CAS: 726169-73-9; N-(2-Aminophenyl)-4-(((4-(Pyridin-3-yl)Pyrimidin-2-yl)Amino)Methyl)Benzamide

上下游产品

CAS号849235-68-3 4-({[4-(Pyridin... | CAS号95-54-5 邻苯二胺(OPD) | CAS号849235-67-2 Methyl 4-((4-(p... | CAS号736080-30-1 Methyl 4-(guani... | CAS号55314-16-4 1-(3-吡啶基)-3-(二甲...

📜4-[[[4-(3-吡啶基)-2-嘧啶基]氨基]甲基]苯甲酸甲酯置于水,(Benzotriazo-1-Yloxy)Tris(Dimethylamino)Phosphonium Hexafluorophosphate,Lithium Hydroxide体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 48.0H,反应生成 过氧化物酶(辣根)
参考文献:Discovery Of Potent,Isoform-Selective Inhibitors Of Histone Deacetylase Containing Chiral Heterocyclic Capping Groups And A N-(2-Aminophenyl)Benzamide Binding Unit
标题:Discovery Of Potent,Isoform-Selective Inhibitors Of Histone Deacetylase Containing Chiral Heterocyclic Capping Groups And A N-(2-Aminophenyl)Benzamide Binding Unit
摘要:The Synthesis Of A Novel Series Of Potent Chiral Inhibitors Of Histone Deacetylase (Hdac) Is Described That Contain A Heterocyclic Capping Group And A N-(2-Aminophenyl)Benzamide Unit That Binds In The Active Site. In Vitro Assays For The Inhibition Of Hdac1,Hdac2,Hdac3-Ncor1,And Hdac8 By The N-(2-Aminophenyl)Benzmide 24A Gave Respective Ic50 Values Of 930,85,12,And 4100 Nm,Exhibiting Class I Selectivity And Potent Inhibition Of Hdac3-Ncor1. Both Imidazolinone And Thiazoline Rings Are Shown To Be Effective Replacements For The Pyrimidine Ring Present In Many Other 2-(Aminophenyl)Benzamides Previously Reported,An Example Of Each Ring System At 1 Mu M Causing An Increase In Histone H3K9 Acetylation In The Human Cell Lines Jurkat And Hela And An Increase In Cell Death Consistent With Induction Of Apoptosis. Inhibition Of The Growth Of Mcf-7,A549,Du145,And Hct116 Cell Lines By 24A Was Observed,With Respective Ic50 Values Of 5.4,5.8,6.4,And 2.2 Mm.
DOI:10.1021/jm400634N

专利信息

专利号:US-2025235415-A1
优先权日:2022-02-23
标 题:Modulation of human breast milk composition
发明人：ROSS MICHAEL G; DESAI MINA
权利人:LUNDQUIST INST FOR BIOMEDICAL INNOVATION AT HARBOR UCLA MEDICAL CENTER
摘要:Compositions and methods for improving a child, such as an infant's health, are provided. The methods entail improving the quality of breast milk in a female human individual that provides breast milk, or expects to provide breast milk, to the child, by administering to the individual an agent that increases the individual's sensitivity to insulin, and/or an agent that reduces the substrate uptake, synthesis or secretion of long chain fatty acids, reduces the substrate uptake, synthesis or secretion of short chain fatty acids, increases the amino acid uptake, protein synthesis or protein secretion of proteins, or reduces the uptake or synthesis of lactose.

专利号:WO-2007145934-A1
优先权日:2006-06-05
标题 :Combination of insulin and ascorbate to enhance wound healing
发明人：MUSSELMANN KURT; HASSELL JOHN R; KANE BRAD; ALEXANDROU BRIDGETTE
权利人:UNIV SOUTH FLORIDA; MUSSELMANN KURT; HASSELL JOHN R; KANE BRAD; ALEXANDROU BRIDGETTE
摘要:Provided is a method of stimulating collagen synthesis and proteoglycan (lumican and keratocan) accumulation. Collagenase isolated keratocytes were cultured with or without insulin with or without ascorbate. Insulin stimulates the synthesis of collagen but does not affect the accumulation of lumican and keratocan. Insulin plus ascorbate, however, stimulates the synthesis of collagen and increased the accumulation of these proteoglycans. The accumulation of PGDS, a KSPG that does not interact with collagen, is not affected by ascorbate. Only the collagen made in the presence of ascorbate was pepsin resistant. EDB overrode the effects of ascorbate on pepsin resistance and proteoglycan accumulation.

