tmx-2

TMX-2172 is a heterobifunctional CDK2 degrader, selectively degrading CDK2 and CDK5, with minimal effects on CDK1, transcriptional CDKs (CDK7 and CDK9), and cell cycle CDKs (CDK4 and CDK6). In ovarian cancer cells (OVCAR8), its anti-proliferative activity is dependent on CDK2 degradation and is linked to high expression of cyclin E1 (CCNE1), which acts as a regulatory subunit of CDK2. As a lead compound for further development, TMX-2172 demonstrates that CDK2 degradation could be a potentially effective strategy for treating ovarian and other cancers with elevated CCNE1 expression.

TMX-2138 is a CDKs PROTAC degrader, with IC50 values of 8.7 nM for CDK1 cyclinB, 10.9 nM for CDK2 cyclinA, 7.0 nM for CDK5 p25, and 25.7 nM for CDK9 cyclinT1. It enhances the ubiquitination and degradation of CDKs and is utilized for ovarian cancer research.

TMX-2039 is a pan-CDK inhibitor that targets cell cycle CDKs (CDK1, CDK2, CDK4, CDK5, and CDK6) and transcription CDKs (CDK7 and CDK9), with IC50 values of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5, and 25 nM, respectively. It serves as a ligand for the target protein in PROTAC applications.

TMX-2164, a potent and irreversible inhibitor of B-cell lymphoma 6 (BCL6), demonstrates an IC50 of 152 nM, indicating strong inhibitory efficacy. It exhibits prolonged target engagement and effectively inhibits cell proliferation.

TMX-201, a TLR7 ligand-phospholipid conjugate, exhibits potent immune-stimulatory activity and is utilized in breast cancer and melanoma research [1].