e3 ligase ligand 8

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.

Pomalidomide-PEG4-C2-NH2 (E3 Ligase Ligand-Linker Conjugates 22) is a synthesized E3 ligase ligand-linker conjugate incorporating the Pomalidomide-based cereblon ligand and 4-unit PEG linker.

VHL Ligand 8, a VHL ligand essential for synthesizing ARD-266, acts as a highly potent VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. It efficiently facilitates the degradation of AR protein in AR-positive prostate cancer cell lines LNCaP, VCaP, and 22Rv1, exhibiting DC50 values ranging from 0.2-1 nM [1].

Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2) is a synthesized E3 ligase ligand-linker conjugate containing a Thalidomide-based cereblon ligand and a linker, useful in the synthesis of PROTACs, as per reference [1].

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.

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.

(S,R,S)-AHPC-C6-PEG3-C4-Cl is a small molecule HaloPROTAC incorporating the (S,R,S)-AHPC based VHL ligand and a 3-unit PEG linker, capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

8-Hydroxyoctanoic acid-thalidomide is a type of E3 ubiquitin ligase ligand-linker conjugate (E3 Ligase Ligand-Linker Conjugates). It is utilized in the synthesis of Lw13.

RR-11055 (Compound 8) is a ligand for the E3 ubiquitin ligase, exhibiting an affinity of 0.38 μM towards cereblon. It is utilized in the synthesis of the PROTAC degrader ERD-1233.

Pomalidomide-C2-Br is a conjugate of an E3 ligase ligand and a linker. It is used in the synthesis of PROTACAR Degrader-8.

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.

SMARCA2 4-ligand-Linker Conjugate-8 is an E3 ubiquitin ligase ligand-linker conjugate.