Azaserine (Synonyms: CI-337,CN 15757,O-Diazoacetyl-L-serine,NSC 742) |
| Catalog No.GC14874 |
Azaserine은 글루타민 길항제이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 115-02-6
Sample solution is provided at 25 µL, 10mM.
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Azaserine은 글루타민 길항제이다. Azaserine은 글루타민 아미도전이효소를 억제해서 퓨린 핵간산의 생성을 방해하고 그 결과 DNA와 RNA 합성을 억제한다 [2]. Azaserine은 헥사민 생합성 경로를 억제해서 UDP-N-아세틸글루코사민과 단백질 O-당화의 생성을 줄이고 세포의 포도당 대사와 단백질의 후 합성 변형에 영향을 미친다 [3]. Azaserine은 주로 췌장 종양 치료에 사용된다 [4].
R28 세포에서 Azaserine (0.1μM; 24시간)은 포도당이 헥사민 생합성 경로 (HBP)로의 진입을 차단해서 고혈당이 인슐린의 항사멸 효과에 미치는 억제 작용을 역전시킨다 [5]. Raji 세포에서 Azaserine (5μM; 24시간)은 세포 성장을 억제한다 [6].
References:
[1]. Livingston R B, Venditti J M, Cooney D A, et al. Glutamine antagonists in chemotherapy[J]. Advances in Pharmacology, 1971, 8: 57-120.
[2]. SARTORELLI A C, BOOTH B A. Inhibition of the synthesis of thymine nucleotides by azaserine[J]. Molecular Pharmacology, 1967, 3(1): 71-80.
[3]. Rajapakse A G, Ming X F, Carvas J M, et al. The hexosamine biosynthesis inhibitor azaserine prevents endothelial inflammation and dysfunction under hyperglycemic condition through antioxidant effects[J]. American Journal of Physiology-Heart and Circulatory Physiology, 2009, 296(3): H815-H822.
[4]. Longnecker D S, Curphey T J. Adenocarcinoma of the pancreas in azaserine-treated rats[J]. Cancer research, 1975, 35(8): 2249-2257.
[5]. Nakamura M, Barber A J, Antonetti D A, et al. Excessive hexosamines block the neuroprotective effect of insulin and induce apoptosis in retinal neurons[J]. Journal of Biological Chemistry, 2001, 276(47): 43748-43755.
[6]. O'Driscoll M, Macpherson P, Xu Y Z, et al. The cytotoxicity of DNA carboxymethylation and methylation by the model carboxymethylating agent azaserine in human cells[J]. Carcinogenesis, 1999, 20(9): 1855-1862.
| 세포 실험 [1]: | |
세포 라인 | R28 세포 |
제조 방법 | 5 mM 포도당, 20 mM 포도당 또는 5 mM 포도당에 1.5 mM 글루코사민이 추가된 (10 nM 인슐린이나 0.1μM Azaserine과 유무에 상관없이) 환경에서 24 시간 동안 배양한 후 R28 세포의 100 mm 플레이트를 빙냉 인산 버퍼로 한 번 세척하고 0.3 mM 퍼클로리산 0.5 mL에서 균질화하였습니다. 세포를 원심분리해서 퍼클로리산을 1:4 트리옥틸아민:1,1,2-트리클로로플루오로에탄과 2 부피로 상청액에서 추출하였습니다. 수용액은 -80℃에서 보관하고 5일 이내에 분석하였다. 핵간산-연결된 헥소스와 헥소사민은 음이온교환 고압 액체 크로마토그래피로 분리 및 측정하였습니다. UDP-HexNAc와 UDP-hexose는 UV 흡수로 정량화되었고 외부 표준과 비교하였습니다. |
반응 조건 | 0.1μM; 24시간 동안 |
응용 분야 | Azaserine은 포도당의 헥사민 생합성 경로 (HBP)로의 진입을 차단해서 고혈당이 인슐린의 항사멸 효과에 미치는 억제 작용을 역전시킵니다. |
References: | |
| Cas No. | 115-02-6 | SDF | |
| Synonyms | CI-337,CN 15757,O-Diazoacetyl-L-serine,NSC 742 | ||
| Chemical Name | O-(2-diazoacetyl)-L-serine | ||
| Canonical SMILES | O=C(C=[N+]=[N-])OC[C@H](N)C(O)=O | ||
| Formula | C5H7N3O4 | M.Wt | 173.1 |
| Solubility | ≥ 21.4 mg/mL in Water | 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 | 5.777 mL | 28.885 mL | 57.7701 mL |
| 5 mM | 1.1554 mL | 5.777 mL | 11.554 mL |
| 10 mM | 577.7 μL | 2.8885 mL | 5.777 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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