Search Result
Results for "
Dual targeting
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-122909
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- HY-115870
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- HY-162603
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HDAC
DNA/RNA Synthesis
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Cancer
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HDAC-IN-74 (PA) is a dual HDAC/Rribonucleotide reductase(RR) inhibitor, with IC50 values of 10.80 μM and 9.34 μM for HDAC and HDAC, respectively. HDAC-IN-74 can be used in anticancer research .
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- HY-162908
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- HY-129666
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- HY-157965
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VEGFR
FAK
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Cancer
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ZINC09875266 is a dual inhibitor targeting VEGFR2 and FAK that can be used in cancer research .
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- HY-164296
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ADC Linker
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Cancer
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SMP-96745 is a dual-drug targeting linker-drug conjugate and can be used for study of cancer .
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- HY-168633
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Bombesin Receptor
PSMA
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Cancer
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PSMA/GRPR ligand 1 (compound 3 ) is a bispecific PSMA/GRPR ligand that shows dual targeting for PSMA(+) and GRPR(+) tumors .
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- HY-162952
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Bcr-Abl
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Cancer
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cSRC/BCR-ABL1-IN-1 (compund 16a) is a dual-target cSRC/BCR-ABL1 kinase inhibitor .
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- HY-P10327
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GLP Receptor
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Metabolic Disease
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PP18 is a novel OXM-based dual GLP-1 and glucagon receptor agonist with EC50 values of 0.487 nM target hGLP-1R and 0.188 nM target hGcgR .
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- HY-141486A
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- HY-144300
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TNP-2198
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Bacterial
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Infection
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Rifasutenizol (TNP-2198) is a dual-targeted antibacterial agent that has a good antibacterial effect on Helicobacter pylori infection. Rifasutenizol can be used in the study of microaerophilic and anaerobic bacterial infections .
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- HY-126320
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EGFR
c-Met/HGFR
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Cancer
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EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC .
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- HY-10725
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Factor Xa
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Cardiovascular Disease
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Tanogitran is a dual inhibitor targeting Factor Xa and thrombin (thrombin), with Ki values of 26 and 2.7 nM, respectively. Tanogitran exhibits anticoagulant activity and can be used for research in thrombotic diseases .
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- HY-P99852
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ABT165; PR1283233
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VEGFR
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Cancer
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Dilpacimab (ABT165) is a potent dual-variable domain immunoglobulin, targets both delta-like ligand 4 (DLL4) and VEGF pathways.. Dilpacimab can be used in research of cancer .
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- HY-D2280
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HDAC
Estrogen Receptor/ERR
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Others
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Estrogen receptor β/HDAC probe 1 (compound P1) is a near-infrared fluorescent probe that dual-targets the estrogen receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC .
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- HY-P99572
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BNT-312; DuoBody-CD40x-4-1BB; GEN1042
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TNF Receptor
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Inflammation/Immunology
Cancer
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Tecaginlimab (BNT-312) is a Fc-inert bispecific antibody for dual targeting and conditional stimulation of CD40 and 4-1BB. Tecaginlimab can enhance priming and reactivation of tumor-specific immunity .
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- HY-161457
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- HY-172699A
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Liposome
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Cancer
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DSPE-PEG3400-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG3400-ANG can be used for drug delivery .
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- HY-172698
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Liposome
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Cancer
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DSPE-PEG1000-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG1000-ANG can be used for drug delivery .
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- HY-172699
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Liposome
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Cancer
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DSPE-PEG2000-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG2000-ANG can be used for drug delivery .
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- HY-172700
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Liposome
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Cancer
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DSPE-PEG5000-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG5000-ANG can be used for drug delivery .
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- HY-163680
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Estrogen Receptor/ERR
Cytochrome P450
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Cancer
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ERα degrader 9 is a dual targeting ligand for estrogen receptor α (ERα) and aromatase (ARO). ERα degrader 9 can be utilized for synthesis of PROTAC ERα Degrader-9 (HY-163679) .
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- HY-P99166
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PD-1/PD-L1
CTLA-4
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Inflammation/Immunology
Cancer
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Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .
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- HY-161145
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EGFR
Apoptosis
Microtubule/Tubulin
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Cancer
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EGFR/microtubule-IN-1 (Compound 10c) is a dual inhibitor targeting EGFR and tubulin. The IC50 for inhibiting EGFR is 10.66 nM. EGFR/microtubule-IN-1 can reduce the phosphorylation levels of EGFR, AKT and ERK, hinder tubulin polymerization, and induce apoptosis .
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- HY-173641
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Molecular Glues
Histone Acetyltransferase
BCL6
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Cancer
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MNN-02-155 is a bivalent molecular glue with with dual binding to p300/CBP and BCL6. MNN-02-155 induces potent activation of the BCL6-target reporter gene and cell death. MNN-02-155 can be used for the study of diffuse large B cell lymphomas (DLBCLs) .
