Search Result
Results for "
turnover
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-137940
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Gentiobiose
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Others
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Others
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β-Gentiobiose (Gentiobiose) is a naturally occurring oligosaccharin with a rapid turnover rate in ripening tomato fruit .
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- HY-15100
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AAE581
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Cathepsin
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Inflammation/Immunology
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Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis .
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- HY-126666
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ADC Cytotoxin
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Inflammation/Immunology
Cancer
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PNU-159682 carboxylic acid (compound 53) is a potent ADCs cytotoxin and encodes a member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily. PNU-159682 carboxylic acid has protein fold and diverse functions, such as cell adhesion, cell-cell signalling, glycoprotein turnover, and roles in inflammation and immune response .
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- HY-134640
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AUTAC4
2 Publications Verification
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AUTACs
Mitophagy
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Neurological Disease
Cancer
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AUTAC4 is a mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC4 downregulates cytosolic proteins and promotes targeted mitochondrial turnover via mitophagy .
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- HY-B0926
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Diatrizoate; Amidotrizoic acid
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Apoptosis
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Inflammation/Immunology
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Diatrizoic acid (Diatrizoate) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Diatrizoic acid induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium .
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- HY-B0926A
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Diatrizoic acid sodium salt; Sodium amidotrizoate
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Apoptosis
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Inflammation/Immunology
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Sodium diatrizoate (Diatrizoic acid sodium salt) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Sodium diatrizoate induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium .
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- HY-10294
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SB-462795
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Cathepsin
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Metabolic Disease
Cancer
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Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo .
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- HY-A0171A
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Ba-30803
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5-HT Receptor
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Neurological Disease
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Benzoctamine hydrochloride (Ba-30803) is a psychoactive agent with anti-anxiety effect. Benzoctamine hydrochloride blocks the central postsynaptic serotonin receptors and decreases 5-HT turnover in the brain .
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- HY-120506
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Others
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Others
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L-366811 is a compound with bradykinin agonist activity, with activity to stimulate phosphatidylinositol turnover and induce uterine contraction. L-366811 stimulates phosphatidylinositol turnover in rat uterine slices and induces rat uterine contraction in vitro, with moderate affinity for the [3H]BK binding site.
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- HY-111283
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(+)-AJ 76; (1S,2R)-AJ 76
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Dopamine Receptor
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Neurological Disease
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AJ-76 ((+)-AJ 76; (1S,2R)-AJ 76) is a dopamine autoreceptor antagonist. AJ-76 can increase the synthesis and turnover of dopamine in the rat brain, while having little effect on the synthesis and turnover of serotonin (5-HT) and norepinephrine. AJ-76 can also antagonize the sedative effects of low-dose apomorphine and has a weak antagonistic effect on postsynaptic dopamine receptor .
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- HY-P2799
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CPK
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Endogenous Metabolite
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Metabolic Disease
Cancer
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Creatine phosphokinase, Rabbit muscle (CPK) catalyzes the reversible reaction of creatine and ATP to form phosphocreatine and ADP. Creatine phosphokinase is a key enzyme for maintaining a constant ATP/ADP ratio during rapid energy turnover .
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- HY-B0657A
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Clodronate disodium salt
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Others
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Inflammation/Immunology
Cancer
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Clodronic acid (Clodronate) disodium salt, a first-generation bisphosphonate, is orally active osteoclastic bone resorption inhibitor. Clodronic acid disodium salt can be used in high bone turnover states, Paget ’s disease and osteolytic bone metastases .
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- HY-W276106
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Others
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Cancer
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KM02894 is an inhibitor of glutamate release. Cancer cells release high levels of glutamate, which disrupts normal bone turnover and may lead to cancer-induced bone pain. KM02894 can be used for cancer related research .
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- HY-153691
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Others
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Others
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BTB01303 is a (glutamate release) inhibitor. Cancer cells release high levels of (glutamate), which disrupts normal bone turnover and may lead to cancer-induced bone pain. BTB01303 has the potential to improve cancer-induced bone pain .
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- HY-B0926R
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Diatrizoate (Standard); Amidotrizoic acid (Standard)
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Apoptosis
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Inflammation/Immunology
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Diatrizoic acid (Standard) is the analytical standard of Diatrizoic acid. This product is intended for research and analytical applications. Diatrizoic acid (Diatrizoate) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Diatrizoic acid induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium .
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- HY-B0926AR
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Apoptosis
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Inflammation/Immunology
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Sodium diatrizoate (Standard) is the analytical standard of Sodium diatrizoate. This product is intended for research and analytical applications. Sodium diatrizoate (Diatrizoic acid sodium salt) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Sodium diatrizoate induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium .
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- HY-B0631
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Others
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Cancer
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Alendronic acid, a bisphosphonate, is a farnesyl diphosphate synthase (FDPS) inhibitor. Alendronic acid inhibits osteoclast-mediated bone resorption. Alendronic acid shows efficacy in postmenopausal osteoporosis, malignant hypercalcemia and Paget’s disease .
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- HY-A0171
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Ba-30803 free base
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Others
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Neurological Disease
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Benzoctamine is an orally active and potent psychoactive agent which possesses tranquillizing properties. Benzoctamine increases the turnover rate of catecholamines. Benzoctamine enhances the [3H]noradrenaline uptake in the rat heart. Benzoctamine also accelerated the disappearance of intracisternally injected [3H]noradrenaline .
