Pladienolide B 是一种有效的癌细胞生长抑制剂，其作用靶向剪接体的 SF3B1 亚单位。Pladienolide B 通过抑制前 mRNA 剪接发挥抗肿瘤作用，诱导调亡。
Pladienolide B Chemical Structure
CAS No. : 445493-23-2
规格
价格
是否有货
数量
100 μg
￥5500
In-stock
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生物活性
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].
体外研究 (In Vitro)
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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[3]
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[3]
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[3]
Cell Line:
HeLa cells
Concentration:
0.1, 0.5, and 2 nM
Incubation Time:
24, 48 hours
Result:
Induced a time- and concentration-dependent decrease in cellular SF3b1 proteins.
体内研究 (In Vivo)
Pladienolide B (2.5-10 mg/kg; i.v.; daily for 5 days) has strong antitumor activities[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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)[4]
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.
分子量
536.70
Formula
C30H48O8
CAS 号
445493-23-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form
-20°C
3 years
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[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.
[2]. Aouida M, et al. CRISPR/Cas9-mediated target validation of the splicing inhibitor Pladienolide B. Biochim Open. 2016 Feb 24;3:72-75.
[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.
[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.
