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Dual-functional inhibitors

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-177129
    Simepdekinra

    LY4100511; DC-853

    		 Interleukin Related Inflammation/Immunology
    Simepdekinra (LY4100511; DC-853) is an IL-17A antagonist. Simepdekinra can be used in the research of moderate to severe plaque-type psoriasis .
    Simepdekinra
  • HY-178040
    Insecticidal agent 26

    		Acetyl-CoA Carboxylase Pyruvate Carboxylase (PC) Parasite Insecticide Infection
    Insecticidal agent 26 (Compound A11), a spiro insecticidal agent, is a dual-functional inhibitor of pest Acetyl-CoA carboxylase (ACC) and Pyruvate carboxylase (PC). Insecticidal agent 26 has potent insecticidal activity against Sogatella furcifera with a LC50 of 11.0  μg/mL, with significant biosafety to bees. Insecticidal agent 26 can be used for management of white-backed planthoppers (WBPs) .
    Insecticidal agent 26
  • HY-178026
    HPPD/PPO-IN-1

    		HPPD Protoporphyrinogen IX oxidase Others
    HPPD/PPO-IN-1 (Compound B14) is dual-functional inhibitor of HPPD and PPO with IC50s of 0.12  μM and 0.51 μM for Arabidopsis thaliana HPPD and Nicotiana tabacum PPO, respectively. HPPD/PPO-IN-1 has broad-spectrum herbicidal activity against weeds with a crop safety to peanuts and cotton. HPPD/PPO-IN-1 can be used for the development of environmentally friendly herbicides .
    HPPD/PPO-IN-1
  • HY-178716
    PTPN2/1-IN-4

    		Phosphatase IFNAR STAT JAK Cancer
    PTPN2/1-IN-4 (Compound WS35) is an orally active, dual-functional inhibitor of PTPN1 and PTPN2 with IC50s of 12.8 and 5.8 nM for PTPN1 and PTPN2, respectively. PTPN2/1-IN-4 modulates the IFNγ-JAK-STAT signaling pathway and significantly augments CD8+ T-cell tumor infiltration. PTPN2/1-IN-4 has potent anticancer activity, robustly inhibiting tumor growth both as a monotherapy and in combination with an anti-PD-1 antibody in B16-OVA syngeneic mouse models .
    PTPN2/1-IN-4
  • HY-175607
    AChE/nAChR-IN-1

    		Cholinesterase (ChE) nAChR Infection Neurological Disease
    AChE/nAChR-IN-1 (Compound 1a) is dual-functional inhibitor of AChE and nAChR. AChE/nAChR-IN-1 has potent toxicity and larvicidal effectiveness against Culex pipiens larvae with a LC50 of 4 ng/mL. AChE/nAChR-IN-1 can be used as larvicides for mosquito-borne diseases research .
    AChE/nAChR-IN-1
  • HY-178017
    BChE/hCA II-IN-1

    		Cholinesterase (ChE) Carbonic Anhydrase Neurological Disease
    BChE/hCA II-IN-1 (Compound 20) is a dual-functional inhibitor of Butyrylcholinesterase (BChE) and human carbonic anhydrase II (hCA II) with IC50s of 76.50 and 10.69  μM for BChE and hCA II, respectively. BChE/hCA II-IN-1 can be used for neurodegenerative diseases like Alzheimer's and glaucoma research .
    BChE/hCA II-IN-1
  • HY-175605
    α-Amylase/α-Glucosidase-IN-21

    		Glycosidase Amylases Metabolic Disease
    α-Amylase/α-Glucosidase-IN-21 (Compound 4) is a dual-functional inhibitor of α-Glucosidase and α-Amylase with IC50s of 0.27 and  0.19 µg/mL for α-Glucosidase and α-Amylase, respectively. α-Amylase/α-Glucosidase-IN-21 has an antidiabetic activity.α-Amylase/α-Glucosidase-IN-21 can be used for diabetes mellitus research .
    α-Amylase/α-Glucosidase-IN-21
  • HY-179560
    PMV6-PEG4-BI2536

