|Pladienolide B 目录号 GC18780|
Sample solution is provided at 25 µL, 10mM.
|Cas No.||445493-23-2||SDF||Download SDF|
|溶解度||Soluble in methanol, ethanol, DMSO, DMF||储存条件||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
Spliceosomes mediate the processing of pre-mRNA into mature mRNA., Each spliceosome is a multiunit complex containing several proteins and RNA molecules that work in unison to repeatedly cleave and rejoin segments of mRNA., Pladienolide B is a macrocyclic lactone that selectively binds splicing factor 3b and inhibits mRNA splicing., Through this action, pladienolide B potently blocks the growth of proliferating cells with mean IC50 values of 1.6 nM for six gastric cancer cell lines., In xenograft tumors generated in mice using human cancer cells, pladienolide B blocks mRNA splicing and induces apoptosis, clearing tumors within two weeks after treatment.
. Naro, C., and Sette, C. Phosphorylation-mediated regulation of alternative splicing in cancer. Int.J.Cell Biol. 2013, 1-16 (2013).
. Webb, T.R., Joyner, A.S., and Potter, P.M. The development and application of small molecule modulators of SF3b as therapeutic agents for cancer. Drug Discovery Today 18(1-2), 43-49 (2013).
. Yokoi, A., Kotake, Y., Takahashi, K., et al. Biological validation that SF3b is a target of the antitumor macrolide pladienolide. FEBS Journal 278(24), 4870-4880 (2011).
. Kotake, Y., Sagane, K., Owa, T., et al. Splicing factor SF3b as a target of the antitumor natural product pladienolide. Nature Chemical Biology 3, 570-575 (2007).
. Effenberger, K.A., Anderson, D.D., Bray, W.M., et al. Coherence between cellular responses and in vitro splicing inhibition for the anti-tumor drug pladienolide B and its analogs. The Journal of Biological Chemisty 289, 1938-1947 (2014).
. Sato, M., Muguruma, N., Nakagawa, T., et al. High antitumor activity of pladienolide B and its derivative in gastric cancer. Cancer Science 105(1), 110-116 (2014).