Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 =650 nM). Thailanstatin A inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC 50 s against . Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC.

Thailanstatin A（TST-A）是我们小组从Burkholderia thailandensis MSMB43 [2] 中发现的一种高效抗增殖天然产物。在DU-145、NCI-H232A、MDA-MB-231和SKOV-3细胞中，Thailanstatin A展示了强大的抗增殖活性，GI 50 值处于单nM范围内（1.11-2.69 nM）[3]。