Pladienolide B

• CAT Number: I011370
• CAS Number: 445493-23-2
• Molecular Formula: C30H48O8
• Molecular Weight: 536.70
• Purity: ≥95%
• Synonyms: [(2S,3S,4E,6S,7R,10R)-7,10-dihydroxy-2-[(2E,4E,6S)-7-[(2R,3R)-3-[(2R,3S)-3-hydroxypentan-2-yl]oxiran-2-yl]-6-methylhepta-2,4-dien-2-yl]-3,7-dimethyl-12-oxo-1-oxacyclododec-4-en-6-yl] acetate
• InChI: InChI=1S/C30H48O8/c1-8-24(33)21(5)29-25(37-29)16-18(2)10-9-11-19(3)28-20(4)12-13-26(36-22(6)31)30(7,35)15-14-23(32)17-27(34)38-28/h9-13,18,20-21,23-26,28-29,32-33,35H,8,14-17H2,1-7H3/b10-9+,13-12+,19-11+/t18-,20+,21-,23-,24+,25-,26+,28-,29-,30-/m1/s1
• InChIKey: SDOUORKJIJYJNW-QHOUZYGJSA-N
• SMILES: CCC(C(C)C1C(O1)CC(C)C=CC=C(C)C2C(C=CC(C(CCC(CC(=O)O2)O)(C)O)OC(=O)C)C)O

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[1][2][3].
Pladienolide B (0.1-2 nM; 24-72 hours) inhibits human cervical carcinoma cells viability[3].
Pladienolide B (0.1-2 nM; 24-48 hours) reduces SF3b1 expression in human cervical carcinoma cells[3].
Pladienolide B induces (0.1-2 nM; 24 hours) cell cycle arrest and apoptosis[3].
Pladienolide B (2.5-10 mg/kg; i.v.; daily for 5 days) has strong antitumor activities[4].

Reference

[1]. Effenberger KA, et al. Coherence between cellular responses and in vitro splicing inhibition for the anti-tumor drug pladienolide B and its analogs. J Biol Chem. 2014 Jan 24;289(4):1938-47.
 [Content Brief]

[2]. Aouida M, et al. CRISPR/Cas9-mediated target validation of the splicing inhibitor Pladienolide B. Biochim Open. 2016 Feb 24;3:72-75.
 [Content Brief]

[3]. Zhang Q, et al. Inhibition of SF3b1 by pladienolide B evokes cycle arrest, apoptosis induction and p73 splicing in human cervical carcinoma cells. Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):1273-1280.
 [Content Brief]

[4]. Mizui Y, et al. Pladienolides, new substances from culture of Streptomyces platensis Mer-11107. III. In vitro and in vivo antitumor activities. J Antibiot (Tokyo). 2004 Mar;57(3):188-96.
 [Content Brief]