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Results for "

bivalent inhibitor

" in MedChemExpress (MCE) Product Catalog:

15

Inhibitors & Agonists

1

Inhibitory Antibodies

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100653
    AZD5153
    2 Publications Verification

    		 Epigenetic Reader Domain Apoptosis Cancer
    AZD5153 is a bivalent, selective, and orally active BET/BRD4 bromodomain inhibitor with an IC50 of value of 5 nM for full-length BRD4 (FL-BRD4). AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 can be used for the study of cancer, such as acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma .
    AZD5153
  • HY-125232
    MS645

    		Epigenetic Reader Domain Cancer
    MS645 is a bivalent BET bromodomains (BrD) inhibitor with a Ki of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells .
    MS645
  • HY-162299
    EGFR kinase inhibitor 3

    		EGFR Cancer
    EGFR kinase inhibitor 3 (compound 2) is a bivalent ATP-allosteric EGFR kinase inhibitor with IC50s of <10 nM, 1.5 nM, 0.059 nM, 0.064 nM for WT EGFR, EGFR-activating mutations L858R, L858R/T790M and L858R/T790M/C797S, respectively. EGFR kinase inhibitor 3 is a C-linked inhibitor .
    EGFR kinase inhibitor 3
  • HY-108350
    MI-2-2

    		Epigenetic Reader Domain Cancer
    MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation .
    MI-2-2
  • HY-162300
    EGFR kinase inhibitor 4

    		EGFR Cancer
    EGFR kinase inhibitor 4 (Compound 4) is a bivalent ATP-allosteric EGFR inhibitor (IC50: 1.8 nM for mutant EGFR (LRTMCS)). EGFR kinase inhibitor 4 can be used for research of NSCLC .
    EGFR kinase inhibitor 4
  • HY-176508
    KDX1381

    		Casein Kinase Cancer
    KDX1381 is a bivalent CK2α inhibitor (IC50: 17 nM, KD: 54 nM). KDX1381 has antitumor activity in mouse 786-O and A375 tumor xenograft models. KDX1381 combined with VEGFR inhibitors or DNA damaging agents enhances antitumor efficacy in mouse hepatocellular carcinoma and glioma models .
    KDX1381
  • HY-176233
    Transthyretin-IN-4

    		Transthyretin (TTR) Cardiovascular Disease
    Transthyretin-IN-4 (Compound B26) is a bivalent inhibitor of transthyretin (TTR) amyloidosis (bIC50: 0.09 µM, pIC50: 1.4 µM). Transthyretin-IN-4 is used in the study of fatal heart failure with preserved ejection fraction (HFpEF) and fatal arrhythmias .
    Transthyretin-IN-4
  • HY-162152
    biKEAP1

    		Keap1-Nrf2 Inflammation/Immunology
    biKEAP1 (compound 3) is an inhibitor targeting the dimerKEAP1. biKEAP1 binds to cellular KEAP1 dimers and releases the NRF2 protein sequestered by KEAP1, resulting in immediate activation of NRF2. biKEAP1 also promotes nuclear translocation of NRF2 and directly inhibits proinflammatory cytokine transcription. biKEAP1 can reduce acute inflammation and reduce inflammatory damage in acute inflammation models .
    biKEAP1
  • HY-169244
    CDK-TCIP1

    		CDK Bcl-2 Family Cancer
    CDK-TCIP1 is a bivalent molecule linking CDK9 inhibitor SNS-032 (HY-10008) to BCL6 ligand BI3812 (HY-111381). CDK-TCIP1 potently and specifically kills BCL6-overexpressing cells with EC50 of 7.7 nM for SUDHL5 cells .
    CDK-TCIP1
  • HY-P991518
    IBI-322

    		PD-1/PD-L1 CD47 Cancer
    IBI-322 is a bispecific antibody targeting PD-L1 and CD47. IBI-322 attenuates CD47 activity in monovalent binding and blockes PD-L1 activity in bivalent binding. IBI-322 selectively binds to CD47+PD-L1+ tumor cells, effectively inhibits CD47-SIRPα signal and triggered strong tumor cell phagocytosis in vitro .
    IBI-322
  • HY-111373
    RapaLink-1
    5+ Cited Publications

    		 mTOR Autophagy Cancer
    RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity .
    RapaLink-1
  • HY-174350
    CK2-IN-15

    		Casein Kinase SARS-CoV Infection
    CK2-IN-15 (Compound Biv5) is a selective and potent bivalent protein kinase CK2 inhibitor with an IC50 value of 51 pM. CK2-IN-15 significantly reduces the replication of SARS-CoV-2 in HEK-ACE2-TMPRSS2 and Vero cells, and also reduces viral replication in an ex vivo model of human nasal epithelial cells. CK2-IN-15 is promising for research of β-coronavirus infection-related diseases .
    CK2-IN-15
  • HY-150684
    GXH-II-052

    		Epigenetic Reader Domain Cancer
    GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc .
    GXH-II-052
  • HY-149521
    PI3K-IN-47

    		PI3K Cancer
    PI3K-IN-47 (Compound 27) is a bivalent PI3K inhibitor (IC50: 0.44 nM for PI3Kα, 7.18 nM, 13.92 nM, 22.83 nM for PI3Kβ, PI3Kγ, PI3Kδ). PI3K-IN-47 induces cell cycle arrest in G1 phase, inhibits colony formation and cell migration. PI3K-IN-47 inhibits tumor growth in HGC-27 xenograft mice .
    PI3K-IN-47
  • HY-150683
    NC-III-49-1

    		Epigenetic Reader Domain Cancer
    NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc .
    NC-III-49-1

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