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gbm-cell

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21

Inhibitors & Agonists

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12456
    Duocarmycin SA

    		Antibiotic ADC Payload DNA Alkylator/Crosslinker Necroptosis Apoptosis Cancer
    Duocarmycin SA is an orally active antitumor antibiotic with an IC50 of 10 pM . Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro .
    Duocarmycin SA
  • HY-108476
    INDY
    2 Publications Verification

    		 DYRK Cancer
    INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .
    INDY
  • HY-162153
    CYY292

    		FGFR Cancer
    CYY292 is an FGFR1 inhibitor that specifically targets the FGFR1/AKT/Snail pathway in GBM cells. CYY292 dose-dependently inhibits cancer cell proliferation, epithelial-mesenchymal transition, stemness, invasion, and migration in vitro .
    CYY292
  • HY-124813
    PDZ1i

    113B7

    		 FAK EGFR MMP NF-κB SDCBP Cancer
    PDZ1i (113B7) is a inhibitor of MDA-9/Syntenin, with selective binding to the PDZ1 domain. PDZ1i inhibits radiation-induced invasion of glioblastoma (GBM) cells, radiosensitizes GBM cells, and impairs GBM-related signaling pathways (including Src/EphA2, EGFRvIII/FAK, and NF-κB). PDZ1i reduces radiation-induced secretion of invasion-related proteases (MMP-2, MMP-9, ADAM9). PDZ1i shows anti-tumor effects in nude mice bearing intracranial U1242-luc xenografts or GBM xenografts. PDZ1i can be used for the study of glioblastoma (GBM), breast cancer and prostate cancer .
    PDZ1i
  • HY-111187
    KX2-361

    KX-02

    		 Src Microtubule/Tubulin Apoptosis Cancer
    KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell .
    KX2-361
  • HY-155888
    IV-255

    		Epigenetic Reader Domain Cancer
    IV-255 is a selective small molecule inhibitor of the BRG1 bromodomain. IV-255 increases the extent of DNA damage induced by Temozolomide (HY-17364) and Bleomycin (HY-108345). IV-255 inhibits the invasiveness of GBM cells. IV-255 enhances Temozolomide-induced cell death and the apoptosis-inducing activity of Temozolomide .
    IV-255
  • HY-148833
    MDM2-p53-IN-16

    		MDM-2/p53 Cancer
    MDM2-p53-IN-16 is a MDM2-p53 complex inhibitor with an IC50 value of 4.3 nM to dissociate human p53/MDM2 complex. MDM2-p53-IN-16 reactivates p53, and induces Glioblastoma Multiforme (GBM) cell apoptosis and cell-cycle arrest. MDM2-p53-IN-16 can be used for the cancer research .
    MDM2-p53-IN-16
  • HY-N3001
    Isolinderalactone
    1 Publications Verification

    		 STAT VEGFR Bcl-2 Family Survivin IAP NF-κB Apoptosis Caspase Neurological Disease Inflammation/Immunology Cancer
    Isolinderalactone is a sesquiterpene that exhibits anti-cancer, anti-inflammatory, and neuroprotective effects. Isolinderalactone inhibits VEGF expression and tyrosine phosphorylation of VEGFR2. Isolinderalactone decreases viability and induces apoptosis in U-87 glioblastoma (GBM) cells and colorectal cancer (CRC) cells. Isolinderalactone induces G2/M phase cell cycle arrest, ROS generation, pJNK/p38 MAPK activation, in colorectal cancer (CRC) cells. Isolinderalactone blocks LPS (HY-D1056)-induced NF-κB activation while activating Nrf2-HMOX1 signaling in RAW264.7 macrophages. Isolinderalactone improves cognitive dysfunction in APP/PS1 mice. Isolinderalactone can be used for the study of Glioblastoma multiforme (GBM), colorectal cancer, Alzheimer’s disease and acute lung injury .
    Isolinderalactone
  • HY-144720
    BRG1-IN-1

    		SWI/SNF Complex Cancer
    BRG1-IN-1 (Compound 11d) is a potent inhibitor of SMARCA4/BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors .
    BRG1-IN-1
  • HY-114413
    YZ129

    		HSP Apoptosis Cancer
    YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell proliferation and migration .
    YZ129
  • HY-175299
    Hedgehog IN-11

    		Hedgehog Apoptosis DNA Methyltransferase Cancer
    Hedgehog IN-11 is an orally active Hedgehog inhibitor. Hedgehog IN-11 downregulates the expression of O6-methylguanine-DNA methyltransferase (MGMT) to impair the Temozolomide (TMZ) (HY-17364) resistance by inhibiting the Hedgehog pathway. Hedgehog IN-11 shows improved inhibition of cell migration and invasion, and induced cell apoptosis in TMZ-resistant GBM cell lines. Hedgehog IN-11 is predicted by computer simulation to have good blood-brain barrier penetration. Hedgehog IN-11 can be used for the study of glioblastoma (GBM) .
    Hedgehog IN-11
  • HY-13610B
    N1,N11-Diethylnorspermine hydrobromide

    		Caspase Cancer
    N1,N11-Diethylnorspermine hydrobromide is a potent anticancer agent. N1,N11-Diethylnorspermine hydrobromide is a spermine analog that activates polyamine catabolism. N1,N11-Diethylnorspermine hydrobromide induces the release of cytochrome c from mitochondria, resulting in activation of caspase 3. N1,N11-Diethylnorspermine hydrobromide kills glioblastoma multiforme (GBM) cells through induction of SSAT (spermidine/spermine N1-acetyltransferase) coupled with H2O2 production .
    N1,N11-Diethylnorspermine hydrobromide
  • HY-155580
    MAO A/HSP90-IN-2

    		Monoamine Oxidase HSP Cancer
    MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC50 values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape [1].
    MAO A/HSP90-IN-2
  • HY-N9341
    Norswertianin

    		Autophagy Cancer
    Norswertianin, a xanthone compound, serves as a powerful anti-glioma compound. Norswertianin induces GBM cells differentiation through oxidative stress and Akt/mTOR dependent autophagy .
    Norswertianin
  • HY-147789
    FPDT

    		Akt Neurological Disease Cancer
    FPDT is an anti-glioblastoma agent. FPDT displays the IC50 value of 45–68 μM for GBM cells and >100 μM for astrocytes. Anti-glioblastoma activity of FPDT is linked to downregulation of the AKT pathway .
    FPDT
  • HY-12616
    ACT-209905

    		LPL Receptor Cancer
    ACT-209905 is a S1P1 receptor agonist. ACT-209905 can inhibit glioblastoma (GBM) cell growth and migration. ACT-209905 also has immunomodulating activity, and can be used in research of autoimmune diseases .
    ACT-209905
  • HY-157168
    TrkA-IN-6

    		Trk Receptor Neurological Disease
    TrkA-IN-6 (compound R48) is a hydrazone-like, selective inhibitor of tropomyosin kinase type A receptor kinase (TrkA). TrkA-IN-6 exhibited a higher cytotoxic effect on U87 GBM cells than Temozolomide (HY-17364), with an IC50 of 68.99 μM .
    TrkA-IN-6
  • HY-155889
    IV-275

    		Epigenetic Reader Domain Cancer
    IV-275 is an inhibitor of both BRG1 and BRM bromodomains. IV-275 increases the extent of DNA damage induced by Temozolomide (HY-17364) and Bleomycin (HY-108345). IV-275 inhibits the invasiveness of GBM cells. IV-275 enhances Temozolomide-induced cell death and the apoptosis-inducing activity of Temozolomide .
    IV-275
  • HY-172586
    GSK-3α/β-IN-1

    		GSK-3 PKA Neurological Disease Cancer
    GSK-3α/β-IN-1 is GSK-3α/β inhibitor with IC50 s of 0.265 μM and 0.255 μM for GSK-3α and GSK-3β, respectively. GSK-3α/β-IN-1 also inhibits PKA with an IC50 of 0.188 μM. GSK-3α/β-IN-1 potently inhibits cell viability of three Glioblastoma (GBM) cell lines (IC50 : 3-6 μM, 72 h) with no toxicity to human astrocytes and good metabolic stability. GSK-3α/β-IN-1 has potential CNS activity in all-human blood-brain barrier (BBB) model of GBM .
    GSK-3α/β-IN-1
  • HY-170778
    Tubulin polymerization-IN-77

    		Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-77 (Compound 15c) is a tubulin polymerization inhibitor that exerts anti-glioblastoma activity by inhibiting tubulin polymerization. Tubulin polymerization-IN-77 demonstrates significant blood-brain barrier permeability, effectively inducing G2/M phase arrest and triggering apoptosis in GBM cells, while also significantly inhibiting tumor cell migration .
    Tubulin polymerization-IN-77
  • HY-108476R
    INDY (Standard)

    		Reference Standards DYRK Cancer
    INDY (Standard) is the analytical standard of INDY (HY-108476). This product is intended for research and analytical applications. INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .
    INDY (Standard)

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