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Dual inhibition

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-104042
    Vorasidenib
    5+ Cited Publications

    AG-881

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation .
    Vorasidenib
  • HY-12299
    WH-4-023
    5 Publications Verification

    Dual LCK/SRC inhibitor

    		 Src Cancer
    WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
    WH-4-023
  • HY-103160A
    EHNA hydrochloride
    5 Publications Verification

    		 Adenosine Deaminase Phosphodiesterase (PDE) Influenza Virus Infection Cardiovascular Disease Neurological Disease Cancer
    EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
    EHNA hydrochloride
  • HY-50878A
    Crizotinib hydrochloride
    Maximum Cited Publications
    86 Publications Verification

    PF-02341066 hydrochloride

    		 Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
    Crizotinib hydrochloride
  • HY-144315
    CYD19

    Snail/HDAC-IN-1

    		 HDAC Cancer
    CYD19 is a potent Snail/HDAC dual target inhibitor. CYD19 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. CYD19 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
    CYD19
  • HY-108347
    CP-100356 hydrochloride
    5+ Cited Publications

    		 P-glycoprotein BCRP Metabolic Disease
    CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM) .
    CP-100356 hydrochloride
  • HY-N6712
    Thiolutin
    4 Publications Verification

    Acetopyrrothin

    		 Antibiotic Bacterial Deubiquitinase NOD-like Receptor (NLR) DNA/RNA Synthesis Pyroptosis HMG-CoA Reductase (HMGCR) Infection Cardiovascular Disease Cancer
    Thiolutin (Acetopyrrothin) is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC50 = 4 μM) and Rpn11 (IC50 = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin-induced cardiotoxicity (DOXIC) [1][2][3][4][5].
    Thiolutin
  • HY-B2004
    Thifluzamide

    		Environmental Pollutants Fungal Mitochondrial Metabolism Infection
    Thifluzamide is a fungicide that inhibits fungal respiration by blocking the ubiquinone-binding site in mitochondrial complex II. Thifluzamide exhibits significant activity against Basidiomycota pathogens (such as Rhizoctonia cerealis, Ustilago and Puccinia genera) and is commonly used in studies on wheat sharp eyespot. Thifluzamide displays a dual mechanism in regulating lipid metabolism: it reduces fatty acid synthase activity to inhibit endogenous fatty acid synthesis, and increases carnitine palmitoyltransferase-I activity to accelerate fatty acid β-oxidation, thereby reducing total cholesterol and triglyceride levels in the liver. Thifluzamide also induces hepatotoxicity in zebrafish models and carries a risk of developmental toxicity. Thifluzamide inhibition of Rhizoctonia cerealis may result in low to moderate levels of drug resistance, leading to the generation of stable drug-resistant mutants .
    Thifluzamide
  • HY-172429
    Enozertinib

    ORIC-114

    		 EGFR Neurological Disease Cancer
    Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
    Enozertinib
  • HY-U00177
    GDP366
    2 Publications Verification

    		 Survivin Cancer
    GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.
    GDP366
  • HY-15838
    ID-8
    5 Publications Verification

    		 DYRK Cancer
    ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs .
    ID-8
  • HY-123538
    GRK2 Inhibitor 1

    		Dopamine Receptor G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a dual GRK2/β-ARK1 inhibitor that induces dopamine (DA) inhibition reversal (DIR). GRK2 Inhibitor 1 can also block serotonin-induced or neurotensin-induced DIR reversal. Note: DIR refers to the phenomenon in which neurons in addiction-related brain pathways become less sensitive to DA inhibition when exposed to moderate concentrations of DA for a long time .
    GRK2 Inhibitor 1
  • HY-175479
    GLPG4970

    		Salt-inducible Kinase (SIK) TNF Receptor Interleukin Related Inflammation/Immunology
    GLPG4970 is a potent, selective and orally active salt-inducible kinase 2/3 (SIK2/SIK3) dual inhibitor with IC50 values of 0.3 nM and 0.7 nM. GLPG4970 has weak inhibition of hERG channel with an IC50 of 29 μM. GLPG4970 can decrease TNFα release and increase IL-10 release GLPG4970 can be used for the researches of inflammation and immunology, such as colitis .
    GLPG4970
  • HY-172429A
    Enozertinib hemihydrate

