protac linker-8

PEG3-O-CH2COOH (PROTAC Linker 8) is a PEG-based linker utilized in the synthesis of SNIPERs.

Fmoc-8-amino-3,6-dioxaoctanoic acid (Fmoc-NH-PEG2-CH2COOH) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs) and a PEG-based PROTAC linker for the synthesis of PROTACs.

Boc-NH-PEG8-CH2CH2COOH is a PEG-based PROTAC linker utilized in PROTAC synthesis.

E3 ligase Ligand 8, a ligand for E3 ubiquitin ligase, can be connected to protein ligands through linkers to form PROTACs, which induce ubiquitination-mediated degradation of cancer-promoting proteins.

m-PEG8-O-alkyne is a PEG-based PROTAC linker utilized in the synthesis of PROTACs (proteolysis-targeting chimeras).

Azido-PEG8-NHS ester is an 8 unit PEG linker with cleavable properties, commonly employed in the synthesis of antibody-drug conjugates (ADCs)[1]. This compound also serves as a PEG- and Alkyl ether-based PROTAC linker, enabling its utilization in the synthesis of PROTACs[2].

Fmoc-NH-PEG8-NHS ester is a PEG-based PROTAC linker employed in PROTAC synthesis [1].

m-PEG8-Ms is a PROTAC linker belonging to the PEG class and can be used to synthesize PROTAC compounds.

Mal-amido-PEG8-NHS ester, a PEG-based PROTAC linker, is utilized in the synthesis of PROTACs.

Biotin-PEG8-acid is a PEG-based PROTAC linker labeled with biotin, utilized in PROTAC synthesis.

Boc-NH-PEG8-CH2CH2NH2 is a PEG-based PROTAC linker utilized in PROTAC synthesis.

cIAP1 Ligand-Linker Conjugates 8 comprises an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound is specifically utilized for the purpose of SNIPER design[1].

(S, R, S)-AHPC-PEG3-N3 (VHL Ligand-Linker Conjugates 8) is a synthesized E3 ligase ligand-linker conjugate. (S, R, S)-AHPC-PEG3-N3 incorporates the (S, R, S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.

PROTAC AR Degrader-8 (Compound NP18) functions as a PROTAC degrader targeting the androgen receptor (AR) and effectively degrades AR-FL in both 22Rv1 and LNCaP cells with DC50 values of 0.018 μM and 0.14 μM, respectively. It also degrades AR-V7 in 22Rv1 cells with a DC50 of 0.026 μM. Additionally, PROTAC AR Degrader-8 inhibits the proliferation of 22Rv1 and LNCaP cancer cells, exhibiting IC50 values of 0.038 μM and 1.11 μM. It induces cell cycle arrest at the G2 M phase and triggers apoptosis in 22Rv1 cells (apoptosis). Demonstrating anticancer efficacy, PROTAC AR Degrader-8 shows activity in both mouse and zebrafish models. [Pink: ligand for target protein AR ligand-33; Black: linker; Blue: ligand for E3 ligase Cereblon]

SMD-1087 is a selective PROTAC targeting SMARCA2 with a DC50 of 8 nM and a maximum degradation (Dmax) of 89%, while its DC50 for SMARCA4 exceeds 1 μM. The compound is composed of an E3 ligase ligand, (S,R,S)-AHPC-Me [blue part], a target protein ligand SMI-1074 [red part], and a PROTAC linker, (1r,4r)-tert-Butyl 4-(bromomethyl)cyclohexanecarboxylate [black part]. Notably, its target protein ligand plus linker section corresponds to the SMARCA2 Ligand-Linker Conjugate-1.

Pom-8PEG is an E3 ubiquitin ligase ligand-linker conjugate consisting of a cereblon (CRBN) ligand and an 8-unit PEG linker. This compound can be utilized for the synthesis of PROTAC, including the IDO1 PROTAC degrader.

Thalidomide-NH-PEG8-Ts is a chemically synthesized conjugate comprised of a Thalidomide-based cereblon ligand and an 8-unit PEG linker, functioning as an E3 ligase ligand-linker in PROTAC technology applications, such as the degradation of IDO1 by a PROTAC degrader.

Boc-8-aoc-oh can be used as a PROTAC linker in the synthesis of PROTACs. Boc-8-aoc-oh is an alkane chain with terminal carboxlic acid and Boc-protected amino groups. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond. The Boc group can be deprotected under mild acidic conditions to form the free amine.

N-Fmoc-8-aminooctanoic acid can be used as a PROTAC linker in the synthesis of PROTACs. N-Fmoc-8-aminooctanoic acid is an alkane chian with terminal Fmoc-protected amine and carboxylic acid groups. The Fmoc group can be deprotected under basic condition to obtain the free amine which can be used for further conjugations. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond.