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MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50 of 0.1 and 1.2 ¦ÌM for the inhibition of proteasome and calpain, respectively. The Ki of MG132 is 4 nM. MG132 inhibits TNF-¦Á-induced NF-¦ÊB activation and I¦ÊB¦Á degradation with an IC50 of 3 µM and prevents ¦Â-secretase cleavage. MG132 induces neurite outgrowth in PC12 cells and has anticancer properties in vitro. MG132 reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. MG132 activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis.

June 21, 2017

prudect name : MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50 of 0.1 and 1.2 ¦ÌM for the inhibition of proteasome and calpain, respectively. The Ki of…

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L-663,536;1-[(4-CHLOROPHENYL)METHYL]-3-[(1,1-DIMETHYLETHYL)THIO]-ALPHA,ALPHA-DIMETHYL-5-(1-METHYLETHYL)-1H-INDOLE-2-PROPANOIC ACID;MK-886;3-[tert-Butylthio-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic Acid, Sodium Salt;1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-alpha,alpha-dimethyl-5-(1-methylethyl)-1H-indole-2-propanoic acid;3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid;3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic acid;3-[3-tert-Butylthio-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic acid

prudect name : L-663,536;1-[(4-CHLOROPHENYL)METHYL]-3-[(1,1-DIMETHYLETHYL)THIO]-ALPHA,ALPHA-DIMETHYL-5-(1-METHYLETHYL)-1H-INDOLE-2-PROPANOIC ACID;MK-886;3-[tert-Butylthio-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic Acid, Sodium Salt;1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-alpha,alpha-dimethyl-5-(1-methylethyl)-1H-indole-2-propanoic acid;3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid;3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic acid;3-[3-tert-Butylthio-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic acidMK-886 Synonyms: L-663,536CAS NO: 118414-82-7Molecular Formula: C27H33ClNO2S.NaMolecular Weight: 494.07Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com References PubMed…

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MK-0752 is a potent gamma secretase (¦Ã-secretase) inhibitor in clinical development with an IC50 of 5 nM for A¦Â40 in human SH-SY5Y cells.Defining the metabolic fate of amyloid precursor protein (APP) in the central nerve system (CNS) is critically important for the development of ¦Ã-secretase inhibitors to treat Alzheimer¡¯s disease (AD), as a substrate build-up of APP fragments could potentially lead to an overshoot in neurotoxic amyloid peptides. The lack of A¦Â rebound in the CNS could be attributed to the shunting of APP (possibly beta C-terminal fragments, e.g. C99) to ¦Ã-secretase independent degradation. MK-0752 reduced A¦Â40 in a dose-dependent manner. Dose-dependent reductions in plasma, brain and CSF A¦Â40 were observed in guinea-pigs following single oral doses of 10¨C30 mg/kg (brain IC50 = 0.44 ¦ÌM). Concentration required for 50 percent reduction of brain A¦Â40 was 318 nM and 0.15 ¦ÌM in APP-YAC and Tg2576 mice, respectively.

prudect name : MK-0752 is a potent gamma secretase (¦Ã-secretase) inhibitor in clinical development with an IC50 of 5 nM for A¦Â40 in human SH-SY5Y cells.Defining the metabolic fate of…

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HEK293 cells stably expressing the human CGRP receptor are preincubated with various concentrations of MK 3207 in the presence or absence of 50% human serum for 30 minutes at 37 °C. Isobutyl-methylxanthine (300 ¦ÌM) is added to the cells, and then they are incubated for 30 minutes at 37 °C followed by stimulation with 0.3 nM ¦Á-CGRP for 5 minutes at 37 °C. After agonist stimulation cells are washed with PBS and the intracellular cAMP concentration is measured using the cAMP SPA Biotrak direct screening assay. Dose-response curve is plotted, and IC50 value is determined.

prudect name : HEK293 cells stably expressing the human CGRP receptor are preincubated with various concentrations of MK 3207 in the presence or absence of 50% human serum for 30…

