Tag: 400-500

Functionally defined therapeutic targets in diffuse intrinsic pontine glioma [Erratum to document cited in CA163:294035] was written by Grasso, Catherine S.;Tang, Yujie;Truffaux, Nathalene;Berlow, Noah E.;Liu, Lining;Debily, Marie-Anne;Quist, Michael J.;Davis, Lara E.;Huang, Elaine C.;Woo, Pamelyn J.;Ponnuswami, Anitha;Chen, Spenser;Johung, Tessa B.;Sun, Wenchao;Kogiso, Mari;Du, Yuchen;Qi, Lin;Huang, Yulun;Hutt-Cabezas, Marianne;Warren, Katherine E.;Le Dret, Ludivine;Meltzer, Paul S.;Mao, Hua;Quezado, Martha;van Vuurden, Dannis G.;Abraham, Jinu;Fouladi, Maryam;Svalina, Matthew N.;Wang, Nicholas;Hawkins, Cynthia;Nazarian, Javad;Alonso, Marta M.;Raabe, Eric H.;Hulleman, Esther;Spellman, Paul T.;Li, Xiao-Nan;Keller, Charles;Pal, Ranadip;Grill, Jacques;Monje, Michelle. And the article was included in Nature Medicine (New York, NY, United States) in 2015.HPLC of Formula: 1373423-53-0 The following contents are mentioned in the article:

This article was published with four typog. errors in the text; the corrections are given. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0HPLC of Formula: 1373423-53-0).

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.HPLC of Formula: 1373423-53-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

An epigenetic therapy for diffuse intrinsic pontine gliomas was written by Ramaswamy, Vijay;Remke, Marc;Taylor, Michael D.. And the article was included in Nature Medicine (New York, NY, United States) in 2014.Electric Literature of C24H27N5O2 The following contents are mentioned in the article:

A review. Diffuse intrinsic pontine glioma is a uniformly lethal malignant tumor of infancy with no effective therapies. A new study reveals that inhibition of JMJD3 has robust antitumor activity in diffuse intrinsic pontine glioma xenografts. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0Electric Literature of C24H27N5O2).

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Electric Literature of C24H27N5O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Inhibition of demethylases by GSK-J1/J4 was written by Kruidenier, Laurens;Chung, Chun-wa;Cheng, Zhongjun;Liddle, John;Che, KaHing;Joberty, Gerard;Bantscheff, Marcus;Bountra, Chas;Bridges, Angela;Diallo, Hawa;Eberhard, Dirk;Hutchinson, Sue;Jones, Emma;Katso, Roy;Leveridge, Melanie;Mander, Palwinder K.;Mosley, Julie;Ramirez-Molina, Cesar;Rowland, Paul;Schofield, Christopher J.;Sheppard, Robert J.;Smith, Julia E.;Swales, Catherine;Tanner, Robert;Thomas, Pamela;Tumber, Anthony;Drewes, Gerard;Oppermann, Udo;Patel, Dinshaw J.;Lee, Kevin;Wilson, David M.. And the article was included in Nature (London, United Kingdom) in 2014.Computed Properties of C24H27N5O2 The following contents are mentioned in the article:

Our result sshow that GSK-J1 and GSK-J4 inhibit demethylases in addition to KDM6B and KDM6A. Therefore,this compound can not be used alone for demonstrating a role for H3K27 demethylationin biol. processes. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0Computed Properties of C24H27N5O2).

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Computed Properties of C24H27N5O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Inhibition of demethylases by GSK-J1/J4 was written by Heinemann, Bo;Nielsen, Jesper Morten;Hudlebusch, Heidi Rye;Lees, Michael J.;Larsen, Dorthe Vang;Boesen, Thomas;Labelle, Marc;Gerlach, Lars-Ole;Birk, Peter;Helin, Kristian. And the article was included in Nature (London, United Kingdom) in 2014.Reference of 1373423-53-0 The following contents are mentioned in the article:

The recent publication, by Kruidenier, L. etal. ibid 488 (2012), of the first highly potent and specific inhibitor GSK-J1/J4 of the H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A provides a potential tool compound for this histone demethylase subfamily. The inhibitor is not specific for the H3K27me3/me2-demethylase subfamily in vitro and in tissue culture assays. Thus, the inhibitor cannot be used alone for drawing conclusions regarding the specific role of H3K27me3/me2-demethylase activity in biol. processes or disease. The authors’ results show that GSK-J1 and GSK-J4 inhibit demethylases in addition to KDM6B and KDM6A. Therefore, this compound cannot be used alone for demonstrating a role for H3K27 demethylation in biol. processes. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0Reference of 1373423-53-0).

