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Multi-target inhibitor

" in MedChemExpress (MCE) Product Catalog:

144

Inhibitors & Agonists

2

Fluorescent Dye

2

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1

Peptides

4

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22

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-149636
    Multi-target kinase inhibitor 2

    		EGFR CDK VEGFR Cancer
    Multi-target kinase inhibitor 2 (compound 5K) is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values ranging from 40 to 204 nM. 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-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-G0017
    N-Desmethyl imatinib
    1 Publications Verification

    Norimatinib; Imatinib metabolite N-Desmethyl imatinib

    		 Drug Metabolite Others
    N-Desmethyl imatinib (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
    N-Desmethyl imatinib
  • HY-10644
    Lck inhibitor 2

    		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-169216
    Multi-target kinase inhibitor 3

    		Others Cancer
    Multi-target kinase inhibitor 3 (compund 6i) is a potent multi-target anticancer agent .
    Multi-target kinase inhibitor 3
  • HY-136813
    Multitarget AD inhibitor-1

    		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-158334
    NDs-IN-1

    		Cholinesterase (ChE) Monoamine Oxidase NO Synthase PARP p38 MAPK RIP kinase Phospholipase Indoleamine 2,3-Dioxygenase (IDO) Dihydroorotate Dehydrogenase Neurological Disease
    (Neurodegenerative diseases) NDs-IN-1 (Compound 3g) inhibits the activities of key enzymes such as hBACE-1, hAChE and hMAO-B. NDs-IN-1 is a novel non-covalent multi-target inhibitor. NDs-IN-1 is mainly used in the study of neurodegenerative diseases .
    NDs-IN-1
  • HY-158978
    Multitarget AD inhibitor-2

    		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-18817
    AFG210

    		Bcr-Abl FGFR Raf RET VEGFR Cancer
    AFG210 is a potent multi-target kinase inhibitor that primarily inhibits Abl kinase (IC50=330 nM), and also has inhibitory effects on other kinases such as B-Raf, C-Raf, FGFR-1, RET and VEGF receptors. AFG210 can be used to study chronic myeloid leukemia and other diseases with abnormal activation of Abl kinase .
    AFG210
  • HY-G0017A
    N-Desmethyl imatinib mesylate

    Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate

    		 Drug Metabolite Others
    N-Desmethyl imatinib mesylate (Norimatinib mesylate) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
    N-Desmethyl imatinib mesylate
  • HY-167869
    A-849529

    		Drug Metabolite Others
    A-849529 is an acid metabolite of ABT-869 (HY-50751). ABT-869 is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family .
    A-849529
  • HY-120520
    Caylin-1

    		MDM-2/p53 Cancer
    Caylin-1 is an inhibitor of MDM2 and an analog of Nutlin-3. Caylin-1 can bind to Bcl-XL and is used in multi-target anticancer research .
    Caylin-1
  • HY-W591818
    Sunitinib carboxylic acid

    		Drug Derivative Cancer
    Sunitinib carboxylic acid is a carboxylic acid metabolite of Sunitinib (HY-10255A). Sunitinib is a multi-target tyrosine kinase inhibitor, mainly used to inhibit malignant tumors such as gastrointestinal stromal tumors, renal cell carcinoma, and pancreatic neuroendocrine tumors .
    Sunitinib carboxylic acid
  • HY-12009
    Pazopanib Hydrochloride
    15+ 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-B1227
    Carprofen
    2 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-10208
    Pazopanib
    15+ 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-100315
    XL 999

    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
    65 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-132166
    M4205

    IDRX-42

    		 c-Kit PDGFR c-Fms FLT3 Src Cancer
    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. M4205 exhibits antitumor efficacy in xenograft mouse models .
    M4205
  • HY-G0017S1
    N-Desmethyl imatinib-d4

    Norimatinib-d4; Imatinib metabolite N-Desmethyl imatinib-d4

    		 Isotope-Labeled Compounds Others
    N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N-Desmethyl imatinib-d4 (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
    N-Desmethyl imatinib-d4
  • HY-B1227S
    Carprofen-d3

    		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-N10429
    Geissoschizoline

    (+)-Geissoschizoline

    		 Cholinesterase (ChE) Neurological Disease Inflammation/Immunology
    Geissoschizoline ((+)-Geissoschizoline) is a potent inhibitor of human AChE/BChE, with IC50s of 20.40 µM and 10.21 µM, respectively. Geissoschizoline emerges as a possible multi-target prototype that can be very useful in studies of preventing neurodegeneration and restoring neurotransmission. Geissoschizoline aiso is a potent anti-inflammatory agent .
    Geissoschizoline
  • HY-I0678
    Regorafénib N-oxyde (M2)

    		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-10208S
    Pazopanib-d6

    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
    Carprofen (Standard)

    		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-W011873R
    Palmitoleic acid (Standard)

    		Endogenous Metabolite Neurological Disease
    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.
    Palmitoleic acid (Standard)
  • HY-163885
    SSZ

    		Cholinesterase (ChE) Beta-secretase γ-secretase Neurological Disease
    SSZ is a multi-target inhibitor, which targets multiple pathological mechanisms of Alzheimer's disease (AD). SSZ targets acetylcholinesterase, butyrylcholinesterase, β-site amyloid precursor protein cleavage enzyme 1 (BACE1), and γ-secretase. SSZ ameliorates Alzheimer’s diseases and exhibits neuroprotective effect in mice .
    SSZ
  • HY-12009R
    Pazopanib (Hydrochloride) (Standard)

