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K-562 leukemia cells

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14

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3

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1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-125771

    18:0 Lyso-PC; LPC(18:0)

    Endogenous Metabolite HDAC STAT Apoptosis Cancer
    1-Stearoyl-sn-glycero-3-phosphocholine is a lysophosphatidylcholine that inhibits HDAC3 activity and phosphorylation of STAT3 in K562 cells. 1-Stearoyl-sn-glycero-3-phosphocholine induces apoptosis and exhibits anticancer activity in chronic myelogenous leukemia (CML) K562 cells .
    1-Stearoyl-sn-glycero-3-phosphocholine
  • HY-N3584
    Paris saponin VII
    4 Publications Verification

    Chonglou Saponin VII

    Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Apoptosis Cancer
    Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
    Paris saponin VII
  • HY-G0017
    N-Desmethyl imatinib
    1 Publications Verification

    Norimatinib; Imatinib metabolite N-Desmethyl imatinib; CGP 74588

    Drug Metabolite P-glycoprotein Apoptosis Neurological Disease Cancer
    N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib
  • HY-147831

    Eukaryotic Initiation Factor (eIF) Epigenetic Reader Domain Cancer
    HR-19011 is an eIF2α phosphorylation activator targeting heme-regulated inhibitor HRI (EIF2AK1). HR-19011 exhibits growth inhibitory activity against K562 cells with an IC50 value of 3.91 µM. HR-19011 inhibits the growth of hematologic malignancies by targeting HRI to activate the integrated stress response via the HRI-eIF2α-ATF4 axis. HR-19011 shows good safety in vivo. HR-19011 can be used for research on hematologic malignancies (leukemia) .
    HR-19011
  • HY-149470

    Histone Acetyltransferase Cancer
    MOZ-IN-3 (Compound 6j) is a KAT6A (MOZ) acetyltransferase inhibitor (IC50: 30 nM). MOZ-IN-3 has antitumor activity against four different myeloid leukemia cell lines (HL-60, U937, SKNO-1, K562). MOZ-IN-3 has favorable metabolic stability and pharmacokinetics .
    MOZ-IN-3
  • HY-103274

    Bcr-Abl Src c-Kit Apoptosis Neurological Disease Cancer
    PD180970 is a highly potent and ATP-competitive p210 Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210 Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research .
    PD180970
  • HY-114570
    Tiazofurin
    1 Publications Verification

    NSC 286193; Riboxamide

    Nucleoside Antimetabolite/Analog Orthopoxvirus Infection Neurological Disease Cancer
    Tiazofurin (NSC 286193) is a synthetic nucleoside analogue with antineoplastic activity. Tiazofurin is anabolized intracellularly to tiazole-4-carboxamide adenine dinucleotide (TAD), a potent inhibitor of IMP dehydrogenase (IMPDH). Tiazofurin enhances the autosecretion of IL-6 in K562 cells. Tiazofurin also has anti-orthopoxvirus and anti-variola activities. Tiazofurin can be used for the study of leukemia and lung cancer .
    Tiazofurin
  • HY-125834

    PROTACs Bcr-Abl Apoptosis STAT JAK Cancer
    GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .
    GMB-475
  • HY-116392D

    Glucosylceramide Synthase (GCS) Apoptosis Cancer
    PDMP hydrochloride is a glucosylceramide synthase (GCS) inhibitor. PDMP hydrochloride induces apoptosis in K562/A02 cells. PDMP hydrochloride can be used in cancer (such as leukemia) research .
    PDMP hydrochloride
  • HY-N10678

    Others Cancer
    R-30-Hydroxygambogic acid is polyprenylated xanthone epimer that can be isolated from gamboges of Garcinia hanburyi. R-30-Hydroxygambogic acid shows cytotoxicities to Human Leukemia K562 cell lines of IC50 values of 2.89 and 1.27 μM for K562/R and K562/S, respectively. R-30-Hydroxygambogic acid can be used for the research of cancer .
    R-30-Hydroxygambogic acid
  • HY-108969

