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hematological diseases

" in MedChemExpress (MCE) Product Catalog:

21

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2

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1

Isotope-Labeled Compounds

Cat. No. Nombre del producto Target Áreas de investigación Chemical Structure
  • HY-15771
    Tirabrutinib
    Maximum Cited Publications
    7 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-112296
    T025
    4 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-167874

    Heme Oxygenase (HO) NF-κB Transmembrane Glycoprotein Cardiovascular Disease
    ASP-8731 is an orally active BACH1 inhibitor. ASP-8731 activates antioxidant, anti-inflammatory and globin gene pathways by relieving the inhibitory effect of BACH1 on NRF2-mediated gene transcription. ASP-8731 significantly upregulates the expression of HMOX1, FTH1 and various globins (such as HGB, HBG, HBA), increases fetal hemoglobin (HbF) levels, and effectively induces F-cell production in hydroxyurea-unresponsive cells. Meanwhile, ASP-8731 reduces inflammatory responses and white blood cell counts by downregulating VCAM1, ICAM-1 and the phosphorylation level of NF-κB(p65), and blocks heme-induced glutathione depletion and microcirculatory stasis. ASP-8731 holds potential for inhibiting sickle cell disease and related hematological disorders .
    ASP-8731
  • HY-132989

    Biochemical Assay Reagents Bacterial Cardiovascular Disease Infection Inflammation/Immunology
    Mal-Deferoxamine is a maleimide-functionalized trihydroxamate siderophore derivative that can be isolated from Streptomyces pilosus. Mal-Deferoxamine possesses highly specific Fe (III) chelating ability, and the stability of complexes formed between it and non-Fe (III) metal ions is significantly lower. Mal-Deferoxamine exhibits growth inhibitory effects against Gram-positive bacteria, but shows no obvious inhibitory activity against Gram-negative bacteria (MIC>50 μM). Mal-Deferoxamine is mainly suitable for scientific research in hematology and related fields .
    Mal-Deferoxamine
  • HY-156794

    DSP-5336

    Epigenetic Reader Domain FLT3 Cancer
    Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC50=1.4 nM, Kd=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations .
    Enzomenib
  • HY-15771A
    Tirabrutinib hydrochloride
    Maximum Cited Publications
    7 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-W058423

    Drug Intermediate MAP4K Cardiovascular Disease Inflammation/Immunology
    6-Bromo-3-fluoropyridine-2-carbaldehyde (synthetic intermediate of Compound I-90) is a synthetic intermediate. 6-Bromo-3-fluoropyridine-2-carbaldehyde can be used in the synthesis of HPK1 inhibitors. 6-Bromo-3-fluoropyridine-2-carbaldehyde is applicable to research on immune diseases and hematological diseases .
    6-Bromo-3-fluoropyridine-2-carbaldehyde
  • HY-W002314

    Environmental Pollutants Drug Intermediate Phosphatase Cardiovascular Disease
    2-Bromo-4'-hydroxyacetophenone is a PTP1B inhibitor with a Ki value of 42 μM. 2-Bromo-4'-hydroxyacetophenone is also an intermediate. 2-Bromo-4'-hydroxyacetophenone can be used in the synthesis of LXRα/β antagonists. 2-Bromo-4'-hydroxyacetophenone can be used in research on hematological diseases .
    2-Bromo-4'-hydroxyacetophenone
  • 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-W018324

    5hmC

    Endogenous Metabolite Neurological Disease Metabolic Disease Cancer
    5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) .
    5-Hydroxymethylcytosine
  • HY-P10948A

    WDR5 Histone Methyltransferase Cardiovascular Disease
    CS-VIP 8 hydrochloride is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 hydrochloride 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 hydrochloride is promising for research of hematological diseases such as leukemia .
    CS-VIP 8 hydrochloride
  • 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-177117

    MALT1 Infection Neurological Disease Cancer
    Ocipumaltib (Example 2) is an inhibitor of mucosa associated lymphoid tissue protein 1 (MALT1). Ocipumaltib is an antitumor agent. Ocipumaltib can be studied in research for cancer, infection, neurological and hematological diseases .
    Ocipumaltib
  • HY-176868

    HDAC Neurological Disease
    Rodin-C is a selective HDAC inhibitor with IC50s of 0.059, 0.18   and 5.39 μM for HDAC1, HDAC2 and HDAC11, respectively, over HDAC3-10. Rodin-C significantly inhibits the HDAC-CoREST complex with low hematological toxicity. Rodin-C can be used for neurologic disorders such as Alzheimer’s disease research .
    Rodin-C
  • 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
  • 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-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-W018324S

    5hmC-13C,d2

    Isotope-Labeled Compounds Neurological Disease
    5-Hydroxymethylcytosine- 13C,d2 is the 13C and deuterium labeled 5-Hydroxymethylcytosine (HY-W018324). 5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) .
    5-Hydroxymethylcytosine-13C,d2
  • HY-117222

    NF-κB Inflammation/Immunology Cancer
    AM-0216 is a highly selective NF-κB-inducing kinase (NIK) inhibitor with a Ki value of 2 nM. AM-0216 is promising for research of NF-κB-dependent hematologic malignancies (e.g., multiple myeloma) and autoimmune diseases .
    AM-0216
  • HY-156794A

    DSP-5336 enantiomer

    Drug Isomer FLT3 Epigenetic Reader Domain Cardiovascular Disease Cancer
    Enzomenib enantiomer (DSP-5336 enantiomer) is an enantiomer of Enzomenib (HY-156794). Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC50=1.4 nM, Kd=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations .
    Enzomenib enantiomer

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