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bifunctional inhibitor

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17

Inhibitors & Agonists

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-29244
    ATIC-IN-2

    		DNA/RNA Synthesis Cancer
    ATIC-IN-2 (Compound 1) is a competitive inhibitor for the bifunctional enzyme AICAR Tfase/IMPCH (ATIC), that binds to inosine monophosphate cyclohydrolase (IMPCH) with a Ki of 0.13 μM .
    ATIC-IN-2
  • HY-153821
    PROTAC KRAS G12C degrader-2

    		Ras PROTACs Cancer
    PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS .
    PROTAC KRAS G12C degrader-2
  • HY-144258
    PD-1/PD-L1-IN-14

    		PD-1/PD-L1 Inflammation/Immunology Cancer
    PD-1/PD-L1-IN-14 (compound 17) is a bifunctional inhibitor of PD-1/PD-L1 interactions, with an IC50 of 27.8 nM. PD-1/PD-L1-IN-14 (compound 17) inhibits PD-1/PD-L1 interactions and promotes dimerization, internalization, and degradation of PD-L1 .
    PD-1/PD-L1-IN-14
  • HY-111079
    HIV-1 inhibitor-70

    		HIV Reverse Transcriptase Others
    HIV-1 inhibitor-70 (compound 20) is a bifunctional inhibitor that inhibits both wild-type (WT) and K103N mutant reverse transcriptases (RTs) of HIV-1.
    HIV-1 inhibitor-70
  • HY-163320
    AChE/Aβ-IN-5

    		Cholinesterase (ChE) Amyloid-β Neurological Disease
    AChE/Aβ-IN-5 (compound AV-2) is a bifunctional inhibitor that targets AChE and auto-induced Aβ (Amyloid-β) aggregation. AChE/Aβ-IN-5 can significantly improve scopolamine- and Aβ-induced cognitive impairment in mice .
    AChE/Aβ-IN-5
  • HY-155819
    M3/PDE4 modulator-1

    		mAChR Phosphodiesterase (PDE) Inflammation/Immunology
    M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model .
    M3/PDE4 modulator-1
  • HY-172396
    PD-L1/VISTA-IN-2

    		PD-1/PD-L1 VISTA Cancer
    PD-L1/VISTA-IN-2 (Compound S8) is an orally active bifunctional PD-L1/VISTA inhibitor with an IC50 of 1.4 μM for PD-L1 and a KD of 2.1 μM for VISTA. PD-L1/VISTA-IN-2 can activate the tumor immune microenvironment and exert anti-cancer effects .
    PD-L1/VISTA-IN-2
  • HY-120281
    ST-168

    		MEK PI3K Akt Apoptosis Caspase Cancer
    ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values ​​of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research .
    ST-168
  • HY-149558
    CXCR4-IN-2

    		Apoptosis CXCR Cancer
    CXCR4-IN-2 (compound A1) is a bifunctional fluorinated small molecule that is a potent CXCR4 inhibitor with anticancer activity. CXCR4-IN-2 has cytotoxic (IC50: 60 μg/mL; 72 h) and antiproliferative effects on mouse colorectal cancer (CRC) cells. CXCR4-IN-2 induces cell arrest in the G2/M phase and induces apoptosis .
    CXCR4-IN-2
  • HY-172768
    SCUT1-2

    		Bacterial Infection
    SCUT1-2 is a bifunctional antibacterial agent with good oral bioavailability in mice (F=56.8%). SCUT1-2 can kill the vegetative cells of C. difficile with a MIC of 0.06-0.50 μg/mL, and inhibit spore germination in vitro. SCUT1-2 could alleviate the symptoms of weight loss and diarrhea in mice caused by C. difficile infection (CDI) and prevent recurrent CDI .
    SCUT1-2
  • HY-169268
    Aβ-IN-10

    		Amyloid-β Neurological Disease
    Aβ-IN-10 (Compound Alz -5) is a bifunctional copper chelator and an inhibitor for beta-amyloid (Aβ), that interacts with Aβ aggregates and reduces the neurotoxicity. Aβ-IN-10 exhibits antioxidant efficacy, reveals moderate cytotoxicity with the presence of CuCl2 in SH-SY5Y and HepG2 with IC50 of 65.5, 31.2 μM. Aβ-IN-10 reduces the increase of cell stiffness caused by Aβ .
    Aβ-IN-10
  • HY-159493
    BI2536-PEG2-Halo

    		Polo-like Kinase (PLK) Cancer
    BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC50=23 nM), exhibits selective toxicity against p53 mutant cancer cells .
    BI2536-PEG2-Halo
  • HY-162809
    XMU-MP-9

    		Ras Cancer
    XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1 and K-Ras, induces conformational changes in the Nedd4-1/K-Ras complex, promotes the ubiquitination and degradation of multiple K-Ras mutants, and inhibits the proliferation of cells carrying K-Ras mutants. XMU-MP-9 can be used for the study of colon, lung and pancreatic cancer .
    XMU-MP-9
  • HY-158685
    RG7112D

    		MDM-2/p53 Cancer
    RG7112D is a potent MDM2 inhibitor with IC50s of 11 nM and >10000 nM and for MDM2-p53 and VHL-HIF1α by binding HTRF assay, respectively. RG7112D is coupled by an amide bond to VHL-Amine, resulting in a bi-functional molecule, YX-02-030. YX-02-03, a MDM2-PROTAC, potently inhibits MDM2-p53 binding (HTRF IC50=63nM). RG7112D can stabilize MDM2 protein and increase p53 protein levels .
    RG7112D
  • HY-170405
    YB-3–17

    		PROTACs mTOR Cancer
    YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC50=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC50=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC50 of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))
    YB-3–17
  • HY-173499
    HLDA-212

    		Aurora Kinase Apoptosis Cancer
    HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies) .
    HLDA-212
  • HY-171860
    FC-14369

    		PROTACs HIV Cancer
    FC-14369 is a PROTAC degrader targeting HIV-1 Nef protein with a DC50 value of 160 nM. FC-14369 binds to both Nef and Cereblon E3 ubiquitin ligase via its bifunctional structure, inducing Nef ubiquitination and proteasomal degradation to restore cell-surface CD4 and MHC-I expression and inhibit HIV-1 replication. FC-14369 can be used in research on HIV infection and AIDS . (Pink: Nef ligand-2 (HY-171862); Black: Ethylenediamine (HY-Y0275); Blue: Thalidomide (HY-14658))
    FC-14369

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