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Results for "

Multitarget inhibitors

" in MedChemExpress (MCE) Product Catalog:

124

Inhibitors & Agonists

1

Fluorescent Dyes

2

Biochemical Assay Reagents

2

Peptides

1

Inhibitory Antibodies

16

Natural
Products

13

Isotope-Labeled Compounds

1

GMP Molecules

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10208
    Pazopanib
    20+ Cited Publications

    GW786034

    VEGFR c-Kit PDGFR Autophagy FGFR Cancer
    Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib
  • HY-10338
    Foretinib
    10+ Cited Publications

    XL880; GSK1363089; GSK089; EXEL-2880

    VEGFR c-Met/HGFR Cancer
    Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
    Foretinib
  • HY-50751
    Linifanib
    5 Publications Verification

    ABT-869; AL-39324

    PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis Cancer
    Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis .
    Linifanib
  • HY-B1227
    Carprofen
    Maximum Cited Publications
    8 Publications Verification

    COX FAAH Autophagy Endogenous Metabolite Inflammation/Immunology
    Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.
    Carprofen
  • HY-132166
    Velzatinib
    1 Publications Verification

    M4205; IDRX-42

    c-Kit PDGFR c-Fms FLT3 Src Cancer
    Velzatinib (M4205) is a multi-target inhibitor for PDGFRB, PDGFRA, CSF1R, c-Kit, FLT3, and LCK, with an IC50s of 2.6, 50, 5.5, 44, 141 and 141 nM, respectively. Velzatinib exhibits antitumor efficacy in xenograft mouse models .
    Velzatinib
  • HY-12009
    Pazopanib Hydrochloride
    20+ Cited Publications

    GW786034 Hydrochloride

    PDGFR VEGFR FGFR c-Kit c-Fms Autophagy Cancer
    Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib Hydrochloride
  • HY-124526

    Ibcasertib; CS2164

    PDGFR c-Fms Aurora Kinase VEGFR c-Kit Mitosis Cancer
    Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects .
    Chiauranib
  • HY-N6028
    Darutoside
    1 Publications Verification

    COX NF-κB Interleukin Related TNF Receptor Inflammation/Immunology
    Darutoside is an orally effective diterpene compound with significant anti-inflammatory, analgesic, wound healing promotion, and immunomodulatory activities. Darutoside reduces edema and pain responses by inhibiting the expression of COX-2 and the migration of inflammatory cells. It regulates macrophage polarization towards the M2 type by inhibiting the NF-κB pathway, alleviating inflammation and promoting wound healing. Through multi-target regulation of metabolic networks, Darutoside significantly alleviates acute gouty arthritis .
    Darutoside
  • HY-100315

    Tyrosine kinase-IN-1

    VEGFR PDGFR FGFR Cardiovascular Disease Cancer
    XL999 is a multi-target tyrosine kinase inhibitor. XL999 has IC50 values for KDR, Flt-1, FGFR1 and PDGFRα of 4 nM, 20 nM, 4 nM and 2 nM, respectively. XL999 can be used in the research of cancer .
    XL 999
  • HY-13308
    Regorafenib Hydrochloride
    Maximum Cited Publications
    87 Publications Verification

    BAY 73-4506 hydrochloride

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively .
    Regorafenib Hydrochloride
  • HY-N7400

    NOD-like Receptor (NLR) Caspase Insecticide Inflammation/Immunology
    Phaseoloidin is an orally active multi-target inhibitor. Phaseoloidin inhibits the activation of the NLRP3 inflammasome and blocks the caspase-11-GSDMD pyroptosis axis. Phaseoloidin reduces the expression of collagen-degrading enzymes to maintain the integrity of cartilage matrix. Phaseoloidin activates the AMPK/mTOR pathway to enhance autophagic function. Phaseoloidin exerts adverse effects on the growth and development of Manduca sexta and Spodoptera littoralis larvae, inhibits larval growth, and thereby helps Nicotiana attenuata defend against lepidopteran herbivorous insects. Phaseoloidin is applicable to research related to acute gouty arthritis and pulmonary fibrosis .
    Phaseoloidin
  • HY-N0381
    Maackiain
    1 Publications Verification

    DL-​Maackiain

    Keap1-Nrf2 p38 MAPK NOD-like Receptor (NLR) NF-κB mTOR Monoamine Oxidase Nuclear Factor of activated T Cells (NFAT) PKC Apoptosis Pyroptosis Autophagy Dengue Virus Infection Neurological Disease Metabolic Disease
    Maackiain (DL-Maackiain) is an orally active multi-target inhibitor with anti-tumor activity and neuroprotective effects. Maackiain activates the AMPK, NLRP3 and Nrf2/HO-1 pathways, and inhibits key targets such as NF-κB, mTOR, MAO-B, NFATc1 and PKCδ, thereby precisely regulating processes including apoptosis, autophagy and pyroptosis. Maackiain also effectively inhibits microglial activation, osteoclast formation, and proliferation and invasion of tumor cells, and protects dopaminergic neurons from damage. Maackiain is applicable to the research of various diseases such as Alzheimer's disease, osteoporosis, sepsis and dengue fever 。
    Maackiain
  • HY-B0380A