    		Polo-like Kinase (PLK) MDM-2/p53 Cancer
    PMV6-PEG4-BI2536 is a p53-Y220C-PLK1 dual-functional compound, composed of a high-affinity p53-Y220C mutant binder (Kd ≈ 2.5 nM) and a potent PLK1 kinase inhibitor (IC50 = 0.83 nM). PMV6-PEG4-BI2536 triggers TP53 Y220C cell G2/M arrest and apoptosis through PLK1 mislocalization and kinase inhibition, independent of p53 transcriptional reactivation. PMV6-PEG4-BI2536 can be used for the study of TP53 mutant cancers .
    PMV6-PEG4-BI2536
  • HY-175219
    CA-II/Dkk1-IN-1

    		Carbonic Anhydrase Cancer
    CA-II/Dkk1-IN-1 (Compound 5d) is a dual-functional inhibitor of CA-II and Dkk1 with a IC50 of 6.90  nM for CA-II. CA-II/Dkk1-IN-1 has significantly antioxidant activity and superior DNA binding capacity. CA-II/Dkk1-IN-1 can be used for cancers research, such as esophageal, renal, and lung cancer .
    CA-II/Dkk1-IN-1
  • HY-172891
    CDK9/HDAC1/HDAC3-IN-1

    		CDK HDAC Apoptosis Cancer
    CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC50 s of 0.17  μM, 1.73  μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer .
    CDK9/HDAC1/HDAC3-IN-1
  • HY-175805
    EGFR/HDAC-IN-2

    		EGFR HDAC Apoptosis Cancer
    EGFR/HDAC-IN-2 (Compound 38) is dual-functional inhibitor of EGFR and HDAC3 with IC50s of 20.34 and 1.09 nM for CDK9 and HDAC3, respectively. EGFR/HDAC-IN-2 has superior anti-proliferative activity against cancer cells, inhibits cell migration and induces late-stage cell apoptosis. EGFR/HDAC-IN-2 significantly inhibits triple-negative breast cancer (TNBC) tumor growth in xenograft mouse models. EGFR/HDAC-IN-2 can be used for cancers like TNBC research .
    EGFR/HDAC-IN-2
  • HY-175635
    EGFR/VEGFR2-IN-6

    		EGFR VEGFR Cancer
    EGFR/VEGFR2-IN-6 (Compound 3k) is a dual-functional inhibitor of EGFR and VEGFR2 with IC50s of 10.53 and 3.37 μM for EGFR and VEGFR2, respectively. EGFR/VEGFR2-IN-6 has significant anti-proliferation activity against breast cancer cells, and induces G0/G1 cell cycle arrest and cell apoptosis, especially early apoptosis. EGFR/VEGFR2-IN-6 can be used for cancers research .
    EGFR/VEGFR2-IN-6
  • HY-180370
    Nitromemantine

    NitroSynapsin; YQW-036; NMI-6979

    		 iGluR Drug Derivative Cardiovascular Disease Neurological Disease
    Nitromemantine (NitroSynapsin) is a nitrate derivative of Memantine (HY-B0591) and is a dual-functional NMDAR antagonist. Nitromemantine exhibits significant efficacy in rodent models of cerebral infarction through a dual mechanism of blocking channels and regulating receptors via NO/redox regulation. Nitromemantine can target ischemic neurons under hypoxic conditions and enhance its activity. Nitromemantine inhibits the current induced by NMDA, with its IC50 being 2.4 μM. Nitromemantine can be used for the study of cerebral ischemic stroke .
    Nitromemantine
  • HY-175987
    Antimycobacterial agent-12

    		Bacterial Infection
    Antimycobacterial agent-12 (Compound Ec42), a derivative of Platensimycin (HY-127146), is a dual-functional inhibitor KasA and KasB. Antimycobacterial agent-12 has antibacterial activity with a MICs of 2, 2 and 4 μg/mL against Staphylococcus aureus ATCC 29213, Mycobacterium smegmatis and its Isoniazid (HY-B0329)-resistant strain, respectively. Antimycobacterial agent-12 has a superior antimycobacterial activity in M. smegmatis-infected mouse models. Antimycobacterial agent-12 can be used for tuberculosis research .
    Antimycobacterial agent-12

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