Search Result
Results for "
Dual-target
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-113289
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Akt
Androgen Receptor
Bacterial
Drug Metabolite
HSV
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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-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-N4150
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Quercetagetin-7-O-glucoside
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Phosphatase
Tau Protein
NF-κB
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Quercetagitrin (Quercetagetin-7-O-glucoside) is a natural product that can be isolated from the African marigold (Tagetes erecta). Quercetagitrin has anti-inflammatory activity. Quercetagitrin inhibits Tau accumulation. Quercetagitrin can reverse neuroinflammation and cognitive deficits in P301S-Tau transgenic mouse model through inhibiting NF-κB activation. Quercetagitrin is a dual-target inhibitor of PTPN6 (IC50 = 1 μM) and PTPN9 (IC50 = 1.7 μM). Quercetagitrin enhances glucose uptake by mature C2C12 myoblasts. Quercetagitrin can be studied in research for Alzheimer’s disease and type 2 diabetes .
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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-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-122909
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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-174280
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ITK kinase-IN-1
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Itk
JAK
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Inflammation/Immunology
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Modzatinib (ITK kinase-IN-1) is an oral active, selective, covalent ITK/JAK3 dual-target inhibitor with IC50 values of 8 nM and 23 nM, respectively. Modzatinib exhibits anti-inflammatory activity and can be used in the research of autoimmune and inflammatory diseases .
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- HY-147025
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PROTACs
TGF-beta/Smad
HIF/HIF Prolyl-Hydroxylase
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Inflammation/Immunology
Cancer
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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. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine can be used for research on prostate cancer and other cancers .
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- HY-112440
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Methuosis inducer 1
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Microtubule/Tubulin
NF-κB
MDM-2/p53
PI3K
Akt
c-Myc
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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-178281
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Potassium Channel
Sodium Channel
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Neurological Disease
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E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research .
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- HY-P10868
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RLS-0071
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Reactive Oxygen Species (ROS)
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Infection
Inflammation/Immunology
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Pegtarazimod (RLS-0071) is a dual-target anti-inflammatory peptide that exerts its effects by simultaneously regulating the complement system and neutrophil-associated inflammatory pathways. Pegtarazimod reduces ROS production both in vitro and in vivo, and decreases the level of neutrophil elastase, a marker of neutrophil extracellular traps (NETs), in vivo, thereby alleviating inflammatory responses. Pegtarazimod significantly improves the survival rate of mice in multiple in vivo models of acute graft-versus-host disease (aGVHD). Pegtarazimod inhibits the activation of the C1 complex, reduces the herpes zoster-like spread of herpes simplex virus type 1 skin infection, and improves the survival rate of infected mice . Pegtarazimod can be used in research related to acute graft-versus-host disease, acute pulmonary diseases, and skin herpes simplex virus type 1 infection .
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- HY-145260
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Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
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Cancer
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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-147253
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NS 089; NCNP 02
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DNA/RNA Synthesis
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Neurological Disease
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Brogidirsen (NS 089; NCNP 02) is a a dual-targeting antisense oligonucleotide. Brogidirsen can induce dystrophin protein experession. Brogidirsen can be used for the research of Duchenne muscular dystrophy .
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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-P10740
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Peptide-Drug Conjugates (PDCs)
PSMA
Folate Receptor (FR)
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Cancer
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CBP-1018 is a PDC (peptide-drug conjugate) formed by conjugating Monomethyl auristatin E (HY-15162) to a dual-targeting ligand of FLOR1/PSMA (prostate-specific membrane antigen) via a linker (HY-78738). CBP-1018 binds to FLOR1 and prostate-specific membrane antigen (PSMA). CBP-1018 is applicable to the research of solid tumors and metastatic castration-resistant prostate cancer .
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- HY-176165
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CDK
Histone Methyltransferase
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Cancer
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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-159083
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Amyloid-β
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Neurological Disease
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DN5355 is a small molecule compound that targets amyloid β protein (Aβ) and hyperphosphorylated tau protein. DN5355 can inhibit the aggregation of Aβ and tau protein and disaggregate the formed Aβ and tau protein fibers. DN5355 can be used in the study of Alzheimer's disease .
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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-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-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-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-176287
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Dopamine Receptor
GSK-3
PKA
P-glycoprotein
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Neurological Disease
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ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
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- HY-164454
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Aurora Kinase
STAT
JAK
Mitosis
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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-178485
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PI3K
HDAC
Akt
Histone Methyltransferase
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Cancer
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SJY26 is a PI3K/HDAC dual-target inhibitor with IC50s of 0.59 nM (PI3Kα and PI3Kδ), 2.02 nM (PI3Kγ), 12.69 nM (PI3Kβ) and 114 nM (HDAC1). SJY26 exhibits potent broad-spectrum anti-proliferative activity, and is particularly sensitive to Jurkat and PC9R cells. SJY26 inhibited the migration of PC9R cells, arrested the cell cycle and induced cell apoptosis. SJY26 reduces AKT phosphorylation, and decreases histone H3 deacetylation (Ac-H3). SJY26 can be used for the studies of non-small cell lung cancer and leukemia .
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- HY-175973
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Cholinesterase (ChE)
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Neurological Disease
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AChE/BChE-IN-30 (Compound 3g) is a Cholinesterase dual-target competitive inhibitor. AChE/BChE-IN-30 can inhibit AChE and BChE with IC50 values of 0.338 and 2.087 μM and Ki values of 0.045 and 0.789 μM. AChE/BChE-IN-30 can be used for the research of neurological disease, such as Alzheimer's disease .
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- HY-179053
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- HY-129089
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Dopamine Receptor
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Neurological Disease
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(-)-MDO-NPA is an N-propylnorapomorphine analog and a D1R/D2R dual-target ligand. (-)-MDO-NPA has EC50 values of 1949 nM (D1R) and 520 nM (D2R) for β-arrestin. (-)-MDO-NPA has EC50 values of 717.5 nM (D1R) and 7.7 nM (D2R) for cAMP. (-)-MDO-NPA can be used in the research of dopamine-related diseases such as Parkinson’s disease .
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- HY-P2548
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EGFR
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Others
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pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification .
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- HY-174457
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STAT
Carbonic Anhydrase
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
Caspase
Bcl-2 Family
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Cancer
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STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC) .
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- HY-W877997
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E3 Ligase Ligand-Linker Conjugates
Drug Derivative
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Cancer
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Pomalidomide 5'-pip-acid is an E3 ligase ligand-linker conjugate derived from the molecular glue Pomalidomide (HY-10984), which can be used to synthesize the dual-target PROTAC degrader PROTAC CBP/p300/BRD4 Degrader-1 (HY-181758) targeting CBP/p300 and BRD4. Pomalidomide 5'-pip-acid shows anti-proliferative activity against cancer cells with an IC50 of 2.73 nM. Pomalidomide 5'-pip-acid induces anti-proliferative effects in cancer cells. Pomalidomide 5'-pip-acid is applicable to research related to prostate cancer and colorectal cancer .
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- HY-176547
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FGFR
Cytochrome P450
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Endocrinology
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FGFR2/3-IN-3 is a dual-target FGFR2/3 inhibitor with IC50s of 2.7 nM (TEL-FGFR2) and 3.9 nM (TEL-FGFR3), respectively. FGFR2/3-IN-3 has effective activity against both wild-type and mutant FGFR3. FGFR2/3-IN-3 has low CYP3A4 inhibitory effect and hERG toxicity. FGFR2/3-IN-3 improves the imbalance between chondrocyte proliferation and differentiation and promotes bone growth by inhibiting the signaling pathway mediated by mutant FGFR3. FGFR2/3-IN-3 shows a growth-promoting effect in a dwarfism mouse model and has the potential to study bone development disorder-related diseases such as achondroplasia (ACH) .
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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-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-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-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-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-150755
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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-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-178366
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Influenza Virus
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Infection
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PAC/NP-IN-1 (Compound 30) is a dual-target anti-influenza agent that specifically binds to nucleoprotein (NP) and the C-terminal domain of PA protein (PAc). PAC/NP-IN-1 inhibits influenza A virus A/WSN/33 (H1N1) (EC50 = 3.63 μM, IC50 = 3.08 μM). PAC/NP-IN-1 can be used for the study of influenza infection .
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- HY-175262
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Bacterial
Cytochrome P450
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Infection
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Mtb-IN-12 (Compound 5m) is a dual-target inhibitor that can target the CYP125 (KD: 40 nM; KI: 0.1 μM) and CYP142 (KD: 160 nM; KI: 0.05 μM) enzymes of Mycobacterium tuberculosis. Mtb-IN-12 exhibits good inhibitory activity against both drug-sensitive strains and multidrug-resistant tuberculosis strains, with low toxicity to macrophages. Mtb-IN-12 can be used in the research of anti-tuberculosis drugs .