    Opioid Receptor Toll-like Receptor (TLR) Calcium Channel Potassium Channel IRAK ERK JNK NF-κB Akt Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
    Trimebutine maleate
  • HY-B0380

    Opioid Receptor Toll-like Receptor (TLR) Calcium Channel Potassium Channel IRAK ERK JNK NF-κB Akt Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
    Trimebutine
  • HY-N2157
    Pteryxin
    1 Publications Verification

    (+)-Pteryxin

    Cholinesterase (ChE) NF-κB NOD-like Receptor (NLR) Keap1-Nrf2 Reactive Oxygen Species (ROS) Nuclear Factor of activated T Cells (NFAT) p38 MAPK Neurological Disease Metabolic Disease Inflammation/Immunology
    Pteryxin ((+)-Pteryxin) is an orally active multi-target inhibitor that targets NF-κB, MAPK, NLRP3 inflammasome, and Nrf2/ARE pathways. Pteryxin is also a BChE inhibitor (IC50=12.96 μg/mL) with a low inhibitory efficiency on AChE. Pteryxin inhibits the Ca 2+-calcineurin-NFATc1 pathway by blocking NF-κB/MAPK signaling, inhibiting NLRP3 inflammasome activation, and reducing ROS generation, and activates Nrf2-mediated antioxidant enzyme expression. Pteryxin has anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin can be used in the study of inflammatory diseases, osteoporosis, diabetes, and Alzheimer's disease .
    Pteryxin
  • HY-10644

    Src Inflammation/Immunology
    Lck inhibitor 2 is a multi-target tyrosine kinase inhibitor with IC50s of 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively.
    Lck inhibitor 2
  • HY-111186

    WL 108366

    Glucocorticoid Receptor MMP VKOR Others
    Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects .
    Flocoumafen
  • HY-I0678

    Drug Metabolite PDGFR Cancer
    Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
    Regorafénib N-oxyde (M2)
  • HY-W015515

    (S)-3,7-Dimethyloct-6-en-1-ol

    Environmental Pollutants TNF Receptor Beta-secretase γ-secretase ERK Cholinesterase (ChE) Neurological Disease Inflammation/Immunology
    L-Citronellol ((S)-3,7-Dimethyloct-6-en-1-ol) is a natural product with anti-allergic and neuroprotective effects. L-Citronellol inhibits mast cell activation and the release of inflammatory factors by inhibiting the ERK pathway. L-Citronellol inhibits BACE1/PSEN1 and AChE, reduces TNF-α expression and lipid peroxidation, demonstrating the potential of multi-target anti-Alzheimer's disease (AD) .
    L-Citronellol
  • HY-128872

    EHP-101; VCE-​004.8

    PPAR Cannabinoid Receptor HIF/HIF Prolyl-Hydroxylase Metabolic Disease Inflammation/Immunology
    Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity .
    Etrinabdione
  • HY-116116

    SIM010603

    c-Kit RET VEGFR Cancer
    Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis .
    Tafetinib
  • HY-156959

    JAK TRP Channel MetAP Infection Inflammation/Immunology
    Ovalicin is a multi-target inhibitor that targets MetAP2, HRH2, JAK2 and TRPV1, with anti-inflammatory and anti-atopic dermatitis activities. Ovalicin covalently binds to MetAP2 to inhibit its function, thereby blocking the replication of Enterocytozoon bieneusi and Vittaforma corneae. Ovalicin alleviates intestinal injury and prolongs survival in infected mouse models, without showing obvious hepatorenal toxicity. Ovalicin attenuates LPS-induced calcium influx, reduces the infiltration of macrophages and mast cells in the skin, and regulates the expression of inflammation-related genes such as IL-31, effectively relieving allergic symptoms in mouse models. Ovalicin can be used for the research of microsporidiosis and atopic dermatitis .
    Ovalicin
  • HY-10208S

    GW786034-d6

    Isotope-Labeled Compounds VEGFR c-Kit PDGFR Autophagy FGFR Cancer
    Pazopanib-d6 is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib-d6
  • HY-B1227R

    Reference Standards COX FAAH Autophagy Endogenous Metabolite Inflammation/Immunology
    Carprofen (Standard) is the analytical standard of Carprofen. This product is intended for research and analytical applications. Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.
    Carprofen (Standard)
  • HY-W015515R