    NSC 366140; PD 115934

    Topoisomerase Apoptosis Cancer
    Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment .
    Pyrazoloacridine
  • HY-17563R

    Deoxyguanosine (Standard); Guanine deoxyriboside (Standard)

    Reference Standards Endogenous Metabolite Cancer
    2'-Deoxyguanosine (Standard) is the analytical standard of 2'-Deoxyguanosine. This product is intended for research and analytical applications. 2’-Deoxyguanosine (Deoxyguanosine) is a purine nucleoside with a variety of biological activities. 2’-Deoxyguanosine can induce DNA division in mouse thymus cells. 2’-Deoxyguanosine is a potent cell division inhibitor in plant cells . In Vitro: 2'-Deoxyguanosine inhibits the clonal growth of HL-60 and K562 leukemia cells with IC50 values of 50 and 80 μM, respectively .
    2'-Deoxyguanosine (Standard)
  • HY-G0017S

    Norimatinib-d8; Imatinib metabolite N-Desmethyl imatinib-d8; CGP 74588-d8

    Isotope-Labeled Compounds Drug Metabolite P-glycoprotein Apoptosis Neurological Disease Cancer
    N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib-d8
  • HY-163854

    HSP Bcl-2 Family Apoptosis Cancer
    HSP70-IN-6 (Compound JL-15) is an inhibitor of Hsp70-Bim protein-protein interaction (PPI) (IC50: 70 nM). HSP70-IN-6 induces apoptosis in chronic myeloid leukemia (CML) cells, with EC50s of 0.43 μM(BV173), 0.88 μM (K562), 0.19 μM (K562-R3) .
    HSP70-IN-6
  • HY-W231513

    MASTL Ser/Thr Protease Aurora Kinase Cancer
    MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC50 values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis .
    MASTL/Aurora A-IN-1
  • HY-125771S

    18:0 Lyso-PC-d35; LPC(18:0)-d35

    Isotope-Labeled Compounds Endogenous Metabolite HDAC STAT Apoptosis Cancer
    1-Stearoyl-sn-glycero-3-phosphocholine-d35 is deuterium labeled 1-Stearoyl-sn-glycero-3-phosphocholine (HY-125771). 1-Stearoyl-sn-glycero-3-phosphocholine is a lysophosphatidylcholine that inhibits HDAC3 activity and phosphorylation of STAT3 in K562 cells. 1-Stearoyl-sn-glycero-3-phosphocholine induces apoptosis and exhibits anticancer activity in chronic myelogenous leukemia (CML) K562 cells .
    1-Stearoyl-sn-glycero-3-phosphocholine-d35
  • HY-169021

    JNK Cancer
    JNK-1-IN-3 (Compound 9e) is an inhibitor of JNK1 that downregulates JNK1 gene expression and inhibits the protein levels of its phosphorylated form, concurrently reducing the expression of its downstream targets, c-Jun and c-Fos, in tumors while restoring p53 activity. JNK-1-IN-3 exhibits broad-spectrum antiproliferative activity, particularly with high inhibitory activity against renal and breast cancer cell lines, demonstrating both in vivo and in vitro anticancer activity .
    JNK-1-IN-3
  • HY-129592

    Apoptosis Cancer
    p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
    p-Tolylmaleimide
  • HY-162658

    HDAC Apoptosis Cancer
    Leuxinostat is an inhibitor for HDAC with IC50 of 30 nM for hHDAC6. Leuxinostat inhibits the proliferation of cells THP1, K562, U937 and MEK1, induces apoptosis in leukemia cells NB4 and MOLT-4. Leuxinostat inhibits the expansion of hematopoietic stem cells and exhibits antileukemic activity in zebrafish models .
    Leuxinostat
  • HY-122359A

    rel-L-Centchroman; Ormeloxifene

    Estrogen Receptor/ERR Apoptosis Reactive Oxygen Species (ROS) Cancer
    rel-Levormeloxifene (rel-L-Centchroman) is the relative configuration of Levormeloxifene (HY-122359). rel-Levormeloxifene is a selective estrogen receptor modulator (SERM). rel-Levormeloxifene inhibits proliferation of leukemia cells with IC50 about 7 μM, arrests cell cycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells .
    rel-Levormeloxifene
  • HY-179247

    Bcr-Abl Cancer
    BCR-ABL1-IN-2 (compound 8) is a potent BCR-ABL1 tyrosine kinase inhibitor. BCR-ABL1-IN-2 exhibits activity in Imatinib (HY-15463) resistant K562/DOX cells with LC50 of 5.29 μM. BCR-ABL1-IN-2 shows no significant toxicity in nontumor cells. BCR-ABL1-IN-2 can be used for chronic myeloid leukemia research .
    BCR-ABL1-IN-2
  • HY-116971

    Histone Methyltransferase Apoptosis Cancer
    DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562 .
    DCG066
  • HY-177768

    HDAC Apoptosis Cancer
    HDAC-IN-96 (Compound 3f) is a selective HDAC1/2 inhibitor with IC50 values of 457.1 and 433.7 nM. HDAC-IN-96 has strong inhibitory activity against multiple hematological tumor cells (RS4;11, K562, RPMI-8226, U266), with IC50 values ranging from 2.11 to 5.35 μM. HDAC-IN-96 can induce cancer cells apoptosis and S phase arrest. HDAC-IN-96 can be used for the research of cancer, such as acute lymphoblastic leukemia .
    HDAC-IN-96
  • HY-N15582

    Apoptosis Inflammation/Immunology Cancer
    Perezone is a sesquiterpenoid benzoquinone found in the roots of Acourtia species. Perezone inhibits the activity of leukemia cell line K-562 and human glioma cell line U-251 (IC50: 6.83 μM). Perezone increases the expression of caspase 3, 8, and 9 genes associated with apoptosis. Perezone has antioxidant and anti-inflammatory activities .
    Perezone
  • HY-N10677

    Others Cancer
    S-30-Hydroxygambogic acid is polyprenylated xanthone epimer that can be isolated from gamboges of Garcinia hanburyi. S-30-Hydroxygambogic acid shows cytotoxicities to Human Leukemia K562 cell lines of IC50 values of 4.49 and 3.61 μM for K562/R and K562/S, respectively. S-30-Hydroxygambogic acid can be used for the research of cancer .
    S-30-Hydroxygambogic acid
  • HY-170323

    Apoptosis Cancer
    4-TM.P binds to the minor groove of DNA, inhibits proliferation of cancer cell K562 with an IC50 of 25 µM, arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell K562. 4-TM.P can be used in anti-leukemia research .
    4-TM.P
  • HY-149805

    Apoptosis Cancer
    Anticancer agent 110 is an anticancer agent with in vitro anticancer activity and excellent anti-leukemia potency. Anticancer agent 110 is highly cytotoxic to K-562 lineage chronic myelogenous leukemia cells at nanomolar concentrations. Anticancer agent 110 causes DNA damage and leads to apoptosis .
    Anticancer agent 110
  • HY-157483

    P-glycoprotein Cancer
    P-gp inhibitor 18 (compound 6G) is a potent inhibitor of P-gp. P-gp inhibitor 18 inhibits rhodamine 123 efflux in the P-gp overexpressed leukemia cells, K562/Dox .
    P-gp inhibitor 18
  • HY-157484

    P-glycoprotein Cancer
    P-gp inhibitor 19 (Compound 6i) is a P-gp inhibitor. P-gp inhibitor 19 can inhibit the efflux of rhodamine 123 (HY-D0816) in P-gp-overexpressing leukemia cells K562/Dox and also restore the sensitivity of DOX-resistant cells .
    P-gp inhibitor 19
  • HY-158968

    MDM-2/p53 Cancer
    MMs02943764 is a 1,2,4-triazole derivative with anticancer activity. MMs02943764 has significant antiproliferative effects on multiple cancer cell lines. PAC, a structural analog of MMs02943764, has significant cytotoxicity against the leukemia cell line K562 (IC50=35.264 μM), reduces the degradation of p53 by inhibiting Mdm2 and Pirh2, and induces K562 cell cycle arrest .
    MMs02943764
  • HY-N1056

    Zerumbetol

    Others Cancer
    Yunnancoronarin A (Zerumbetol) can be isolated from Hedychium forrestii. Yunnancoronarin A is cytotoxic, with IC50 values of 11.08 and 2.19 μM against lung adenocarcinoma cells A549 and leukemia cells K562, respectively .
    Yunnancoronarin A
  • HY-126556

    Microtubule/Tubulin Cancer
    Cytochalasin J is a cytochalasin detivative. Cytochalasin J affects mitotic spindel microtubule organization and kinetochore structure, and exhibits cytotoxicity in human leukemia K562 cell with IC50 of 1.5 μM .
    Cytochalasin J
  • HY-169608

    Bcr-Abl Cancer
    BCR-ABL-IN-11 (Compound 2) is a BCR-ABL inhibitor. BCR-ABL-IN-11 shows anticancer activity against chronic myelogenous leukemia (CML) (IC50 of 129.61 μM for K562 cells) .
    BCR-ABL-IN-11
  • HY-10212A

    CNF2024 mesylate

    HSP β-catenin c-Myc Autophagy Cancer
    BIIB021 (CNF2024) mesylate is the mesylate of BIIB021 (HY-10212). BIIB021 is an orally active Hsp90 inhibitor. BIIB021 inhibits the proliferation of chronic myeloid leukemia (CML) cells, with IC50 values of K562, K562/G, 32Dp210, and 32Dp210-T315I cells are 513.99, 603.53, 110.08, and 148.07 nM, respectively. BIIB021 degrades BCR-ABL protein and inhibits the β-catenin/c-Myc pathway. BIIB021 can also induce autophagy in CML cells. BIIB021 can be used for the research of CML .
    BIIB021 mesylate
  • HY-155522

    Carbonic Anhydrase Cancer
    WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
    WES-1
  • HY-N3584R

    Chonglou Saponin VII (Standard)

    Reference Standards Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Apoptosis Cancer
    Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
    Paris saponin VII (Standard)
  • HY-16958R

    Antibiotic Dimethylargininase (DDAH) Reference Standards Inflammation/Immunology
    Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
    PD 404182 (Standard)
  • HY-162489

    Bcr-Abl Others
    Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI). Tyrosine kinase-IN-8 shows anti-proliferative activity against K562 cells, a chronic myeloid leukemia (CML) cell line (CC50=0.8 µM). Tyrosine kinase-IN-8 can be used in the study of chronic leukemia .
    Tyrosine kinase-IN-8
  • HY-108969R

    NSC 366140 (Standard); PD 115934 (Standard)

    Topoisomerase Apoptosis Reference Standards Cancer
    Pyrazoloacridine (Standard) is the analytical standard of Pyrazoloacridine. This product is intended for research and analytical applications. Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment .
    Pyrazoloacridine (Standard)
  • HY-117285

    Lactoquinomycin A; LQM-A

    Antibiotic Bacterial Infection Cancer
    Lactoquinomycin A is a quinone antibiotic. Lactoquinomycin A has the activity of anti-Gram-positive bacteria and some Gram-negative bacteria, but the effect of anti-Gram-negative bacteria is weak and has no effect on fungi. Lactoquinomycin A inhibits a variety of cell lines including lymphoma L5178Y progenitor, Adriamycin resistant, Bleomycin-resistant, human leukemia K562, mouse leukemia L-1210 and mouse leukemia P 388 with ID50 (μg/mL) of 0.02, 0.006, 0.008, 0.033, 0.013 and 0.03, respectively .
    Medermycin
  • HY-N14774

