SIBA (5'-Isobutylthioadenosine) 是一种Transmethylation抑制剂 (SAH (HY-19528) 类似物)，具有强大的抗增殖活性。SIBA 通过阻断甲基化，特别是阻断病毒 mRNA 的5' 端加帽，可逆地抑制 HSV-1 的产生。SIBA 还能抑制肿瘤细胞系的体外生长和体内转移扩散。SIBA 可用于癌症，HSV-1 感染和抗疟疾的研究。
| 生物活性 | SIBA (5'-Isobutylthioadenosine) is atransmethylationinhibitor (SAH(HY-19528) analogue), with potent anti-proliferative activity. SIBA reversibly inhibits the production ofHSV-1by blocking methylation, specifically by blocking the 5' end-capping of viral mRNA. SIBA also inhibits the growth of tumour cells in vitro and metastatic spread in vivo. SIBA can be used incancer, HSV-1infectionand anti-malaria studies[1][2][3]. |
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体外研究
(In Vitro) | SIBA (0.5 mM; 24-96 h) shows strong anti-proliferative activity against 3LL and RMS-J1 tumour cells[1].
SIBA (1 mM; 12, 24 h) reversibly inhibits HSV production in HEp2 cells (infected by HSV-1)[2].
SIBA inhibits protein synthesis by 98% after 10 h infection of HEp2 cells (infected by HSV-1)[2].
SIBA (1 mM; 8.5 h) inhibits protein synthesis and RNA methylation in HEp2 cells (infected by HSV-1)[2].
SIBA (0.5, 1.0 mM; 24, 48 h) inhibits the conversion of putrescine into spermidine and/or spermine and that this inhibition is a reversible one (interferes with polyamine biosynthesis, probably by blocking aminopropyltransferase)[3].
Cell Proliferation Assay[1] | Cell Line: | 3 LL and RMS-J1 cells | | Concentration: | 0.5 mM | | Incubation Time: | 24-96 h | | Result: | Inhibited 3LL and RMS-J1 tumor cell growth potently by 96% and 88%, respectively. |
Cell Viability Assay[2] | Cell Line: | HEp2 cells (infected by HSV-1) | | Concentration: | 1 mM | | Incubation Time: | 12, 24 h | | Result: | Decreased virus production by 88.4 and 98.2% when at 12 and 24 h, respectively. |
Cell Viability Assay[2] | Cell Line: | HEp2 cells (infected by HSV-1) | | Concentration: | 1 mM | | Incubation Time: | 8.5 h | | Result: | Reduced protein synthesis by 41.3% in normal medium and by 63.5% in medium poor in methionine.
Inhibited RNA methylation by 65.4%. |
Cell Viability Assay[3] | Cell Line: | chick embryo fibroblasts | | Concentration: | 0.5, 1.0 mM | | Incubation Time: | 24, 48 h | | Result: | Inhibited the uptake of the radioactive diamine and that the inhibition was dose-dependent.
Markedly inhibited the formation of [14C]spermidine and [14C]spermine from [14C]putrescine.
Inhibited the growth of chick embryo fibroblasts mainly after exposure for 48 h. |
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体内研究
(In Vivo) | SIBA (150 mg/kg; i.p.; twice weekly for 3 weeks) inhibits tumor growth in vivo[1].
SIBA (15 mg/kg; i.p.; thrice weekly for 4 weeks) inhibits metastatic spread of RMS-J1 cells in vivo[1].
| Animal Model: | C57BL/6 female mice (4-8 weeks old)[1]. | | Dosage: | 150 mg/kg | | Administration: | Intraperitoneal injection; twice weekly for 3 weeks. | | Result: | Significantly reduced the median number of lung metastases. |
| Animal Model: | Adult syngeneic Wistar AG rats (8-week-old; subcutaneously grafted with RMS-J1 cells)[1]. | | Dosage: | 15 mg/kg | | Administration: | Intraperitoneal injection; thrice weekly for 4 weeks. | | Result: | Inhibited in vivo metastatic spread of RMS-J1 cells, and showed median numbers of lung metastatic nodules was 26. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(294.63 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.9463 mL | 14.7314 mL | 29.4629 mL | | 5 mM | 0.5893 mL | 2.9463 mL | 5.8926 mL | | 10 mM | 0.2946 mL | 1.4731 mL | 2.9463 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.37 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.37 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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