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- HY-147025
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PROTACs
TGF-beta/Smad
HIF/HIF Prolyl-Hydroxylase
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Inflammation/Immunology
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(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine has a multi-path anti-fibrosis function and a renal protection function for research of renal anemia .
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- HY-106056
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D 16726
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Estrogen Receptor/ERR
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Cancer
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Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
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- HY-145428
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Notch
γ-secretase
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Cancer
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BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression .
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- HY-160528
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Molecular Glues
Epigenetic Reader Domain
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Cancer
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IBG3 is a dual-JQ1-containing BET molecular glue degrader that targets protein degradation via intramolecular bivalent glues. IBG3 is a BRD2 and BRD4 bifunctional degrader with DC50 values of 8.6 pM and 6.7 pM, respectively .
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- HY-P99714
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MGD019
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PD-1/PD-L1
CTLA-4
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Cancer
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Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART). Lorigerlimab can block PD-1 and CTLA-4, and improves T-cell responses. Lorigerlimab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
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- HY-162143
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SphK
Akt
mTOR
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Cancer
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SKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells .
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- HY-155672
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5-HT Receptor
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Neurological Disease
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JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
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- HY-146160
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PARP
HDAC
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Cancer
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PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities .
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- HY-144825
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Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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Chol-CTPP is a ligand with dual targeting effect on blood-brain barrier (BBB) and glioma cells. Lip-CTPP can be gained by Chol-CTPP and another mitochondria targeting ligand (Chol-TPP). Lip-CTPP is a promising potential carrier to exert the anti-glioma effect of doxorubicin (DOX) and lonidamine (LND) collaboratively. Lip-CTPP elevates the inhibition rate of tumor cell proliferation, migration and invasion, promote apoptosis and necrosis, and interfere with mitochondrial function .
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- HY-P99623
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MGD006; S80880
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CD3
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Cancer
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Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
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- HY-162519
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LZ90
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NAMPT
PD-1/PD-L1
Apoptosis
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Metabolic Disease
Inflammation/Immunology
Cancer
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LZFPN-90 (LZ90) is a dual NAMPT/PD-L1 targeting compound. LZFPN-90 inhibits PD-1/PD-L1 interaction and NAMPT activity. LZFPN-90 inhibits cell growth in a NAMPT-dependent manner and blocks the cell cycle, subsequently inducing apoptosis. LZFPN-90 exerted target-dependent antitumor activities, affecting metabolic processes and the immune system .
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- HY-150755
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- HY-163537
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Cholinesterase (ChE)
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Neurological Disease
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AChE/BuChE-IN-5 (compound 5a) is a dual target inhibitor. AChE/BuChE-IN-5 has excellent nanomolar inhibitory activity on acetylcholinesterase (AChE) (IC50=46.9 nM) and butyryl cholinesterase (BuChE) (IC50=3.5 nM). AChE/BuChE-IN-5 can be used for Alzheimer's Disease research .
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- HY-162349
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HDAC
PARP
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Cancer
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PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits different subtypes of PARPs and HDACs with IC50s of 83.3 nM (PARP1), 3.1 nM (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM respectively. (HDAC6) . br/ .
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- HY-12680
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PRN694
1 Publications Verification
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Itk
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Inflammation/Immunology
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PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo .
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- HY-144315
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Snail/HDAC-IN-1
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HDAC
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Cancer
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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 .
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- HY-P10740
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Peptide-Drug Conjugates (PDCs)
Antifolate
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Cancer
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CBP-1018 is a PDC (peptide drug conjugate) consisting of a dual targeting FRα/prostate-specific membrane antigen (PSMA) ligand (blue part) coupled to Monomethyl auristatin E (HY-15162) (red part) via a linker (HY-78738) (black part). CBP-1018 is expected to be used in breast cancer research .
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- HY-168475
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Apoptosis
WDR5
HDAC
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Cancer
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DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. DD0-2363 inhibits cells proliferation and induces apoptosis in acute myeloid leukemia cells. DD0-2363 has antitumor activity and can be used in the research of acute myeloid leukemia .
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- HY-173081
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SARS-CoV
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Infection
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4"-(2-(p-Chlorophenyl)acetoxyl)spiramycin (Compound 2d) is a broad-spectrum anti-coronaviral agent via targeting frameshifting element (FSE). 4"-(2-(p-Chlorophenyl)acetoxyl)spiramycin inhibits HCoV-OC43 and HCoV-229E with EC50 values of 0.85 μM and 1.45 μM. 4"-(2-(p-Chlorophenyl)acetoxyl)spiramycin shows a dual-target mechanism that acts on both viral FSE RNA and host DIS3L2 .
