SIBA

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SIBA 是 SAH 的合成类似物，作为 S-腺苷甲硫氨酸介导的转甲基化的抑制剂。 SIBA在体外可干扰多种酶活性，如SAH水解酶、甲硫腺苷磷酸化酶和cAMP磷酸二酯酶。

SIBA is a synthetic analogue of SAH,?acts as an inhibitor of S-adenosylmethionine-mediated transmethylation. SIBA can interfere with a variety of enzymatic?activities in vitro, such as SAH hydrolase,?methylthioadenosine phosphorylase and cAMP phosphodiesterase. SIBA reversibly blocks the multiplication of herpes?simplex type 1 virus (HSV)?.

SIBA (0.5 mM; 24-96 h) shows strong anti-proliferative activity against 3LL and RMS-J1 tumour cells.SIBA (1 mM; 12, 24 h) reversibly inhibits HSV production in HEp2 cells (infected by HSV-1).SIBA inhibits protein synthesis by 98% after 10 h infection of HEp2 cells (infected by HSV-1).SIBA (1 mM; 8.5 h) inhibits protein synthesis and RNA methylation in HEp2 cells (infected by HSV-1).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). Cell Proliferation Assay 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 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 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 AssayCell Line:chick embryo fibroblastsConcentration:0.5, 1.0 mMIncubation 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.

SIBA (150 mg/kg; i.p.; twice weekly for 3 weeks) inhibits tumor growth in vivo.SIBA (15 mg/kg; i.p.; thrice weekly for 4 weeks) inhibits metastatic spread of RMS-J1 cells in vivo. Animal Model:C57BL/6 female mice (4-8 weeks old).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).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.

5'-Isobutylthioadenosine | 5'-Deoxy-5'-isobutylthioadenosine

Microbiology/Virology

HSV

HSV|Nucleoside Antimetabolite/Analog

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35899-54-8

339.41

C14H21N5O3S

>98% (HPLC)

DMSO:90 mg/mL (265.17 mM)

CC(C)CSC[C@H]([C@H]([C@H]1O)O)O[C@H]1n1c2ncnc(N)c2nc1

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(-20℃)

With Ice Pack

≥ 2 years