October 21, 2021 | Page 2 of 2

An overview of features, applications of compound:C2H4N4

Safety of 1H-1,2,4-Triazol-5-amine. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact El Sayed, MT; Sarhan, AE; Ahmed, E; Khattab, RR; Elnaggar, M; El-Messery, SM; Shaldam, MA; Hassan, GS or concate me.

An article Novel Pyruvate Kinase (PK) Inhibitors: New Target to Overcome Bacterial Resistance WOS:000520610800040 published article about TRANSITION-METAL COMPOUNDS; DENSITY-FUNCTIONAL THEORY; MOLECULAR-STRUCTURES; DOCKING; MOLYBDENUM; INDOLES; MANNICH; BONDS in [El Sayed, Mardia T.] Natl Res Ctr, Chem Ind Res Div, Appl Organ Chem Dept, Dokki 12311, Egypt; [Sarhan, Alaadin E.] Natl Res Ctr, Pharmaceut Div, Therapeut Chem Dept, Dokki 12311, Egypt; [Ahmed, Entsar] Al Azhar Univ, Chem Dept, Fac Sci, Girls Branch, Cairo, Egypt; [Khattab, Reham R.] Natl Res Ctr, Chem Ind Res Div, Photochem Dept, Dokki 12311, Egypt; [Elnaggar, Mohamed] Univ Sharjah, Fac Sci, Chem Dept, Sharjah 27272, U Arab Emirates; [El-Messery, Shahenda M.] Mansoura Univ, Fac Pharm, Dept Organ Pharmaceut Chem, POB 35516, Mansoura, Egypt; [Shaldam, Moataz A.] Kafrelsheikh Univ, Fac Pharm, Dept Pharmaceut Chem, Kafr Al Sheikh 33516, Egypt; [Hassan, Ghada S.] Mansoura Univ, Fac Pharm, Dept Med Chem, Mansoura 35516, Egypt in 2020.0, Cited 39.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5. Safety of 1H-1,2,4-Triazol-5-amine

In the present investigation, some novel nitro Mannich bases derived from Michael type addition of activated nitro olefin, beta-nitrostyrene with various amines either primary or secondary including some amino sugars were designed and synthesized. The produced Mannich bases have been full characterized through different spectroscopic techniques. Antimicrobial evaluation has been performed against the Gram positive S. aureus and methicillin-resistant S. aurues (MRSA) infections. 5 of the synthesized compounds represent the best candidates in the biological screening, they have exhibited good activity with MIC values range from 100 to 250 mu g/ml. The active agents have been tested for pyruvate kinase inhibition activity with % of inhibition range from 30 to 79 % with IC50 in a nano molar range. They also exhibited significant Pyruvate kinase inhibition in nanomolar range with IC50 of 1066, 662, 1887, 418 and 1128 ng/ml, respectively (versus 196 ng/ml for AZD7545). Molecular docking calculations for active agents were performed. A complete conformational analysis molecular modeling utilizing Gaussian 09 program (HF/DFT) was used to verify the mode of bonding through the optimized geometries as well as essential quantum parameters were calculated using frontier energies (EHOMO & ELUMO) for the active candidates indicating the overall stability of the structure.

Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Archives for Chemistry Experiments of 1H-1,2,4-Triazol-5-amine

About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Mohamed, HS; Abdel-Latif, MK; Ahmed, SA or concate me.. Quality Control of 1H-1,2,4-Triazol-5-amine

An article Synthesis, Characterization, and DFT Calculations of Quinoline and Quinazoline Derivatives WOS:000579454600025 published article about DENSITY-FUNCTIONAL THERMOCHEMISTRY; BEARING BRIDGEHEAD NITROGEN; SPECTROSCOPIC CHARACTERIZATION; SMALL-MOLECULE; POTENT; OPTIMIZATION; INHIBITORS; AMETOCTRADIN; POLYMERASE; AGENTS in [Mohamed, H. S.] Beni Suef Univ, Res Inst Med & Aromat Plants, Bani Suwayf 62511, Egypt; [Abdel-Latif, M. K.; Ahmed, S. A.] Beni Suef Univ, Fac Sci, Dept Chem, Bani Suwayf 62511, Egypt in 2020.0, Cited 41.0. Quality Control of 1H-1,2,4-Triazol-5-amine. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5

