4 (n boc amino) 1,6 heptanedioic acid

4-(N-Boc-amino)-1,6-heptanedioic acid is an alkyl ether-based linker suitable for PROTAC synthesis [1].

Propynol Ethoxylate is a PEG-based linker for PROTACs [Proteolysis Targeting Chimeras] that connects two essential ligands, facilitating the formation of PROTAC molecules and enabling selective protein degradation via the ubiquitin-proteasome system within cells.

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor with IC50 values of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively, effectively degrading the BRD4 protein in PC3 prostate cancer cells[1].

PROTAC IRAK4 degrader-6 is a potent Cereblon-based compound designed to degrade [interleukin-1 receptor-associated kinase 4 (IRAK4)].

LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4 6 degrader[1]. [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non-Small Cell Lung Cancer: A Phase Ib Study. [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4 6 (cdk4 6) by conjugation of cdk4 6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

PROTAC SMARCA2 4-degrader-26 is a PROTAC targeting the SMARCA2 4 proteins. It is composed of the ligand for PROTAC targeting proteins, 2-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetic acid, an E3 ligase component (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, and a PROTAC linker (S)-2-Amino-3,3-dimethylbutanoic acid. The coupled complex of the E3 ubiquitin ligase ligand + Linker is referred to as (S,R,S)-AHPC.

BET-IN-6, a ligand with potent and high affinity for inhibiting BRD2 BRD4, plays a crucial role in the synthesis of PROTAC BRD2 BRD4 degrader-1 [1], targeting the protein BRD2 4.

Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride (ZJT1) serves as a cereblon-based E3 ubiquitin ligase ligand, utilizing Pomalidomide (CRBN) for cereblon protein recruitment. This compound can be conjugated with a protein ligand through a linker to create a PROTAC [1].

PROTAC ER Degrader-14 (compound 86) is a PROTAC-type estrogen receptor ERR degrader. It comprises an E3 ubiquitin ligase ligand (blue part) (S)-Deoxy-thalidomide, a PROTAC linker (black part) N-Boc-piperazine, and a target protein ligand (red part) ER ligand-6. The combination of the E3 ligase and linker forms tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate.

HDAC4 CHDI Degrader 11 is a potent, selective degrader of HDAC4 (PROTAC) with DC_50 values of 4 nM and 6 nM in Jurkat E6-1 and Jurkat cells, respectively. This compound integrates the class IIa HDAC inhibitor trifluoromethyloxadiazole with a ligand for the Von Hippel-Lindau (VHL) protein through a linker. Demonstrating significant efficacy, HDAC4 CHDI Degrader 11 achieves a DC_50 value of 1 nM in a mouse cell model of Huntington's disease. For enhanced degradation in neuroblastoma cell lines, it can be administered alongside the P-glycoprotein inhibitor, Elacridar.

4-(6-Methyl-1,2,4,5-tetrazin-3-yl)phenol is an alkyl chain-derived PROTAC linker used in the synthesis of PROTACs[1].

OARV-771, a VHL-based BET degrader (PROTAC) featuring enhanced cell permeability, demonstrates DC50 values of 6 nM for Brd4, 1 nM for Brd2, and 4 nM for Brd3, respectively [1].