61-82-5 -| Page 115 of 154

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About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Yu, L; Liu, WJ; Guo, ZW; Li, ZQ; Jiang, HY; Zou, Q; Mao, ZL; Fang, HC; Zhang, ZY; Wang, N; Chen, XS or concate me.. COA of Formula: C2H4N4

Category: Triazoles. I found the field of Plant Sciences very interesting. Saw the article Interaction between MdMYB63 and MdERF106 enhances salt tolerance in apple by mediating Na+/H+ transport published in 2020.0, Reprint Addresses Wang, N; Chen, XS (corresponding author), Shandong Agr Univ, Coll Hort Sci, State Key Lab Crop Biol, 61 Daizong Rd, Tai An 271018, Shandong, Peoples R China.. The CAS is 61-82-5. Through research, I have a further understanding and discovery of 1H-1,2,4-Triazol-5-amine.

Salt stress is an important environmental factor affecting the growth and production of agricultural crops and fruits worldwide, including apple (Males x domestica). In this study, we demonstrate that a salt-responsive MYB transcription factor (TF), designated as MdMYB63, promotes survival under salt stress. Overexpression of MdMYB63 in apple calli significantly enhanced salt tolerance. Screening of the AP2/ERF family of TFs identified MdERF106 as an interaction partner of MdMYB63. Further analyses showed that the MdMYB63-MdERF106 complex significantly promotes the expression of downstream MdSOS1, thereby improving the Na+ expulsion and salt tolerance of apple. These functional analyses of MdMYB63 have provided valuable insights into the regulatory network of salt tolerance, and lay a theoretical foundation for the cultivation of new salt-tolerant apple varieties.

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

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About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Shahnavaz, Z; Khaligh, NG; Zaharani, L; Johan, MR; Hamizi, NA or concate me.. Product Details of 61-82-5

Shahnavaz, Z; Khaligh, NG; Zaharani, L; Johan, MR; Hamizi, NA in [Shahnavaz, Zohreh; Khaligh, Nader Ghaffari; Zaharani, Lia; Johan, Mohd Rafie; Hamizi, Nor Aliya] Univ Malaya, Nanotechnol & Catalysis Res Ctr, Inst Postgrad Studies, 3rd Floor,Block A, Kuala Lumpur 50603, Malaysia published The structure elucidation of new ionic liquid and its application for the synthesis of a series of novel triazolo[1,5-a]pyrimidine scaffolds in 2020.0, Cited 35.0. 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.

In the present study, the chemical structure of 4,4′-trimethylene-N,N’-dipiperidinium chlorosulfonate is elucidated by 1D NMR, and 2D NMR, FTIR, Raman analyses, and Mass spectra. It was indicated that the chlorosulfonic acid could not act as a sulfonating agent in the reaction with secondary amines like TMDP due to due more steric hindrance of the sulfur atom by chlorine and oxygen atoms. Raman and FTIR spectra are demonstrated as two high-value optical techniques to the elucidation and identification of chemical structures that confirmed C3(v) symmetry for chlorosulfonate anion in the ionic liquid. Then, the solvent-catalyst activity of ionic liquid was demonstrated in the one-pot synthesis of a series of novel triazolo-pyrimidines under mild conditions. The ionic liquid was retrieved and reused several times without reducing its catalytic efficiency. (C) 2020 Elsevier B.V. All rights reserved.

About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Shahnavaz, Z; Khaligh, NG; Zaharani, L; Johan, MR; Hamizi, NA or concate me.. Product Details of 61-82-5

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Category: Triazoles. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Qu, L; Li, HL; Guo, D; Wang, Y; Zhu, JH; Yin, LY; Peng, SQ or concate me.

In 2020.0 SCI REP-UK published article about FARNESYL DIPHOSPHATE SYNTHASE; ZINC-FINGER PROTEIN; ISOPRENOID BIOSYNTHESIS; MOLECULAR CHARACTERIZATION; MEVALONATE PATHWAY; IN-VITRO; GENE; CLONING; PLANT; EVOLUTION in [Qu, Long; Yin, Li-Yan] Hainan Univ, Sch Life & Pharmaceut Sci, Haikou 570228, Hainan, Peoples R China; [Qu, Long; Li, Hui-Liang; Guo, Dong; Wang, Ying; Zhu, Jia-Hong; Peng, Shi-Qing] Chinese Acad Trop Agr Sci, Inst Trop Biosci & Biotechnol, Minist Agr, Key Lab Biol & Genet Resources Trop Crops, 4 Xueyuan Rd, Haikou 571101, Hainan, Peoples R China in 2020.0, Cited 46.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5. Category: Triazoles

Farnesyl pyrophosphate synthase (FPS) is a key enzyme that catalyzes the formation of farnesyl pyrophosphate, the main initiator for rubber chain initiation in Hevea brasiliensis Muell. Arg. The transcriptional regulatory mechanisms of the FPS gene still not well understood. Here, a WRKY transcription factor designated HbWRKY27 was obtained by screening the latex cDNA library applied the HbFPS1 promoter as bait. HbWRKY27 interacted with the HbFPS1 promoter was further identified by individual Y1H and EMSA assays. HbWRKY27 belongs to group IIe WRKY subfamily which contains a typical WRKY domain and C-X5-CX23-HXH motif. HbWRKY27 was localized to the nucleus. HbWRKY27 predominantly accumulated in latex. HbWRKY27 was up-regulated in latex by ethrel, salicylic acid, abscisic acid, and methyl jasmonate treatment. Transient expression of HbWRKY27 led to increasing the activity of the HbFPS1 promoter in tobacco plant, suggesting that HbWRKY27 positively regulates the HbFPS1 expression. Taken together, an upstream transcription factor of the key natural rubber biosynthesis gene HbFPS1 was identified and this study will provide novel transcriptional regulatory mechanisms of the FPS gene in Hevea brasiliensis.

Category: Triazoles. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Qu, L; Li, HL; Guo, D; Wang, Y; Zhu, JH; Yin, LY; Peng, SQ or concate me.

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Product Details of 61-82-5. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Xie, SF; Huang, LQ; Zhong, L; Lai, BL; Yang, M; Chen, WB; Zhang, YQ; Dong, W or concate me.

Product Details of 61-82-5. Xie, SF; Huang, LQ; Zhong, L; Lai, BL; Yang, M; Chen, WB; Zhang, YQ; Dong, W in [Xie, Shang-Fang; Huang, Li-Qian; Zhong, Li; Lai, Bi-Lin; Yang, Meng; Chen, Wen-Bin; Dong, Wen] Guangzhou Univ, Sch Chem & Chem Engn, Guangzhou Key Lab Environm Funct Mat & Technol, Guangzhou 510006, Guangdong, Peoples R China; [Zhang, Yi-Quan] Nanjing Normal Univ, Sch Phys Sci & Technol, Jiangsu Key Lab NSLSCS, Nanjing 210023, Jiangsu, Peoples R China published Structures, Single-Molecule Magnets, and Fluorescent Properties of Four Dinuclear Lanthanide Complexes Based on 4-Azotriazolyl-3-hydroxy-2-naphthoic Acid in 2019.0, Cited 67.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.

Four isostructural dinuclear lanthanide complexes based on 4-azotriazolyl-3-hydroxy-2-naphthoic acid (H(3)ATNA) and 3-hydroxy-2-naphthoic acid (H(2)NA) ligands, {[Ln(2)(HATNA)(2)(HNA)(2)(H2O)(4)].6DMF} (Ln = Dy (1), Tb (2), Sm (3), Eu (4); DMF = N,N-dimethylformamide) have been prepared and characterized by X-ray diffraction crystallography, dc/ac magnetic characterization, and fluorescent spectrometry. The crystallographic data reveal dinuclear lanthanide cores of complexes 1-4, bridged by phenoxo and mu(1,3) carboxyl groups. Each nine-coordinated Ln(III) ion is located in a slightly distorted monocapped square antiprism. The ligand of H(3)ATNA displays a unique antenna effect in complex 4. Complexes 1-3 display only two ligand-centered fluorescent emissive peaks around 450 and 600 nm, and complex 4 shows four characteristic Eu(III)centered emission bands at 593, 618, 653, and 698 nm under excitation at 348 nm. Complex 1 exhibits single-molecule magnet behavior that is rationalized through ab initio calculations.

Product Details of 61-82-5. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Xie, SF; Huang, LQ; Zhong, L; Lai, BL; Yang, M; Chen, WB; Zhang, YQ; Dong, W or concate me.

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About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Shahnavaz, Z; Khaligh, NG; Mihankhah, T; Johan, MR or concate me.. HPLC of Formula: C2H4N4

I found the field of Chemistry very interesting. Saw the article Design, synthesis, characterization, and physical property determination of a new ionic liquid: the preparation of triazolo-pyrimidines at room temperature under metal-free conditions published in 2020.0. Recommanded Product: 1H-1,2,4-Triazol-5-amine, Reprint Addresses Khaligh, NG (corresponding author), Univ Malaya, Nanotechnol & Catalysis Res Ctr, Inst Postgrad Studies, Kuala Lumpur 50603, Malaysia.. The CAS is 61-82-5. Through research, I have a further understanding and discovery of 1H-1,2,4-Triazol-5-amine

A new ionic liquid is synthesized, and its chemical structure is characterized by FTIR, 1D NMR and 2D NMR, and mass analyses. The thermal behavior and thermal stability of this ionic liquid are investigated. The results approved the formation of 4,4MODIFIER LETTER PRIME-trimethylene-N,NMODIFIER LETTER PRIME-dipiperidinium sulfate instead of 4,4MODIFIER LETTER PRIME-trimethylene-N,NMODIFIER LETTER PRIME-dipiperidinium hydrogen sulfate. Moreover, the synthesis of triazolo-pyrimidine derivatives was successfully conducted in the presence of new ionic liquid at room temperature under metal-free conditions, which demonstrated the catalytic efficiency of this ionic liquid. The workup was carried out without the utilization of high-cost column chromatography. After extraction of desired products, the residual ionic liquid could be recycled and reused in the next runs. New ionic liquid exhibited high catalytic activity even after fifth run with no significant change in the chemical structure.

About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Shahnavaz, Z; Khaligh, NG; Mihankhah, T; Johan, MR or concate me.. HPLC of Formula: C2H4N4

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About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Baklykov, AV; Rusinov, GL; Rusinov, VL; Charushin, VN; Kopchuk, DS; Zyryanov, GV; Artem’ev, GA or concate me.. Application In Synthesis of 1H-1,2,4-Triazol-5-amine

Recommanded Product: 61-82-5. Authors Baklykov, AV; Rusinov, GL; Rusinov, VL; Charushin, VN; Kopchuk, DS; Zyryanov, GV; Artem’ev, GA in MAIK NAUKA/INTERPERIODICA/SPRINGER published article about in [Baklykov, A. V.; Rusinov, G. L.; Rusinov, V. L.; Charushin, V. N.; Kopchuk, D. S.; Zyryanov, G. V.; Artem’ev, G. A.] Russian Acad Sci, Postovskii Inst Organ Synth, Ural Branch, Ul S Kovalevskoi Akad Skaya 22-20, Ekaterinburg 620990, Russia; [Baklykov, A. V.; Rusinov, G. L.; Rusinov, V. L.; Charushin, V. N.; Kopchuk, D. S.; Zyryanov, G. V.] Yeltsin Ural Fed Univ, Ul Mira 19, Ekaterinburg 620002, Russia in 2019.0, Cited 7.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5

5-Methyl-1,2,4-triazolo[1,5-a]pyrimidin-7(4H)-one, an intermediate product in the synthesis of the antiviral drug Triazid (R), was obtained for the first time by condensation of 3H-1,2,4-triazol-5-amine with ethyl acetoacetate in the presence of a catalytic amount of ZnCl2 in supercritical carbon dioxide (200 bar) under solvent-free conditions. Depending on the temperature and reaction time, the conversion was 90%.

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About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Kachaeva, MV; Pilyo, SG; Hartline, CB; Harden, EA; Prichard, MN; Zhirnov, VV; Brovarets, VS or concate me.. SDS of cas: 61-82-5

SDS of cas: 61-82-5. In 2019.0 MED CHEM RES published article about GANCICLOVIR; INHIBITION; MUTATIONS in [Kachaeva, Maryna V.; Pilyo, Stepan G.; Zhirnov, Victor V.; Brovarets, Volodymyr S.] NAS Ukraine, VP Kukhar Inst Bioorgan Chem & Petrochem, Dept Chem Bioact Nitrogen Containing Heterocycl B, 1 Murmanskaya Str, UA-02094 Kiev, Ukraine; [Hartline, Caroll B.; Harden, Emma A.; Prichard, Mark N.] Univ Alabama Birmingham, Dept Pediat, Birmingham, AL 35233 USA in 2019.0, Cited 34.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.

Ten 5-functionalized derivatives of 1,3-oxazole-4-carboxylate and 1,3-oxazole-4-carbonitrile were synthesized and their antiviral activities against the human cytomegalovirus (HCMV) were evaluated in vitro. Bioassays showed that seven compounds exhibited considerably higher antiviral activity (EC50:<0.05M) against a normal laboratory HCMV strain (AD-169) in human foreskin fibroblast cells than Ganciclovir (EC50=0.32M), an anti-HCMV agent in clinical use. Additionally, the HCMV-resistant isolate (GDGr K-17) was tested for sensitivity to 1,3-oxazole derivatives with most antiviral potency against the strain AD169. A one of them (5-((2-hydroxyethyl)(methyl)amino)-2-(4-methylphenyl)-1,3-oxazole-4-carbonitrile) showed very high potency (EC50:<0.05; CC50: >150 mu M, and SI50=3125) towards the resistant isolate compared to standard drugs Cidofovir (EC50=0.10 mu M, CC50: >30 mu M and SI50: <4). But, in contrast to the primary assays, the antiviral activity of these compounds against both the normal strain and the resistant isolate of HCMV were considerably less than one of Cidofovir in secondary assay. These results provided evidence that derivatives of 1,3-oxazole could be useful for developing new anti-HCMV drugs. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Kachaeva, MV; Pilyo, SG; Hartline, CB; Harden, EA; Prichard, MN; Zhirnov, VV; Brovarets, VS or concate me.. SDS of cas: 61-82-5

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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.

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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.

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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.