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- HY-158627
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5-HT Receptor
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Others
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JPC0323 Oleate is a derivative of JPC0323 (HY-155672). JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
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- HY-164233
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PROTACs
HDAC
Apoptosis
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Cancer
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YX968 is a potent and selective HDAC3/8 PROTAC dual degrader with DC50 values of 1.7 and 6.8 nM. YX968 exhibits antitumor activity by promoting apoptosis .(Pink: Target protein ligand (HY-168287); Black: linker (HY-W007700); Blue: E3 ligase ligand (HY-112078))
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- HY-145406
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Adenosine Receptor
HDAC
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Inflammation/Immunology
Cancer
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IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
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- HY-137561A
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PLN-74809 hydrochloride
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Integrin
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Inflammation/Immunology
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Bexotegrast hydrochloride (PLN-74809 hydrochloride) is a small molecule dual selective inhibitor with activity targeting αVβ1 and αVβ6. Bexotegrast hydrochloride is used for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). Bexotegrast hydrochloride inhibits the activation of TGF-β1 by blocking the function of these integrins, thereby preventing the growth of fibrous tissue in the lungs and bile ducts .
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- HY-171027
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Ligands for Target Protein for PROTAC
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Cancer
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PTP1B/TC-PTP IN-1 is a PTP1B and TC-PTP dual inhibitor. PTP1B/TC-PTP IN-1 can be used as a target protein ligand for the synthesis of DU-14 (PTP1B/TC-PTP PROTAC) (HY-164864) .
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- HY-160557
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Epigenetic Reader Domain
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Cancer
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PLK1/BRD4-IN-2 (compound 15) is a BI-2536 (HY-50698) analog and dual inhibitor that targets both Polo-like kinase 1 (PLK1) and BRD4bromodomain (BRD4-BD1 IC50=28 nM, PLK1 IC50=40 nM) .
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- HY-128171
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FLAP
Epoxide Hydrolase
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Inflammation/Immunology
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Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s?of? 30 and 170?nM, respectively, and suppressed the activity of isolated sEH (IC50=20?nM) .
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- HY-149734
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Bacterial
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Infection
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MA220607 is an antibacterial agent with low hemolytic toxicity and a dual-target mechanism of action (MOA). MA220607 promotes FtsZ protein polymerization, also increases the permeability of bacterial membranes and inhibits biofilm formation. The resistance rate of MA220607 is low, and the MICs against Gram-positive bacteria and Gram-negative bacteria are Table 0.062-2 μg/mL and 0.5-4 μg/mL, respectively) .
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- HY-162312
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Deubiquitinase
Apoptosis
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Cancer
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LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
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- HY-168554
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PROTACs
STING
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Inflammation/Immunology
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STING-IN-10 (P8) is a dual STING PROTAC degrader and inhibitor with a DC50 value of 2.58 μM in THP-1 cells. STING-IN-10 has anti-inflammatory activity .(Pink: Target protein ligand (HY-168676); Black: linker (HY-W123015); Blue: E3 ligase ligand (HY-126457))
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- HY-163439
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Amylases
Glycosidase
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Metabolic Disease
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α-Amylase/α-Glucosidase-IN-12 (compound 10k) is a dual inhibitor targeting α-glucosidase and α-amylase with IC50 of 34.52 nM and 24.62 nM, respectively. α-Amylase/α-Glucosidase-IN-12 is an inhibitor designed based on triazolo[4,3-b][1,2,4]triazine and has the potential to be used in diabetes research .
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- HY-111313
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Cholecystokinin Receptor
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Metabolic Disease
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JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease .
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- HY-120826
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Monoamine Oxidase
Adenosine Receptor
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Neurological Disease
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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) .
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- HY-126249
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Aurora Kinase
Polo-like Kinase (PLK)
Apoptosis
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Cancer
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AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3 Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM .
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- HY-162803
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Apoptosis
c-Met/HGFR
STAT
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Cancer
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c-Met-IN-24 (compound 3g) is a dual-target inhibitor of STAT-3 ( =4.7 μM) and c-MET ( =12.67 μM) with anticancer activity. c-Met-IN-24 arrests the G2/M cell cycle and induces apoptosis in SNB-75 cells. c-Met-IN-24 can be used in the study of central nervous system cancers .
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- HY-138215
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ERK
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Cancer
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ADTL-EI1712 is a potent, orally active, and selective dual-target inhibitor of ERK1 and ERK5, inhibition rates of ERK1/5 at 1 μM are 93.54% and 89.35%, respectively. ADTL-EI1712 can induce regulated cell death, a form of cell death that relies on the activation of genetically encoded machinery, to overcome compensatory mechanism in specific cancer cells in vitro and in vivo .
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- HY-157480
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EGFR
Aurora Kinase
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Cancer
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EGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of L858R EGFR and AURKB with IC50s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research .
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- HY-164455
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STAT
JAK
Aurora Kinase
Mitosis
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Inflammation/Immunology
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AJI-214 is a dual-target inhibitor of Aurora kinase A and JAK2. AJI-214 directly blocks Aurora kinase A to inhibit T cell mitotic progression and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-214 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
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- HY-168968S
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EGFR
Histone Demethylase
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Cancer
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ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
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- HY-159484
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HSP
Guanylate Cyclase
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Cardiovascular Disease
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Hsp110/sGC-modulator-1 (compound 17i), an orally active Hsp110/sGC dual-target regulator, exhibits optimal Hsp110 and sGC molecular activities as well as remarkable cell malignant phenotypes inhibitory and vasodilatory effects. Hsp110/sGC-modulator-1 (compound 17i) attenuates pulmonary vascular remodeling and right ventricular hypertrophy via Hsp110 suppression .