Treatment of 3-methylcyclohexanone with ethyl formate in the presence of sodium methoxide afforded sodium (2-methyl-6-oxocyclohexylidene)methanolate which reacted with aminopyrazoles, aminotriazole, and aminotetrazole to produce fused quinazoline derivatives; its reactions with cyanothioacetamide, cyanoacetamide, and cyanoacetohydrazide gave tetrahydroquinoline-3-carbonitrile derivatives. The reactions of 8-methyl-2-sulfanyl-5,6,7,8-tetrahydroquinoline-3-carbonitrile with alkylating agents led to the formation of thieno[2,3-b]quinoline derivatives. DFT computational studies of the synthesized compounds were carried out using B3LYP/6-311+G** and HF/6-311+G** approximations. The calculated HOMO and LUMO energies showed that charge transfer occurs in their molecules.

About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Mohamed, HS; Abdel-Latif, MK; Ahmed, SA or concate me.. Quality Control of 1H-1,2,4-Triazol-5-amine

What about chemistry interests you the most C2H4N4

About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Ben Ali, A; El Bakri, Y; Lai, CH; Sebhaoui, J; El Ghayati, L; Essassi, E; Mague, JT or concate me.. HPLC of Formula: C2H4N4

HPLC of Formula: C2H4N4. Authors Ben Ali, A; El Bakri, Y; Lai, CH; Sebhaoui, J; El Ghayati, L; Essassi, E; Mague, JT in INT UNION CRYSTALLOGRAPHY published article about in [Ben Ali, Abdelkader] Mohammed V Univ Rabat, Fac Sci, Ctr Sci Mat, Lab Chim Appl Mat, Ave Ibn,BP 1014, Rabat, Morocco; [El Bakri, Youness; Sebhaoui, Jihad; El Ghayati, Lhoussaine; Essassi, El Mokhtar] Univ Mohammed 5, Fac Sci, Ctr Rech Sci Med, URAC 21,Pole Competence Pharmacochim, Av Ibn Battouta,BP 1014, Rabat, Morocco; [Lai, Chin-Hung] Chung Shan Med Univ, Dept Med Appl Chem, Taichung 40241, Taiwan; [Lai, Chin-Hung] Chung Shan Med Univ Hosp, Dept Med Educ, Taichung 40241, Taiwan; [Mague, Joel T.] Tulane Univ, Dept Chem, New Orleans, LA 70118 USA in 2019.0, Cited 38.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5

In the title molecule, C13H16N4O3, the mean planes of the phenyl and triazole rings are nearly perpendicular to one another as a result of the intramolecular C-H center dot center dot center dot O and C-H center dot center dot center dot pi(ring) interactions. In the crystal, layers parallel to (101) are generated by O-H center dot center dot center dot N, N-H center dot center dot center dot O and N-H center dot center dot center dot N hydrogen bonds. The layers are connected by inversion-related pairs of C-H center dot center dot center dot O hydrogen bonds. The experimental molecular structure is close to the gas-phase geometryoptimized structure calculated by DFT methods. Hirshfeld surface analysis indicates that the most important interaction involving hydrogen in the title compound is the H center dot center dot center dot H contact. The contribution of the H center dot center dot center dot O, H center dot center dot center dot N, and H center dot center dot center dot H contacts are 13.6, 16.1, and 54.6%, respectively.

About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Ben Ali, A; El Bakri, Y; Lai, CH; Sebhaoui, J; El Ghayati, L; Essassi, E; Mague, JT or concate me.. HPLC of Formula: C2H4N4

Why Are Children Getting Addicted To C2H4N4

Computed Properties of C2H4N4. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Chhetri, S; Adak, NC; Samanta, P; Murmu, NC; Srivastava, SK; Kuila, T or concate me.

