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hematological diseases

" in MedChemExpress (MCE) Product Catalog:

10

Inhibitors & Agonists

2

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15771
    Tirabrutinib
    5 Publications Verification

    ONO-4059; GS-4059

    Btk Apoptosis Inflammation/Immunology Cancer
    Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies .
    Tirabrutinib
  • HY-15771A
    Tirabrutinib hydrochloride
    5 Publications Verification

    ONO-4059 hydrochloride; GS-4059 hydrochloride

    Btk Apoptosis Inflammation/Immunology Cancer
    Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies .
    Tirabrutinib hydrochloride
  • HY-145696

    PROTACs JAK Inflammation/Immunology Cancer
    SJ10542 is a potent and selective JAK2/3 PROTAC degrader. In PDX cells lSJBALL020589, SJ10542 has DC50 values of 14 and 11 nM for JAK2 and JAK3, respectively. SJ10542 exhibits antitumor activity and can be used for the research of hematological malignancies and autoimmune diseases . (Pink: Target protein ligand (HY-47073); Black: Linker (HY-W251248); Blue: E3 ligase ligand (HY-W890189); E3 ligase ligand+Linker (HY-176425))
    SJ10542
  • HY-112296
    T025
    2 Publications Verification

    CDK Apoptosis DYRK Cancer
    T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
    T025
  • HY-169678

    G Protein-coupled Receptor Kinase (GRK) Inflammation/Immunology Cancer
    GRK6-IN-5 is a GRK6 polypeptide inhibitor, with IC50 value of 4.48 μΜ. GRK6-IN-5 can be used to study hematological malignancies, inflammation diseases, and autoimmune disorders .
    GRK6-IN-5
  • HY-P10948

    WDR5 Histone Methyltransferase Cardiovascular Disease
    CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia .
    CS-VIP 8
  • HY-P10948A

    WDR5 Histone Methyltransferase Cardiovascular Disease
    CS-VIP 8 TFA is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 TFA induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 TFA is promising for research of hematological diseases such as leukemia .
    CS-VIP 8 TFA
  • HY-128231

    G Protein-coupled Receptor Kinase (GRK) Inflammation/Immunology Cancer
    GRK6-IN-4 is a G protein coupled receptor 6 kinase (GRK6) inhibitor with an IC50 of 1.56 μM. GRK6-IN-4 can be utilized in research related to hematological malignancies, inflammatory diseases, and autoimmune disorders .
    GRK6-IN-4
  • HY-147754

    Btk JAK Inflammation/Immunology
    JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research .
    JAK3/BTK-IN-6
  • HY-153953

    Bcl-2 Family Cancer
    Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor, with an IC50 of 0.9 nM. Bcl-2-IN-11 shows weak inhibition of Bcl-xl (IC50 > 1000 nM). Bcl-2-IN-11 can be used for the research of a variety of cancers caused by abnormal overexpression of Bcl-2 family proteins: especially malignant hematologic diseases of acute lymphoid leukemia, etc. Bcl-2-IN-11 can also avoid toxic side effects caused by Bcl-xl inhibition, such as thrombocytopenia .
    Bcl-2-IN-11

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