    ORIC-114 hemihydrate

    		 EGFR Neurological Disease Cancer
    Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
    Enozertinib hemihydrate
  • HY-112293
    GW2974

    		EGFR Cancer
    GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research .
    GW2974
  • HY-178360
    NP1192

    		PROTACs Histone Acetyltransferase HIF/HIF Prolyl-Hydroxylase PD-1/PD-L1 PTEN Metabolic Disease Inflammation/Immunology Cancer
    NP1192 is a potent, selective PROTAC NAT10 degrader that depletes NAT10 protein and inhibits ac4C modification in cancer cells. NP1192 demonstrates dual inhibition of hypoxia-driven glycolysis and immunosuppression via NAT10/HIF-1α/PD-L1 axis disruption, achieving superior antitumor efficacy and synergizing with anti-PD-L1 both in vitro and in vivo. NP1192 can be used for ovarian, cervical, and glioblastoma cancer research. (Blue: CRBN ligand (HY-148834); Black: linker; Pink: NAT10 ligand (HY-16706)) .
    NP1192
  • HY-174366
    JMC14

    		c-Fms PI3K Cancer
    JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC50 values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity .
    JMC14
  • HY-19876
    PL37

    Debio-0827

    		 Opioid Receptor Aminopeptidase Neprilysin Neurological Disease Metabolic Disease
    PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities). PL37 exerts its anti-hyperalgesic effects by activating μ-opioid receptors (µ-opioid receptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain .
    PL37
  • HY-149819
    CDK/HDAC-IN-3

    		HDAC CDK Cancer
    CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .
    CDK/HDAC-IN-3
  • HY-156523
    TNIK&MAP4K4-IN-1

    		MAP4K Cancer
    TNIK&MAP4K4-IN-1 (compound A-39) is a dual inhibitor of TNIK and MAP4K4/HGK with IC50s of 1.29 nM and <10 nM，respectively，in human hepaticstellate cell LX-2. TNIK&MAP4K4-IN-1 can be used for cancer and fibrosis inhibition .
    TNIK&MAP4K4-IN-1
  • HY-155066
    FD274

    		PI3K mTOR Apoptosis Cancer
    FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 arrests HL-60 cell cycle at G1 phase and increases apoptosis. FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
    FD274
  • HY-129496
    NP-313

    		Thrombin Cardiovascular Disease
    NP-313 is a potent antithrombotic agent that inhibits platelet aggregation and activation. NP-313 has dual inhibition of thromboxane A 2 synthesis and selective inhibition of SOCC-mediated Ca 2+ inward flow .
    NP-313
  • HY-179496
    ChE/GSK-3β-IN-1

    		GSK-3 Cholinesterase (ChE) Amyloid-β Neurological Disease
    ChE/GSK-3β-IN-1 (compound 18o) is a potent dual ChE/GSK-3β inhibitor. ChE/GSK-3β-IN-1 exhibits dual inhibition of AChE (IC50 = 1.7 μM), butyrylcholinesterase (BChE) (IC50 = 5.3 μM), and GSK-3β (IC50 = 5.7 μM). ChE/GSK-3β-IN-1 inhibits Aβ1-42 self-aggregation. ChE/GSK-3β-IN-1 can be used for Alzheimer’s disease (AD) research .
    ChE/GSK-3β-IN-1
  • HY-176561
    IOR-160

    		Casein Kinase HDAC Cancer
    IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research .
    IOR-160
  • HY-135447
    BM-531

    		Prostaglandin Receptor Others
    BM-531 is a dual-acting agent for thromboxane receptor (TXA2) antagonism and thromboxane synthase inhibition. BM-531 exerts anti-aggregatory effects on human citrated platelet-rich plasma (PRP), inhibiting Arachidonic acid (HY-109590A)-induced aggregation with an ED100 of 0.125 μM and U-46619 (HY-108566)-induced aggregation with an ED50 of 0.482 μM. BM-531 inhibits high-K +-induced contraction of porcine uterine smooth muscle .
    BM-531
  • HY-120826
    A2AAR/hMAO-B-IN-1

    		Monoamine Oxidase Adenosine Receptor Neurological Disease
    A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC50: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
    A2AAR/hMAO-B-IN-1
  • HY-157290
    HL403

    		Epigenetic Reader Domain Src Cancer
    HL403 is a potent and dual BRD4/Src inhibitor. HL403 has IC50 values of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 shows anti-cancer activity .
    HL403
  • HY-117761
    MHY908

    		PPAR Metabolic Disease Cancer
    MHY908 is a potent dual agonist of PPARα and PPARγ . MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity .
    MHY908
  • HY-161515
    BRD4/NAMPT-IN-1

    		NAMPT Epigenetic Reader Domain Cancer
    BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .
    BRD4/NAMPT-IN-1
  • HY-141864
    ITK/TRKA-IN-1

    		Itk Inflammation/Immunology
    ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC50 value of 1.0 nM and 96 % inhibition, respectively.
    ITK/TRKA-IN-1
  • HY-177081
    Envometinib

    		MEK Cancer
    Envometinib (Compound B) is a dual-MEK inhibitor that works through Deep Cyclic Inhibition (DCI). Envometinib has antitumor activity in various in vivo models. Envometinib can be studied in RAS and RAF mutated cancer such as colorectal cancer and melanoma .
    Envometinib
  • HY-120126
    ML378

    CID71710938; JJH-254

    		 Phospholipase Metabolic Disease
    ML378 (CID71710938) is a dual LYPLA1 and LYPLA2 inhibitor, with IC50s of 122 nM and 245 nM respectively. ML378 also shows potent inhibition of ABHD6 (IC50 = 3.15 nM). ML378 can be used for elucidating the patho/physiological roles of the LYPLA1 and LYPLA2 .
    ML378
  • HY-158763
    MPI8

    TG0205221

    		 SARS-CoV Cathepsin Virus Protease Infection
    MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). MPI8 can be used in clinical studies of COVID-19 .
    MPI8
  • HY-158763A
    MPI8 TFA

    TG0205221 TFA

    		 SARS-CoV Cathepsin Virus Protease Infection
    MPI8 (TG0205221) TFA is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 TFA exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). MPI8 TFA can be used in clinical studies of COVID-19 .
    MPI8 TFA
  • HY-103160B
    EHNA

    		Adenosine Deaminase Phosphodiesterase (PDE) Influenza Virus Infection Cardiovascular Disease Neurological Disease Cancer
    EHNA is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
    EHNA
  • HY-108347A
    CP-100356

    		P-glycoprotein BCRP Metabolic Disease
    CP-100356 is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 is also a weak inhibitor of OATP1B1 (IC50 = ∼66 µM). CP-100356 is devoid of inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM) .
    CP-100356
  • HY-P11004
    A3-APO

    		Bacterial Antibiotic Infection
    A3-APO is an antimicrobial peptide. A3-APO has a significant antimicrobial activity by a dual mode of action with both membrane disintegration and intracellular target inhibition. A3-APO can deactivate bacterial toxins and increase the expression of anti-inflammatory cytokines (such as IL-4 and IL-10), without antimicrobial resistance. A3-APO accelerates burn wounds healing in mice infection model of Acinetobacter baumannii and Staphylococcus aureus .
    A3-APO
  • HY-165478
    FCE 28260

    		5 alpha Reductase Endocrinology
    FCE 28260 is an orally active 4-azacyclic 5α-reductase (5αR) inhibitor. FCE 28260 exhibits IC₅₀ values for human 5αR type 1 and 5αR type 2 of 36 and 3.3 nM, respectively, and for human and rat prostates with IC₅₀ values of 16 and 15 nM, respectively. FCE 28260 simultaneously blocks the production of dihydrotestosterone (DHT) in the prostate and peripheral tissues. FCE 28260 can significantly inhibit the induction of prostatic and seminal vesicle hyperplasia by testosterone (T) in rat models, without inhibiting the growth of the prostate in DHT implantation models. FCE 28260 can be used for the studies DHT-dependent diseases such as benign prostatic hyperplasia (BPH) .
    FCE 28260
  • HY-50878AS
    Crizotinib-d9 hydrochloride

    PF-02341066-d9 hydrochloride

    		 c-Met/HGFR Autophagy Anaplastic lymphoma kinase (ALK) ROS Kinase Isotope-Labeled Compounds Cancer
    Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
    Crizotinib-d9 hydrochloride
  • HY-178441
    PKM2-IN-11

    		Pyruvate Kinase Reactive Oxygen Species (ROS) Apoptosis Microtubule/Tubulin Metabolic Disease Cancer
    PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer .
    PKM2-IN-11
  • HY-169001
    5-HT2A/5-HT2C inverse agonist 1

    		5-HT Receptor Neurological Disease
    5-HT2A/5-HT2C inverse agonist 1 is a potent and dual 5-HT2A and 5-HT2C receptor inverse agonist with a hERG inhibitions, thus avoiding cardiovascular risks. 5-HT2A/5-HT2C inverse agonist 1 shows significant antipsychotic efficacy in the MK-801 (HY-15084B)-induced mouse model. 5-HT2A/5-HT2C inverse agonist 1 is promising for research of psychosis .
    5-HT2A/5-HT2C inverse agonist 1
  • 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-165587
    BM-573

    		Prostaglandin Receptor Cardiovascular Disease
    BM-573 is an orally active dual thromboxane A₂ (TXA₂) modulator with an IC50 of 1.3 nM. BM-573 possesses both thromboxane synthase (TxAS) inhibition and thromboxane receptor (TP) antagonistic effects. BM-573 can completely inhibit platelet aggregation induced by Arachidonic acid (HY-109590) or U-46619 (TXA₂ analogues). BM-573 completely blocks the generation of TXB₂ (the stable metabolite of TXA₂) in human platelets and does not inhibit cyclooxygenase (COX-1/COX-2), thus avoiding interference with other prostaglandin synthesis. BM-573 has an inhibitory effect on U-46619-induced contractions in rat gastric fundus smooth muscle (ED₅₀ = 4.2 μM), but has no effect on contractions caused by PGE₂, PGF₂α, or PGI₂. BM-573 can be used in the study of atherosclerosis, myocardial infarction, pulmonary hypertension and shock .
    BM-573
  • HY-163755
    GPER activator 1

    		Estrogen Receptor/ERR Inflammation/Immunology
    GPER activator 1 (compound 6-26) is a GPER-selective compound without cytotoxicity. GPER activator 1 exhibits dual inhibition of TNFα- and IL-6-induced inflammation .
    GPER activator 1
  • HY-141543
    YW2065

    		β-catenin Cancer
    YW2065 is an Axin-1 stabilizer. Axin-1 is a scaffolding protein that regulates proteasome degradation of β-catenin. YW2065 exhibits anti-colorectal cancer effects via dual activities of wnt/β-catenin signaling inhibition and AMPK activation .
    YW2065
  • HY-162228
    VI-60

    		COX Phospholipase Inflammation/Immunology
    VI-60 is a dual, orally active inhibitor of cPLA2 and COX-2, which reveals an anti-inflammtory efficacy through the inhibition of p38 MAPK/cPLA2/COX-2/PGE2 pathway .
    VI-60
  • HY-160682
    EGFR/HER2-IN-12

    		EGFR Others
    EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant .
    EGFR/HER2-IN-12
  • HY-106720
    Amosulalol

    YM 09538

    		 Adrenergic Receptor Cardiovascular Disease
    Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
    Amosulalol
  • HY-106720A
    Amosulalol hydrochloride

    YM 09538 hydrochloride

    		 Adrenergic Receptor Cardiovascular Disease
    Amosulalol (YM 09538) hydrochloride is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol hydrochloride exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol hydrochloride decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
    Amosulalol hydrochloride
  • HY-121736
    AGI-12026

    AGI-026

    		 Isocitrate Dehydrogenase (IDH) Neurological Disease
    AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
    AGI-12026

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