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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-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-151263
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HDAC
G-quadruplex
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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-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-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-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-175516
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FXR
PPAR
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Inflammation/Immunology
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dual FXR/PPARδ agonist-2 is a FXR/PPARδ dual agonist through hybridation of FXR agonist GW-4064 and PPARδ agonist GW-0742.dual FXR/PPARδ agonist-2 displays potent dual-target activities with a FXR agonistic EC50 of 12.28 nM and 69 % PPARδ activation at 100 nM. dual FXR/PPARδ agonist-2 shows anti-fibrotic effects in pulmonary fibrosis mouse model .
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- HY-170793
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PD-1/PD-L1
VISTA
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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-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-179031
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EGFR
VEGFR
Apoptosis
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Cancer
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EGFR/VEGFR2-IN-7 (Compound 3e) is a dual-target EGFR/VEGFR2 inhibitor, with IC50 values of 142 (EGFR) and 71 nM (VEGFR2). EGFR/VEGFR2-IN-7 exhibits broad-spectrum and potent anti-proliferative activity, especially being sensitive to breast cancer. EGFR/VEGFR2-IN-7 induces cell cycle arrest and apoptosis, inhibits cell migration and invasion. EGFR/VEGFR2-IN-7 can be used for research on breast cancer .
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-
- HY-149617
-
|
|
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-155227S
-
|
|
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
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-
- HY-158310
-
|
|
SOS1
EGFR
Ras
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM) .
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-
- HY-159519
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
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-N4150R
-
|
Quercetagetin-7-O-glucoside (Standard)
|
Reference Standards
Phosphatase
Tau Protein
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Quercetagitrin (Standard) is the analytical standard of Quercetagitrin. This product is intended for research and analytical applications. Quercetagitrin (Quercetagetin-7-O-glucoside) is a natural product that can be isolated from the African marigold (Tagetes erecta). Quercetagitrin has anti-inflammatory activity. Quercetagitrin inhibits Tau accumulation. Quercetagitrin can reverse neuroinflammation and cognitive deficits in P301S-Tau transgenic mouse model through inhibiting NF-κB activation. Quercetagitrin is a dual-target inhibitor of PTPN6 (IC50 = 1 μM) and PTPN9 (IC50 = 1.7 μM). Quercetagitrin enhances glucose uptake by mature C2C12 myoblasts. Quercetagitrin can be studied in research for Alzheimer’s disease and type 2 diabetes .
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-
- HY-159510
-
|
|
Apoptosis
VEGFR
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
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
-
|
|
Small Interfering RNA (siRNA)
HDAC
Apoptosis
|
Cancer
|
|
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-168633
-
|
|
Bombesin Receptor
PSMA
|
Cancer
|
|
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-179049
-
|
|
EGFR
Microtubule/Tubulin
Akt
ERK
Autophagy
Atg8/LC3
p62
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
EGFR/tubulin-IN-1 (Compound 26) is a dual-target inhibitor of EGFR and tubulin. EGFR/tubulin-IN-1 significantly reduces the levels of p-EGFR, p-AKT, and p-ERK in cells, disrupting the microtubule structure of the cells. EGFR/tubulin-IN-1 significantly inhibits the proliferation of H1975 cells and significantly blocks the cells in the G2/M phase. EGFR/tubulin-IN-1 induces the expression of autophagy markers LC3B-II and Beclin-1, while down-regulating the expression of p62. EGFR/tubulin-IN-1 induces ferroptosis, with increased ROS content and depletion of glutathione (GSH). EGFR/tubulin-IN-1 inhibits epithelial-mesenchymal transition (EMT) and tumor metastasis. EGFR/tubulin-IN-1 has a significant tumor-suppressing effect in the H1975 transplanted tumor nude mouse model. EGFR/tubulin-IN-1 can be used for the study of non-small cell lung cancer .
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-
- HY-147253A
-
|
NS 089 sodium; NCNP 02 sodium
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
Brogidirsen (NS 089; NCNP 02) sodium is a a dual-targeting antisense oligonucleotide. Brogidirsen sodium can induce dystrophin protein experession. Brogidirsen sodium can be used for the research of Duchenne muscular dystrophy .
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-
- HY-161457
-
-
- HY-163680
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
|
Cancer
|
|
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-177908
-
|
|
STING
PI3K
|
Cancer
|
|
SH-273 is a dual targeting compound. SH-273 has dual function to stimulate STING function (EC50: 100 nM) and inhibits PI3Kγ (IC50: 7 nM). SH-273 can be used in the research of pancreatic cancer .
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-
- HY-163537
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
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-172700
-
|
|
Liposome
|
Cancer
|
|
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-174211
-
|
|
JNK
|
Cancer
|
|
JNK-IN-23 (Compound K12) is an inhibitor of JNK. JNK-IN-23 inhibits the proliferation of MDA-MB-231 (GIC50: 30 nM). JNK-IN-23 blocks TNBC metastatic growth in vivo. JNK-IN-23 inhibits the growth of lung metastases by dual targeting of glutaminase-1 (GLS) and pyruvate dehydrogenase complex (PDHC) .
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-
- HY-144825
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
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-162601
-
|
|
Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
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-158328A
-
-
- HY-117688
-
|
|
HDAC
Topoisomerase
Apoptosis
|
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-180673
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
Mpro/RdRp-IN-1 (Compound 1) is a dual-target inhibitor against SARS-CoV-2, targeting RdRp (EC50 = 25.45) and Mpro (IC50 = 125.4 μM). Mpro/RdRp-IN-1 exhibits EC₅₀ for HCoV-OC43 of 4.79 μM, and the selectivity index (SI) is 10.89. Mpro/RdRp-IN-1 can be used for studying SARS-CoV-2 and HCoV-OC43 infections .
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-
- HY-179684
-
|
|
CGRP Receptor
5-HT Receptor
ERK
Epigenetic Reader Domain
|
Neurological Disease
|
|
PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC50 = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine .
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-
- HY-181050
-
|
|
PROTACs
Src
Btk
Apoptosis
|
Cancer
|
|
DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively. DFCI-002-06 retains higher anti-tumor activity than the HCK/BTK dual-target inhibitor (HY-15805), inducing apoptosis in cancer cells. DFCI-002-06 can be used for the study of MYD88 mutant B-cell malignancies .
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-
- HY-120089
-
|
|
FLT3
ERK
Akt
STAT
Apoptosis
|
Cancer
|
|
UNC1666 is an ATP-competitive dual-target Mer/Flt3 tyrosine kinase inhibitor with IC50 values of 0.55 nM and 0.69 nM, and Ki values of 0.16 nM and 0.67 nM, respectively. UNC1666 reduces the phosphorylation levels of Mer and Flt3, suppresses downstream pro-survival signaling pathways (Erk1/2, Akt and Stat), induces cell apoptosis, and decreases colony formation of acute myeloid leukemia cells. UNC1666 is applicable to research related to acute myeloid leukemia .
|
-
- HY-179607
-
|
|
CCR
|
Inflammation/Immunology
Cancer
|
|
LUF8100 is a dual-target antagonist of CCR2/CCR5 with pKi values for CCR2 and CCR5 of 5.23 and 4.97 respectively. LUF8100 can be used for research on immune homeostasis and cancer .
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-
- HY-180916
-
|
|
Carbonic Anhydrase
Reactive Oxygen Species (ROS)
NOD-like Receptor (NLR)
Apoptosis
|
Neurological Disease
|
|
CAII-IN-11 (Compound A1) is a dual-target compound that contains a hCA II inhibitor (IC₅₀ = 2 nM) portion and a NO donor portion. CAII-IN-11 also has inhibitory activity against hCA IX, hCA XII, and hCA I, with IC50 values of 6, 3, and 152 nM respectively. CAII-IN-11 significantly increases the intracellular cGMP level in human trabecular meshwork cells. CAII-IN-11 reduces the apoptosis of retinal ganglion cells by reducing oxidative stress (ROS levels), inhibiting astrocytes and the NLRP3 inflammasome activation. CAII-IN-11 has hypotensive activity in rabbit models and can be used for the study of glaucoma .
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-
- HY-181140
-
|
|
CDK
PARP
|
Cancer
|
|
UNPD139734 is a CDK-1 inhibitor and PARP-1 inhibitor that forms stable complexes with each target protein. UNPD139734 serves as a lead compound for structural optimization to develop dual-target anticancer agents targeting CDK-1 and PARP-1. UNPD139734 can be used for the research of breast cancer .
