Flezurafenib is an oral inhibitor of pan-RAF with potential antineoplastic activity.

YX0597 is a potent and selective CDK9 PROTAC degrader that reduces RNA polymerase II S2 phosphorylation and MCL1 expression in GA0518 and AGS cells. It effectively inhibits GEAC cell growth, including radiation-resistant tumors, and suppresses tumor proliferation, metastasis, and cancer stem cells.

YW-N-7 TFA is a PROTAC that targets the inhibition and degradation of RET with a DC50 of 88 nM. It also exhibits antitumor activity in a KIF5B-RET-driven xenograft mouse model.

Ivospemin is a spermine analogue and polyamine inhibitor that lowers polyamine levels by inhibiting the activity of the polyamine biosynthetic enzyme ornithine decarboxylase (ODC) in cancer cell lines. It shows potential as a treatment for metastatic pancreatic adenocarcinoma.

PM534 is a potent microtubule-targeting agent (MTA) that binds the colchicine-binding domain (CBD) and inhibits tubulin assembly with IC50 values ranging from 0.8 to 3.2 nM. It also significantly inhibits tumor growth in mouse xenograft models of human non-small cell lung cancer.

ID11916 is an orally available antagonist of Androgen receptor (AR) that blocks androgen binding, AR nuclear translocation, and transcriptional activity. It also inhibits PDE5 and exhibits anti-proliferative activity. ID11916 inhibits tumor growth in the MDA-MB-453 xenograft model.

Certepetide is a cyclic peptide that enhances delivery of coadministered anticancer drugs and modulates the tumor microenvironment. It binds αvβ3/5-integrins on tumor endothelium, undergoes proteolytic cleavage, and the resulting fragment binds neuropilin-1, triggering active tumor-specific drug transport. It also depletes immunosuppressive T cells, enhances cytotoxic T cells, and inhibits metastasis.

ATUX-1215 is an orally bioavailable diarylmethyl-4-aminopyran sulfonamide that activates protein phosphatase 2A (PP2A) by stabilizing AC heterodimers and promoting heterotrimer formation with B subunits. It restores suppressed PP2A activity in IPF models, improving lung function, reducing collagen deposition, and downregulating fibrotic cytokines. ATUX-1215 also exhibits potent antifibrotic effects.

RJG-2051 is a selective covalent SuTEx inhibitor of AKR1C3 with an IC50 of 13 nM that targets a noncatalytic tyrosine residue (Y24), effectively blocking its enzymatic activity and disrupting androgen, estrogen, and prostaglandin metabolism.

Ecubectedin (PM14) is a transcriptional inhibitor that forms DNA adducts, blocking RNA synthesis and the transcription of protein-coding genes. It also exhibits potent antiproliferative activity in human solid cancer models both in vitro and in vivo.