An article Synergistic effect of Fe3O4 anchored N-doped rGO hybrid on mechanical, thermal and electromagnetic shielding properties of epoxy composites WOS:000467349000035 published article about REDUCED GRAPHENE; NANOCOMPOSITE; NANOPARTICLES; OXIDE in [Chhetri, Suman; Adak, Nitai Chandra; Samanta, Pranab; Murmu, Naresh Chandra; Kuila, Tapas] Council Sci & Ind Res Cent Mech Engn Res Inst, Surface Engn & Tribol Div, Durgapur 713209, India; [Chhetri, Suman; Adak, Nitai Chandra; Samanta, Pranab; Murmu, Naresh Chandra; Kuila, Tapas] Acad Sci & Innovat Res AcSIR, Ghaziabad 201002, India; [Srivastava, Suneel Kumar] Indian Inst Technol Kharagpur, Dept Chem, Kharagpur 721302, W Bengal, India in 2019.0, Cited 42.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5. Computed Properties of C2H4N4

Herein, Fe3O4 nano-particles are anchored over nitrogen doped reduced graphene oxide Fe3O4@N-rGO) structure to accommodate electric and magnetic components, so that it could match both the conduction and polarization loss to augment the attenuation of electromagnetic radiation. The formation of condensed heteroaromatic structure and decoration of Fe3O4 particles on r-GO structure are confirmed by photoelectron spectroscopy (XPS). high-resolution transmission electron microscopy (HRTEM), X-ray diffraction (XRD). The Fe3O4@N-rGO hybrid is subsequently dispersed in epoxy matrix, which result in significantly higher electrical conductivity (1.31 s/m) and electromagnetic interference (EMI) shielding efficiency (- 26 dB at 1 mm thickness). It was assumed that presence of electric-magnetic integrated Fe3O4@N-rGO hybrid in epoxy matrix significantly improved the interfacial polarization and anisotropy energy, which was reflected in absorption loss value of -27 dB. The composites also exhibited enhanced mechanical and thermo-mechanical properties coupled with improved thermal stability.

Computed Properties of C2H4N4. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Chhetri, S; Adak, NC; Samanta, P; Murmu, NC; Srivastava, SK; Kuila, T or concate me.

What unique challenges do researchers face in 1H-1,2,4-Triazol-5-amine

Name: 1H-1,2,4-Triazol-5-amine. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Nayak, A; Smetana, V; Mudring, AV; Rogers, RD or concate me.

Name: 1H-1,2,4-Triazol-5-amine. Nayak, A; Smetana, V; Mudring, AV; Rogers, RD in [Nayak, Amrita; Rogers, Robin D.] Univ Alabama, Coll Arts & Sci, Tuscaloosa, AL 35487 USA; [Smetana, Volodymyr; Mudring, Anja-Verena; Rogers, Robin D.] Stockholm Univ, Dept Mat & Environm Chem, S-10691 Stockholm, Sweden published Anhydrous vs Hydrated f-Element Acetate Polymers Dictated by the Stoichiometry of Protic Acidic/Basic Azole Mixtures in 2021.0, Cited 36.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.