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- HY-174130
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Parasite
PI4K
PKG
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Infection
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PI4Kβ/PKG-IN-1 (Compound 19) is an orally active dual inhibitor targeting Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). PI4Kβ/PKG-IN-1 exhibits potent antiplasmodial activity. PI4Kβ/PKG-IN-1 is promising for research of malaria .
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- HY-161083
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PARP
Histone Methyltransferase
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Cancer
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PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
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- HY-17444
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PPAR
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Metabolic Disease
Cancer
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Tesaglitazar is a dual-target PPARα/γ agonist with an EC50 of 13.4 μM for rat PPARα and 3.6 μM for human PPARα. Tesaglitazar affects lipid and glucose metabolism by activating PPARα and PPARγ receptors, and has the potential to improve blood sugar and relieve pain. Tesaglitazar can be used to induce in vivo tumor models and can be used in the study of type 2 diabetes, dyslipidemia, and neuropathic pain .
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- HY-169212
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PI3K
Annexin A
ERK
VEGFR
STAT
Raf
FAK
Akt
Ras
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Cancer
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I194496 is a potent cystathionine γ-lyase (CSE) inhibitor, with an IC50 of 0.79 mM. I194496 can inhibit the growth of human TNBC cells via the dual targeting PI3K/Akt and Ras/Raf/ERK pathway and suppress the metastasis of human TNBC cells via down-regulating Anxa2/STAT3 and VEGF/FAK/Paxillin signaling pathways .
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- HY-113289
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Akt
Androgen Receptor
Bacterial
Drug Metabolite
HSV
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
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Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
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- HY-172827
-
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PROTACs
Epigenetic Reader Domain
|
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PROTAC BRD4 degrader-30 is an ISOX-DUAL-Based PROTAC degrader selectively targeting BRD4 (IC50 = 65 nM). PROTAC BRD4 degrader-30 can be used for research of c-Myc oncoprotein and cancer cell pathophysiology. (Pink: BRD4 ligand (HY-172828); Blue: CRBN ligand (HY-103596); Black: linker (HY-Y0139); CRBN ligand+linker: HY-138847) .
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- HY-162601
-
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Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
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Cancer
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D-01 is a dual-targeting inhibitor of HIF-1α and EZH2 (IC50: 4.86 μM and 0.99 μM respectively). D-01 inhibits the expression of H3K27me3 protein. D-01 inhibits the migration, clone and the invasion of A549 cells, and also inhibits tube formation of HUVECs. D-01 can be used for research of lung cancer .
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- HY-112440
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Methuosis inducer 1
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Others
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Cancer
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HZX-02-059 is a potent methuosis inducer and dual-target PIKfyve/tubulin inhibitor with anticancer activity. Methuosis mainly disrupts the balance of endocytosis and exocytosis, forming a large number of vesicles and inducing cell death. HZX-02-059 also induces cell vacuolization, promotes apoptosis, downregulates the p53 pathway, inhibits PI3K/AKT phosphorylation, and inhibits c-Myc and NF-κB transcription .
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- HY-158328A
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-
- HY-169509
-
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PARP
Necroptosis
Topoisomerase
RIP kinase
Mixed Lineage Kinase
|
Cancer
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Topoisomerase I/II Inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of Topoisomerase I/II, capable of inducing DNA damage and PARP-1 activation, which subsequently leads to the activation of RIPK1, RIPK3, and MLKL, ultimately triggering necroptosis. Topoisomerase I/II Inhibitor 8 demonstrates remarkable anticancer activity by effectively targeting the nuclei of cancer cells and inducing cell death through necroptosis, showing great clinical potential in circumventing drug resistance in cancer treatment .
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- HY-163006
-
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EGFR
c-Met/HGFR
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Cancer
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EGFR/c-Met-IN-1 (compound TS-41) is a dual-target inhibitor of EGFR/c-Met. The IC50 for inhibiting EGFR L858R and c-Met is 68.1 nM and 0.26 nM respectively. . EGFR/c-Met-IN-1 induces apoptosis and cell cycle arrest in A549-P cells, downregulating the phosphorylation of EGFR, c-Met, and downstream AKT. EGFR/c-Met-IN-1 inhibits tumor growth in vitro and in vivo .
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- HY-148521
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CDK
FLT3
PROTACs
Apoptosis
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Cancer
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PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML .
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- HY-164454
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Aurora Kinase
STAT
JAK
Mitosis
|
Inflammation/Immunology
|
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AJI-100 is a dual-target inhibitor of Aurora kinase A and JAK2 with IC50 values of 12.7 nM and 18.5 nM, respectively. AJI-100 directly blocks Aurora kinase A to inhibit T cell mitosis and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-100 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
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- HY-149283
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JAK
HDAC
Apoptosis
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Cancer
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JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .
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- HY-P10762
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LDC 10B
|
Peptide-Drug Conjugates (PDCs)
Folate Receptor (FR)
TRP Channel
|
Cancer
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CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) conjugated to MMAE (HY-15162), targeting Folate receptor α (FRα) and TRPV6. CBP-1008 binds to FRα with high affinity and TRPV6 with low affinity. CBP-1008 has antitumor activity, and can be used in advanced solid tumor research (eg: colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma and follicular dendritic cell sarcoma) .
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- HY-159513
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Bcl-2 Family
Apoptosis
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Cancer
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Bcl-2/Mcl-1-IN-4 (compound 20) is a dual inhibitor targeting Bcl-2 (Ki=0.49 μM) and Mcl-1 (Ki=0.51 μM). Bcl-2/Mcl-1-IN-4 significantly inhibits cancer cell proliferation and effectively induces apoptosis in U937 cells. Bcl-2/Mcl-1-IN-4 can be used in cancer research .
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-
- HY-14863
-
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CTA-018
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VD/VDR
Cytochrome P450
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Others
Endocrinology
|
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Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
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-
- HY-170793
-
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PD-1/PD-L1
VISTA
|
Cancer
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PD-L1/VISTA-IN-1 (Compound P17) is an orally active dual-target inhibitor of PD-L1 and VISTA. PD-L1/VISTA-IN-1 can block the PD-1/PD-L1 interaction (IC50: 0.1492 μM) and the VISTA pathway (KD: 0.2723 μM), thereby reactivating T cells. PD-L1/VISTA-IN-1 has anti-tumor activity .
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- HY-151263
-
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HDAC
G-quadruplex
|
Cancer
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|
G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer .
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-
- HY-116191
-
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PI3K
mTOR
|
Cancer
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WJD008 is a potent dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers .
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-
- HY-174221
-
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IMPDH
HDAC
Apoptosis
|
Cancer
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|
IMPDH II/HDAC1-IN-1 (Compound C12) is an orally active dual-target inhibitor of IMPDH II and IMPDH II (IC50 values are 84.69 nM and 81.75 nM, respectively). IMPDH II/HDAC1-IN-1 has significant anti-tumor activity and has an anti-proliferative effect on K-562 cells (IC50 = 305.31 nM). IMPDH II/HDAC1-IN-1 exerts a synergistic anti-tumor effect by simultaneously targeting IMPDH II and HDAC1, inhibiting tumor cell proliferation and inducing apoptosis. IMPDH II/HDAC1-IN-1 can be used in the study of cancers such as chronic myeloid leukemia (CML) .
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-
- HY-149617
-
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Cytochrome P450
PD-1/PD-L1
|
Infection
|
|
CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target (CYP51/PD-L1) inhibitor, with IC50 values of 0.17 and 0.021 μM, respectively. CYP51/PD-L1-IN-4 exhibits excellent antifungal and antidrug-resistant fungal activity in vitro. CYP51/PD-L1-IN-4 can be used for fungal infections research .
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-
- HY-172919
-
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Phosphodiesterase (PDE)
NAMPT
Apoptosis
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Cancer
|
|
PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC50=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD +), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer .
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-
- HY-172617
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BMI1
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
APD-94 is a dual inhibitor targeting tubulin and Bmi-1. APD-94 interfers tubulin normal polymerization. APD-94 suppresses the expression of Bmi-1. APD-94 causes cell cycle arrest at the G2/M phase in cancer cells and induces apoptosis, thus inhibiting cancer cell proliferation. APD-94 represses the growth of HT29 cell xenografts in NOD/SCID mice. APD-94 can be used for colorectal cancer study .
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-
- HY-117688
-
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HDAC
Topoisomerase
Apoptosis
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Cancer
|
|
WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cell cycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer .
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-
- HY-163786
-
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PROTACs
CDK
Apoptosis
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Cancer
|
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PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cell cycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984))
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-
- HY-162606
-
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Monoamine Oxidase
Cholinesterase (ChE)
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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 .
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-
- HY-163105
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Microtubule/Tubulin
|
Cancer
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|
Tubulin/NEDDylation-IN-1 (compound C11) is a dual inhibitor of tubulin (Microtubule/Tubulin)-NEDDylation (IC50 for tubulin=2.40 μM), which has strong anti-proliferative activity. Neddylation is a protein post-translational modification that covalently tags the ubiquitin-like protein NEDD8 to target proteins. Tubulin/NEDDylation-IN-1 forms hydrogen bonds with residues of tubulin and E1 NEDD8 activating enzyme (NAE) through methoxy and dithiocarbamate groups and inhibits NEDDylation and microtubulin in an ATP-dependent manner. tube polymerization .
