35

NCT-503

35 Cited Publications

Cat. No.: HY-101966

CAS No.: 1916571-90-8

Purity: 99.69%

Target:

Phosphoglycerate Dehydrogenase (PHGDH)

Research Areas:

Metabolic Disease Cancer

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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14

Olitigaltin

14 Cited Publications

Cat. No.: HY-19940

CAS No.: 1450824-22-2

Synonyms: TD139; GB0139

Target:

Galectin Akt β-catenin Apoptosis ERK

Research Areas:

Neurological Disease Metabolic Disease Inflammation/Immunology Cancer

Olitigaltin (TD139) is a high-affinity Galectin-3 inhibitor with a K_d 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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14

Succinyl phosphonate trisodium salt

14 Cited Publications

Cat. No.: HY-12688A

CAS No.: 864167-45-3

Purity: ≥98.0%

Category:

Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields Cancer

Target:

Mitochondrial Metabolism Reactive Oxygen Species (ROS) Amyloid-β

Succinyl phosphonate trisodium salt is a α-Ketoglutarate Dehydrogenase Complex (KGDHC) modulator with neuroprotective activity. Succinyl phosphonate trisodium salt protects this complex, reduces cellular succinyl-CoA concentration, downregulates protein succinylation levels, and inhibits the activity of the α-ketoglutarate dehydrogenase complex. Succinyl phosphonate trisodium salt corrects hypoxic or ethanol-induced behavioral impairments, modulates exploratory behavior and emotional stress responses, and improves hypoxia tolerance. Succinyl phosphonate trisodium salt reduces glutamate excitotoxicity, restores the activity of the α-ketoglutarate dehydrogenase complex, reverses the changes in glutamate dehydrogenase and glutamine synthetase activities induced by β-amyloid (Amyloid-β), modulates cognitive function, and prevents β-amyloid-induced neuronal damage. Succinyl phosphonate trisodium salt improves microglial senescence, alleviates neuroinflammation, reactive oxygen species (ROS) production, lipid peroxidation, and the expression of proinflammatory cytokines. Succinyl phosphonate trisodium salt can be used in the research of Alzheimer's disease, aging-related neuroinflammation, and Parkinson's disease .

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8

Setmelanotide

8 Cited Publications

Cat. No.: HY-19870

CAS No.: 920014-72-8

Synonyms: RM-493; BIM-22493; IRC-022493

Target:

Melanocortin Receptor Calmodulin AMPK

Setmelanotide (RM-493) is a blood-brain barrier-permeable, selective MC4R agonist with a K_i 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

Setmelanotide monoacetate

8 Cited Publications

Cat. No.: HY-19870C

CAS No.: 2759937-80-7

Synonyms: RM-493 monoacetate; BIM-22493 monoacetate; IRC-022493 monoacetate

Target:

Melanocortin Receptor Calmodulin AMPK

Research Areas:

Cardiovascular Disease Metabolic Disease Inflammation/Immunology

Setmelanotide monoacetate (RM-493 monoacetate) is a blood-brain barrier-permeable, selective MC4R agonist with a K_i value of 2.1 nM for hMC4R. Setmelanotide monoacetate activates the CaMKK2/AMPK signaling pathway. Setmelanotide monoacetate 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 monoacetate is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression .

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8

SKI II

8 Cited Publications

Cat. No.: HY-13822

CAS No.: 312636-16-1

Purity: 99.25%

Target:

SphK Dihydroceramide Desaturase 1 (DES1) Apoptosis Reactive Oxygen Species (ROS) mTOR PERK Keap1-Nrf2

Research Areas:

Infection Neurological Disease Cancer

SKI-II is an orally active dual-target inhibitor of SphK1/2 and DES1, with K_i 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 .

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7

Quinine (hydrochloride)

7 Cited Publications

Cat. No.: HY-110082

CAS No.: 130-89-2

Target:

Flavivirus Dengue Virus Parasite Potassium Channel

Research Areas:

Cardiovascular Disease Infection Cancer

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

PS10

6 Cited Publications

Cat. No.: HY-121744

CAS No.: 1564265-82-2

Purity: 98.51%

Target:

PDHK

Research Areas:

Inflammation/Immunology

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 (K_d= 239 nM) than for Hsp90 (K_d= 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

AS2863619

6 Cited Publications

Cat. No.: HY-126675A

CAS No.: 2241300-51-4

Purity: 99.94%

Target:

STAT CDK Apoptosis TGF-beta/Smad

Research Areas:

Inflammation/Immunology

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

AS2863619 free base

6 Cited Publications

Cat. No.: HY-126675

CAS No.: 2241300-50-3

Purity: 99.68%

Target:

CDK TGF-beta/Smad Apoptosis STAT

Research Areas:

Inflammation/Immunology

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 .

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5

PKA Inhibitor Fragment (6-22) amide

5 Cited Publications

Cat. No.: HY-P1290

CAS No.: 121932-06-7

Synonyms: PKI-(6-22)-amide

Target:

PKA

Research Areas:

Neurological Disease

PKA Inhibitor Fragment (6-22) amide is a highly potent and specific competitive inhibitor of PKA, with K_i values of 1.7 nM and 1.6 nM against human and bovine PKA catalytic subunits, respectively. The IC₅₀ of PKA Inhibitor Fragment (6-22) amide targeting bovine PKA is 8.6 nM. PKA Inhibitor Fragment (6-22) amide effectively abolishes PKA activity in mouse brain and spinal cord, and exerts in vivo efficacy via intracerebroventricular administration. PKA Inhibitor Fragment (6-22) amide significantly reverses low-dose morphine analgesic tolerance in mice and blocks photoaffinity labeling of cAMP-dependent protein kinase. PKA Inhibitor Fragment (6-22) amide can be applied to research in fields related to the mechanism of morphine analgesic tolerance and skin wound healing .

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5

PKA Inhibitor Fragment (6-22) amide TFA

5 Cited Publications

Cat. No.: HY-P1290A

Synonyms: PKI-(6-22)-amide TFA

Target:

PKA

Research Areas:

Neurological Disease

PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a K_i of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice .

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