Thailanstatin A

Description

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 AAasAasAalinker-lessAAasAasAa ADC.