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Results for "

U-87 cell

" in MedChemExpress (MCE) Product Catalog:

93

Inhibitors & Agonists

1

Inhibitory Antibodies

11

Natural
Products

10

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12033
    2-Methoxyestradiol
    Maximum Cited Publications
    33 Publications Verification

    2-ME2; NSC-659853

    Microtubule/Tubulin Reactive Oxygen Species (ROS) Apoptosis Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
    2-Methoxyestradiol
  • HY-B1490
    Imipramine hydrochloride
    5+ Cited Publications

    Serotonin Transporter Apoptosis Autophagy Neurological Disease Inflammation/Immunology Cancer
    Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects .
    Imipramine hydrochloride
  • HY-N0662
    Amentoflavone
    15+ Cited Publications

    Didemethyl-ginkgetin

    Reactive Oxygen Species (ROS) Apoptosis Bacterial Fungal RSV GABA Receptor Infection Neurological Disease Inflammation/Immunology Cancer
    Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase .
    Amentoflavone
  • HY-B1490A
    Imipramine
    5+ Cited Publications

    Serotonin Transporter Autophagy Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
    Imipramine
  • HY-P99250
    Onartuzumab
    2 Publications Verification

    MetMAb

    c-Met/HGFR Cancer
    Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity .
    Onartuzumab
  • HY-B0754A
    Hematoporphyrin dihydrochloride
    10+ Cited Publications

    Hematoporphyrin IX dihydrochloride

    Apoptosis Endogenous Metabolite Cancer
    Hematoporphyrin dihydrochloride (Hematoporphyrin IX dihydrochloride), a photosensitizer, is a substrate for affinity chromatography of heme-binding proteins. Hematoporphyrin dihydrochloride can induce apoptosis in U87 glioma cells and decrease tumor growth in vivo when exposed to red light .
    Hematoporphyrin dihydrochloride
  • HY-A0077
    Perphenazine
    3 Publications Verification

    Dopamine Receptor Histamine Receptor 5-HT Receptor Adrenergic Receptor Apoptosis Autophagy Neurological Disease Inflammation/Immunology Endocrinology Cancer
    Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation .
    Perphenazine
  • HY-100475
    KYP-2047
    1 Publications Verification

    Apoptosis MDM-2/p53 Prolyl Endopeptidase (PREP) Neurological Disease Inflammation/Immunology Cancer
    KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an Ki value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation .
    KYP-2047
  • HY-111449
    BAY-218
    2 Publications Verification

    AHR antagonist 1

    Aryl Hydrocarbon Receptor Inflammation/Immunology Cancer
    BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC50 of 39.9 nM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses .
    BAY-218
  • HY-B0754

    Hematoporphyrin IX

    Apoptosis Endogenous Metabolite Cancer
    Hematoporphyrin (Hematoporphyrin IX), a photosensitizer, is a substrate for affinity chromatography of heme-binding proteins. Hematoporphyrin can induce apoptosis in U87 glioma cells and decrease tumor growth in vivo when exposed to red light .
    Hematoporphyrin
  • HY-12833
    AMZ30
    1 Publications Verification

    Phosphatase Akt ERK Others
    AMZ30 is selective protein phosphatase methylesterase-1(PME-1) inhibitor with IC50s of 600 nM and 3.5 µM in human cell lysates and in HEK 293T cells, respectively. AMZ30 shows >100-fold selectivity relative to other serine hydrolases. AMZ30 reduces the demethylated form of PP2A in living cells. AMZ30 attenuates muscle cell differentiation. AMZ30 increases the resistance of U87MG and U251MG glioblastoma cells to t-BHP-induced oxidative stress. AMZ30can be used for the study of glioblastoma .
    AMZ30
  • HY-108693