Continuing our investigations of ionic liquid (IL) based routes to a library of f-element/soft donor complexes which could be studied crystallographically, we have explored the dissolution of f-element salts in protic imidazole-based ILs containing only soft donors at high temperatures to drive off volatiles, including water and carboxylic or mineral acids. Here we present our results, reacting acidic and basic azoles in 1:3 or 1:1 stoichiometric compositions at elevated temperature, followed by saturation with Nd(OAc)(3)center dot xH(2)O or Ce(OAc)(3)center dot xH(2)O, which led to 13 new metal-acetate polymeric complexes identified by single-crystal X-ray diffraction. We found that the diversity in coordination modes of the simple acetate ligand that interfere with substitution of the softer N donors led to several readily crystallizable complexes forming two distinct groups with respect to f-element interaction with the ionic liquid precursors. When the acidic/basic azole ratio was 1:3, acetate and a neutral basic azole were found to be coordinated to the metal centers but no water, although in one case (2) water was observed in the secondary coordination sphere: [Ce(mu(2)-OAc)(3)(C(1)im)](n) (1, C(1)im = 1-methylimidazole), [Nd(mu(2)-(OAc)(3)(C(1)im)](n)center dot nH(2)O (2), [Ce(mu(2)-OAc)(3)(C(2)im)](n) (3, C(2)im = 1-ethylimidazole), [Ln(mu(2)-OAc)(3)DMF](n) (Ln = Nd (4), Ce (5); dimethylformamide (DMF) was substituted for the azole mixture), and [Nd(mu(2)-OAc)(3)(C(4)im)](n) (6, C(4)im = 1-butylimidazole). However, when the stoichiometric ratio was 1:1, water was always observed coordinated to the metal ions with the acidic azole included in the structure as a solvate or cocrystal, despite a higher reaction temperature: [Nd(mu(2)-OAc)(3)(OH2)](n)center dot n(1,2,3-Taz) (7,1,2,3-Taz = 1,2,3-triazole), [Ln(mu(2)-OAc)(3)(OH2)](n)center dot n(4,5-DCim) (Ln = Nd (8), Ce (9), 4,5-DCim = 4,5-dicyanoimidazole), [Ln(mu(2)-OAc)(3)(OH2)](n)center dot n(3,5-diNH(2)-1,2,4-Taz) (Ln = Nd (10), Ce (11), 3,5diNH(2)-1,2,4-Taz = 3,5-diamino-1,2,4-triazole), [Ce(mu(2)-OAc)(3)(OH2)](n)center dot n(3-NH2-1,2,4-Taz) (12, 3-NH2-1,2,4-Taz = 3-amino-1,2,4-triazole), and [Nd(mu(2)-OAc)(3)(OH2)](n)center dot n(5-NH2-Tz) (13, 5-NH2-Tz = 5-aminotetrazole). All of the compounds retain the Ln:OAc- ratio of 1:3 and form 1D polymeric chains; however, they exhibit a variety of coordination modes affecting the degree of chain condensation. The isolation of both hydrated and anhydrous products revealed different abilities of the investigated soft N-donors to compete with O-donors finding their place in the coordination sphere of the lanthanide or in the crystal lattice.

Name: 1H-1,2,4-Triazol-5-amine. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Nayak, A; Smetana, V; Mudring, AV; Rogers, RD or concate me.

A new application aboutC2H4N4

Product Details of 61-82-5. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Wang, GY; Zheng, T; Zhang, SQ; Ye, JW; Ning, GL or concate me.

Product Details of 61-82-5. Authors Wang, GY; Zheng, T; Zhang, SQ; Ye, JW; Ning, GL in ELSEVIER published article about in [Ye, Junwei; Ning, Guiling] Dalian Univ Technol, State Key Lab Fine Chem, 2 Linggong Rd, Dalian 116012, Peoples R China; Dalian Univ Technol, Sch Chem Engn, 2 Linggong Rd, Dalian 116012, Peoples R China in 2021.0, Cited 47.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5

A novel pyridinium salt derivative, 2,3,4,5,6-pentaphenyl-1-(1H-1,2,4-triazol-3-yl)pyridinium perchlorate (1) has been designed and synthesized by using pyrylium perchlorate and 3-amino-1H-1,2,4-triazole as ingredients, which can be exploited for the binding and specific sensing of anion via hydrogen bonds. Compound 1 exhibits intense blue emission in solution with maximum emission at 469 nm with a red shift relative to that (426 nm) of solid state. The luminescence intensity of 1 could be selectively and sensitivity quenched with acetate ion and fluorine ion among various anions including F-, Cl-, Br-, I-, AcO- and NO3-. Furthermore, the possible detection mechanism was investigated. This work could contribute a credible potential sensing application of 1,2,4-triazolyl substituted pentaphenylpyridinium salts towards the specific anions in biological and environmental concerns. (C) 2021 Elsevier B.V. All rights reserved.

Product Details of 61-82-5. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Wang, GY; Zheng, T; Zhang, SQ; Ye, JW; Ning, GL or concate me.

Something interesting about 1H-1,2,4-Triazol-5-amine

Safety of 1H-1,2,4-Triazol-5-amine. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Zhang, CY; Fang, H; Shi, XT; He, F; Wang, RY; Fan, JB; Bai, PF; Wang, JY; Park, CH; Bellizzi, M; Zhou, XP; Wang, GL; Ning, YS or concate me.

