6 o 2 propyn 1 yl d galactose

6-O-2-Propyn-1-yl-D-galactose functions as an irreversible glycolinker, facilitating the attachment of cytotoxic drugs for applications in antibody-drug conjugation (ADC).

NH2-PEG6-Boc is a PEG-based PROTAC linker used in PROTAC synthesis[1] and a non-cleavable 6-unit PEG ADC linker for antibody-drug conjugates (ADCs) synthesis[2].

(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound used in the synthesis of ARV-771. ARV-771 is a BET PROTAC degrader that relies on von Hippel-Landau (VHL) E3 ligase and exhibits potent degradation of BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound acts as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, facilitating the recruitment of von Hippel-Lindau (VHL) protein.

Azido-PEG6-amine is a polyethylene glycol (PEG)-based linker compound commonly employed in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1]. Additionally, it serves as a non-cleavable 6-unit PEG linker in the synthesis of antibody-drug conjugates (ADCs)[2].

Azido-PEG6-NHS ester is a cleavable 6-unit polyethylene glycol (PEG) linker, commonly employed in the synthesis of antibody-drug conjugates (ADCs)[1], and serves as a PEG- and alkyl ether-based linker for the synthesis of proteolysis targeting chimeras (PROTACs)[2].

CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1 2 ~20 hours)[1][2].

YT 6-2 analog-1 (compound 2-3) serves as an autophagy-targeting ligand (ATL) aimed at p62 SQSTM1, useful in synthesizing the AUTOTAC degrader ATC-324 for the Androgen Receptor (AR). ATC-324 promotes the formation of AR p62 complexes, leading to the autophagic-lysosomal degradation of AR. It effectively reduces nuclear AR levels, downregulates the expression of AR and AR-v7 target genes, and can degrade common AR mutants found in prostate cancer (PCa).

E3 Ligase Ligand-linker Conjugate 147 is a conjugate of an E3 ligase ligand and a PROTAC linker, utilized in the synthesis of BRD9 Degrader-1 (Compound 13-7). Comprising the E3 ligase ligand BRD9 ligand-7 and the PROTAC linker 2-((1R,5S,6s)-3-Azabicyclo[3.1.0]hexan-6-yl)ethan-1-ol, this conjugate plays a critical role in biochemical applications.

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.

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].

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.

Abemaciclib metabolite M18 (LSN3106729) is a potent cyclin-dependent kinase (CDK) inhibitor with antitumor properties. It has been incorporated alongside a cereblon (CRBN) ligand to develop a proteolysis-targeting chimera (PROTAC) that selectively degrades CDK4 6 [1] [2].

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.