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nanomolar efficacy

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22

Inhibitors & Agonists

2

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-134813
    MRTX1133
    45+ Cited Publications

    		 Ras Cancer
    MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
    MRTX1133
  • HY-153810
    Mosnodenvir

    JNJ-1802

    		 Virus Protease Flavivirus Dengue Virus Infection
    Mosnodenvir (JNJ-1802) is an orally active pan serotype dengue virus (DENV) inhibitor, with EC50 values ranging from 0.057 to 11 nM for four dengue virus (DENV) serotypes. Mosnodenvir blocks viral replication by inhibiting the formation of complexes between two viral proteins, nonstructural protein 3 (NS3) and NS4B, thereby preventing the formation of new viral RNA. Mosnodenvir exhibits picomolar to nanomolar antiviral activity in vitro and has antiviral efficacy in mice and non-human primates .
    Mosnodenvir
  • HY-137464A
    OATD-01
    1 Publications Verification

    		 Glycosidase Inflammation/Immunology
    OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research .
    OATD-01
  • HY-139602
    (+)-JNJ-A07
    2 Publications Verification

    		 Flavivirus Dengue Virus Virus Protease Infection
    (+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models .
    (+)-JNJ-A07
  • HY-145561
    Cudetaxestat

    BLD-0409; PAT-409

    		 Phosphodiesterase (PDE) LPL Receptor Inflammation/Immunology Cancer
    Cudetaxestat (BLD-0409; PAT-409) is an orally active and noncompetitive autotaxin (ATX) inhibitor. Cudetaxestat inhibits the activity of ATX, reduces the production of LPA, and thereby blocks the signal transduction of the ATX-LPA axis. Cudetaxestat can still maintain nanomolar-level biochemical efficacy even when the concentration of the LPC substrate increases. Cudetaxestat can be used for the study of various diseases related to LPA including fibrosis, tumor metastasis, inflammation and autoimmune diseases, etc .
    Cudetaxestat
  • HY-W002942
    Ferroptosis-IN-21

    1,2,3,4-Tetrahydroquinolin-8-ol; 8-hydroxy-1,2,3,4-tetrahydroquinoline

    		 Ferroptosis Reactive Oxygen Species (ROS) Inflammation/Immunology
    Ferroptosis-IN-21 is a ferroptosis inhibitor that protects against renal I/R injury by suppressing ferroptosis and directly scavenging peroxyl radicals. Ferroptosis-IN-21 displays broad-spectrum anti-ferroptotic efficacy across multiple inducers in renal tubular epithelial cells, with nanomolar potency and robust suppression of lipid Reactive Oxygen Species (ROS). Ferroptosis-IN-21 significantly ameliorates renal I/R injury in mice, reducing histological damage, functional impairment, and inflammatory cytokine expression, while decreasing lipid peroxidation biomarkers such as 4-hydroxynonenal. Ferroptosis-IN-12 can be used for research in the field of ferroptosis-targeted drug development .
    Ferroptosis-IN-21
  • HY-160696
    ORIC-533

    		CD73 Cancer
    ORIC-533 is an orally active, highly selective, AMP-competitive CD73 inhibitor that potently blocks adenosine production with sub-nanomolar affinity (Ka=0.03 nM). In multiple myeloma, ORIC-533 restores and enhances the cytotoxicity of the immune system against tumor cells through multiple immunological mechanisms, including reversing the immunosuppressive microenvironment, inducing immunogenic cell death, and activating dendritic cells, T cells and NK cells, with no direct toxicity to normal cells. The combination of ORIC-533 with Daratumumab (HY-P9915) synergistically enhances anti-tumor efficacy, significantly increases intratumoral CD8 + T cell infiltration and inhibits tumor growth in vivo .
    ORIC-533
  • HY-108988
    Albicidin

    		Antibiotic Bacterial Topoisomerase DNA/RNA Synthesis Infection
    Albicidin is a peptide antibiotic with phytotoxic activity. Albicidin potently inhibits bacterial and plant DNA gyrase at nanomolar concentrations, blocks DNA replication, and exhibits excellent antibacterial efficacy against multidrug-resistant bacteria. Albicidin possesses bactericidal activity against Gram-positive and Gram-negative microorganisms, and acts as a virulence factor for the systemic plant infection by Xanthomonas albilineans. Albicidin can be used in studies related to bacterial infections and sugarcane leaf blight .
    Albicidin
  • HY-156786
    TLD-1433

    		Reactive Oxygen Species (ROS) Influenza Virus SARS-CoV HSV Infection
    TLD-1433 is the fourth-generation ruthenium (II) based photodynamic compound (PDC). TLD-1433 is activated by green light (525 ± 25 nm) and efficiently generates ROS to achieve pathogen inactivation. After photoinactivation, TLD-1433 significantly induces lipid peroxidation of the cell membrane, which can directly damage the integrity of the viral envelope. TLD-1433 has ID50 for enveloped viruses (such as H1N1 influenza virus, coronavirus OC43, HSV-1, Zika virus) is as low as nanomolar level; for non-enveloped viruses (such as adenovirus Ad5, mammalian rotavirus MRV), a concentration of micro-molar level is required for inactivation. TLD-1433 has antigen retention property and can be used for the preparation of inactivated vaccines .
    TLD-1433
  • HY-170978
    PROTAC CDK9 degrader-11

    		PROTACs CDK Cancer
    PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models .(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
    PROTAC CDK9 degrader-11
  • HY-135495
    AM-0466

    		Sodium Channel Histamine Receptor Inflammation/Immunology
    AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .
    AM-0466
  • HY-173564
    DW34

    		Epigenetic Reader Domain Necroptosis Inflammation/Immunology
    DW34 is an orally active pan-BRD4-D1 biased inhibitor with additional BRD4-D2 inhibitive activity. DW34 displays comparable inhibitive efficacy to I-BET151 (HY-13235) (EC50 = 0.16 μM) with low nanomolar EC50 values of 0.14 μM. DW34 significantly reduces liver inflammation induced by LPS (HY-D1056) and APAP (HY-66005) via reducing chemokine expression and cellular necrosis .
    DW34
  • HY-162763
    FLQY2

    		Apoptosis Cancer
    FLQY2 is a camptothecin analog that exhibits outstanding antitumor efficacy against various solid tumors. FLQY2 possesses both in vitro and in vivo anti-pancreatic cancer activity, inhibiting cell proliferation, colony formation, inducing apoptosis, and causing cell cycle arrest at nanomolar concentrations .
    FLQY2
  • HY-170420
    JNK-1-IN-5

    		JNK Others
    JNK-1-IN-5 (Compound 14) is a potent JNK1 inhibitor with sub-nanomolar efficacy. JNK-1-IN-5 suppresses TGF-β-induced epithelial-mesenchymal transition. JNK-1-IN-5 is promising for research of anti-pulmonary fibrosis agent targeting JNK1 .
    JNK-1-IN-5
  • HY-149928
    NNRT-IN-1

    		HIV Infection
    NNRT-IN-1 (compound 8r) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor featuring significantly anti-resistance efficacy. NNRT-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC50s in the nanomolar range. NNRT-IN-1 displays favorable pharmacokinetic properties .
    NNRT-IN-1
  • HY-19925
    AIC-292

    		HIV Infection
    AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .
    AIC-292
  • HY-12284
    NVP-QAV680

    		Prostaglandin Receptor Inflammation/Immunology
    NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats .
    NVP-QAV680
  • HY-119799
    UK-500001

    		Phosphodiesterase (PDE) Inflammation/Immunology
    UK-500001 is an orally active inhibitor for phosphodiesterase 4 (PDE4), which inhibits PDE4D3 (IC50 is 0.28 nM), PDE4B2 (IC50 is 22.8 nM), PDE4A4 (IC50 is 26.1 nM) and PDE4C2 (IC50 is 271 nM). UK-500001 exhibits anti-inflammatory efficacy and inhibits TNF-α and IFN-γ release in human and rodent macrophagic cell lines in nanomolar levels. UK-500001 ameliorates chronic obstructive pulmonary disease (COPD) and asthma .
    UK-500001
  • HY-181821
    MMV1581361

    		Parasite Na+/K+ ATPase Infection
    MMV1581361 is a PfATP4 inhibitor and an orally active, transmission-blocking agent with nanomolar activity against Plasmodium falciparum blood-stage isolates. MMV1581361 disrupts sodium ion (Na +) homeostasis in Plasmodium falciparum. MMV1581361 inhibits male gamete exflagellation, reduces oocyst intensity, and blocks transmission of Plasmodium falciparum. MMV1581361 demonstrates efficacy in the humanized Plasmodium falciparum NOD scid IL2Rγ null mouse model. MMV1581361 can be used for the research of malaria .
    MMV1581361
  • HY-179375
    LCI133

    		CDK Aurora Kinase Cancer
    LCI133 is afirst-in-class,nanomolar-potent, selective multikinase inhibitor targeting CDK4/6/9 and AURKA/B (IC50 = 4.7/10.2/4.1 nM and 2.8/10.6 nM). LCI133 induces S/G2 cell-cycle arrest and robust apoptosis in MYCN-amplified neuroblastoma BE(2)-C cells. LCI133 demonstrates significant antitumor efficacy in a BE(2)-C neuroblastoma xenograft model .
    LCI133
  • HY-182317
    (+)-Mosnodenvir

    		Drug Isomer Dengue Virus Infection
    (+)-Mosnodenvir is an isomer of Mosnodenvir (HY-153810). Mosnodenvir (JNJ-1802) is an orally active pan serotype dengue virus (DENV) inhibitor, with EC50 values ranging from 0.057 to 11 nM for four dengue virus (DENV) serotypes. Mosnodenvir blocks viral replication by inhibiting the formation of complexes between two viral proteins, nonstructural protein 3 (NS3) and NS4B, thereby preventing the formation of new viral RNA. Mosnodenvir exhibits picomolar to nanomolar antiviral activity in vitro and has antiviral efficacy in mice and non-human primates .
    (+)-Mosnodenvir
  • HY-179404
    KRASG12C IN-18

    		Ras Cancer
    KRASG12C IN-18 is an orally active covalent KRAS G12C inhibitor that achieves complete covalent engagement of KRAS G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS G12C and resistance-associated variants, including KRAS G12C/R68S, with low-nanomolar IC50 values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS G12C-driven solid tumor and KRAS G12C/R68S xenograft models and can be used for colorectal cancer research .
    KRASG12C IN-18

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