Thailanstatin A |
| Catalog No.GC62288 |
La thailanstatina A es un inhibidor ultrapotente del empalme del ARN eucariÓtico (IC50=650 nM). La thailanstatina A ejerce efectos a través de la uniÓn no covalente a la subunidad SF3b del subcomplejo U2 snRNA del spliceosoma y muestra IC50 de nM bajo a sub-nM contra mÚltiples lÍneas celulares de cÁncer. La thailanstatina A, una carga Útil para los ADC, se conjuga con las lisinas en trastuzumab y produce ADC \Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding "linker-less" ADC.en_es_2021q4.md
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1426953-21-0
Sample solution is provided at 25 µL, 10mM.
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Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding "linker-less" ADC[1][2][3].
Thailanstatin A (TST-A) is a potent antiproliferative natural product discovered by our group from Burkholderia thailandensis MSMB43[2].Thailanstatin A (DU-145, NCI-H232A, MDA-MB-231 and SKOV-3 cells) exhibits potent antiproliferative activities with GI50s in the single nM range (1.11-2.69 nM)[3].
[1]. Puthenveetil S, et al. Natural Product Splicing Inhibitors: A New Class of Antibody-Drug Conjugate (ADC) Payloads. Bioconjug Chem. 2016;27(8):1880-1888.
[2]. Ghosh AK, et al. Enantioselective Synthesis of Thailanstatin A Methyl Ester and Evaluation of in Vitro Splicing Inhibition. J Org Chem. 2018;83(9):5187-5198.
[3]. Liu X, et al. Genomics-guided discovery of thailanstatins A, B, and C As pre-mRNA splicing inhibitors and antiproliferative agents from Burkholderia thailandensis MSMB43. J Nat Prod. 2013;76(4):685-693.
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