Pladienolide B

Research use only, not for human use.

Pladienolide B is a potent spliceosome inhibitor, a macrolide isolated from Streptomyces obtusususus Mer-12, which targets the SF3B1 subunit of the spliceosome.

Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis.

Pladienolide B (0.1-2 nM; 24-72 hours) inhibits human cervical carcinoma cells viability.Pladienolide B (0.1-2 nM; 24-48 hours) reduces SF3b1 expression in human cervical carcinoma cells.Pladienolide B induces (0.1-2 nM; 24 hours) cell cycle arrest and apoptosis.Cell Viability Assay Cell Line:HeLa cells Concentration:0.1, 0.5, 1, 1.5, 2 nM Incubation Time:24, 48, 72 hours Result:Significantly decreased cell viability, and the decrease was concentration- and time-dependent.Apoptosis Analysis Cell Line:HeLa cells Concentration:0.1, 0.5, and 2 nM Incubation Time:24 hours Result:The apoptotic cells were highly induced at 24 hours.RT-PCR Cell Line:HeLa cells Concentration:0.1, 0.5, and 2 nM Incubation Time:24, 48 hour Result:Induced a time- and concentration-dependent decrease in cellular SF3b1 proteins.

Pladienolide B (2.5-10 mg/kg; i.v.; daily for 5 days) has strong antitumor activities.Animal Model:Female or male BALB/c nu/nu mice (7 weeks of age) (PC-3, OVCAR-3, DU-145, WiDr, and HCT-116, BSY-1 xenografts)Dosage:2.5, 5, and 10 mg/kg Administration:I.v.; daily for 5 days Result:Showed strong growth inhibitory or regressive activities against these xenografts.

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Apoptosis

Apoptosis

Apoptosis

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445493-23-2

536.7

C30H48O8

>98% (HPLC)

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C([C@@H](/C=C/C=C(\C)/[C@@H]1[C@@H](C)/C=C/[C@H](OC(C)=O)[C@](C)(O)CC[C@@H](O)CC(=O)O1)C)[C@@H]2[C@@]([C@@H]([C@H](CC)O)C)(O2)[H]

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(-20℃)

With Ice Pack

≥ 2 years