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Description: IC50 Value: 0.34uM(for K562 cell)[1] M344 is a potent HDAC inhibitor, which can also induced expression of the pro-apoptotic genes, Puma and Bax, together with the morphological features of apoptosis, in MCF-7 cells. in vitro: In contrast to the significant induction of p21(waf1/cip1) mRNA expression following treatment with M344 (10¦ÌM) for 1 or 3 days, there was a significant decrease in p53 mRNA expression, although p53 protein levels were unchanged. Similar treatment with M344 also induced expression of the pro-apoptotic genes, Puma and Bax, together with the morphological features of apoptosis, in MCF-7 cells [2]. With the addition of M344, the platinum-sensitive breast and ovarian cancer cell lines that displayed relatively high BRCA1 protein levels demonstrated significant potentiation of cisplatin cytotoxicity in association with a reduction of BRCA1 protein[3]. M344 up-regulates SMN2 protein expression in fibroblast cells derived from SMA patients up to 7-fold after 64 h of treatment [5]. in vivo: M344 was a highly effective inhibitors of histone deacetylases as potential therapeutic tools for high-risk embryonal tumors of the nervous system of childhood[4].

prudect name : Description: IC50 Value: 0.34uM(for K562 cell)[1] M344 is a potent HDAC inhibitor, which can also induced expression of the pro-apoptotic genes, Puma and Bax, together with the…

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Matrine can reduce aminotransferase, liver disease to reduce symptoms and prevent cell replication system of hepatitis B virus.

prudect name : Matrine can reduce aminotransferase, liver disease to reduce symptoms and prevent cell replication system of hepatitis B virus.Matrine Synonyms: SophocarpidineCAS NO: 519-02-8Molecular Formula: C15H24N2OMolecular Weight: 248.37Purity: ≥98%Solubility:…

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Micafungin is a semisynthetic lipopeptide substances by fungi Coleophomaempetri derived fermentation product development. Micafungin can specifically inhibit fungal cell wall component ¦Â (1,3)-D-glucan synthesis, destruction of fungal cell structure, to dissolve.

prudect name : Micafungin is a semisynthetic lipopeptide substances by fungi Coleophomaempetri derived fermentation product development. Micafungin can specifically inhibit fungal cell wall component ¦Â (1,3)-D-glucan synthesis, destruction of fungal…

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Maraviroc is a new class of oral HIV treatment drug.

prudect name : Maraviroc is a new class of oral HIV treatment drug.Maraviroc Synonyms: Selzentry, UK-427857, CelsentriCAS NO: 376348-65-1Molecular Formula: C29H41F2N5OMolecular Weight: 513.67Purity: 99%Solubility: Storage: −20°C 2 years web site:…

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prudect name : methyl 4-(2-hydroxyethoxy)-3-methoxybenzoateSynonyms: CAS NO: 21903-52-6Molecular Formula: C11H14O5Molecular Weight: 226.23Purity: 98% minSolubility: Storage:

prudect name : methyl 4-(2-hydroxyethoxy)-3-methoxybenzoate Synonyms: CAS NO: 21903-52-6Molecular Formula: C11H14O5Molecular Weight: 226.23Purity: 98% minSolubility: Storage: −20°C web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18525111

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3-(2-Chloroethyl)-3,4-Dihydro-4-Oxoimidazo[5,1-D]-1,2,3,5-Tetrazine-8-Carboxamide; Imidazo(5,1-D)-1,2,3,5-Tetrazine-8-Carboxamide,3-(2-Chloroethyl)-3,4-Dihydro-4; 3-(2-Chloroethyl)-3,4-Dihydro-4-Oxoimidazo(5,1-D)-1,2,3,5-Tetrazine-8-Carbox

prudect name : 3-(2-Chloroethyl)-3,4-Dihydro-4-Oxoimidazo[5,1-D]-1,2,3,5-Tetrazine-8-Carboxamide; Imidazo(5,1-D)-1,2,3,5-Tetrazine-8-Carboxamide,3-(2-Chloroethyl)-3,4-Dihydro-4; 3-(2-Chloroethyl)-3,4-Dihydro-4-Oxoimidazo(5,1-D)-1,2,3,5-Tetrazine-8-CarboxMitozolomide Synonyms: CAS NO: 85622-95-3 Molecular Formula: C7H7ClN6OMolecular Weight: 242.62Purity: 98% minSolubility: In DMSOStorage: −20°C 2 years web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18525082

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