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-
- HY-180819
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-33 (Compound 3N) is a dual-target inhibitor of AChE and BChE, with IC50 values of 12.81 and 44.54 nM respectively. AChE/BChE-IN-33 exhibits selective cytotoxicity against SH-SY5Y cells. AChE/BChE-IN-33 can be used for the study of Alzheimer's disease and neuroblastoma .
|
-
- HY-181811
-
|
|
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
PJ17 is a potent dual-target inhibitor of AChE and GSK-3β, with IC50 values of 8.84 μM and 4.19 μM, respectively. PJ17 shows no significant neurotoxic effect in primary cerebellar granule neuron cultures. PJ17 serves as a template for the design of multitarget drugs. PJ17 can be used for the research of Alzheimer's disease .
|
-
- HY-179280
-
|
|
Herbicide
Reactive Oxygen Species (ROS)
|
Others
|
|
Herbicidal agent 13 (Compound II-13) is a herbicidal agent. Herbicidal agent 13 retains the dual-target binding capabilities for PDS and ZDS, with Kd values of 71.8 μM and 0.586 mM against SynPDS and AtZDS, respectively. Herbicidal agent 13 increases ROS. Herbicidal agent 13 exhibits postemergence herbicidal activity against dicotyledonous weeds and monocotyledonous weed POLFU .
|
-
- HY-180551
-
|
|
PROTACs
RET
Trk Receptor
|
Endocrinology
Cancer
|
|
ZW-6-052 (compound 20), the derivative of ZW-18-116 (HY-180550), is a dual-target PROTAC degrader for the oncoproteins TRKA and RET. ZW-6-052 induces degradation of TMP3-TRKA in KM12 mouse xenograft models. ZW-6-052 can be used for RET or TRKA-derived cancer research, such as thyroid, lung, and colon cancers .
|
-
- HY-D3171
-
|
|
Fluorescent Dye
Cholinesterase (ChE)
|
Neurological Disease
|
|
AD-BChE/HClO is a dual-target two-photon fluorescent probe. AD-BChE/HClO can release 4-methylumbelliferone via butyrylcholinesterase-mediated hydrolysis of the ester bond at position 7, as well as hypochlorous acid-mediated thiocarbonyl oxidation. AD-BChE/HClO enables two-photon imaging in nerve cells and mouse brain tissues via tail vein injection. AD-BChE/HClO can be used for the research of Alzheimer's disease .
|
-
- HY-181694
-
|
|
Topoisomerase
HDAC
Apoptosis
Kinesin
RAD51
|
Cancer
|
|
SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity .
|
-
- HY-178455
-
|
|
Influenza Virus
|
Infection
|
|
Influenza virus-IN-10 is a dual-target antiviral agents for influenza that targets both PAC (KD = 8.9 μM) and NP (KD = 52.5 μM) simultaneously. Influenza virus-IN-10 exhibits an EC50 values of 1.64 μM) against influenza A virus (H1N1, A/WSN/33) and broad-spectrum activity against other influenza strains, including influenza B virus and multiple subtypes of influenza A .
|
-
- HY-180550
-
|
|
PROTACs
RET
Trk Receptor
|
Endocrinology
Cancer
|
|
ZW-18-116 (compound 9) is a dual-target PROTAC degrader for the oncoproteins TRKA and RET. ZW-18-116 induces the degradation of oncoproteins TRKA and RET by recruiting the CRBN E3 ligase. ZW-18-116 exhibits potent anti-proliferative activity in various cancer cell lines harboring RET or TRKA fusions. ZW-18-116 can be used for RET or TRKA-derived cancer research, such as thyroid, lung, and colon cancers .
|
-
- HY-181084
-
|
|
PROTACs
BCL6
Aquaporin
PARP
Caspase
CDK
|
Cancer
|
|
PROTAC BCL6/GSPT1 Degrader-1 is a dual-target PROTAC degrader that targets BCL6 and GSPT1. PROTAC BCL6/GSPT1 Degrader-1 inhibits cell proliferation, promotes DNA damage, and induces cell cycle arrest and apoptosis in diffuse large B-cell lymphoma. PROTAC BCL6/GSPT1 Degrader-1 can be used for research on tumors such as lymphoma .
|
-
- HY-181759
-
|
|
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor targeting CBP, p300, and BRD4. CBP/p300/BRD4 ligand-1 competitively binds to the functional domains of target proteins without disrupting key interactions. CBP/p300/BRD4 ligand-1 can be used for the construction of dual-target PROTAC degraders (HY-181758) in studies related to prostate cancer and other cancers .
|
-
- HY-181519
-
|
|
DNA Alkylator/Crosslinker
Aldose Reductase
Glycosidase
|
Metabolic Disease
Inflammation/Immunology
|
|
ALR2/α-GLY-IN-1 is a potent dual-target inhibitor that targets aldose reductase ALR2 and α-glucosidase (IC50 values are 0.72 μM and 0.82 μM, respectively; Ki values are 1.67 μM and 1.37 μM, respectively). ALR2/α-GLY-IN-1 also acts as a DNA binder, which stably interacts with calf thymus double-stranded DNA through non-covalent interactions such as groove-binding mode and water-bridged hydrogen bonds. ALR2/α-GLY-IN-1 can be used in studies related to diabetes and its complications .
|
-
- HY-180585
-
|
|
Monoamine Oxidase
Guanylate Cyclase
PKG
Collagen
|
Cardiovascular Disease
|
|
LOXL2/sGC modulator-2 (Compound 9k) is a selective and orally active lysyl oxidase-like 2 (LOXL2) and soluble guanylate cyclase (sGC) dual-target regulator. LOXL2/sGC modulator-2 shows inhibitory activity for LOXL2 with an IC50 of 0.1 μM and can activate sGC. LOXL2/sGC modulator-2 can ameliorate vascular remodeling and reduce pulmonary artery pressure. LOXL2/sGC modulator-2 can downregulate PKG1, PCNA, α-SMA, collagen I and fibronectin levels. LOXL2/sGC modulator-2 can be used for the research of pulmonary arterial hypertension .
|
-
- HY-180292
-
|
|
VEGFR
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
Tubulin/VEGFR-2-IN-2 is an orally active tubulin and VEGFR-2 inhibitor with IC50s of 3.27 and 0.09 μM, respectively. Tubulin/VEGFR-2-IN-2 exerts the antitumor effects through multifaceted pathways, including enhancing reactive oxygen species (ROS) generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Tubulin/VEGFR-2-IN-2 demonstrates anti-angiogenic properties by significantly impairing endothelial cell migration, invasion, and tube formation in vitro. Tubulin/VEGFR-2-IN-2 suppresses angiogenesis, tumor growth, and metastasis in vivo. Tubulin/VEGFR-2-IN-2 can be used for non-small lung cancer, breast cancer, gastric cancer and lymphoma .
|
-
- HY-183564
-
|
|
RIP kinase
Necroptosis
Interleukin Related
|
Inflammation/Immunology
|
|
RIPK1/RIPK3-PPI-IN-1 is an orally active dual-target inhibitor of RIPK1/RIPK3, with a Kd value of 2.4 nM for RIPK1 and 24 nM for RIPK3. RIPK1/RIPK3-PPI-IN-1 inhibits the phosphorylation of RIPK1, RIPK3 and MLKL, thereby suppressing necroptosis. RIPK1/RIPK3-PPI-IN-1 restores body temperature, improves survival rate, and reduces IL-1β/IL-6 levels in serum and multiple organs of Mus musculus, thus alleviating TNF-α-induced systemic inflammatory response syndrome. RIPK1/RIPK3-PPI-IN-1 can be used in research related to systemic inflammatory response syndrome .
|
-
- HY-181758
-
|
|
PROTACs
Epigenetic Reader Domain
Histone Acetyltransferase
c-Myc
Apoptosis
|
Cancer
|
|
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer .
|
-
- HY-182905
-
|
|
Somatostatin Receptor
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus .
|
-
- HY-180836
-
|
|
Molecular Glues
IKZF Family
Apoptosis
|
Cancer
|
|
DIX-01 is a molecular gel degrader that can simultaneously induce the degradation of IKZF1/3 and GSPT1 mediated by CRBN. Its DC50 values are: IKZF1 (19.80 nM), IKZF3 (45.31 nM), and GSPT1 (120.1 nM). DIX-01 exhibits nanomolar-level potent anti-proliferative activity in various cancer cell lines. DIX-01 induces apoptosis in MV4-11 cells and significantly inhibits the growth of leukemia cells in zebrafish. DIX-01 can be used for the study of malignant hematological tumors .
|
-
- HY-172698
-
|
|
Liposome
|
Cancer
|
|
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 .
|
-
- HY-180449
-
|
|
Microtubule/Tubulin
Wnt
|
Cancer
|
|
Anticancer agent 291 (Compound 2406) is an anti-cancer agent. Anticancer agent 291 interferes with the integrity of the β-tubulin cytoskeleton and inhibits the Wnt/β-catenin signal transduction. Anticancer agent 291 significantly inhibits the invasion, migration and colony formation of tumor cells. Anticancer agent 291 induces the cell cycle of EC-9706 and HT-29 cells to arrest at the G2/M phase and inhibits cell proliferation. Anticancer agent 291 can be used for the study of gastrointestinal cancer .
|
-
- HY-152253
-
|
|
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 .
|
-
- 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 .
|
-
- HY-170947
-
|
|
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-170651
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CDK
HDAC
Apoptosis
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Cancer
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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-179003
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mTOR
Glutaminase
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
Ferroptosis
Glutathione Peroxidase
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Cancer
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mTOR/GLS1-IN-1 (Compoud 9d) is a potent dual targeted mTOR/GLS1 inhibitor. Has anti proliferative activity against various tumor cells. mTOR/GLS1-IN-1 dose dependently induces ROS accumulation, induces autophagosome formation, and induces apoptosis. mTOR/GLS1-IN-1 can increase Fe 2+, decrease GPX4, and induce ferroptosis. mTOR/GLS1-IN-1 can inhibit cell migration, invasion, and angiogenesis. mTOR/GLS1-IN-1 can be used in the research of cancer, such as breast cancer .