    Antibiotic Bacterial Infection
    Lactoquinomycin B is a quinone antibiotic. Lactoquinomycin B has the activity of anti-Gram-positive bacteria and some Gram-negative bacteria, but the effect of anti-Gram-negative bacteria is weak and has no effect on fungi. Lactoquinomycin B inhibits a variety of cell lines including lymphoma L5178Y progenitor, Adriamycin resistant, Bleomycin-resistant, human leukemia K562, mouse leukemia L-1210 and mouse leukemia P 388 with ID50 (μg/mL) of 0.43, 0.21, 0.19, 0.16, 0.2 and 0.12, respectively .
    Lactoquinomycin B
  • HY-170604

    MMP Cardiovascular Disease Cancer
    MMP-2 Inhibitor-4 (Compound 5g) is an MMP-2 inhibitor with an IC50 of 152.62 nM. MMP-2 Inhibitor-4 can reduce the levels of MMP-2 in the K562 cell line through stable binding at the MMP-2 active site, and it demonstrates strong antiangiogenic effects in the ACHN cell line. MMP-2 Inhibitor-4 holds promise for research in chronic myeloid leukemia (CML) .
    MMP-2 Inhibitor-4
  • HY-125322

    Bacterial Infection
    Reveromycin C is a polyketide originally isolated from Streptomyces that has antifungal activity against C. albicans (MICs=2.0 and >500 μg/mL at pH 3 and 7.4, respectively). Reveromycin C inhibits EGF-induced mitogenic activity in the Balb/MK mouse epidermal cell line. It also reverses the morphology of sarcoma-virus-transformed NRK rat kidney cells (EC50=1.58 μg/mL) and inhibits proliferation of KB cells and K562 human chronic myelogenous leukemia cells (IC50=2.0 μg/mL for both).
    Reveromycin C
  • HY-128634

    Apoptosis PI3K MEK Cancer
    CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer .
    Anticancer agent 164
  • HY-G0017A

    Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate; CGP 74588 mesylate

    Drug Metabolite P-glycoprotein Apoptosis Neurological Disease Cancer
    N-Desmethyl imatinib mesylate (Norimatinib mesylate) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib mesylate binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib mesylate induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib mesylate exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib mesylate can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib mesylate
  • HY-G0017S1

    Norimatinib-d4; Imatinib metabolite N-Desmethyl imatinib-d4; CGP 74588-d4

    Isotope-Labeled Compounds Drug Metabolite P-glycoprotein Apoptosis Neurological Disease Cancer
    N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib-d4
  • HY-G0017R

    Norimatinib (Standard); Imatinib metabolite N-Desmethyl imatinib (Standard); CGP 74588 (Standard)

    Reference Standards Drug Metabolite P-glycoprotein Apoptosis Others
    N‑Desmethyl imatinib (Standard) is the analytical standard of N‑Desmethyl imatinib (Norimatinib) (HY-G0017R). This product is intended for research and analytical applications. N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib (Standard)
  • HY-180968

    PROTACs Bcr-Abl Cancer
    GMB-805 is a BCR-Abl PROTAC degrader with a DC50 of 30 nM in K562 cells. GMB-805 exerts antiproliferative activity in K562 cells. GMB-805 exhibits potent anti-tumor activity with favorable safety profile in vivo. GMB-805 can be used for chronic myeloid leukemia research .
    GMB-805
  • HY-180963

    PROTACs Bcr-Abl Cancer
    Lys-PEG1-Dasa is a BCR-ABL PROTAC degrader with an DC50 of 0.98 nM in K562 cells. Lys-PEG1-Dasa exerts growth inhibitory with IC50 of 0.4569 nM in K562 cells. Lys-PEG1-Dasa can be used for chronic myeloid leukemia research .
    Lys-PEG1-Dasa
  • HY-180969

    PROTACs Bcr-Abl Cancer
    SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. SIAIS056 time-dependently inhibits the BCR-ABL signaling pathway, accompanied by decreased phosphorylation of BCR-ABL and the downstream molecules STAT5 and CRKL in K562 cells. SIAIS056 induces the degradation of several clinically relevant resistance-conferring mutations of BCR-ABL. SIAIS056 exhibits anti-proliferative activity and induces substantial tumor regression in K562 xenograft models. SIAIS056 can be used for leukemia research .
    SIAIS056

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