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-
- HY-160481
-
|
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Tau Protein
MicroRNA
|
Neurological Disease
|
|
MG-1102 is first-in-class dual binder of monomeric tau and pre-miRNA-146a. MG-1102 shows specific inhibition of miRNA146a with IC50s of 0.21 mM and 0.36 mM specific inhibition of doublelabeled pre-miRNA146a and mono-labeled pre-miRNA146a, respectively. MG-1102 interacts with tau monomers with a Kd of 3.21 mM by surface plasmon resonance (SPR). MG-1102 is a potential multi-target-directed ligands (MTDLs) for Alzheimer’s disease (AD) .
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-
- HY-176165
-
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CDK
Histone Methyltransferase
|
Cancer
|
|
CDK9/EZH2-IN-1 (Compound D16) is a CDK9/EZH2 dual-target inhibitor (IC50: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC50 values are 136.3, 171.3 and 315.7 nM, respectively) .
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-
- HY-156094
-
|
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
|
JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HDAC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion .
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-
- HY-170347
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4 degrader-36 (Compound 29) is an effective dual degrader of SMARCA2/4,with DC50 values of 0.22 nM and 0.85 nM for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2/4 degrader-36 has anti-cell proliferation activity (Pink: Target Protein Ligand (HY-170354); Black: Linker (HY-W895794); Blue: E3 Ligase Ligand (HY-170353); E3 Ligase Ligand-Linker Conjugate (HY-170356)) .
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-
- HY-152254
-
|
|
FAAH
Cannabinoid Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection .
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-
- HY-152253
-
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FAAH
Cannabinoid Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-2 are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection .
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-
- HY-170947
-
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STAT
Quinone Reductase
|
Cancer
|
|
Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
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-
- HY-159078
-
|
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DNA/RNA Synthesis
|
Cancer
|
|
PolQi1 is a selective inhibitor targeting the Polθ domain of DNA polymerase. PolQi1 inhibits the Polθ-mediated microhomology end joining (TMEJ/alt-EJ) pathway, reducing insertion/deletion (Indels) and imprecise editing events during DNA repair. PolQi1 can enhance the efficiency and accuracy of homology-directed repair (HDR) or Prime editing, and reduce off-target effects; and in combination with DNA-PK inhibitor AZD-7648 (HY-111783), exert efficient genome editing capabilities with dual pathway regulation. PolQi1 can be mainly used in gene editing research (such as CRISPR-Cas9 or Prime editing system optimization) to improve the precision editing efficiency of difficult-to-edit cells (such as primary hepatocytes and mouse embryos) .
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-
- HY-170779
-
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FAP
|
Cancer
|
|
DOTA-NI-FAPI-04 is a FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention capabilities. DOTA-NI-FAPI-04 chelates metallic isotopes (such as 68Ga and 177Lu) through DOTA to produce radioactive probes ([ 68Ga]Ga/DOTA-NI-FAPI-04 and [ 177Lu]Lu/DOTA-NI-FAPI-04), which can be used for research in tumor diagnostics and therapeutic agents. DOTA-NI-FAPI-04 holds dual targeting potential in the fields of cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly suitable for scenarios where the tumor stroma and hypoxic regions synergistically interact .
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-
- HY-162319
-
|
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Apoptosis
HDAC
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity .
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-
- HY-145260
-
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Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
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-
- HY-170651
-
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CDK
HDAC
Apoptosis
|
Cancer
|
|
CDK4/6/HDAC-IN-1 (Compound N14) is a dual-targeting inhibitor of CDK4/6 and HDAC (IC50: CDK4 = 7.23 nM, CDK6 = 13.20 nM, HDAC1 = 55.66 nM, HDAC6 = 48.38 nM). CDK4/6/HDAC-IN-1 induces cell Apoptosis and G0/G1 phase arrest through HDAC-p21-CDK signaling pathway. CDK4/6/HDAC-IN-1 inhibits hepatocellular carcinoma .
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-
- HY-155222
-
|
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Epigenetic Reader Domain
HDAC
|
Cancer
|
|
TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026) .
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- HY-161410
-
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PROTACs
Apoptosis
Bcl-2 Family
|
Cancer
|
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WH244 is a second generation BCL-2 and BCL-xL dual depressant (PROTAC). The primary activity of WH244 is the specific degradation of BCL-2 and BCL-xL proteins (BCL-xL: DC50=0.6 nM, BCL-2: DC50=7.4 nM). WH244 promotes their ubiquitination and subsequent proteasome degradation by targeting these proteins, thereby restoring the cell's apoptosis pathway. WH244 has good antitumor activity. (Pink: BCL-2/BCL-xL ligand (HY-161415); Blue: E3 ligase ligand (HY-112078); Black: linker) .
