thailanstatin a

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

Thailanstatin A cyclohexane diamine formic is an analogue of Spliceostatin. It effectively inhibits the proliferation of various cells, including N87 (IC50 = 0.33 μM), BT474 (IC50 = 0.34 μM), MDA-MB-361-DYT2 (IC50 = 0.88 μM), and MDA-MB-468 (IC50 = 0.27 μM). Additionally, Thailanstatin A cyclohexane diamine formic can be utilized as a drug-linker conjugate in ADC (antibody-drug conjugate) molecules.

MC-VC-PAB-Cyclohexanediamine-Thailanstatin A, a spliceostatin analog and drug-linker conjugate for antibody-drug conjugates (ADC), comprises the cytotoxic component Thailanstatin A and the cleavable linker (MC-vc-PAB). This compound is utilized in the synthesis of ADCs [1].

MC-Thailanstatin A serves as a drug-linker conjugate for ADC (Antibody-Drug Conjugates) synthesis. It is utilized in the formation of ADCs [1].

Thailanstatin C, an antiproliferative agent derived from Burkholderia thailandensis MSMB43, functions as a potent inhibitor of pre-mRNA splicing (IC50 = 6.84 μM).

Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis.

Thailanstatin B is a potent pre-mRNA splicing inhibitor [IC50=6.18 μM] and exhibits antiproliferative activity.