82 Results for "

U251

" in MedChemExpress (MCE) Product Catalog:
Products (82)

82 Results for "U251" in MCE Product Catalog:

39
39 Cited Publications
Cat. No.: HY-13768
CAS No.: 123948-87-8
Synonyms: SKF 104864A; NSC 609669
Research Areas:  

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 .
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7
7 Cited Publications
Cat. No.: HY-144828
CAS No.: 2682850-41-3
Purity:  ≥97.0%
Research Areas:  

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 .
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4
4 Cited Publications
Cat. No.: HY-19939S
CAS No.: 1476074-39-1
Synonyms: M9831
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 .
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3
3 Cited Publications
Cat. No.: HY-14543
CAS No.: 106516-24-9
Purity:  99.92%
Synonyms: Lu 23-174
Sertindole (Lu 23-174) is an orally active 5-HT2A, 5-HT2C, dopamine D2, and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells .
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2
2 Cited Publications
Cat. No.: HY-107643
CAS No.: 313397-13-6
Purity:  99.90%
Synonyms: CBLC4H10
Target:  

P-glycoprotein

Research Areas:  

Cancer

Reversan (CBLC4H10) inhibits drug efflux mediated by P-glycoprotein (Pgp) and multidrug resistance protein 1 (MRP1), and exhibits oral activity. Reversan shows activity against glioblastoma multiforme and neuroblastoma models .
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2
2 Cited Publications
Cat. No.: HY-146320
CAS No.: 407587-01-3
Purity:  99.57%
Target:  

Chloride Channel

Research Areas:  

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 .
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1
1 Cited Publications
Cat. No.: HY-N6722
CAS No.: 72741-87-8
Synonyms: Tridolgosir
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 .
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1
1 Cited Publications
Cat. No.: HY-N2392
CAS No.: 75288-96-9
Kukoamine A, a spermine alkaloid, is an orally active and brain-penetrant component found in the root barks of Lycium chinense (L. chinense) Miller. Kukoamine A inhibits purified Crithidia fasciculata trypanothione reductase and soybean lipoxygenase, activates μ-opioid receptor. Kukoamine A can inhibt cancer cell proliferation, migration and invasion, cause G0/G1 phase cell cycle arrest and induce apoptosis. Kukoamine A exerts neuroprotective effect and can induce autophagy . Kukoamine A inhibits LPS (HY-D1056)-induced NO, ROS, PGE2, TNF-α, IL-1β, IL-6 production and COX-2 activity. Kukoamine A reverses palmitic acid-induced insulin resistance, lipid accumulation, and oxidative stress via downregulation of Srebp-1c. Kukoamine A can be used for the research of cancer, infection, inflammation, metabolic and neurological disease, such as glioblastoma and Parkinson's disease .
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1
1 Cited Publications
Cat. No.: HY-12833
CAS No.: 1313613-09-0
Purity:  99.76%
Target:  

Phosphatase Akt ERK

Research Areas:  

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 .
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1
1 Cited Publications
Cat. No.: HY-N1983
CAS No.: 38395-02-7
Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
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1
1 Cited Publications
Cat. No.: HY-12401A
CAS No.: 2989453-29-2
Purity:  98.04%
Target:  

Mps1

Research Areas:  

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 .
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Cat. No.: HY-163385
Target:  

DNA Methyltransferase

Research Areas:  

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 .
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Cat. No.: HY-162002
CAS No.: 2765448-96-0
Target:  

ATM/ATR

Research Areas:  

Cancer

WSD0628 is a brain penetrant and potent ATM inhibitor with profound radiosensitizing effect .
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Cat. No.: HY-B0380A
CAS No.: 34140-59-5
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) .
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Cat. No.: HY-P11287A
DOTA-Pep-1L TFA is a polypeptide formed by the conjugation of DOTA and Pep-1L. DOTA-Pep-1L TFA specifically binds to IL13RA2 and can be used for the synthesis of targeted polypeptides. DOTA-Pep-1L TFA yields the isotopically labeled product [ 225Ac]DOTA-Pep-1L, which exerts α-radiation killing effects on orthotopic glioma cells and extends the median survival time of mice bearing orthotopic glioma models after stereotactic injection. DOTA-Pep-1L TFA can be used for PET imaging, tumor targeting and glioma research .
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Cat. No.: HY-123927
CAS No.: 1809170-59-9
Purity:  96.41%
Target:  

VEGFR Ephrin Receptor

Research Areas:  

Inflammation/Immunology Cancer

UniPR1331 is an orally active 3β-hydroxy-Δ5-choline acid derivative that inhibits Eph-ephrin interactions. UniPR1331 blocks the interaction of VEGFR2 with its natural ligand vascular endothelial growth factor and inhibits subsequent autophosphorylation, signaling, and pro-angiogenic activation of endothelial cells. UniPR1331 exhibits anti-angiogenesis, anti-cancer and anti-inflammation effects. UniPR1331 can be used for the researches of cancer and inflammation, such as glioma and colitis .
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Cat. No.: HY-132302
CAS No.: 2360523-76-6
Purity:  99.91%
Research Areas:  

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 .
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Cat. No.: HY-131943
CAS No.: 2361327-08-2
Purity:  99.36%
DS44960156 is a selective MTHFD2 inhibitor with moderate to low blood-brain barrier penetration (IC50=1.6 μM, Ki=1.23 μM). DS44960156 specifically binds to the active site of MTHFD2, disrupts redox homeostasis and blocks serine-mediated one-carbon metabolism, thereby increasing the NAD +/NADH ratio and ROS levels. DS44960156 not only effectively inhibits the proliferation of glioma cells, but also enhances the sensitivity of cells to glutamine starvation-induced death. DS44960156 binds to plasma proteins, shows no mutagenicity, carcinogenicity or acute oral toxicity, and serves as a research agent for glioblastoma multiforme and other cancers .
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Cat. No.: HY-147637
CAS No.: 2611459-57-3
Purity:  99.32%
Target:  

Ephrin Receptor

Research Areas:  

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 .
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Cat. No.: HY-175207
CAS No.: 3109469-27-1
Target:  

Glycosidase

Research Areas:  

Cancer

CHI3L1-IN-3 is a CHI3L1 inhibitor. CHI3L1-IN-3 binds to CHI3L1 with Kds of 13.76 μM and 13.5 μM in MST and SPR assays, respectively. CHI3L1-IN-3 demonstrates extended plasma half-lives and microsomal stability, along with reduced intrinsic clearance. CHI3L1-IN-3 induces dose-dependent cytotoxicity, reduces spheroid mass and inhibits migration in a 3D multicellular glioblastoma (GBM) spheroid model. CHI3L1-IN-3 can be used for the study of GBM .
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