TGF-β Receptor Modulator

PROTAC AR Degrader-9 is a topically applicable androgen receptor (AR) PROTAC degrader. PROTAC AR Degrader-9 recruits Cereblon (CRBN) E3 ubiquitin ligase to induce AR ubiquitination and proteasomal degradation in human dermal papilla cells (HDPCs) with a DC₅₀ of 262.38 nM. PROTAC AR Degrader-9 possesses excellent skin retention, modulates androgenetic alopecia (AGA)-related downstream paracrine factors including TGF-β1 and β-catenin, promotes hair regeneration in mice. and exhibits favorable skin pharmacokinetics profiles with minimal systemic exposure. PROTAC AR Degrader-9 can be used for the study of androgenetic alopecia (AGA).

L-744832 is a farnesyl transferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer.