T8395

Nomegestrol acetate is a widely used progestin-like drug,which is characterized as a full agonist at the progesterone receptor

ARN 11391 enhances the function of the IP3-gated calcium channel ITPR1 (Inositol 1,4,5-trisphosphate (IP3) receptor type 1), boosting intracellular calcium ion signaling by directly targeting ITPR1. Furthermore, ARN 11391 amplifies calcium signaling in cells with mutant ITPR1 linked to SCA29, a variant of spinocerebellar ataxia.

TM2 TEAD inhibitor is an effective and reversible inhibitor of TEA domain transcription factors, exhibiting IC₅₀ values of 38 nM and 156 nM for TEAD4 auto-palmitoylation and TEAD2 palmitoylation, respectively. TM2 TEAD inhibitor blocks TEAD-YAP binding and suppresses its transcriptional activity, exhibiting significant antiproliferative effects in YAP-dependent cancer cells. It demonstrates potent efficacy both as a monotherapy and in combination with MEK inhibitors. Furthermore, TM2 TEAD inhibitor strongly inhibits YAP-dependent liver organoid growth in vitro, supporting its potential application as an anticancer therapeutic strategy.

Pomalidomide 4'-PEG5-amine, a cereblon ligand designed for PROTAC research and development, features an integrated E3 ligase ligand and a PEG5 linker ending in an amine for easy conjugation to target protein ligands. It is among a series of functionalized tool molecules specifically crafted for PROTAC R&D.

VH 032 amide-alkylC7-acid is a specialized compound designed for PROTAC research and development, serving as a functionalized von-Hippel-Lindau (VHL) protein ligand. It combines an E3 ligase ligand with an alkylC7 linker, ending in a terminal carboxylic acid for efficient conjugation to target protein ligands. This compound is among a series of functionalized tool molecules aimed at facilitating PROTAC R&D efforts.