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- HY-D3311
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Fluorescent Dye
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Cancer
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M1219 is a GSH/ATP dual near-infrared activated fluorescent probe that enables independent real-time monitoring of dynamic changes in intracellular GSH and ATP without spectral crosstalk (GSH: Ex=640 nm, Em=740~800 nm; ATP: Ex=594 nm/610 nm, Em=650~700 nm). M1219 not only visualizes the metabolic regulatory mechanism of TNBC under single/dual-target inhibition of SLC7A11/GLUT1 and accurately evaluates its in vivo efficacy, but also achieves precise localization of the TNBC tumor invasion boundary. M1219 can be used for the research of triple-negative breast cancer .
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- HY-178907
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Serotonin Transporter
5-HT Receptor
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Neurological Disease
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SERT/5-HT-IN-1 (compound D17) is an orally active and potent dual target inhibitor of SERT/5-HT3A (SERT IC50 = 1.5 nM, NET IC50 = 49 nM, DAT IC50 = 91 nM, 5-HT3A Ki = 12 nM). SERT/5-HT-IN-1 has an IC50 of 39 nM to 5-HT3A. SERT/5-HT-IN-1 has a lower risk of liver, kidney, and cardiac toxicity. SERT/5-HT-IN-1 can be used for research on depressive disorders .
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- HY-178475
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Carbonic Anhydrase
Glutathione Peroxidase
Ferroptosis
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Cancer
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CA IX/GPX4-IN-1 (Compound 22abcb) is a dual targeted inhibitor of CA IX and GPX4 activity. CA IX/GPX4-IN-1 can effectively kill SUM159PT cells (IC50 = 416 nM) by inducing iron death under hypoxic conditions. CA IX/GPX4-IN-1 has an IC50 of 663 nM to CA IX in SUM159PT-CAIX-FL cells. CA IX/GPX4-IN-1 can significantly inhibit tumor growth and can be reversed by ferroptosis inhibitors. CA IX/GPX4-IN-1 can be used for research on breast cancer and other cancers .
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- HY-170779
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FAP
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Cancer
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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-159591
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Ras
Akt
ERK
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Cancer
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YK-8S is a dual-targeted K-Ras (G12D/G12C) covalent inhibitor. YK-8S shows no significant binding to wild-type K-Ras and other mutants (G12R, G13D, Q61R/K). YK-8S exhibits anti-proliferative activity against H358 (G12C) and AGS (G12D) cells. YK-8S inhibits the phosphorylation of p-AKT/p-ERK in BaF3/G12D and G12C cells. YK-8S can be used for pancreatic cancer, colorectal cancer and other tumors with high incidence of G12D .
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-
- HY-174403
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Bcl-2 Family
c-Myc
Apoptosis
Caspase
|
Cancer
|
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c-MYC/BCL2 ligand 1 iodide is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56 μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 iodide inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 iodide inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 iodide significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 iodide can be used for the research of breast cancer.
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- HY-178984
-
|
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PI3K
Epigenetic Reader Domain
DNA/RNA Synthesis
Akt
c-Myc
AMPK
|
Cancer
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PI3Kα-IN-28 (Compound 23) is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 and KYSE450 cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer .
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- HY-163679
-
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Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
|
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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| Cat. No. |
Product Name |
Type |
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- HY-D2280
-
|
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Fluorescent Dye
|
|
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-D3171
-
|
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Fluorescent Dye
|
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AD-BChE/HClO is a dual-target two-photon fluorescent probe. AD-BChE/HClO can release 4-methylumbelliferone via butyrylcholinesterase-mediated hydrolysis of the ester bond at position 7, as well as hypochlorous acid-mediated thiocarbonyl oxidation. AD-BChE/HClO enables two-photon imaging in nerve cells and mouse brain tissues via tail vein injection. AD-BChE/HClO can be used for the research of Alzheimer's disease .
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- HY-D3311
-
|
|
Fluorescent Dye
|
|
M1219 is a GSH/ATP dual near-infrared activated fluorescent probe that enables independent real-time monitoring of dynamic changes in intracellular GSH and ATP without spectral crosstalk (GSH: Ex=640 nm, Em=740~800 nm; ATP: Ex=594 nm/610 nm, Em=650~700 nm). M1219 not only visualizes the metabolic regulatory mechanism of TNBC under single/dual-target inhibition of SLC7A11/GLUT1 and accurately evaluates its in vivo efficacy, but also achieves precise localization of the TNBC tumor invasion boundary. M1219 can be used for the research of triple-negative breast cancer .
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| Cat. No. |
Product Name |
Type |
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- HY-172699A
-
|
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Biochemical Assay Reagents
|
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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-172700
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Biochemical Assay Reagents
|
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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-172698
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Biochemical Assay Reagents
|
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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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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10868
-
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RLS-0071
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Reactive Oxygen Species (ROS)
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Infection
Inflammation/Immunology
|
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Pegtarazimod (RLS-0071) is a dual-target anti-inflammatory peptide that exerts its effects by simultaneously regulating the complement system and neutrophil-associated inflammatory pathways. Pegtarazimod reduces ROS production both in vitro and in vivo, and decreases the level of neutrophil elastase, a marker of neutrophil extracellular traps (NETs), in vivo, thereby alleviating inflammatory responses. Pegtarazimod significantly improves the survival rate of mice in multiple in vivo models of acute graft-versus-host disease (aGVHD). Pegtarazimod inhibits the activation of the C1 complex, reduces the herpes zoster-like spread of herpes simplex virus type 1 skin infection, and improves the survival rate of infected mice . Pegtarazimod can be used in research related to acute graft-versus-host disease, acute pulmonary diseases, and skin herpes simplex virus type 1 infection .
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-
- HY-P10740
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|
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Peptide-Drug Conjugates (PDCs)
PSMA
Folate Receptor (FR)
|
Cancer
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|
CBP-1018 is a PDC (peptide-drug conjugate) formed by conjugating Monomethyl auristatin E (HY-15162) to a dual-targeting ligand of FLOR1/PSMA (prostate-specific membrane antigen) via a linker (HY-78738). CBP-1018 binds to FLOR1 and prostate-specific membrane antigen (PSMA). CBP-1018 is applicable to the research of solid tumors and metastatic castration-resistant prostate cancer .
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-
- HY-P2548
-
|
|
EGFR
|
Others
|
|
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99572
-
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BNT-312; DuoBody-CD40x-4-1BB; GEN1042
|
TNF Receptor
|
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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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-168968S
-
|
|
|
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
-
|
|
|
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 |
|
Classification |
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- HY-159519
-
|
|
|
Azide
|
|
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-178475
-
|
|
|
Alkynes
|
|
CA IX/GPX4-IN-1 (Compound 22abcb) is a dual targeted inhibitor of CA IX and GPX4 activity. CA IX/GPX4-IN-1 can effectively kill SUM159PT cells (IC50 = 416 nM) by inducing iron death under hypoxic conditions. CA IX/GPX4-IN-1 has an IC50 of 663 nM to CA IX in SUM159PT-CAIX-FL cells. CA IX/GPX4-IN-1 can significantly inhibit tumor growth and can be reversed by ferroptosis inhibitors. CA IX/GPX4-IN-1 can be used for research on breast cancer and other cancers .
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| Cat. No. |
Product Name |
|
Classification |
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- HY-113289
-
|
|
|
Cholesterol
|
|
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-147253
-
|
NS 089; NCNP 02
|
|
Antisense Oligonucleotides
|
|
Brogidirsen (NS 089; NCNP 02) is a a dual-targeting antisense oligonucleotide. Brogidirsen can induce dystrophin protein experession. Brogidirsen can be used for the research of Duchenne muscular dystrophy .
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-
- HY-172699A
-
|
|
|
Pegylated Lipids
|
|
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 .
|
-
- HY-147253A
-
|
NS 089 sodium; NCNP 02 sodium
|
|
Antisense Oligonucleotides
|
|
Brogidirsen (NS 089; NCNP 02) sodium is a a dual-targeting antisense oligonucleotide. Brogidirsen sodium can induce dystrophin protein experession. Brogidirsen sodium can be used for the research of Duchenne muscular dystrophy .
|
-
- HY-172700
-
|
|
|
Pegylated Lipids
|
|
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 .
|
-
- HY-172698
-
|
|
|
Pegylated Lipids
|
|
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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