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.

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.

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.

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.

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.

GDC-2992 (RO7656594, Compound 28A) is an orally active degrader of androgen receptor (AR) with a DC50 of 2.7 nM. It binds to AR and cereblon (CRBN), inducing AR ubiquitination and degradation. GDC-2992 also inhibits cell proliferation in VCaP cells and exhibits potential to reduce treatment resistance and disease relapse in prostate cancer.

WH244 is a second-generation PROTAC that selectively degrades the anti-apoptotic proteins BCL-xL and BCL-2 with a DC50 of 0.6 nM for BCL-xL and 7.4 nM for BCL-2.

SPA-10091-HCl is a degrader of DOT1L that selectively degrades DOT1L protein through the nuclear ubiquitin-proteasome pathway, thereby suppressing H3K79 methylation in CRPC cells. It also inhibits DOT1L enzymatic activity with an IC50 of 0.87 μM, induces apoptosis, and significantly reduces tumor growth in vivo.

Golidocitinib 1-hydroxy-2-naphthoate is a derivative of Golidocitinib, an oral, potent, selective inhibitor of Janus kinase 1 (JAK1) with an IC50 of 70 nM. It exhibits enhnaced antitumor activity and can be used for the treatment of cancer, including peripheral T cell lymphoma (PTCL).