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U251

" in MedChemExpress (MCE) Product Catalog:

52

Inhibitors & Agonists

1

Inhibitory Antibodies

7

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N7980

    NF-κB Cancer
    Rubipodanone A, a naphthohydroquinone dimer, shows cytotoxicity against A549, BEL-7402, HeLa, HepG2, SGC-7901 and U251 cells. Rubipodanone A also shows obvious activating effect at 20 and 40 μM for NF-κB .
    Rubipodanone A
  • HY-156418

    DNA/RNA Synthesis Cancer
    KY386 is a potent, selective inhibitor of DHX33 helicase, with the IC50 of 19 nM. KY386 inhibits U251-MG cells (DHX33-overexpressing cancer cell strain) with IC50 of 20 nM.and shows potent anti-cancer activity and moderate metabolic stability .
    KY386
  • HY-163835

    Ephrin Receptor Cancer
    UniPR1454 targets EphA2 receptor, inhibits the EphA2-ephrin A1 interaction with an IC50 of 2.6 μM. UniPR1454 inhibits the proliferation of glioblastoma cell U251 .
    UniPR1454
  • HY-129932

    Drug Derivative Cancer
    Pyrrolidine ricinoleamide ((R)-5d) is a fatty acid amide that exhibits effective antiproliferative activity against a series of cancer cells, including human glioma U251 cells. Pyrrolidine ricinoleamide can be used in cancer research .
    Pyrrolidine ricinoleamide
  • HY-P991419

    VEGFR Cancer
    MSB-0254 is a human monoclonal antibody (mAb) targeting VEGFR2/KDR/CD309. MSB-0254 inhibits the invasion, migration, and vascular mimetic (VM) formation of U251 and primary glioma cells. MSB-0254 inhibits the growth of U251 and GL261 cell transplanted tumors. MSB-0254 reduces the expression of CD34, VEGFR2, Ki67, MMP2, MMP9, and CD34/PAS. MSB-0254 can be used in advanced solid tumors research .
    MSB-0254
  • HY-124242

    Drug Derivative Cancer
    (S)-α-Methylbenzyl ricinoleamide (compound (R,S)-3d) is a fatty acid amide. (S)-α-Methylbenzyl ricinoleamide shows antiproliferative activity, inhibits the growth of human ovarian cancer cells NCI-ADR/RES and glioma cells U251 with GI50s of 1.9 μg/mL and 3.6 μg/mL, respectively .
    (S)-α-Methylbenzyl ricinoleamide
  • HY-170893

    Carbonic Anhydrase Cancer
    CAIX/CAXII-IN-4 (Compound 7h) is the inhibitor for carbonic anhydrase (CA) that binds CA IX, CA XII and CA II with Ki of 1.324 μM, 0.435 μM and 3.035 μM. CAIX/CAXII-IN-4 exhibits board-spectrum antitumor efficacy, inhibits the proliferation of CNS cancer U251 with GI50 of 0.361 μM .
    CAIX/CAXII-IN-4
  • 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-13768S

    SKF 104864A-d5; NSC 609669-d5

    Isotope-Labeled Compounds Topoisomerase Autophagy Cancer
    Topotecan-d5 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±0.24 μM of GSCs-U87 .
    Topotecan-d5
  • HY-155532

    Apoptosis Cancer
    10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
    10m/ZS44
  • 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-N10871

    SARS-CoV Cancer
    Neocryptomerin, a biflavonoid, shows inhibitory activity against U251, MCF-7, HeLa cell. Neocryptomerin has favorable binding affinities in the active pocket of SARS-CoV-2. Neocryptomerin is the leading compound of rational compounds against COVID-19 .
    Neocryptomerin
  • 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-169476

    Drug Derivative Cancer
    Pyrrolidine linoleamide is a derivative of linoleic acid amide with anticancer activity. Pyrrolidine linoleamide exhibits antiproliferative activity against a range of cancer cell lines, with IC50 values of 12.0, 27.5, 7.7, 21.9, 36.6, 32.6, and 33.9 μg/mL against U251, MCF-7, NCI-ADR/RES, 786-0, NCI-H460, PC-3, and OVCAR-3 cell lines, respectively .
    Pyrrolidine linoleamide
  • HY-173431

    Dopamine Receptor Reactive Oxygen Species (ROS) Cancer
    Dopamine D4 receptor ligand 3 (Compound 16) is a dopamine D4 receptor (D4R) antagonist (pKi: 8.86). Dopamine D4 receptor ligand 3 has pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors in HEK-293T cells, respectively. Dopamine D4 receptor ligand 3 inhibits the viability of three human glioma cell lines, U87 MG, T98G, and U251 MG. Dopamine D4 receptor ligand 3 induces ROS production and mitochondrial dysfunction in glioma cells .
    Dopamine D4 receptor ligand 3
  • HY-N1107

    NSC 119993; NSC 277290; Odorigeni

    Others Cancer
    Uzarigenin (NSC 119993; NSC 277290; Odorigeni) is a carnolide can be isolated from Pergularia tomentosa and exhibits antiproliferative activity. Uzarigenin resists the proliferation of PC3 cells, HeLa cells, Calu-1 cells, MCF-7 cells and U251MG cells, with IC50 values of 0.3 μM, 3.0 μM, 8.0 μM, 6.0 μM and 6.0 μM respectively .
    Uzarigenin
  • HY-147637

    Ephrin Receptor Cancer
    EphA2 agonist 1 (Compound 7bg) is a potent EphA2 receptor agonist. EphA2 agonist 1 shows great potency and selectivity toward EphA2 overexpressed glioblastoma cells and stimulates EphA2 phosphorylation .
    EphA2 agonist 1
  • HY-129440

    PDGFR ERK Caspase Metabolic Disease Inflammation/Immunology
    N-(p-Coumaroyl) Serotonin is a selective inhibitor of PDGFRβ, ERK1/2 and caspase-8 with antioxidant, anti-atherosclerotic and anti-inflammatory properties. N-(p-Coumaroyl) Serotonin inhibits glioblastoma cells (U251MG, T98G) with IC50 of 48-81 μM, while the IC50 for normal fibroblasts is 181-197 μM. N-(p-Coumaroyl) Serotonin inhibits PDGF signaling (reducing receptor phosphorylation), blocks Ca 2+ influx, and induces apoptosis (activating caspase-8). N-(p-Coumaroyl) Serotonin can improve atherosclerosis and aortic wall enlargement, and can also be used in the study of glioblastoma .
    N-(p-Coumaroyl) Serotonin
  • HY-162002

    ATM/ATR Cancer
    WSD0628 is a brain penetrant and potent ATM inhibitor with profound radiosensitizing effect .
    WSD0628
  • HY-144828
    RIP1/RIP3/MLKL activator 1
    3 Publications Verification

    RIP kinase Mixed Lineage Kinase Necroptosis Cancer
    RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potent anti-glioma agent. RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability .
    RIP1/RIP3/MLKL activator 1
  • HY-146141

    Ephrin Receptor Cancer
    EphA2 agonist 2 (Lead compound) is a selective EphA2 agonist with antitumor activities. EphA2 agonist 2 can cross the BBB .
    EphA2 agonist 2
  • HY-163385

    DNA Methyltransferase Cancer
    ALKBH1-IN-1 (Compound 13h) is a selective ALKBH1 inhibitor, with an IC50 of 0.026 μM and 1.39 μM in the fluorescence polarization and enzyme activity assay, respectively. ALKBH1-IN-1 can modulate the level of DNA 6mA modifications. ALKBH1-IN-1 can be used to study the functions of ALKBH1 and DNA 6mA .
    ALKBH1-IN-1
  • HY-170405

    PROTACs mTOR Cancer
    YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC50=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC50=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC50 of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))
    YB-3–17
  • HY-13768

    SKF 104864A; NSC 609669

    Topoisomerase Autophagy Apoptosis Cancer
    Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity .
    Topotecan
  • HY-B0380AR

    Reference Standards Opioid Receptor Apoptosis Potassium Channel NF-κB Akt IRAK JNK Toll-like Receptor (TLR) ERK Calcium Channel Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
    Trimebutine maleate (Standard)
  • HY-N9292

    Others Cancer
    Friedelin-3,4-lactone (Compound 4) is a triterpene can be isolated from the leaves of Garcia parViflora with weak antitumor activity .
    Friedelin-3,4-lactone
  • HY-12768B

    BLZ945 dihydrochloride

    c-Fms Neurological Disease Cancer
    Sotuletinib (BLZ945) dihydrochloride is an orally active and blood-brain barrier-permeable CSF1-R-specific inhibitor (IC50=1 nM). Sotuletinib (BLZ945) dihydrochloride induces tumor cell apoptosis and effectively inhibits tumor growth in mouse models. Sotuletinib dihydrochloride can be used in cancer and amyotrophic lateral sclerosis (ALS) research .
    Sotuletinib dihydrochloride
  • HY-B0380A

    Opioid Receptor Toll-like Receptor (TLR) Calcium Channel Potassium Channel IRAK ERK JNK NF-κB Akt Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
    Trimebutine maleate
  • HY-13768C

    SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate

    Topoisomerase Apoptosis Autophagy Cancer
    Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity .
    Topotecan hydrochloride hydrate
  • HY-163290

    Fluorescent Dye Monoamine Oxidase Cancer
    HDAC-MB a probe that is activated by HDAC6 and can detect and eliminate glioma cells through activation by HDAC6. HDAC-MB reveals antimetastatic and antiproliferative properties, inhibits glioma invasion and induces cellular apoptosis .
    HDAC-MB
  • HY-154988

    MARK Neurological Disease Cancer
    MARK4 inhibitor 4 is a MARK4 inhibitor with an IC50 of 1.49 μM. MARK4 inhibitor 4 can be used in cancer and tau lesion-related research .
    MARK4 inhibitor 4
  • HY-N6722
    Swainsonine
    1 Publications Verification

    Tridolgosir

    Apoptosis Antibiotic Infection Cancer
    Swainsonine (Tridolgosir) is an natural indolizidine alkaloid, a potent and reversible α-mannosidase inhibitor. Swainsonine induces apoptosis and cell cycle arrest at G2/M phase. Swainsonine shows anti-tumor activity .
    Swainsonine
  • HY-148174

    DGK Cancer
    JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation .
    JNJ-3790339
  • HY-12401A
    Mps1-IN-3 hydrochloride
    1 Publications Verification

    Mps1 Cancer
    Mps1-IN-3 hydrochloride is a potent and selective Mps1 inhibitor with an IC50 value of 50 nM. Mps1-IN-3 hydrochloride can inhibit the proliferation of glioblastoma cells, and effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft model .
    Mps1-IN-3 hydrochloride
  • HY-168883

    Apoptosis Pyruvate Kinase Cancer
    PKM2 modulator 2 (compound C599) is a potent PKM2 inhibitor. PKM2 modulator 2 shows antiproliferative activity. PKM2 modulator 2 induces apoptosis. PKM2 modulator 2 has the potential for the research of glioblastoma .
    PKM2 modulator 2
  • HY-168882

    Apoptosis Pyruvate Kinase Cancer
    PKM2 modulator 1 (compound C998) is a potent PKM2 inhibitor. PKM2 modulator 1 shows antiproliferative activity. PKM2 modulator 1 induces apoptosis. PKM2 modulator 1 has the potential for the research of glioblastoma .
    PKM2 modulator 1
  • HY-146320
    ANO1-IN-1
    1 Publications Verification

    Chloride Channel Cancer
    ANO1-IN-1 (Compound 9c) is a selective ANO1 channel blocker with an IC50 of 2.56 μM and 15.43 μM against ANO1 and ANO2, respectively. ANO1-IN-1 suppresses strongly proliferation of glioblastoma cells .
    ANO1-IN-1
  • HY-146321

    Chloride Channel Cancer
    ANO1-IN-2 (Compound 10q) is a selective ANO1 channel blocker with an IC50 of 1.75 μM and 7.43 μM against ANO1 and ANO2, respectively. ANO1-IN-2 suppresses strongly proliferation of glioblastoma cells .
    ANO1-IN-2
  • HY-110147A

    Furin Infection
    SSM3 tetraTFA is a potent synthetic furin inhibitor with an EC50 and a Ki of 54 nM and 12 nM, respectively. SSM3 tetraTFA is able to block furin-dependent cell surface processing of anthrax protective antigen-83 in vitro .
    SSM3 tetraTFA
  • HY-160649

    Drug-Linker Conjugates for ADC Topoisomerase Cancer
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan is an agent linker conjugate for ADC, with an inhibitor for Topoisomerase Exatecan (HY-13631) with IC50 of 22 μM. MC-Gly-Gly-Phe-Gly-GABA-Exatecan targets various antibodies, exhibits cytotoxic and antitumor efficacy in vitro and in vivo .
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
  • HY-110147B

    Furin Infection
    SSM3 tetraTFA hydrate is a potent synthetic furin inhibitor with an EC50 and a Ki of 54 nM and 12 nM, respectively. SSM3 tetraTFA hydrate is able to block furin-dependent cell surface processing of anthrax protective antigen-83 in vitro .
    SSM3 tetraTFA hydrate
  • HY-161385

    Topoisomerase Cancer
    Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM .
    Topoisomerase I inhibitor 16
  • HY-19939S
    VX-984
    4 Publications Verification

    M9831

    DNA-PK Cancer
    VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
    VX-984
  • HY-120115

    Olaparib-bodipy FL

    PARP Fluorescent Dye Cancer
    PARPi-FL (Olaparib-bodipy FL) is a small-molecule fluorescent inhibitor of PARP1 that can specifically bind to PARP1. PARPi-FL can be used as a fluorescent imaging agent for tumor detection, diagnosis, and surgical guidance .
    PARPi-FL
  • HY-113916

    AT13387 lactate

    HSP Cancer
    Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC) .
    Onalespib lactate
  • HY-116107

    Necroptosis Cancer
    AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines .
    AG311
  • HY-151883

    Apoptosis MDM-2/p53 Cancer
    APE1-IN-2 (compound AP1) is a Pt(IV) proagent, targeting a critical BER protein, apurinic/apyrimidinic endonuclease 1 (APE1). APE1-IN-2 shows anticancer activity. APE1-IN-2 induces intracellular accumulation of platinum and activates DNA damage response and apoptosis signals .
    APE1-IN-2
  • HY-132302A

    Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK Cancer
    Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice .
    Hu7691 free base
  • HY-132302

    Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK Cancer
    Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice .
    Hu7691
  • HY-147409

    CDK Cancer
    Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics .
    Ulecaciclib

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