    Leukotriene Receptor Apoptosis Inflammation/Immunology
    β-Tocotrienol is an isomer of vitamin E. β-Tocotrienol is a less potent antioxidant than α-tocotrienol. β-Tocotrienol can be found in the tocotrienol-rich fraction (TRF) of palm oil, which possesses anti-carcinogenic effects in vitro on human colon carcinoma and prostate cancer cells. β-Tocotrienol inhibits the growth of A549 (GI50 = 1.38 μM) and U87MG (GI50 = 2.53 μM) cells. β-Tocotrienol also induces apoptosis in cancer cells. β-Tocotrienol can inhibit PD-L1 expression and mitigates PD-L1-mediated immune suppression in vitro and in vivo .
    β-Tocotrienol
  • HY-116273

    Phospholipase Cancer
    ML299 is a selective allosteric modulator and a dual inhibitor of phospholipases D1 and D2 (IC50 values are 6 and 12 nM, respectively). ML299 decreases invasive migration in U87-MG glioblastoma cells .
    ML299
  • HY-12033S2

    2-ME2-d5; NSC-659853-d5

    Isotope-Labeled Compounds Microtubule/Tubulin Reactive Oxygen Species (ROS) Apoptosis Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol-d5 is the deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
    2-Methoxyestradiol-d5
  • HY-168708

    Histone Demethylase Apoptosis Cancer
    AH2-14c is an inhibitor for DNA demethylase ALKBH2. AH2-14c inhibits the cell viability (IC50 is 4.56 µM) and migration of GBM U87. AH2-14c regulates the expression of apoptosis-related genes, and induces apoptosis in GBM U87 cell .
    AH2-14c
  • HY-155439

    FAK Cancer
    FAK-IN-14 (compound 8d) is a focal adhesion kinase(FAK) inhibitor with an IC50 value of 0.2438 nM. FAK-IN-14 induces U87-MG cell early apoptosis and arrest the cell at the G2/M phase .
    FAK-IN-14
  • HY-149530

    EGFR Apoptosis Cancer
    EGFR-IN-86 (compound 4i) is an EGFR inhibitor (IC50: 1.5 nM) with high activity against glioblastoma. EGFR-IN-86 induces apoptosis and arrests the U87 cell cycle in the G2/M phase .
    EGFR-IN-86
  • HY-173066

    PROTACs Indoleamine 2,3-Dioxygenase (IDO) Cancer
    NU227326 is a blood-brain barrier penetrant IDO1 PROTAC degrader, with a DC50 of 4.5 nM in HiBiT degradation assays. NU227326 degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively (WB assays). NU227326 is applicable to research related to glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer .
    NU227326
  • 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-15398C

    Epicholecalciferol

    Hedgehog Cancer
    3-epi-Vitamin D3 (Epicholecalciferol) (Compound 4), a Vitamin D3 analogue, is a Hedgehog pathway inhibitor with an IC50 of 39.2 μM measured in U87MG cells .
    3-epi-Vitamin D3
  • HY-168969

    PROTACs Neurological Disease Cancer
    AA-BR-157 is a metallothionein 2A (MT2A) PROTAC degrader. AA-BR-157 increases intracellular zinc levels, downregulates DIAPH3, disrupts cytoskeleton remodeling, and reduces the migration and invasion abilities of cancer cells. AA-BR-157 can be used for research on triple-negative breast cancer and glioblastoma .
    AA-BR-157
  • HY-150401

    ADC Payload Topoisomerase Cancer
    Exatecan-amide-cyclopropanol (compound 1) is a anticancer agent. Exatecan-amide-cyclopropanol shows anti-proliferation activity against SK-BR-3 and U87 cells, with IC50 values of 0.12 and 0.23 nM, respectively .
    Exatecan-amide-cyclopropanol
  • HY-B1490R

    Reference Standards Serotonin Transporter Apoptosis Autophagy Neurological Disease Inflammation/Immunology Cancer
    Imipramine (hydrochloride) (Standard) is the analytical standard of Imipramine (hydrochloride). This product is intended for research and analytical applications. Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects .
    Imipramine hydrochloride (Standard)
  • HY-136479

    Sirtuin Cancer
    F0911-7667 is a SIRT1 activator that induces autophagic cell death in U87MG and T98G cells by activating the AMPK-mTOR-ULK complex. CWR tripeptide was also identified as a SIRT1 activator that reduced p53 acetylation in IMR32 neuroblastoma cells and protected cells from cell death induced by Aβ fragments .
    F0911-7667
  • HY-116165

    Phospholipase Cancer
    ML298 is a potent and selective inhibitor of Phospholipase D2 (PLD2) with an IC50 of 355 nM. ML298 decreases invasive migration in U87-MG glioblastoma cells .
    ML-298
  • HY-13768S1

    Isotope-Labeled Compounds Topoisomerase Autophagy Cancer
    Topotecan-d6 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95 μM of GSCs-U87 .
    Topotecan-d6
  • HY-156349

    Apoptosis Others
    Sec61-IN-4 (Compound 16b) is a Sec61 inhibitor (IC50: 0.04 nM in U87-MG cells) .
    Sec61-IN-4
  • HY-175291

    MMP Cadherin Cancer
    Cystatin B agonist 1 is an orally active MMP-2/9 inhibitor. Cystatin B agonist 1 exhibits inhibitory effects with IC50 values of 3.95 and 3.43 μM against U87 and T98G cells, respectively. Cystatin B agonist 1 induces the cell-cycle arrest at S phase, inhibits angiogenesis, and suppresses migration and invasion of MG cells. Cystatin B agonist 1 inhibits tumor growth in U87 MG xenograft model. Cystatin B agonist 1 can be used for the study of malignant glioma (MG) .
    Cystatin B agonist 1
  • HY-175213

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells .
    Mutant IDH1-IN-7
  • HY-129094

    CXCR Cancer
    ICT5040 is a small molecule CXCR4 antagonist (IC50=3.8 μM). ICT5040 inhibits CXCL12-mediated proliferation and migration, and suppresses CXCL12-induced intracellular calcium mobilisation in U87 glioma cells .
    ICT5040
  • HY-155684

    PROTACs VEGFR PDGFR Ephrin Receptor Cancer
    SA-PA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues .
    SA-PA
  • HY-12033S1

    2-ME2-13C6; NSC-659853-13C6

    Isotope-Labeled Compounds Microtubule/Tubulin Reactive Oxygen Species (ROS) Apoptosis Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
    2-Methoxyestradiol-13C6
  • HY-175530

    OLIG2 Cancer
    OLIG2-IN-1 is a potent and selective oligodendrocyte transcription factor 2 (OLIG2) inhibitor. OLIG2-IN-1 directly and dose-dependently downregulates nuclear OLIG2 levels with an IC50 value of 0.88 μM. OLIG2-IN-1 exhibits strong anti-proliferative activity in U87 and U251 cells with IC50 values of 7.02 μM and 6.43 μM, respectively. OLIG2-IN-1 can be used for the research of cancer, such as glioblastoma multiforme .
    OLIG2-IN-1
  • HY-12033S

    Isotope-Labeled Compounds Microtubule/Tubulin Reactive Oxygen Species (ROS) Apoptosis Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
    2-Methoxyestradiol-13C,d3
  • HY-B1490AS

    Isotope-Labeled Compounds Serotonin Transporter Neurological Disease Inflammation/Immunology Cancer
    Imipramine-d6 is the deuterium labeled Imipramine hydrochloride. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
    Imipramine-d6
  • HY-B1490S1

    Isotope-Labeled Compounds Serotonin Transporter Autophagy Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Imipramine-d3 (hydrochloride) is deuterium labeled Imipramine (hydrochloride). Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
    Imipramine-d3 hydrochloride
  • HY-B1490AR

    Serotonin Transporter Autophagy Apoptosis Reference Standards Neurological Disease Inflammation/Immunology Cancer
    Imipramine (Standard) is the analytical standard of Imipramine. This product is intended for research and analytical applications. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
    Imipramine (Standard)
  • HY-144808