专利号:US-2005003521-A1
优先权日:2003-03-11
标题:Addressable microarray device, methods of making, and uses thereof
发明人：O'CONNOR DAVID; NORTON BARTON; KLEIN GERALD
摘要:The present invention relates to devices and methods for performing an array of chemical reactions. The device includes a substrate having an array of microwells. Each microwell within the array includes a porous region defined in the first side and extending partially through the substrate. The porous region is formed by the selective removal of a substrate constituent, such that the porous region is defined by a continuous portion of the substrate. A wide range of functional groups, sample molecules, and chemical moieties that can be easily introduced into the described microwells and immobilized therein, particularly onto the porous region of the substrate, therefore the devices of the present invention are useful as supports for the synthesis of compounds, such as biomolecules, and for a range of methods involving chemical reactions and assays.

专利号:US-2018150597-A1
优先权日:2016-11-29
标题 :Method for optimal design of polynucleotides sequences for analysis of specific events in any genetic region of interest
发明人：BERTHOUMIEUX SARA; FOURNE YANNICK; KOMATSU JUN; FER FREDERIC; BENSIMON AARON
权利人:GENOMIC VISION SA
摘要:Methods including in-silico steps for design and synthesis of Genomic Morse Code (“GMCâ€?) probes including design of combinations of polynucleotide sequences and labelling colors for analysis of large rearrangements in targeted genetic regions as well as allele characterization of complex regions and localization of events such as replication, DNA reparation or epigenetics in particular regions. Color-encoded sets of probes that produce characteristic or unique color patterns when painted on a target nucleic acid sequence. Methods for using color-encoded sets of probes.

专利号:US-11649285-B2
优先权日:2016-08-03
标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
发明人：KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
权利人:BIO TECHNE CORP
摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

专利号:US-7338932-B2
优先权日:2000-05-11
标题 :Methods of modulating functions of polypeptide GalNAc-transferases and of screening test substances to find agents herefor, pharmaceutical compositions comprising such agents and the use of such agents for preparing medicaments
发明人：CLAUSEN HENRIK; BENNETT ERIC PAUL; HASSAN HELLE; REIS CELSO ALBUQUERQUE
权利人:GLYCOZYM APS
摘要:Attachment of O-glycans to proteins is controlled by a large family of homologous polypeptide GalNAc-transferases. Polypeptide GalNAc-transferases contain a C-terminal sequence with similarity to lectins. This invention discloses that the putative lectin domains of GalNAc-transferase isoforms, GalNAc-T4, -T7, -T2, and -T3, are functional and recognize carbohydrates, glycopeptides, and peptides and discloses the lectin domains of GalNAc-T1-T16. These lectin domains have different binding specificities and modulate the functions of GalNAc-transferase isoforms differently. Novel methods for identification of inhibitors or modulators of binding activities mediated by lectin domains of polypeptide GalNAc-transferases are disclosed. Direct binding activity of GalNAc-transferase lectins has been demonstrated for the first time and methods to measure lectin mediated binding of isolated lectins or enzymes with lectin domains are disclosed. The present invention specifically discloses a novel selective inhibitor of polypeptide GalNAc-transferase lectin domains, which provides a major advancement in that this inhibitor and related inhibitors sharing common characteristics of activity bind lectin domains without serving as acceptor substrate for glycosyltransferases involved in synthesis of O-glycans. This inhibitor is represented by the β-anomeric configuration of GalNAc-benzyl, GalNAcβ-benzyl. Methods for inhibiting intracellular transport, cell surface expression, and secretion of mucins and O-glycosylated glycoproteins without affecting O-glycosylation processing are disclosed using the novel selective inhibitor identified.