3-Deazaadenosine Chemical Structure
CAS No. : 6736-58-9
3-Deazaadenosine 是一(yī)種 S-腺苷高(gāo)半胱氨酸水解酶 (S-adenosylhomocysteine hydrolase) 抑制劑，Ki 值為(wèi) 3.9 µM；3-Deazaadenosine 具有(yǒu)抗炎、抗增殖、抗 HIV 等活性。
| 規格 | 10 mg/支 |
| 貨号 | GM-2022131 |
| 生物活性 | 3-Deazaadenosine (hydrochloride) is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity. |
| IC50 & Target | IC50: 0.15 (HIV-1, A012 isolate), 0.20 µM (HIV-1, A018 isolate)[1] Ki: 3.9 µM (S-adenosylhomocysteine hydrolase)[1] |
| 體外研究 (In Vitro) | 3-Deazaadenosine is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM. 3-Deazaadenosine shows anti-HIV effect, and inhibits p24 antigen in peripheral blood mononuclear (PBMCs) cells infected with HIV-1 isolates (A012 and A018) with IC50s of 0.15 and 0.20 µM, respectively[1]. 3-Deazaadenosine (1-100 µM) inhibits LPS-induced expression of TNF-α mRNA, increases DNA binding activity of NF-κB, and causes proteolytic degradation of IκBα, but Not IκBβ in RAW 264.7 cells. 3-Deazaadenosine (100 µM) enhances nuclear translocation of NF-κB, but blocks LPS-induced NF-κB transcriptional activity, and such inhibition is augmented by the addition of homocysteine[2]. 3-Deazaadenosine (50, 100 µM) dose-dependently inhibits the phosphorylation of Raf and ERK, protein-dependent kinase 1, protein kinase B (Akt), and forkhead transcription factor FoxO1a. 3-Deazaadenosine (50 µM) suppresses vascular smooth muscle cell (VSMC) proliferation via interfering with Ras signaling[3]. WE has not independently confirmed the accuracy of these methods. They are for reference only. |
| 分子(zǐ)量 | 302.71 |
| Formula | C₁₁H₁₅ClN₄O₄ |
| CAS 号 | 86583-19-9 |
| 運輸條件 | Room temperature in continental US; may vary elsewhere. |
| 儲存方式 | 4°C, sealed storage, away from moisture |
| *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
參考文獻
| [1]. Gordon RK, et al. Anti-HIV-1 activity of 3-deaza-adenosine analogs. Inhibition of S-adenosylhomocysteine hydrolase and nucleotide congeners. Eur J Biochem. 2003 Sep;270(17):3507-17. |
| [2]. Jeong SY, et al. 3-deazaadenosine, a S-adenosylhomocysteine hydrolase inhibitor, has dual effects on NF-kappaB regulation. Inhibition of NF-kappaB transcriptional activity and promotion of IkappaBalpha degradation. J Biol Chem. 1999 Jul 2;274(27):18981-8. |
| [3]. Sedding DG, et al. 3-Deazaadenosine prevents smooth muscle cell proliferation and neointima formation by interfering with Ras signaling. Circ Res. 2009 May 22;104(10):1192-200. |
