inhibitor with IC50 values of 12-120, 12-120 nM, respectively .
    INS018 055
  • HY-157390
    DPP-4-IN-9

    		Dipeptidyl Peptidase Metabolic Disease
    DPP-4-IN-9 (compound 6l) is a potent inhibitor of dipeptidyl peptidase DPP-4 (IC50: 8.22 nM). DPP-4-IN-9 has antihyperglycemic activity .
    DPP-4-IN-9
  • HY-155241
    α-Amylase/α-Glucosidase-IN-4

    		Glycosidase Amylases Metabolic Disease
    α-Amylase/α-Glucosidase-IN-4 (compound 5) is a dual inhibitor of α-glucosidase (Glucosidase) and α-amylase (Amylases) with IC50s of 0.15 μM and 1.10 μM, respectively. α-Amylase/α-Glucosidase-IN-4 has potential antidiabetic activity .
    α-Amylase/α-Glucosidase-IN-4
  • HY-146268
    CaMKIIα-IN-1

    		CaMK Neurological Disease
    CaMKIIα-IN-1 (Compound 4d) is an orally active Ca 2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability .
    CaMKIIα-IN-1
  • HY-116713
    PfDHODH-IN-3

    		Parasite Dihydroorotate Dehydrogenase Infection
    PfDHODH-IN-3 (compound 2) is an orally active PfDHODH inhibitor with strong antimalarial activity (IC50=47 nM). PfDHODH-IN-3 can inhibit the growth of Plasmodium in animals .
    PfDHODH-IN-3
  • HY-162856
    TRPV1-IN-2

    		TRP Channel Neurological Disease
    TRPV1-IN-2 ((R)-32) is a TRPV1 inhibitor. TRPV1-IN-2 has protective effects on ED epilepsy models .
    TRPV1-IN-2
  • HY-168563
    BuChE-IN-15

    		Cholinesterase (ChE) FAAH Neurological Disease
    BuChE-IN-15 (compound D12) is a selective BuChE/FAAH dual inhibitor with and show IC50 values of 81 and 400 nM for hBuChE and hFFAH, respectively. BuChE-IN-15 possesses good BBB penetration, and shows neuroprotection.BuChE-IN-15 can be used for study of Alzheimer .
    BuChE-IN-15
  • HY-126898
    5-LO/mPGES1-IN-1

    		Lipoxygenase PGE synthase Inflammation/Immunology
    5-LO/mPGES1-IN-1 (Compound 16) is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO). IC50 values are 0.3 and 0.4 μM, respectively. 5-LO/mPGES1-IN-1 has anti-inflammatory activity .
    5-LO/mPGES1-IN-1
  • HY-151158
    EGFR/HER2-IN-7

    		EGFR Cancer
    EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC50s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC50=0.907 μM) .
    EGFR/HER2-IN-7
  • HY-151154
    EGFR/HER2/DHFR-IN-1

    		EGFR Cancer
    EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis .
    EGFR/HER2/DHFR-IN-1
  • HY-157316
    TZ-NBD

    		Fluorescent Dye Others
    TZ-NBD is a dual-channel sensitive fluorescence probe that exhibits fast response, and excellent selectivity to detect biothiols in vitro and in vivo .
    TZ-NBD
  • HY-155349
    AChE/BuChE-IN-4

    		Cholinesterase (ChE) Neurological Disease
    AChE/BuChE-IN-4(compound 4a) is aorally activeandbrain-penetrantmultitarget-directedAChE/BuChEinhibitor againstAChEandBuChE, with theIC50of 2.08 and 7.41 μM .
    AChE/BuChE-IN-4

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