AGK 2 |
| Catalog No.GC17881 |
AGK 2는 선택적 SIRT2 억제제로 IC50가 3.5 µM이다. AGK2는 SIRT1과 SIRT3를 IC50 30과 91 µM로 억제한다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 304896-28-4
Sample solution is provided at 25 µL, 10mM.
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AGK 2는 선택적 SIRT2 억제제로 IC50가 3.5 µM이다. AGK2는 SIRT1과 SIRT3를 IC50 30과 91 µM로 억제한다.
AGK2(0.01-20 µM; 24시간)는 체외에서 매스트 셀의 탈그래느레이션을 억제한다. AGK2 처리는 RBL-2H3 세포에서 높은 수준의 β-hexosaminidase와 히스타민을 낮춘다[3]. AGK2(1-5 µM; 24시간)는 HSF1 단백질의 안정성을 억제하여 HeLa 세포의 세포 성장과 이동을 억제한다[4]. AGK2에 의한 Sirtuin 2(SIRT2) 억제는 기본 감염 및 결핵 재발 중 BCG 백신의 효과를 크게 향상시키고 향상된간세포 기억(TSCM) 반응을 통해 이를 실현한다[5].
AGK2(1 µmol/쥐; i.p.; 26시간)는 LPS 처리된 쥐 뇌 조직에서 BV2 미세 글리아의 활성화와 iNOS 및 SIRT2의 표현을 억제할 수 있다[6]. AGK2(1 µmol/쥐; i.p.; 26시간) 전처리는 또한 급성 간 기능불전(ALF) 간 조직에서 pro-염증 사이토카인의 수준을 낮춘다. AGK2는 티오아세트 아미드(TAA) 유도 생존율을 개선한다[7]. AGK2(82 mg/kg; i.p.; 7일) 치료는 serum HBV DNA, HBeAg 및 HBsAg 수준을 억제하고 HBV 전기적 쥐의 간 HBV DNA, RNA 및 HBc도 억제한다[8].
References:
[1]. Tatum PR, Sawada H, et,al. Identification of novel SIRT2-selective inhibitors using a click chemistry approach. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1871-4. doi: 10.1016/j.bmcl.2014.03.026. Epub 2014 Mar 20. PMID: 24675380.
[2]. Outeiro TF, Kontopoulos E, et,al. Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science. 2007 Jul 27;317(5837):516-9. doi: 10.1126/science.1143780. Epub 2007 Jun 21. PMID: 17588900.
[3]. Kim YY, Hur G, et,al. AGK2 ameliorates mast cell-mediated allergic airway inflammation and fibrosis by inhibiting FcεRI/TGF-β signaling pathway. Pharmacol Res. 2020 Sep;159:105027. doi: 10.1016/j.phrs.2020.105027. Epub 2020 Jun 18. PMID: 32565308.
[4]. Kim HW, Kim SA, et,al. Sirtuin inhibitors, EX527 and AGK2, suppress cell migration by inhibiting HSF1 protein stability. Oncol Rep. 2016 Jan;35(1):235-42. doi: 10.3892/or.2015.4381. Epub 2015 Nov 2. PMID: 26530275.
[5]. Bhaskar A, Pahuja I, et,al. SIRT2 inhibition by AGK2 enhances mycobacteria-specific stem cell memory responses by modulating beta-catenin and glycolysis. iScience. 2023 Apr 10;26(5):106644. doi: 10.1016/j.isci.2023.106644. PMID: 37192966; PMCID: PMC10182326.
[6]. Jiao F, Wang Y, et,al. AGK2 Alleviates Lipopolysaccharide Induced Neuroinflammation through Regulation of Mitogen-Activated Protein Kinase Phosphatase-1. J Neuroimmune Pharmacol. 2020 Jun;15(2):196-208. doi: 10.1007/s11481-019-09890-x. Epub 2019 Nov 30. PMID: 31786712.
[7]. Jiao FZ, Wang Y, et,al. Protective role of AGK2 on thioacetamide-induced acute liver failure in mice. Life Sci. 2019 Aug 1;230:68-75. doi: 10.1016/j.lfs.2019.05.061. Epub 2019 May 23. PMID: 31129140.
[8]. Yu HB, Jiang H, et,al. AGK2, A SIRT2 Inhibitor, Inhibits Hepatitis B Virus Replication In Vitro And In Vivo. Int J Med Sci. 2018 Sep 7;15(12):1356-1364. doi: 10.7150/ijms.26125. PMID: 30275764; PMCID: PMC6158674.
| 세포 실험 [1]: | |
세포 라인 | RBL-2H3세포 |
제조 방법 | 세포는 AGK2와 함께 재배되었고 총 β-glucosamine 활성이 측정되었습니다. |
반응 조건 | 0.01–20 μM;24 시간 동안 |
응용 분야 | AGK2 처리는 RBL-2H3 세포에서 높은 수준의 β-hexosaminidase와 히스타민을 낮췄습니다. |
| 동물 실험 [2]: | |
동물 모형 | 수컷 C57BL/6 J 쥐 (6–7주령) |
제조 방법 | 쥐는 네 그룹으로 나뉘어져 있습니다: 컨트롤, LPS, AGK2+LPS, AGK2 그룹입니다. LPS 그룹은 복강 주사를 통해 LPS(10 mg/kg)를 투여받았습니다. AGK2의 복용 량은 1 μmol/쥐였습니다. AGK2(25mg)은 DMSO에 녹아 10 mM 모공을 형성했습니다. 그리고 그 용액은 정상 염수(NS)로 희석되어 AGK2(400 μM, 4% DMSO)의 최종 농도를 형성했습니다. AGK2 + LPS 그룹과 AGK2 그룹에 대해 2.5 ml AGK2(400 μM)가 각 쥐의 복강에 주입되었습니다. AGK2는 AGK2+LPS 그룹에서는 LPS 투여 2시간 전에 주어졌습니다. 동일한 부피의 4% DMSO 용액이 컨트롤 그룹에도 주입되었습니다. 모든 쥐는 LPS 치료 후 24시간에 희생되어 뇌 조직을 수확했습니다. |
제형 | 1 μmol/쥐; i.p;26시간 동안 |
응용 분야 | AGK2는 쥐 뇌에서 LPS 처리 후 염증성 사이토카인의 표현을 억제했습니다. |
참고문헌: [1]. Kim YY, Hur G, et,al. AGK2 ameliorates mast cell-mediated allergic airway inflammation and fibrosis by inhibiting FcεRI/TGF-β signaling pathway. Pharmacol Res. 2020 Sep;159:105027. doi: 10.1016/j.phrs.2020.105027. Epub 2020 Jun 18. PMID: 32565308. [2]. Jiao F, Wang Y, et,al. AGK2 Alleviates Lipopolysaccharide Induced Neuroinflammation through Regulation of Mitogen-Activated Protein Kinase Phosphatase-1. J Neuroimmune Pharmacol. 2020 Jun;15(2):196-208. doi: 10.1007/s11481-019-09890-x. Epub 2019 Nov 30. PMID: 31786712. | |
| Cas No. | 304896-28-4 | SDF | |
| Chemical Name | (E)-2-cyano-3-(5-(2,5-dichlorophenyl)furan-2-yl)-N-(quinolin-5-yl)acrylamide | ||
| Canonical SMILES | ClC(C(C1=CC=C(/C=C(C#N)/C(NC2=C3C(N=CC=C3)=CC=C2)=O)O1)=C4)=CC=C4Cl | ||
| Formula | C23H13Cl2N3O2 | M.Wt | 434.27 |
| Solubility | ≥ 9.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3027 mL | 11.5136 mL | 23.0271 mL |
| 5 mM | 0.4605 mL | 2.3027 mL | 4.6054 mL |
| 10 mM | 0.2303 mL | 1.1514 mL | 2.3027 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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