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-
- HY-W023758
-
|
4-(4-Bromo-1H-pyrazol-5-yl)pyridine
|
DNA/RNA Synthesis
|
Cancer
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|
HDGFRP2/PSIP1-IN-1 (compound BPP) is a dual inhibitor targeting the PWWP domain of hepatocarcinogenic growth factor-related protein 2 (HDGFRP2) and its homologous protein PSIP1, hinder the development and progression of diffuse intrinsic pontine glioma (DIPG). HDGFRP2/PSIP1-IN-1 binds to HDGFRP2 with a Kd value of 7 μM and a ligand efficiency of 0.47; it binds to the PSIP1 PWWP domain with a Kd value of 27 μM; meanwhile, it has a Kd value of 14 μM for HDGFRP3, indicating its effectiveness as an inhibitor of the HDGFRP2 PWWP subfamily .
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-
- HY-155227S
-
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Isotope-Labeled Compounds
EGFR
Anaplastic lymphoma kinase (ALK)
BRK
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC50 of 1.08 nM for EGFR and an IC50 of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment
|
-
- HY-P99573
-
|
MGD-013
|
LAG-3
|
Inflammation/Immunology
Cancer
|
|
Tebotelimab (MGD-013) is a humanized IgG4κ bispecific PD-1/LAG-3 dual-affinity re-targeting (DART) antibody. Tebotelimab binds cell-surface expressed PD-1 and LAG-3 with EC50s of 1.65 nM and 0.41 nM in NS0 cells, respectively. Tebotelimab blocks PD-1/PD-L1, PD-1/PD-L2 and LAG-3/HLA (MHC-II) interactions and PD-1 signaling. Tebotelimab restores exhausted T-cell responses and and enhances antitumour immunity .
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-
- HY-149209
-
|
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PROTACs
CDK
STAT
Early 2 Factor (E2F)
|
Cancer
|
|
LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
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-
- HY-173280
-
|
CHNQD-01228
|
Arf Family GTPase
BMX Kinase
|
Cancer
|
|
Brefeldin A 4-O-nicotinate (CHNQD-01228) is a dual inhibitor of Arf1 and BMX proteins. The IC50 value for the proliferation of T24 cells is 0.22 μM. It can also dose-dependently inhibit the migration and colony formation of T24 cells, induce G1 phase arrest and trigger Apoptosis. Brefeldin A 4-O-nicotinate exerts its anti-cancer activity by targeting the BMX protein to inhibit the AKT/p-AKT and STAT3/p-STAT3 signaling pathways, as well as by inhibiting the Arf1 protein to eliminate bladder cancer stem cells and activate anti-tumor immunity. Brefeldin A 4-O-nicotinate can be used in the research related to bladder cancer .
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-
- HY-158310
-
|
|
SOS1
EGFR
Ras
|
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) .
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-
- HY-121856
-
|
|
Others
|
Inflammation/Immunology
|
|
Flumizole, a derivative of substituted 5,6-diaryl-2,3-dihydroimidazo[2,1-b]thiazoles, was synthesized and evaluated for its immunoregulatory and anti-inflammatory properties in animal models such as rat adjuvant-induced arthritis and mouse oxazolone-induced contact sensitivity assays. This compound class combines structural elements from flumizole and levamisole, aiming to enhance therapeutic efficacy. Symmetrically substituted 5,6-diaryl compounds with specific alkyl heteroatom or halogen substitutions showed optimal potency in the arthritis model. However, variations in activity were less consistent in the contact sensitivity assay. Flumizole and related compounds demonstrate potential as dual-action agents, targeting inflammation and immune modulation, offering promise for therapeutic development in immune-related disorders .
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-
- HY-159519
-
|
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Apoptosis
EGFR
|
Cancer
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EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
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- HY-164445
-
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STAT
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Cancer
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STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
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- HY-159510
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Apoptosis
VEGFR
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
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Cancer
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VEGFR-2-IN-51 (compound 19) is an orally active dual-target inhibitor of VEGFR-2 (IC50=15.33 μM) and tubulin (IC50=0.76 μM) with anti-tumor activity. VEGFR-2-IN-51 induces tumor cell apoptosis by reducing mitochondrial membrane potential and increasing reactive oxygen species (ROS) levels. VEGFR-2-IN-51 exerts anti-angiogenic effects by blocking the VEGFR-2/PI3K/AKT signaling pathway. In addition, VEGFR-2-IN-51 has significant anti-proliferative activity against the gastric cancer cell line MGC-803 (IC50=0.005 μM) .
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- HY-172878
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Small Interfering RNA (siRNA)
HDAC
Apoptosis
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Cancer
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HDAC/PSMD14-IN-1 (Compound 8B) is a thiolutin derivative. HDAC/PSMD14-IN-1 is a orally active dual-target inhibitor of PSMD14/HDAC1 (IC50 238.7 nM/141.2 nM, respectively). HDAC/PSMD14-IN-1 has good cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). HDAC/PSMD14-IN-1 can induce apoptosis. HDAC/PSMD14-IN-1 has anti-tumor activity in a KYSE30 cell mouse xenograft model. HDAC/PSMD14-IN-1 can be used in anti-esophageal cancer research .
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- HY-163679
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Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
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Cancer
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PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
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- HY-117947
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Histone Methyltransferase
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Cancer
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(R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
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- HY-172892
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PI3K
Reactive Oxygen Species (ROS)
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Cancer
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PI3K-IN-59 (Compound 3d) is a PI3K inhibitor (IC50: 17.44 μM). PI3K-IN-59 has significant antiproliferative activity and exhibits potent inhibitory effects on breast cancer 4T1 cells (IC50: 3.70 μM) and colon cancer CT26 cells (IC50: 1.98 μM) as well as human breast cancer cells (IC50: 19.72 μM). PI3K-IN-59 exerts a dual anti-tumor mechanism by inhibiting PI3Kα enzymatic activity and triggering the Fenton reaction to generate hydroxyl radicals (•OH). PI3K-IN-59 shows promising anti-4T1 tumor effects and is suitable for synergistic targeting studies in breast and colon cancers .
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| Cat. No. |
Product Name |
Type |
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- HY-D2280
-
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Fluorescent Dyes/Probes
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Estrogen receptor β/HDAC probe 1 (compound P1) is a near-infrared fluorescent probe that dual-targets the estrogen receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC .
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| Cat. No. |
Product Name |
Type |
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- HY-172699A
-
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Drug Delivery
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DSPE-PEG3400-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG3400-ANG can be used for drug delivery .
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- HY-172698
-
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Drug Delivery
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DSPE-PEG1000-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG1000-ANG can be used for drug delivery .
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- HY-172699
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Drug Delivery
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DSPE-PEG2000-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG2000-ANG can be used for drug delivery .
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- HY-172700
-
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Drug Delivery
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DSPE-PEG5000-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG5000-ANG can be used for drug delivery .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10327
-
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GLP Receptor
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Metabolic Disease
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PP18 is a novel OXM-based dual GLP-1 and glucagon receptor agonist with EC50 values of 0.487 nM target hGLP-1R and 0.188 nM target hGcgR .
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- HY-P10740
-
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Peptide-Drug Conjugates (PDCs)
Antifolate
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Cancer
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CBP-1018 is a PDC (peptide drug conjugate) consisting of a dual targeting FRα/prostate-specific membrane antigen (PSMA) ligand (blue part) coupled to Monomethyl auristatin E (HY-15162) (red part) via a linker (HY-78738) (black part). CBP-1018 is expected to be used in breast cancer research .
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- HY-P10762
-
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LDC 10B
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Peptide-Drug Conjugates (PDCs)
Folate Receptor (FR)
TRP Channel
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Cancer
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CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) conjugated to MMAE (HY-15162), targeting Folate receptor α (FRα) and TRPV6. CBP-1008 binds to FRα with high affinity and TRPV6 with low affinity. CBP-1008 has antitumor activity, and can be used in advanced solid tumor research (eg: colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma and follicular dendritic cell sarcoma) .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99852
-
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ABT165; PR1283233
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VEGFR
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Cancer
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Dilpacimab (ABT165) is a potent dual-variable domain immunoglobulin, targets both delta-like ligand 4 (DLL4) and VEGF pathways.. Dilpacimab can be used in research of cancer .
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- HY-P99572
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BNT-312; DuoBody-CD40x-4-1BB; GEN1042
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TNF Receptor
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Inflammation/Immunology
Cancer
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Tecaginlimab (BNT-312) is a Fc-inert bispecific antibody for dual targeting and conditional stimulation of CD40 and 4-1BB. Tecaginlimab can enhance priming and reactivation of tumor-specific immunity .
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- HY-P99166
-
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PD-1/PD-L1
CTLA-4
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Inflammation/Immunology
Cancer
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Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .
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- HY-P99714
-
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MGD019
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PD-1/PD-L1
CTLA-4
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Cancer
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Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART). Lorigerlimab can block PD-1 and CTLA-4, and improves T-cell responses. Lorigerlimab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
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- HY-P99623
-
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MGD006; S80880
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CD3
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Cancer
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Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
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- HY-P99573
-
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MGD-013
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LAG-3
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Inflammation/Immunology
Cancer
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Tebotelimab (MGD-013) is a humanized IgG4κ bispecific PD-1/LAG-3 dual-affinity re-targeting (DART) antibody. Tebotelimab binds cell-surface expressed PD-1 and LAG-3 with EC50s of 1.65 nM and 0.41 nM in NS0 cells, respectively. Tebotelimab blocks PD-1/PD-L1, PD-1/PD-L2 and LAG-3/HLA (MHC-II) interactions and PD-1 signaling. Tebotelimab restores exhausted T-cell responses and and enhances antitumour immunity .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-168968S
-
|
|
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ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
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-
-
- HY-155227S
-
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ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC50 of 1.08 nM for EGFR and an IC50 of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment
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| Cat. No. |
Product Name |
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Classification |
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- HY-159519
-
|
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Azide
|
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EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
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| Cat. No. |
Product Name |
|
Classification |
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- HY-113289
-
|
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Cholesterol
|
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Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
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