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Results for "

bivalent inhibitor

" in MedChemExpress (MCE) Product Catalog:

10

Inhibitors & Agonists

1

Inhibitory Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-118998
    TX2-121-1

    		EGFR Cancer
    TX2-121-1, a potent and selective Her3 (ErbB3) bivalent ligand, can induce degradation of Her3 with an IC50 of 49 nM. TX2-121-1 can inhibit Her3-dependent signaling .
    TX2-121-1
  • 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-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-111373
    RapaLink-1
    5 Publications Verification

    		 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-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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