    (S)-3,7-Dimethyloct-6-en-1-ol (Standard)

    Reference Standards ERK Beta-secretase γ-secretase Cholinesterase (ChE) TNF Receptor Neurological Disease Inflammation/Immunology
    L-Citronellol ((S)-3,7-Dimethyloct-6-en-1-ol) is an analytical standard for L-Citronellol (HY-W015515). This product is intended for research and analytical applications. L-Citronellol is a natural product with anti-allergic and neuroprotective effects. L-Citronellol inhibits mast cell activation and the release of inflammatory factors by inhibiting the ERK pathway. L-Citronellol inhibits BACE1/PSEN1 and AChE, reduces TNF-α expression and lipid peroxidation, demonstrating the potential of multi-target anti-Alzheimer's disease (AD).
    L-Citronellol (Standard)
  • HY-146228

    HSP Apoptosis Topoisomerase EGFR VEGFR Cancer
    HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway .
    HSP90-IN-13
  • HY-B1227S

    COX FAAH Autophagy Endogenous Metabolite Inflammation/Immunology
    Carprofen-d3 is the deuterium labeled Carprofen. Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.
    Carprofen-d3
  • HY-50751G

    ABT-869; AL-39324

    VEGFR PDGFR Cancer
    Linifanib (ABT-869) (GMP) is Linifanib (HY-50751) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Linifanib is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib (GMP) promotes the generation and reprogramming of iPSCs from somatic cells .
    Linifanib
  • HY-I0678S

    PDGFR Drug Metabolite Cancer
    Regorafénib N-oxyde-d3(M2) is the deuterium labeled Regorafénib N-oxyde M2 . Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively .
    Regorafénib N-oxyde-d3 (M2)
  • HY-50751R

    ABT-869 (Standard); AL-39324 (Standard)

    PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis Reference Standards Cancer
    Linifanib (Standard) is the analytical standard of Linifanib. This product is intended for research and analytical applications. Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis .
    Linifanib (Standard)
  • HY-178454

    Monoamine Oxidase Amyloid-β Mitochondrial Metabolism Apoptosis Reactive Oxygen Species (ROS) COX NF-κB Neurological Disease
    Multitarget AD-IN-3 is a brain-penetrant neuroprotective agent. Multitarget AD-IN-3 can selectively inhibit MAO-B with an IC50 of 4.42 μM and a SI of 18.12. Multitarget AD-IN-3 can eliminate ROS. Multitarget AD-IN-3 Multitarget AD-IN-3 can inhibit 1-42 self-aggregation and can reverse Aβ1-42-induced mitochondrial membrane depolarization and inhibit apoptosis. Multitarget AD-IN-3 can be used for the research of neurological disease, such as Alzheimer’s disease .
    Multitarget AD-IN-3
  • HY-149636

    EGFR CDK VEGFR Apoptosis Cancer
    Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells .
    Multi-target kinase inhibitor 2
  • HY-10338R

    XL880 (Standard); GSK1363089 (Standard); GSK089 (Standard); EXEL-2880 (Standard)

    Reference Standards VEGFR c-Met/HGFR Cancer
    Foretinib (Standard) is the analytical standard of Foretinib. This product is intended for research and analytical applications. Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
    Foretinib (Standard)
  • HY-172198

    GSK-3 β-catenin DYRK JNK CDK CDKL Neurological Disease
    GSK3-IN-10 (Compound 4) is a multi-target inhibitor, that mainly targets GSK3α and GSK3β with IC50 of 1.0 nM and 2.0 nM. GSK3-IN-10 inhibits the activation of β-catenin, promotes the neuronal survival, and exhibits a protective effect against endoplasmic reticulum stress .
    GSK3-IN-10
  • HY-12009R

    GW786034 Hydrochloride (Standard)

    Reference Standards PDGFR VEGFR FGFR c-Kit c-Fms Autophagy Cancer
    Pazopanib (Hydrochloride) (Standard) is the analytical standard of Pazopanib (Hydrochloride). This product is intended for research and analytical applications. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib Hydrochloride (Standard)
  • HY-10208R

    GW786034 (Standard)

    Reference Standards VEGFR c-Kit PDGFR Autophagy FGFR Cancer
    Pazopanib (Standard) is the analytical standard of Pazopanib. This product is intended for research and analytical applications. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib (Standard)
  • HY-W705479

    GW786034-d3 hydrochloride

    Isotope-Labeled Compounds Autophagy PDGFR FGFR c-Fms VEGFR c-Kit Cancer
    Pazopanib-d3 (hydrochloride) (GW786034-d3 (hydrochloride)) is deuterium labeled Pazopanib (Hydrochloride). Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib-d3 hydrochloride
  • HY-13308R

    BAY 73-4506 hydrochloride (Standard)