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Reference of 1373423-53-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Functionally defined therapeutic targets in diffuse intrinsic pontine glioma was written by Grasso, Catherine S.;Tang, Yujie;Truffaux, Nathalene;Berlow, Noah E.;Liu, Lining;Debily, Marie-Anne;Quist, Michael J.;Davis, Lara E.;Huang, Elaine C.;Woo, Pamelyn J.;Ponnuswami, Anitha;Chen, Spenser;Johung, Tessa B.;Sun, Wenchao;Kogiso, Mari;Du, Yuchen;Qi, Lin;Huang, Yulun;Hutt-Cabezas, Marianne;Warren, Katherine E.;Le Dret, Ludivine;Meltzer, Paul S.;Mao, Hua;Quezado, Martha;van Vuurden, Dannis G.;Abraham, Jinu;Fouladi, Maryam;Svalina, Matthew N.;Wang, Nicholas;Hawkins, Cynthia;Nazarian, Javad;Alonso, Marta M.;Raabe, Eric H.;Hulleman, Esther;Spellman, Paul T.;Li, Xiao-Nan;Keller, Charles;Pal, Ranadip;Grill, Jacques;Monje, Michelle. And the article was included in Nature Medicine (New York, NY, United States) in 2015.Computed Properties of C24H27N5O2 The following contents are mentioned in the article:

Diffuse intrinsic pontine glioma (DIPG) is a fatal childhood cancer. We performed a chem. screen in patient-derived DIPG cultures along with RNA-seq analyses and integrated computational modeling to identify potentially effective therapeutic strategies. The multi-histone deacetylase inhibitor panobinostat demonstrated therapeutic efficacy both in vitro and in DIPG orthotopic xenograft models. Combination testing of panobinostat and the histone demethylase inhibitor GSK-J4 revealed that the two had synergistic effects. Together, these data suggest a promising therapeutic strategy for DIPG. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0Computed Properties of C24H27N5O2).

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Computed Properties of C24H27N5O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Inhibition of H3K27me3-specific histone demethylases JMJD3 and UTX blocks reactivation of herpes simplex virus 1 in trigeminal ganglion neurons was written by Messer, Harald G. P.;Jacobs, Derek;Dhummakupt, Adit;Bloom, David C.. And the article was included in Journal of Virology in 2015.Safety of Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate The following contents are mentioned in the article:

Herpes simplex virus 1 (HSV-1) genomes are associated with the repressive heterochromatic marks H3K9me2/me3 and H3K27me3 during latency. Previous studies have demonstrated that inhibitors of H3K9me2/me3 histone demethylases reduce the ability of HSV-1 to reactivate from latency. Here we demonstrate that GSK-J4, a specific inhibitor of the H3K27me3 histone demethylases UTX and JMJD3, inhibits HSV-1 reactivation from sensory neurons in vitro. These results indicate that removal of the H3K27me3 mark plays a key role in HSV-1 reactivation. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0Safety of Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate).

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Safety of Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Inhibition of histone H3 lysine-27 demethylase activity relieves rheumatoid arthritis symptoms via repression of IL6 transcription in macrophages was written by Zhao, Zhan;Zhang, Yazhuo;Gao, Danling;Zhang, Yidan;Han, Wenwei;Xu, Ximing;Song, Qiaoling;Zhao, Chenyang;Yang, Jinbo. And the article was included in Frontiers in Immunology in 2022.HPLC of Formula: 1373423-53-0 The following contents are mentioned in the article:

Rheumatoid arthritis (RA) occurs in about 5 per 1,000 people and can lead to severe joint damage and disability. However, the knowledge of pathogenesis and treatment for RA remains limited. Here, we found that histone demethylase inhibitor GSK-J4 relieved collagen induced arthritis (CIA) symptom in exptl. mice model, and the underlying mechanism is related to epigenetic transcriptional regulation in macrophages. The role of epigenetic regulation has been introduced in the process of macrophage polarization and the pathogenesis of inflammatory diseases. As a repressive epigenetic marker, tri-methylation of lysine 27 on histone H3 (H3K27me3) was shown to be important for transcriptional gene expression regulation. Here, we comprehensively analyzed H3K27me3 binding promoter and corresponding genes function by RNA sequencing in two differentially polarized macrophage populations. The results revealed that H3K27me3 binds on the promoter regions of multiple critical cytokine genes and suppressed their transcription, such as IL6, specifically in M-CSF derived macrophages but not GM-CSF derived counterparts. Our results may provide a new approach for the treatment of inflammatory and autoimmune disorders. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0HPLC of Formula: 1373423-53-0).

