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engagement

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25

Inhibitors & Agonists

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Peptides

1

Inhibitory Antibodies

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Natural
Products

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112088
    AZD4573
    Maximum Cited Publications
    10 Publications Verification

    CDK Cancer
    AZD4573 is a potent and highly selective CDK9 inhibitor (IC50 of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies .
    AZD4573
  • HY-148281

    Bcl-2 Family Cancer
    TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells .
    TMX-2164
  • HY-112081A

    Others Others
    BAY-707 acetate is a highly potent and selective substrate-competitive inhibitor of MTH1 with superior cellular target engagement and pharmacokinetic properties.
    BAY-707 acetate
  • HY-157611

    DNA/RNA Synthesis Cancer
    DHX9-IN-17 (186) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.161 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-17
  • HY-157612

    DNA/RNA Synthesis Cancer
    DHX9-IN-16 (208) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.125 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-16
  • HY-157605

    DNA/RNA Synthesis Cancer
    DHX9-IN-11 (469) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.0838 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-11
  • HY-157606

    DNA/RNA Synthesis Cancer
    DHX9-IN-13 (389) is a RNA helicase DHX9 inhibitor, with an EC50 of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-13
  • HY-157607

    DNA/RNA Synthesis Cancer
    DHX9-IN-15 (287) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.232 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-15
  • HY-157604

    DNA/RNA Synthesis Cancer
    DHX9-IN-9 (509) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.0177 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-9
  • HY-157610

    DNA/RNA Synthesis Cancer
    DHX9-IN-14 (161) is a RNA helicase DHX9 inhibitor, with an EC50 of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-14
  • HY-157609

    DNA/RNA Synthesis Cancer
    DHX9-IN-12 (83) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.917 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-12
  • HY-157608

    DNA/RNA Synthesis Cancer
    DHX9-IN-10 (49) is a RNA helicase DHX9 inhibitor, with an EC50 of 9.04 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-10
  • HY-157603

    DNA/RNA Synthesis Cancer
    DHX9-IN-7 (550) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.105 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-7
  • HY-157602

    DNA/RNA Synthesis Cancer
    DHX9-IN-8 (Compound 6) is a RNA helicase DHX9 inhibitor, with an EC50 of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .
    DHX9-IN-8
  • HY-141550

    Others Inflammation/Immunology
    BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP .
    BPK-25
  • HY-156782

    DNA/RNA Synthesis Cancer
    DHX9-IN-1 (example 160) is an inhibitor of ATP-dependent RNA helicase A (DHX9), with an EC50 value of 6.94 μM in DHX9 cellular target engagement. DHX9-IN-1 has antitumor activity .
    DHX9-IN-1
  • HY-P5017

    Oxytocin Receptor Endocrinology
    (Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the β-arrestin engagement and endocytosis toward the oxytocin receptor (OXTR) .
    (Val3,Pro8)-Oxytocin
  • HY-136521

    Epigenetic Reader Domain Cancer
    AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models. AZ13824374 inhibits ATAD2 with pIC50s of 8.2 and 6.2 in ATAD2 FRET assay and ATAD2 NanoBRET assay, respectively .
    AZ13824374
  • HY-136557

    PAD2-IN-1

    Protein Arginine Deiminase Inflammation/Immunology Cancer
    AFM32a (PAD2-IN-1), a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold) .
    AFM32a
  • HY-136557A
    AFM32a hydrochloride
    1 Publications Verification

    PAD2-IN-1 hydrochloride

    Protein Arginine Deiminase Inflammation/Immunology Cancer
    AFM32a (PAD2-IN-1) hydrochloride, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a hydrochloride shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold) .
    AFM32a hydrochloride
  • HY-111573

    RAR/RXR Others
    Anticancer agent 168 is an orally active retinoic acid receptor (RAR/RXR) beta2 agonist with ameliorating effects on spinal cord injury (SCI) .
    KCL-286
  • HY-D0976

    P2X Receptor HIV Infection
    NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .
    NF279
  • HY-117570

    PDI Neurological Disease
    KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family . KSC-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    KSC-34
  • HY-161063

    Dihydrofolate reductase (DHFR) Cancer
    DHFR-IN-14 (compound 32) is a pyrimethamine (Pyr)-type, dihydrofolate reductase (DHFR) inhibitor with potential anticancer activity .
    DHFR-IN-14
  • HY-161064

    Dihydrofolate reductase (DHFR) Cancer
    DHFR-IN-15 (compound 34) is a dihydrofolate reductase (DHFR) inhibitor with potential anticancer activity. DHFR-IN-15 effectively binds to DHFR in cells, reducing DHFR levels to 10 nM .
    DHFR-IN-15

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