Search Result
Results for "
U-87MG
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-116165
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Phospholipase
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Cancer
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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 .
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- HY-15398C
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Epicholecalciferol
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Hedgehog
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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 .
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- HY-156617A
-
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ADC Cytotoxin
Topoisomerase
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Cancer
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(αR)-Cyclopropaneacetamide-Exatecan (compound 2-A), an Exenotecan derivative, is a cytotoxic agent. (αR)-Cyclopropaneacetamide-Exatecan inhibits U87MG and SK-BR-3 cells proliferation, with IC50s of 8.11 and 2.31 μM .
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- HY-155439
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FAK
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Cancer
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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 .
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- HY-B2085
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Arsthinol; Balarsen
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Others
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Cancer
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Arsthinenol is an orally active antitumor agent, that exhibits cytotoxicity in U87MG cells with an IC50 of 31.6 μM. Arsthinenol forms complex with cyclodextrin, inhibits the tumor growth and improves the survival rates of U87MG xenograft mice .
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- HY-156349
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Others
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Others
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Sec61-IN-4 (Compound 16b) is a Sec61 inhibitor (IC50: 0.04 nM in U87-MG cells) .
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-
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- HY-149427
-
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PI3K
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Cancer
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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 .
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- HY-116273
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Phospholipase
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Cancer
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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 .
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- HY-147682
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NF-κB
Apoptosis
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Cancer
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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 .
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- HY-155440
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FAK
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Cancer
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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 .
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- HY-158251
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Others
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Cancer
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BIBD-300 is a PARP-1 imaging agent with high affinity for PARP-1. BIBD-300 can accurately localize C6 and U87MG tumors, which can be used for research in the diagnosis of breast cancer, prostate cancer, glioma, and liver cancer .
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- HY-157125
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PI3K
Apoptosis
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Cancer
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PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
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- HY-157876
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P-glycoprotein
BCRP
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Cancer
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Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research .
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- HY-B1490
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Serotonin Transporter
Apoptosis
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-B1490A
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Serotonin Transporter
Autophagy
Apoptosis
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Neurological Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-136479
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Others
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Cancer
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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 .
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- HY-136765
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PI3K
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Cancer
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PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.
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- HY-B1490AS
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Isotope-Labeled Compounds
Serotonin Transporter
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Neurological Disease
Inflammation/Immunology
Cancer
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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[1][2][3][4][5][6].
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- HY-B1490S
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Serotonin Transporter
Apoptosis
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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Imipramine-d4 (hydrochloride) is the deuterium labeled Imipramine hydrochloride. 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[1][2][3][4][5][6].
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- HY-B1490AS1
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Serotonin Transporter
Isotope-Labeled Compounds
Apoptosis
Autophagy
|
Others
|
Imipramine-d4 is deuterium labeled Imipramine. 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[1][2][3][4][5][6].
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- HY-B1490S1
-
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Isotope-Labeled Compounds
Serotonin Transporter
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
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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[1][2][3][4][5][6].
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- HY-B1490R
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Serotonin Transporter
Apoptosis
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-B1490AS3
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-
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- HY-124267
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SOMG-833
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c-Met/HGFR
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Cancer
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Zgwatinib (SOMG-833) is a potent, selective, and ATP-competitive c-MET inhibitor, with an IC50 of 0.93 nM against c-MET, over 10,000-fold more potent compared with 19 tyrosine kinases (including c-MET family members and highly homologous kinases). Zgwatinib potently inhibits c-MET-driven cell proliferation. Zgwatinib as a potential candidate agent for c-MET-driven human cancers research .
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- HY-156124
-
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Sigma Receptor
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Cancer
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Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts .
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- HY-117991
-
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Others
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Cancer
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DW10075 is a novel, highly selective VEGFR inhibitor that targets the VEGF/VEGF receptor (VEGFR) pathway, which has been shown to be an effective anti-angiogenic approach for cancer therapy. Studies have found that DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3 among 21 kinases, while having no effect on the other 18 kinases, including FGFR and PDGFR. In human umbilical vein endothelial cells (HUVECs), DW10075 significantly prevented VEGF-induced activation of VEGFR and its downstream signaling, thereby inhibiting VEGF-induced HUVEC proliferation. In addition, DW10075 dose-dependently inhibited VEGF-induced HUVEC migration and tube formation, and suppressed angiogenesis in the rat aortic ring model and the chick embryo chorionic membrane model. DW10075 also exhibited antiproliferative activity against 22 different human cancer cell lines, with IC50 values ranging from 2.2 μmol/L (for U87-MG human glioblastoma cells) to 22.2 μmol/L (for A375 melanoma cells). In the nude mouse U87-MG xenograft tumor model, oral administration of DW10075 significantly inhibited tumor growth and reduced the expression of CD31 and Ki67 in tumor tissues. In summary, DW10075 is a potential anti-tumor angiogenesis agent that deserves further development.
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- HY-144450
-
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PI3K
Akt
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Cancer
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PI3K-IN-29 is a potent PI3K inhibitor. PI3K-IN-29 displays good inhibition potencies against U87MG, HeLa and HL60 cells with IC50 values of 0.264, 2.04 and 1.14 µM, respectively. PI3K-IN-29 inhibits PI3K/Akt pathway by inhibiting phosphorylation of Akt that is catalyzed by PI3K .
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- HY-163691
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Carbonic Anhydrase
|
Cancer
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Antitumor agent-163 (Compound 3) is a photosensitizer used in Molecular-Targeted Photodynamic Therapy (MT-PDT) targeting carbonic anhydrase IX (CAIX). Antitumor agent-163 inactivates CAIX protein via singlet oxygen under 540 nm wavelength light, without affecting internal standard proteins such as α-tubulin, β-actin, and proliferating cell nuclear antigen (PCNA). Antitumor agent-163 induces cell membrane damage, inhibits cell viability (IC50 is 0.2 and 0.05 μM for A549 and U87MG). Antitumor agent-163 exhibits antitumor efficacy in mouse model .
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- HY-156019
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FGFR
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Cancer
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FGFR1 inhibitor-10 (Compound 4i) is an FGFR1 inhibitor (IC50: 28 nM). FGFR1 inhibitor-10 inhibits the phosphorylation of FGFR1. FGFR1 inhibitor-10 has anti-angiogenic, anti-invasion activity, and anti-tumor effect .
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- HY-P99219
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MEDI-545; MDX 1103
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IFNAR
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Inflammation/Immunology
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Sifalimumab (MEDI-545) is an anti-IFNα monoclonal antibody. Sifalimumab suppresses the abnormal immune activity by binding to multiple interferon-alpha (IFNα) subtypes. Sifalimumab can be used in systemic lupus erythematosus (SLE) research .
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- HY-13404R
-
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c-Met/HGFR
Apoptosis
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Cancer
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Capmatinib (Standard) is the analytical standard of Capmatinib. This product is intended for research and analytical applications. Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
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- HY-13404
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Capmatinib
Maximum Cited Publications
10 Publications Verification
INC280; INCB28060
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c-Met/HGFR
Apoptosis
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Cancer
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Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
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- HY-13404B
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INC280 hydrochloride; INCB-28060 hydrochloride
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c-Met/HGFR
Apoptosis
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Cancer
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Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
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- HY-13404C
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INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate
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c-Met/HGFR
Apoptosis
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Cancer
|
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .
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- HY-13404A
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INC280 dihydrochloride; INCB28060 dihydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
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- HY-161991
-
|
Caspase
Apoptosis
|
Cancer
|
Caspase-3 activator 4 (compound 4o) is a potent and cross the blood-brain barrier caspase-3 activator. Caspase-3 activator 4 shows antiproliferative activity. Caspase-3 activator 4 induces apoptosis. Caspase-3 activator 4 increases the gene expression of TNF-α. Caspase-3 activator 4 decreases the protein expression of cleaved caspases 3/caspases 3 .
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- HY-147695
-
|
c-Met/HGFR
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Cancer
|
c-Met-IN-12 (compound 4r) is an orally active, potent and selective type II c-Met kinase inhibitor, with an IC50 of 10.6 nM. c-Met-IN-12 displays high inhibitory effects (inhibition rate > 80% in 1 μM) against AXL, Mer and TYRO3 kinases. c-Met-IN-12 can be used a scaffold for further kinase selectivity enhancement. c-Met-IN-12 shows antitumor efficacy .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99219
-
MEDI-545; MDX 1103
|
IFNAR
|
Inflammation/Immunology
|
Sifalimumab (MEDI-545) is an anti-IFNα monoclonal antibody. Sifalimumab suppresses the abnormal immune activity by binding to multiple interferon-alpha (IFNα) subtypes. Sifalimumab can be used in systemic lupus erythematosus (SLE) research .
|
Cat. No. |
Product Name |
Chemical Structure |
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- HY-B1490S
-
|
Imipramine-d4 (hydrochloride) is the deuterium labeled Imipramine hydrochloride. 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[1][2][3][4][5][6].
|
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-
- HY-B1490AS
-
|
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[1][2][3][4][5][6].
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- HY-B1490AS1
-
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Imipramine-d4 is deuterium labeled Imipramine. 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[1][2][3][4][5][6].
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- HY-B1490S1
-
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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[1][2][3][4][5][6].
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- HY-B1490AS3
-
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Imipramine-d4-1 is the deuterium labeled Imipramine (HY-W010179). 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 .
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