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SIBA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SIBA图片
CAS NO:35899-54-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品名称
5'-Isobutylthioadenosine
5'-Deoxy-5'-isobutylthioadenosine
产品介绍
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].

IC50& Target[2]

Plasmodium

 

HSV-1

 

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.
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.
分子量

339.41

性状

Solid

Formula

C14H21N5O3S

CAS 号

35899-54-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL(294.63 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.9463 mL14.7314 mL29.4629 mL
5 mM0.5893 mL2.9463 mL5.8926 mL
10 mM0.2946 mL1.4731 mL2.9463 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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。