I found the field of Biotechnology & Applied Microbiology; Plant Sciences very interesting. Saw the article A fungal effector and a rice NLR protein have antagonistic effects on a Bowman-Birk trypsin inhibitor published in 2020.0. Safety of 1H-1,2,4-Triazol-5-amine, Reprint Addresses Ning, YS (corresponding author), Chinese Acad Agr Sci, Inst Plant Protect, State Key Lab Biol Plant Dis & Insect Pests, Beijing 100193, Peoples R China.; Wang, GL (corresponding author), Ohio State Univ, Dept Plant Pathol, Columbus, OH 43210 USA.. The CAS is 61-82-5. Through research, I have a further understanding and discovery of 1H-1,2,4-Triazol-5-amine

Bowman-Birk trypsin inhibitors (BBIs) play important roles in animal and plant immunity, but how these protease inhibitors are involved in the immune system remains unclear. Here, we show that the rice (Oryza sativa) BBI protein APIP4 is a common target of a fungal effector and an NLR receptor for innate immunity. APIP4 exhibited trypsin inhibitor activityin vitroandin vivo. Knockout ofAPIP4in rice enhanced susceptibility, and overexpression ofAPIP4increased resistance to the fungal pathogenMagnaporthe oryzae. TheM. oryzaeeffector AvrPiz-t interacted with APIP4 and suppressed APIP4 trypsin inhibitor activity. By contrast, the rice NLR protein Piz-t interacted with APIP4, enhancing APIP4 transcript and protein levels, and protease inhibitor activity. Our findings reveal a novel host defence mechanism in which a host protease inhibitor targeted by a fungal pathogen is protected by an NLR receptor.

Brief introduction of 1H-1,2,4-Triazol-5-amine

About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Redenti, S; Marcovich, I; De Vita, T; Perez, C; De Zorzi, R; Demitri, N; Perez, DI; Bottegoni, G; Bisignano, P; Bissaro, M; Moro, S; Martinez, A; Storici, P; Spalluto, G; Cavalli, A; Federico, S or concate me.. Application In Synthesis of 1H-1,2,4-Triazol-5-amine

An article A Triazolotriazine-Based Dual GSK-3 beta/CK-1 delta Ligand as a Potential Neuroprotective Agent Presenting Two Different Mechanisms of Enzymatic Inhibition WOS:000458432600003 published article about PARKINSONS-DISEASE; ALPHA-SYNUCLEIN; PROTEIN-KINASES; PHOSPHORYLATION; MODEL; CK1; TAU in [Redenti, Sara; Marcovich, Irene; De Zorzi, Rita; Spalluto, Giampiero; Federico, Stephanie] Univ Trieste, Dept Chem & Pharmaceut Sci, Via Licio Giorgeri 1, I-34127 Trieste, Italy; [De Vita, Teresa; Cavalli, Andrea] Ist Italiano Tecnol, Drug Discovery & Dev D3, Via Morego 30, I-16163 Genoa, Italy; [Perez, Concepcion; Perez, Daniel I.; Martinez, Ana] CSIC, Ctr Invest Biol, Ave Ramiro Maeztu 9, Madrid 28040, Spain; [Demitri, Nicola; Storici, Paola] Elettra Sincrotrone Trieste SCpA, SS 14,Km 163-5,AREA Sci Pk, I-34149 Trieste, Italy; [Bottegoni, Giovanni] Univ Birmingham, Sir Robert Aitken Inst Med Res, Coll Med & Dent Sci, Sch Pharm,Inst Clin Sci, Edgbaston B15 2TT, England; [Bisignano, Paola] Univ Calif San Francisco, Cardiovasc Res Inst, 555 Mission Bay Blvd South, San Francisco, CA 94158 USA; [Bissaro, Maicol; Moro, Stefano] Univ Padua, Dept Pharmaceut & Pharmacol Sci, Mol Modeling Sect, Via Marzolo 5, I-35131 Padua, Italy in 2019.0, Cited 33.0. Application In Synthesis of 1H-1,2,4-Triazol-5-amine. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5