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- HY-161774
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CD73
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Cancer
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ST80 is an inhibitor for interaction of OTUD4 and CD73. ST80 decreases CD73 protein level, increases CD73 protein turnover, reduces immune evasion of tumor cells, and thus exhibits antitumor efficacy against immunosuppressive triple-negative breast cancer (TNBC) .
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- HY-W420344
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Others
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Others
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Dehydroindapamide is the indole form of Indapamide (HY-B0259). Dehydroindapamide standard can be used to quantitatively measure the Indapamide turnover rate by CYP3A4, which was approximately 10-fold higher than that of Indoline (HY-Y0788), and slightly enhanced affinity for CYP3A4 .
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- HY-162351
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Others
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Metabolic Disease
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EBP-IN-1 (compound 11) is an inhibitor of emopamil-binding protein (EBP), a sterol isomerase in the cholesterol biosynthetic pathway. EBP-IN-1 has a long half-life in rodents and has good metabolic turnover and brain penetration properties. EBP-IN-1 enhances oligodendrocyte formation in human cortical organoids .
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- HY-14607
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HP 749
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Potassium Channel
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Neurological Disease
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Besipirdine (hydrochloride) is a potassium channel blocker with cholinergic and adrenergic activity. The cholinergic activity of Besipirdine (hydrochloride) involves stimulating phosphatidylinositol turnover and reducing potassium currents. The adrenergic activity of Besipirdine (hydrochloride) involves stimulating norepinephrine release, which is attributed to the inhibition of presynaptic α2-adrenergic receptors and the inhibition of norepinephrine uptake. Besipirdine (hydrochloride) may be used in research for Alzheimer's disease .
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- HY-W420344R
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Others
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Others
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Dehydroindapamide (Standard) is the analytical standard of Dehydroindapamide. This product is intended for research and analytical applications. Dehydroindapamide is the indole form of Indapamide (HY-B0259). Dehydroindapamide standard can be used to quantitatively measure the Indapamide turnover rate by CYP3A4, which was approximately 10-fold higher than that of Indoline (HY-Y0788), and slightly enhanced affinity for CYP3A4 .
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- HY-144325
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Cytochrome P450
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Infection
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CYP121A1-IN-1 is a potent CYP121A1 inhibitor with favorable activity against Mycobacterium tuberculosis (H37Rv MIC90∼6.25 μM, ∼2.2 μg/mL). CYP121A1-IN-1 can markedly reduce the production of mycocyclosin via inhibiting the CYP121A1 mediated turnover of cyclo(l-tyrosyl-l-tyrosyl) to mycocyclosin .
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- HY-110143
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Potassium Channel
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Neurological Disease
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CLP257 is a selective K +-Cl ? cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl ? transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally .
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- HY-111537
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Others
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Others
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rel-AZ5576 is a selective CDK9 inhibitor with the activity of downregulating Mcl-1 and MYC mRNA transcription and protein expression in diffuse large B-cell lymphoma by inhibiting CDK9, promoting MYC protein turnover, reducing MYC phosphorylation on the stable Ser62 residue and downregulating MYC transcriptional targets, inhibiting the growth of diffuse large B-cell lymphoma cell lines in vitro and in vivo and independent of the cell origin.
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- HY-141551
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Estrogen Receptor/ERR
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Cancer
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GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research .
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- HY-13777C
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CGP 42446 disodium; CGP42446A disodium; ZOL 446 disodium
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Others
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Cancer
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Zoledronate (CGP 42446) disodium is a potent bisphosphonate that effectively inhibits osteoclastogenesis, reducing bone turnover and stabilizing the bone matrix. Zoledronate disodium has demonstrated notable effectiveness in managing Paget's disease of bone by suppressing metabolic activity and alleviating bone pain. Zoledronate disodium is being investigated in the ongoing ZiPP trial for its potential to prevent disease progression in patients with Paget's disease. Zoledronate disodium also exhibits diverse anti-tumor effects in osteosarcoma, further highlighting its multifunctional therapeutic applications.
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- HY-145086
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Others
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Metabolic Disease
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R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders .
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- HY-111790
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M3258
1 Publications Verification
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Proteasome
Apoptosis
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Cancer
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M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
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- HY-103156
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5-HT Receptor
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Neurological Disease
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NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors .
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- HY-135507A
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5-HT Receptor
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Neurological Disease
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NAS181 free base is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 free base shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 free base increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors .
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- HY-136693
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Others
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Neurological Disease
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L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P3740
-
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Peptides
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Others
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Osteocalcin 30-43 Fragment is an osteocalcin fragment.Osteocalcin 30-43 Fragment is a serum marker of bone turnover .
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- HY-P5378
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Cathepsin S substrate
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Peptides
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Others
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Ac-KQKLR-AMC (Cathepsin S substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin S is a cysteine proteinase involved in the pathogenesis of autoimmune diseases, atherosclerosis, cancer, obesity and related diseases.This peptide is a cathepsin S substrate fluorescently labeled with AMC (Ex/Em=354 nm/442 nm). It can be used to measure cathepsin S activity.)
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- HY-P5377
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Cathepsin K substrate
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Peptides
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Others
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Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
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