    Microtubule/Tubulin Cancer
    Anticancer agent 40 (compound 3e) is a potent anticancer agent. Anticancer agent 40 shows anticancer activities with IC50s of 0.94, 0.98, 0.96, 0.95, 2.13 nM for SKBR-3, SKOV-3, PC-3, U-87, HDF cells, respectively .
    Anticancer agent 40
  • HY-168279

    VEGFR Cancer
    VEGF-IN-1 (compound 6) can reduce the release of VEGF in U87-MG cells and inhibit angiogenesis in vitro. VEGF-IN-1 can inhibit cell proliferation by inducing autophagy in tumor cells, with an IC50 value of 28.35 μM for U87-MG cells .
    VEGF-IN-1
  • HY-114459

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells .
    Mutant IDH1-IN-4
  • HY-146275

    LXR Cancer
    LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma .
    LXRβ agonist-3
  • HY-172159

    HDAC Apoptosis Cancer
    FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively. (Pink: PRMT5 ligand (HY-168864); Blue: E3 ligase ligand HY-W957284); Black: linker (HY-W881439); E3+linker (HY-172185 )) .
    FF2039
  • HY-170577

    Pyruvate Kinase Apoptosis Cancer
    PKM2-IN-8 (Compound 9b) is a pyruvate kinase M2 (PKM2) inhibitor (IC50 = 0.31 μM). PKM2-IN-8 has potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 can induce early apoptosis and reduce lactate levels. PKM2-IN-8 can be used for the research of glioblastoma .
    PKM2-IN-8
  • HY-168899

    FAK Apoptosis Cancer
    FAK-IN-24 (Compound 9f) is a FAK inhibitor (IC50: 0.815 nM). FAK-IN-24 induces DNA damage and apoptosis. FAK-IN-24 has anti-glioblastoma activity. FAK-IN-24 inhibits proliferation of glioblastoma cell lines U87-MG (IC50 = 15 nM) and U251 (IC50 = 20 nM). FAK-IN-24 inhibits tumor growth in U87-MG xenograft model .
    FAK-IN-24
  • HY-178178

    PARP Reactive Oxygen Species (ROS) DNA/RNA Synthesis Apoptosis Cancer
    PARP1-IN-46 is a potent PARP-1 inhibitor with an IC50 of 2.4 nM. PARP1-IN-46 demonstrates remarkable anti-proliferative activity in both rat (C6) and human (U87MG) glioma cells. PARP1-IN-46 promotes PARP cleavage, triggers DNA damage, and increases ROS. PARP1-IN-46 effectively inhibits the migration, invasion and colony formation of glioma cells, and ultimately induces cell apoptosis. PARP1-IN-46 can be used to the study of glioma .
    PARP1-IN-46
  • HY-178034

    PROTACs Oxysterol-binding Protein-related Protein (ORP) Cancer
    PROTAC OSBP Degrader-1 (Compound 5) is a Oxysterol-binding protein (OSBP) PROTAC degrader with a DC50 of 322 nM (24 h). PROTAC OSBP Degrader-1 can rapidly penetrate into cells and induce massive recruitment of OSBP at the Trans-Golgi network. PROTAC OSBP Degrader-1 has potent anticancer activity with potent cytotoxicity against U-87 MG, A549, MCF7, HeLa and MDA-MB-231 cells . Pink: OSBP ligand (HY-178035); Blue: CRBN ligase ligand (HY-10984); Black: linker
    PROTAC OSBP Degrader-1
  • HY-147682

    NF-κB Apoptosis Cancer
    NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
    NF-κB-IN-5
  • HY-149427

    PI3K Cancer
    PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
    PI3Kα-IN-12
  • HY-131065

    c-Met/HGFR Cancer
    MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity .
    MET kinase-IN-2
  • HY-155440

    FAK Cancer
    FAK-IN-15 (Compound 9b) is a focal adhesion kinase (FAK) inhibitor with an IC50 value of 0.2691 nM. FAK-IN-15 has anti-tumor activity with an IC50 value of 1.033 μM against U87-MG cells .
    FAK-IN-15

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