Glycogen synthase kinase 3 beta (GSK-3 beta) and casein kinase 1 delta (CK-1 delta) are emerging targets for the treatment of neuroinflammatory disorders, including Parkinson’s disease. An inhibitor able to target these two kinases was developed by docking-based design. Compound 12, 3-(7-amino-5-(cyclohexylamino)-[1,2,4]triazolo[1,5-a][1,3,5]triazin-2-yl)-2-cyanoacrylamide, showed combined inhibitory activity against GSK-3 beta and CK-1 delta [IC50(GSK-3 beta)=0.17 mu m; IC50(CK-1 delta)=0.68 mu m]. In particular, classical ATP competition was observed against CK-1 delta, and a co-crystal of compound 12 inside GSK-3 beta confirmed a covalent interaction between the cyanoacrylamide warhead and Cys199, which could help in the development of more potent covalent inhibitors of GSK-3 beta. Preliminary studies on in vitro models of Parkinson’s disease revealed that compound 12 is not cytotoxic and shows neuroprotective activity. These results encourage further investigations to validate GSK-3 beta/CK-1 delta inhibition as a possible new strategy to treat neuroinflammatory/degenerative diseases.

Properties and Exciting Facts About 1H-1,2,4-Triazol-5-amine

Formula: C2H4N4. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Wang, S; Zhao, LJ; Shi, XJ; Ding, LN; Yang, LL; Wang, ZZ; Shen, DD; Tang, K; Li, XJ; Mamun, MAA; Li, HJ; Yu, B; Zheng, YC; Wang, SM; Liu, HM or concate me.

Authors Wang, S; Zhao, LJ; Shi, XJ; Ding, LN; Yang, LL; Wang, ZZ; Shen, DD; Tang, K; Li, XJ; Mamun, MAA; Li, HJ; Yu, B; Zheng, YC; Wang, SM; Liu, HM in AMER CHEMICAL SOC published article about CULLIN-RING LIGASES; NEDD8-ACTIVATING ENZYME; E3 LIGASE; DEGRADATION; NEDDYLATION; DISCOVERY; CARCINOMA; UBIQUITINATION; AMPLIFICATION; PROGRESSION in [Wang, Shuai; Zhao, Lijie; Shi, Xiao-Jing; Ding, Lina; Wang, Zhi-Zheng; Shen, Dandan; Tang, Kai; Li, Xiao-Jing; Mamun, M. A. A.; Li, Huiju; Yu, Bin; Zheng, Yi-Chao; Wang, Shaomeng; Liu, Hong-Min] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Henan, Peoples R China; [Wang, Shuai; Zhao, Lijie; Shi, Xiao-Jing; Ding, Lina; Wang, Zhi-Zheng; Shen, Dandan; Tang, Kai; Li, Xiao-Jing; Mamun, M. A. A.; Li, Huiju; Yu, Bin; Zheng, Yi-Chao; Wang, Shaomeng; Liu, Hong-Min] Zhengzhou Univ, Inst Drug Discovery & Dev, Zhengzhou 450001, Henan, Peoples R China; [Wang, Shaomeng] Univ Michigan, Dept Internal Med, 1600 Huron Pkwy, Ann Arbor, MI 48109 USA; [Wang, Shaomeng] Univ Michigan, Dept Pharmacol, 1600 Huron Pkwy, Ann Arbor, MI 48109 USA; [Wang, Shaomeng] Univ Michigan, Dept Med Chem, 1600 Huron Pkwy, Ann Arbor, MI 48109 USA; [Wang, Shuai; Zhao, Lijie; Shi, Xiao-Jing; Ding, Lina; Wang, Zhi-Zheng; Shen, Dandan; Tang, Kai; Li, Xiao-Jing; Mamun, M. A. A.; Li, Huiju; Yu, Bin; Zheng, Yi-Chao; Liu, Hong-Min] Coinnovat Ctr Henan Prov New Drug R&D Preclin Saf, Zhengzhou 450001, Henan, Peoples R China; [Wang, Shuai; Zhao, Lijie; Shi, Xiao-Jing; Ding, Lina; Wang, Zhi-Zheng; Shen, Dandan; Tang, Kai; Li, Xiao-Jing; Mamun, M. A. A.; Li, Huiju; Yu, Bin; Zheng, Yi-Chao; Liu, Hong-Min] Zhengzhou Univ, Minist Educ China, Key Lab Adv Technol Drug Preparat Technol, Zhengzhou 450001, Henan, Peoples R China; [Yang, Linlin] Zhengzhou Univ, Sch Basic Med Sci, Dept Pharmacol, Zhengzhou 450001, Henan, Peoples R China; [Yu, Bin] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210023, Jiangsu, Peoples R China in 2019.0, Cited 53.0. Formula: C2H4N4. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5

The cullin-RING ubiquitin ligases (CRLs) are responsible for about 20% of cellular protein degradation and regulate diverse cellular processes, and the dysfunction of CRLs is implicated in human diseases. Targeting the CRLs has become an emerging strategy for the treatment of human diseases. Herein, we describe the discovery of a hit compound from our in-house library and further structure-based optimizations, which have enabled the identification of new triazolo[1,5-a]pyrimidine-based inhibitors targeting the DCN1-UBC12 interaction. Compound WS-383 blocks the DCN1-UBC12 interaction (IC50 = 11 nM) reversibly and shows selectivity over selected kinases. WS-383 exhibits cellular target engagement to DCN1 in MGC-803 cells. WS-383 inhibits Cul3/1 neddylation selectively over other cullins and also induces accumulation of p21, p27, and NRF2. Collectively, targeting the DCN1-UBC12 interaction would be a viable strategy for selective neddylation inhibition of Cul3/1 and may be of therapeutic potential for disease treatment in which Cul3/1 is dysregulated.

Some scientific research about 61-82-5

Recommanded Product: 1H-1,2,4-Triazol-5-amine. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Eggert, S; Gruebl, T; Rajender, R; Rupp, C; Sander, B; Heesch, A; Zimmermann, M; Hoepfner, S; Zentgraf, H; Kins, S or concate me.

Recommanded Product: 1H-1,2,4-Triazol-5-amine. In 2020.0 CELL MOL LIFE SCI published article about APP; TRANSPORT; SIGNALS; UBIQUITINATION; DEGRADATION; TRAFFICKING; MEMBRANE; INTERNALIZATION; LOCALIZATION; COMPONENTS in [Eggert, Simone; Gruebl, Tomas; Rajender, Ritu; Rupp, Carsten; Sander, Bianca; Heesch, Amelie; Zimmermann, Marius; Kins, Stefan] Tech Univ Kaiserslautern, Dept Human Biol & Human Genet, Erwin Schrodinger Str 13, D-67663 Kaiserslautern, Germany; [Hoepfner, Sebastian] MPI Mol Cell Biol & Genet, Dresden, Germany; [Hoepfner, Sebastian] Bird & Bird LLM, Munich, Germany; [Zentgraf, Hanswalter] DKFZ, Heidelberg, Germany in 2020.0, Cited 75.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.

Endocytosis of the amyloid precursor protein (APP) is critical for generation of beta-amyloid, aggregating in Alzheimer’s disease. APP endocytosis depending on the intracellular NPTY motif is well investigated, whereas involvement of the YTSI (also termed BaSS) motif remains controversial. Here, we show that APP lacking the YTSI motif (Delta YTSI) displays reduced localization to early endosomes and decreased internalization rates, similar to APP Delta NPTY. Additionally, we show that the YTSI-binding protein, PAT1a interacts with the Rab5 activator RME-6, as shown by several independent assays. Interestingly, knockdown of RME-6 decreased APP endocytosis, whereas overexpression increased the same. Similarly, APP Delta NPTY endocytosis was affected by PAT1a and RME-6 overexpression, whereas APP Delta YTSI internalization remained unchanged. Moreover, we could show that RME-6 mediated increase of APP endocytosis can be diminished upon knocking down PAT1a. Together, our data identify RME-6 as a novel player in APP endocytosis, involving the YTSI-binding protein PAT1a.