    VEGFR Autophagy PDGFR Raf RET Reference Standards Cancer
    Regorafenib (Hydrochloride) (Standard) is the analytical standard of Regorafenib (Hydrochloride). This product is intended for research and analytical applications. Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively .
    Regorafenib Hydrochloride (Standard)
  • HY-10208S2

    GW786034-d3

    Isotope-Labeled Compounds Autophagy VEGFR c-Kit PDGFR FGFR Cancer
    Pazopanib-d3 (GW786034-d3) is deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively .
    Pazopanib-d3
  • HY-I0678S1

    Drug Metabolite Cancer
    Regorafénib N-oxyde (M2)- 13C,d3 is the 13C- and deuterium labeled Regorafénib N-oxyde (M2). Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
    Regorafénib N-oxyde (M2)-13C,d3
  • HY-B0380S1

    Isotope-Labeled Compounds Opioid Receptor Toll-like Receptor (TLR) Calcium Channel Potassium Channel IRAK ERK JNK NF-κB Akt Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
    Trimebutine-d5 fumarate
  • HY-178344

    Calcium Channel Sodium Channel Cardiovascular Disease
    Multi-target kinase-IN-6 is a Multiple target kinase inhibitor. Multi-target kinase-IN-6 can inhibit cardiac RyR2- and NaV1.5-channels but stimulate SERCA2a pump activity. Multi-target kinase-IN-6 can be used for the research of cardiovascular disease, such as heart failure .
    Multi-target kinase-IN-6
  • HY-174128

    ERK Apoptosis Cancer
    Multi-target kinase-IN-5 (Compound 23) is an orally active ERK1/2 inhibitor (IC50 values are 3.04 nM and 1.57 nM, respectively). Multi-target kinase-IN-5 significantly inhibits cancer cell proliferation, migration and invasion, and induces cell apoptosis and cell cycle arrest. Multi-target kinase-IN-5 inhibits the phosphorylation of ERK1/2 and downregulates the activity of its downstream substrate RSK to exert anti-tumor effects. Multi-target kinase-IN-5 can be used in cancer research .
    Multi-target kinase-IN-5
  • HY-172771

    PI3K DNA-PK P-glycoprotein Cancer
    Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrug resistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs .
    Multi-target kinase inhibitor 4
  • HY-169216

    EGFR VEGFR CDK Cancer
    Multi-target kinase inhibitor 3 (compund 6i) is a multi-kinase target inhibitor with anticancer activity. Multi-target kinase inhibitor 3 inhibits EGFR, HER2, VEGFR-2, and CDK2 with IC50s of 0.063 μM, 0.054 μM, 0.119 μM, and 0.448 μM, respectively. Multi-target kinase inhibitor 3 has a good inhibitory effect on breast cancer cells MCF-7, with an IC50 of 6.10 μM .
    Multi-target kinase inhibitor 3
  • HY-158310

    SOS1 EGFR Ras Infection Neurological Disease Metabolic Disease Cancer
    SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM) .
    SOS1/EGFR-IN-1
  • HY-136813

    Beta-secretase Amyloid-β Cholinesterase (ChE) Neurological Disease
    Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50Aβ=3.09 μM), tau aggregation. Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s research .
    Multitarget AD inhibitor-1
  • HY-178157

    CDK EGFR VEGFR Cancer
    Multi-target kinase-IN-7 (Compound 1e) is an orally active multi-target kinase inhibitor (IC50 values: CDK2=0.314 μM, EGFR=0.183 μM, HER-2=0.197 μM, VEGFR-2=0.235 μM). Multi-target kinase-IN-7 is promising for research of solid tumors (e.g., lung, breast, prostate cancer) .
    Multi-target kinase-IN-7
  • HY-158978

    Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    Multitarget AD inhibitor-2 (Compound VN-19) is a multitargeting inhibitor acetylcholinesterase (AChE, IC50=0.14 μM), butyrylcholinesterase (BChE, IC50=11.6 μM), monoamine oxidase B (MAO B, IC50=0.45 μM). Multitarget AD inhibitor-2 inhibits self-induced aggregation of amyloid beta protein Aβ1-42 (inhibition rate is 47.3% at 20 μM), and downregulates the level of ROS in SH-SY5Y (80 inhibition rate at 25 μM). Multitarget AD inhibitor-2 ameliorates the cognitive decline in Scopolamine (HY-N0296)-induced Alzheimer’s Disease zebrafish models .
    Multitarget AD inhibitor-2
  • HY-155349

    Cholinesterase (ChE) Neurological Disease
    AChE/BuChE-IN-4(compound 4a) is a multitarget-directed AChE/BuChE inhibitor againstAChEandBuChE, with the IC50 of 2.08 and 7.41 μM .
    AChE/BuChE-IN-4

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