e3 ligase ligand 8

E3 ligase Ligand 8 是 E3 泛素连接酶配体。它能够利用 linker 与靶蛋白配体连接，形成 PROTAC 分子。PROTAC 可诱导促癌蛋白发生泛素化降解。

VHL Ligand 8 是一种 von Hippel-Lindau (VHL) 蛋白配体，可用于合成 ARD-266 。ARD-266 是一种基于 VHL E3 连接酶的高效雄激素受体 (AR) PROTAC 降解剂。ARD-266 在 AR 阳性 LNCaP，VCaP 和 22Rv1 前列腺癌细胞系中有效诱导 AR 蛋白降解，DC50值为 0.2-1 nM。

Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2) is a synthesized E3 ligase ligand-linker conjugate comprising a Thalidomide-based cereblon ligand and a linker. This compound is 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) 包含基于 (S,R,S)-AHPC 的 VHL 配体和 3 个单元 PEG linker，是一种合成的 E3 连接酶配体-linker 偶联物。

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

Pomalidomide-PEG4-C2-NH2 (E3 Ligase Ligand-Linker Conjugates 22) 是一种合成的 E3 连接酶配体- linker 偶联物，用于 PROTAC 技术中。

8-Hydroxyoctanoic acid-thalidomide 属于 E3 泛素酶配体+连接子偶联物(E3 Ligase Ligand-Linker Conjugates)类化合物。此化合物可被应用于合成 Lw13。

RR-11055 (Compound 8) 作为 E3 连接酶的配体，具有 0.38 μM 对 cereblon 的亲和力。该化合物还可用于合成 PROTAC 降解剂 ERD-1233。

Pomalidomide-C2-Br 是 E3 连接酶配体与连接子的偶联物，适用于合成 [PROTACAR Degrader-8]。

PROTAC AR Degrader-8 (Compound NP18) 是一种针对雄激素受体 (AR) 的 PROTAC 降解剂，可以在 22Rv1 细胞和 LNCaP 细胞中有效降解 AR-FL，DC50 分别为 0.018 μM 和 0.14 μM，并且在 22Rv1 细胞中降解 AR-V7，DC50 为 0.026 μM。此化合物能够抑制癌细胞 22Rv1 和 LNCaP 的增殖，IC50 分别为 0.038 μM 和 1.11 μM，并且在 G2 M 期阻滞细胞周期，诱导凋亡 (apoptosis) 在 22Rv1 细胞中。PROTAC AR Degrader-8 在小鼠和斑马鱼模型中展现了抗癌活性。(Pink: ligand for target protein AR ligand-33; Black: linker; Blue: ligand for E3 ligase Cereblon)

SMD-1087 是一种专门靶向 SMARCA2 的 PROTAC（DC50=8 nM，Dmax=89%），而其对 SMARCA4 的 DC50 超过 1 μM。SMD-1087 由 E3 连接酶配体 (S,R,S)-AHPC-Me（blue part）、靶蛋白配体 SMI-1074（red part）、以及 PROTAC linker (1r,4r)-tert-Butyl 4-(bromomethyl)cyclohexanecarboxylate（black part）构成。值得注意的是，其中的靶蛋白配体与 Linker 部分一起构成了 SMARCA2 Ligand-Linker Conjugate-1。

(S,R,S)-AHPC-Me-8-Sulfamoyloctanoic acid 是一种用于合成XZ338的E3泛素酶配体-连接子偶联物（E3 ligase ligand-linker conjugate）。

EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50= 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 μM. EN219 (1 μM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP human breast cancer cells in a proteomic profiling assay. It has been linked to the bromodomain and extra terminal domain (BET) inhibitor ligand (+)-JQ1 for use as a proteolysis-targeting chimera (PROTAC) to degrade bromodomain-containing protein 4 (BRD4) in 231MFP cells. 1.Luo, M., Spradlin, J.N., Boike, L., et al.Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product functionCell Chem. Biol.28(4)559-566(2021)

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 consisting of a Thalidomide-based cereblon ligand and an 8-unit PEG linker. This conjugate serves as an E3 ligase ligand-linker in PROTAC technology applications, including the degradation of IDO1 by a PROTAC degrader.

SMARCA2 4-ligand-Linker Conjugate-8 为 E3 泛素连接酶配体-连接子偶联物.