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.HPLC of Formula: 1373423-53-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Histone modification of pain-related gene expression in spinal cord neurons under a persistent postsurgical pain-like state by electrocautery was written by Katsuda, Yosuke;Tanaka, Kenichi;Mori, Tomohisa;Narita, Michiko;Takeshima, Hideyuki;Kondo, Takashige;Yamabe, Yoshiyuki;Matsufuji, Misa;Sato, Daisuke;Hamada, Yusuke;Yamaguchi, Keisuke;Ushijima, Toshikazu;Inada, Eiichi;Kuzumaki, Naoko;Iseki, Masako;Narita, Minoru. And the article was included in Molecular Brain in 2021.Name: Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate The following contents are mentioned in the article:

Chronic postsurgical pain (CPSP) is a serious problem. We developed a mouse model of CPSP induced by electrocautery and examined the mechanism of CPSP. In this mouse model, while both incision and electrocautery each produced acute allodynia, persistent allodynia was only observed after electrocautery. Under these conditions, we found that the mRNA levels of Small proline rich protein 1A (Sprr1a) and Annexin A10 (Anxa10), which are the key modulators of neuropathic pain, in the spinal cord were more potently and persistently increased by electrocautery than by incision. Furthermore, these genes were overexpressed almost exclusively in chronic postsurgical pain-activated neurons. This event was associated with decreased levels of tri-methylated histone H3 at Lys27 and increased levels of acetylated histone H3 at Lys27 at their promoter regions. On the other hand, persistent allodynia and overexpression of Sprr1a and Anxa10 after electrocautery were dramatically suppressed by systemic administration of GSK-J4, which is a selective H3K27 demethylase inhibitor. These results suggest that the effects of electrocautery contribute to CPSP along with synaptic plasticity and epigenetic modification. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0Name: Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate).

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Name: Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

KDM6B promotes activation of the oncogenic CDK4/6-pRB-E2F pathway by maintaining enhancer activity in MYCN-amplified neuroblastoma was written by D′Oto, Alexandra;Fang, Jie;Jin, Hongjian;Xu, Beisi;Singh, Shivendra;Mullasseril, Anoushka;Jones, Victoria;Abu-Zaid, Ahmed;von Buttlar, Xinyu;Cooke, Bailey;Hu, Dongli;Shohet, Jason;Murphy, Andrew J.;Davidoff, Andrew M.;Yang, Jun. And the article was included in Nature Communications in 2021.Reference of 1373423-53-0 The following contents are mentioned in the article:

The H3K27me2/me3 histone demethylase KDM6B is essential to neuroblastoma cell survival. However, the mechanism of KDM6B action remains poorly defined. We demonstrate that inhibition of KDM6B activity 1) reduces the chromatin accessibility of E2F target genes and MYCN, 2) selectively leads to an increase of H3K27me3 but a decrease of the enhancer mark H3K4me1 at the CTCF and BORIS binding sites, which may, consequently, disrupt the long-range chromatin interaction of MYCN and E2F target genes, and 3) phenocopies the transcriptome induced by the specific CDK4/6 inhibitor palbociclib. Overexpression of CDK4/6 or Rb1 knockout confers neuroblastoma cell resistance to both palbociclib and the KDM6 inhibitor GSK-J4. These data indicate that KDM6B promotes an oncogenic CDK4/6-pRB-E2F pathway in neuroblastoma cells via H3K27me3-dependent enhancer-promoter interactions, providing a rationale to target KDM6B for high-risk neuroblastoma. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0Reference of 1373423-53-0).

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Reference of 1373423-53-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

KDM6B-dependent chromatin remodeling underpins effective virus-specific CD8+ T cell differentiation was written by Li, Jasmine;Hardy, Kristine;Olshansky, Moshe;Barugahare, Adele;Gearing, Linden J.;Prier, Julia E.;Sng, Xavier Y. X.;Nguyen, Michelle Ly Thai;Piovesan, Dana;Russ, Brendan E.;La Gruta, Nicole L.;Hertzog, Paul J.;Rao, Sudha;Turner, Stephen J.. And the article was included in Cell Reports in 2021.Reference of 1373423-53-0 The following contents are mentioned in the article:

Naive CD8⁺ T cell activation results in an autonomous program of cellular proliferation and differentiation. However, the mechanisms that underpin this process are unclear. Here, we profile genome-wide changes in chromatin accessibility, gene transcription, and the deposition of a key chromatin modification (H3K27me3) early after naive CD8⁺ T cell activation. Rapid upregulation of the histone demethylase KDM6B prior to the first cell division is required for initiating H3K27me3 removal at genes essential for subsequent T cell differentiation and proliferation. Inhibition of KDM6B-dependent H3K27me3 demethylation limits the magnitude of an effective primary virus-specific CD8⁺ T cell response and the formation of memory CD8⁺ T cell populations. Accordingly, we define the early spatiotemporal events underpinning early lineage-specific chromatin reprogramming that are necessary for autonomous CD8⁺ T cell proliferation and differentiation. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0Reference of 1373423-53-0).

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Reference of 1373423-53-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia