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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
290 Results for "
tolerance
" in MedChemExpress (MCE) Product Catalog:
Products (290)
290 Results for "tolerance" in MCE Product Catalog:
33
33 Cited Publications
Research Areas:
NCT-503 is a blood-brain barrier-permeable, non-competitive PHGDH inhibitor with an IC50 of 2.5 μM against human PHGDH. NCT-503 reduces glucose-derived serine production and the incorporation of one-carbon units into nucleotides without decreasing PHGDH protein expression. NCT-503 prevents high selenium-induced insulin resistance in mice by regulating blood glucose and insulin levels and improving glucose tolerance, and also inhibits the growth of tumors overexpressing PHGDH. NCT-503 can be used in research related to insulin resistance and breast cancer .
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15 Cited Publications
CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes .
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14 Cited Publications
13
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Olitigaltin (TD139) is a high-affinity Galectin-3 inhibitor with a Kd value of 14 nM. Olitigaltin inhibits the activity of the AKT/β-catenin pathway, induces Apoptosis, and downregulates SREBP1 expression. Olitigaltin enhances the phosphorylation level of ERK. Olitigaltin alleviates bleomycin (HY-17565A)-induced advanced pulmonary fibrosis in mice. Olitigaltin delays the onset of diabetes, and improves glucose tolerance and serum insulin levels. Olitigaltin alleviates liver injury. Olitigaltin maintains the structure of hippocampal excitatory synapses, restores γ-wave power in the hippocampal CA1 region, inhibits hippocampal neuroinflammation, and improves cognitive function in neuroinflammation models. Olitigaltin can be used in research related to thyroid cancer, idiopathic pulmonary fibrosis, type 1 diabetes, hepatitis, and cognitive dysfunction induced by neuroinflammation .
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8 Cited Publications
Cat. No.: HY-19870
CAS No.: 920014-72-8
Synonyms: RM-493; BIM-22493; IRC-022493
Target:
Setmelanotide (RM-493) is a blood-brain barrier-permeable, selective MC4R agonist with a Ki value of 2.1 nM for hMC4R. Setmelanotide activates the CaMKK2/AMPK signaling pathway. Setmelanotide mediates body weight homeostasis, feeding regulation and energy expenditure modulation; it reduces food intake, induces weight loss, decreases obesity severity, increases daytime activity and energy expenditure, lowers levels of leptin, triglycerides, fasting insulin and diastolic blood pressure, improves insulin sensitivity, glucose tolerance and fatty liver condition, and reverses respiratory depression. Setmelanotide is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression .
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8 Cited Publications
Cat. No.: HY-19870C
CAS No.: 2759937-80-7
Synonyms: RM-493 monoacetate; BIM-22493 monoacetate; IRC-022493 monoacetate
Target:
Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology
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8 Cited Publications
Target:
SphK Dihydroceramide Desaturase 1 (DES1) Apoptosis Reactive Oxygen Species (ROS) mTOR PERK Keap1-Nrf2
Research Areas:
SKI-II is an orally active dual-target inhibitor of SphK1/2 and DES1, with Ki values of 16 µM and 0.3 µM against SphK1 and DES1, respectively. SKI-II activates the PERK-Nrf2 antioxidant pathway by stabilizing Nrf2, and synergizes with Temozolomide (HY-17364) to induce oxidative/endoplasmic reticulum stress and cancer cell death under hypoxic conditions. In vivo, SKI-II inhibits SphK activity, promotes ceramide accumulation and apoptosis, and synergizes with Cisplatin (HY-17394) to reverse drug resistance via the ras/MAPK pathway. SKI-II reduces measles virus replication by inhibiting mTORC1 activity. SKI-II binds to VCP to induce M1 polarization, enhances host tolerance to Staphylococcus aureus infection, and exerts radioprotective effects through Nrf2 activation and accelerated DNA repair. SKI-II can be used in research related to glioblastoma, acute myeloid leukemia, gastric cancer, measles virus infection, Staphylococcus aureus infection, and acute radiation syndrome .
7
Research Areas:
Quinine hydrochloride is an alkaloid extracted from cinchona bark and exhibits oral activity, acting as a potassium channel inhibitor. Quinine hydrochloride modulates the tolerance of red blood cells and presents dose-dependent toxicity and embryonic effects. Quinine hydrochloride is a typical hemolysin that directly lyses red blood cells, with cellular components of red blood cell membranes as its action targets. Quinine hydrochloride disrupts red blood cell membranes and induces hemolysis at high concentrations, while merely weakening the anti-hemolytic capacity of red blood cells at low concentrations. Quinine hydrochloride continuously reduces red blood cell tolerance after in vivo administration, and high doses can also alter blood cell counts. Quinine hydrochloride can be applied to researches related to red blood cell hemolysis, cancer and malaria .
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6 Cited Publications
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Research Areas:
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) . PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase
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6 Cited Publications
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AS2863619 is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 targets Stat5a-CDK8/19 to promote the differentiation of CD4 + T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 can be applied to research in related fields such as periodontitis-induced bone defects .
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6 Cited Publications
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Research Areas:
AS2863619 free base is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 free base targets Stat5a-CDK8/19 to promote the differentiation of CD4 + T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 free base also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 free base exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 free base can be applied to research in related fields such as periodontitis-induced bone defects .
5
Target:
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5
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5
Category:
Microorganisms Antibiotics Animal Husbandry Disease Research Antibacterial Disease Research Fields Other Antibiotics Cancer
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4
Target:
4
4
4 Cited Publications
Cat. No.: HY-N2593
CAS No.: 32507-66-7
3
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3
3 Cited Publications
Cat. No.: HY-P1291
CAS No.: 201422-03-9
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3
3 Cited Publications
Cat. No.: HY-P1291A
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