    		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-172198
    GSK3-IN-10

    		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-111186
    Flocoumafen

    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-10208R
    Pazopanib (Standard)

    		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
    Pazopanib-d3 hydrochloride

    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-10208S2
    Pazopanib-d3

    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-12009S
    Pazopanib-13C,d3 hydrochloride

    GW786034-13C,d3 hydrochloride

    		 VEGFR PDGFR Autophagy c-Fms FGFR c-Kit Cancer
    Pazopanib- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride[1]. 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[2][3].
    Pazopanib-13C,d3 hydrochloride
  • HY-B1227S1
    Carprofen-13C,d3

    		FAAH COX Autophagy Endogenous Metabolite Inflammation/Immunology
    Carprofen- 13C,d3 is the deuterium and 13C labeled Carprofen[1]. 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[2][3][4].
    Carprofen-13C,d3
  • HY-10208S1
    Pazopanib-13C,d3

    GW786034-13C,d3

    		 VEGFR PDGFR Autophagy FGFR c-Kit Cancer
    Pazopanib- 13C,d3 is the deuterium and 13C labeled Pazopanib[1]. 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[2][3].
    Pazopanib-13C,d3
  • HY-124526
    Chiauranib

    Ibcasertib; CS2164

    		 VEGFR PDGFR c-Kit Aurora Kinase c-Fms 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-15163A
    Zotiraciclib hydrochloride

    		FLT3 JAK CDK Cancer
    Zotiraciclib hydrochloride is a novel small molecule multi-target enzyme inhibitor with activity in inhibiting tumor growth. Zotiraciclib hydrochloride exerts its anti-tumor effect by reducing the level of Myc through inhibiting cyclin-dependent kinase 9 (CDK9). Zotiraciclib hydrochloride may be useful for inhibiting cancers that cross the blood-brain barrier. The high protein level of MCL-1 of Zotiraciclib hydrochloride is associated with survival, suggesting that it may serve as a prognostic factor and inhibitory target in further studies .
    Zotiraciclib hydrochloride
  • HY-111186R
    Flocoumafen (Standard)

    		VKOR Glucocorticoid Receptor MMP Others
    Flocoumafen (Standard) is the analytical standard of Flocoumafen. This product is intended for research and analytical applications. 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 (Standard)
  • HY-144292
    HDAC-IN-30

    		HDAC Cancer
    HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6 (IC50=42.7 nM), HDAC8 (IC50=131 nM). HDAC-IN-30 exhibits potent antitumor efficacy .
    HDAC-IN-30
  • HY-I0678S
    Regorafénib N-oxyde-d3 (M2)

    		PDGFR Drug Metabolite Cancer
    Regorafénib N-oxyde-d3(M2) is the deuterium labeled Regorafénib N-oxyde M2[1]. 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[2].
    Regorafénib N-oxyde-d3 (M2)
  • HY-50751G
    Linifanib

    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-I0678S1
    Regorafénib N-oxyde (M2)-13C,d3

    		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-170417
    hAChE/hBuChE/GSK-3β-IN-1

    		Cholinesterase (ChE) GSK-3 Neurological Disease
    hAChE/hBuChE/GSK-3β-IN-1 (Compound 6c) is a BBB-penatrable and multi-target anti-Alzheimer's disease compound. hAChE/hBuChE/GSK-3β-IN-1 is the inhibitors of hAChE (IC50: 28.88 nM), hBuChE (IC50: 131.90 nM) and GSK-3β (IC50: 51.42 nM). hAChE/hBuChE/GSK-3β-IN-1 is the tau and Aβ protein aggregation inhibitors .
    hAChE/hBuChE/GSK-3β-IN-1
  • HY-146228
    HSP90-IN-13

    		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-113658
    ts-SA

    		Endogenous Metabolite Others
    ts-SA is a carbonic anhydrase (CA) inhibitor with activity against seven human CA homologues. ts-SA can bind to the Zn(II) ion in the enzyme active site in a deprotonated form. The organic skeleton of ts-SA extends in the enzyme cavity and participates in multiple interactions with amino acid residues and water molecules. Due to its structural differences, the inhibitory performance of ts-SA is significantly better than that of another pyridine derivative. ts-SA exhibits low nanomolar inhibitory activity and is a multi-target CA inhibitor .
    ts-SA
  • HY-50751
    Linifanib
    4 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-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-162585
    5-HT1AR agonist 1

    		5-HT Receptor Neurological Disease
    5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs .
    5-HT1AR agonist 1
  • HY-162606
    MAO-A/B-IN-3

    		Monoamine Oxidase Cholinesterase (ChE) Neurological Disease
    MAO-A/B-IN-3 (Compound 12) stands out as a key dual MAO-AChE inhibitor, displaying excellent multi-target efficacy against MAO-A, MAO-B, and AChE with IC50 values of 67 nM, 29 nM, and 1370 nM respectively. MAO-A/B-IN-3 is adept at altering the A site (hydrophobic ring) and C site (semicarbazone chain) within ketone amine-based MTDLs to bolster the inhibitory potential against MAO-A/B while notably diminishing activity against AChE. MAO-A/B-IN-3 is poised for research applications in the field of neurodegenerative diseases .
    MAO-A/B-IN-3

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