FC 11 is a highly potent focal adhesion Ki nase (FAK) PROTAC®Degrader (DC50 values are 40 to 370 pM depending on cell line), which is composed of the FAK inhibitor PF 562217 joined by a linker to the cereblon-binding ligand Pomalidomide. The effects of FC 11 are reversible upon compound wash out. FC 11 also degrades autophosphorylated FAK (pFAKtyr397), displaying near complete degradation after 3 hours at 100 nM in TM3 cells.
Pomalidomide-PEG3-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
Thalidomide-O-amido-C3-COOH is a synthesized conjugate of an E3 ligase ligand-linker compound that combines a cereblon ligand derived from Thalidomide with a linker commonly employed in PROTAC technology.
Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is an E3 ligase ligand-linker conjugate which is designed using Thalidomide-based cereblon ligand and a 3-unit PEG linker. This compound is synthesized specifically for utilization in PROTAC technology.
Thalidomide-O-amido-PEG1-(C1-PEG)2-C2-NH2 is a synthesized conjugate compound known as an E3 ligase ligand-linker. It incorporates a cereblon ligand based on Thalidomide and a 3-unit PEG linker. This compound is specifically designed for use in PROTAC technology applications.
Lenalidomide-PEG3-iodine, an E3 ligase ligand-linker conjugate, consists of a cereblon-based Lenalidomide ligand and a 3-unit polyethylene glycol (PEG) linker. This compound is utilized in creating various proteolysis targeting chimeras (PROTACs), including the highly effective PROTAC BTK degrader SJF620, which has a degradation concentration 50 (DC50) of 7.9 nM[1].
Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride is a chemical compound that has been synthesized as an E3 ligase ligand-linker conjugate. This compound incorporates a cereblon ligand derived from Thalidomide and a 3-unit PEG linker. It is specifically designed for use in PROTAC technology, which utilizes small molecules to induce protein degradation [1].
PROTAC CARM1/IKZF3 degrader-1 (Compound 074) 抑制CARM1并减少其底物BAF155的甲基化。它是通过CRBN依赖途径降解IKZF 1/3的PROTAC降解剂,抑制MYC蛋白表达,以减缓多发性骨髓瘤细胞的增殖,并诱导H929细胞凋亡 (apoptosis)。此外,该化合物能够克服对免疫调节药物(IMiD,如泊马度胺)的耐药性,适用于癌症和免疫学研究。(Pink: ligand for target protein CARM1/IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)