e3 ligase ligand 1

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) 是一种化学化合物，应用于合成ARV-771，一种极其强效的BET蛋白降解剂。该化合物在对去势抵抗的细胞中特异性地降解BET蛋白，其DC50值显著小于1 nM。作为VHL ligand 2 hydrochloride，(S,R,S)-AHPC-Me hydrochloride作为来源于(S,R,S)-AHPC的VHL配体，用于募集von Hippel-Lindau (VHL)蛋白。

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

E3 ligase Ligand 10 serves as a ligand for E3 ubiquitin ligase and can be conjugated to a protein ligand through a linker, resulting in the formation of PROTACs. These PROTACs act as inducers of ubiquitination-mediated degradation, specifically targeting cancer-promoting proteins[1].

E3 ligase Ligand 13 is an E3 ubiquitin ligase ligand that can be employed to create PROTACs, which are connected to the ligand for the protein through a linker. PROTACs serve as inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].

E3 ligase Ligand 14 is a ligand that binds to E3 ubiquitin ligase and can be conjugated to a protein ligand via a linker to create PROTACs. These PROTACs are capable of promoting ubiquitination-mediated degradation of cancer-promoting proteins[1].

E3 ligase Ligand 18 is a ligand that binds to E3 ubiquitin ligase, and it can be chemically attached to a protein ligand through a linker to create PROTACs. The resulting PROTACs function as inducers of ubiquitination-mediated degradation, targeting cancer-promoting proteins[1].

Cereblon modulator 1 是一种 GSPT1 选择性cereblon (CRBN)E3 连接酶调节剂，以分子胶的方式作用。它通过 CRL4CRBN选择性靶向 GSPT1 进行泛素化和蛋白酶体降解。

(S,R,S)-AHPC hydrochloride (Protein degrader 1 hydrochloride) 是基于 VH032 的 VHL 配体，可用于募集 von Hippel-Lindau (VHL) 蛋白。它能够利用 linker 与靶蛋白配体连接，得到 PROTAC 分子。

Thalidomide 4-fluoride (E3 ligase Ligand 4) 是一种基于 Thalidomide 的 Cereblon 配体，可用于募集 CRBN 蛋白。它能够利用 linker 与 IRAK4 靶蛋白配体连接，得到 PROTAC IRAK4 degrader-1。

(S,R,S)-AHPC (VH032-NH2) 是一种 VH032-based VHL ligand，可用于募集 von Hippel-Lindau (VHL)蛋白。它能够利用 linker 与靶蛋白配体连接，得到 PROTAC 分子。

AR antagonist 1 是 AR 拮抗剂，能够与 E3 连接酶配体结合，与 VHL 蛋白结合亲和力较弱，用于 PROTACARD-266 合成。

Thalidomide-O-amido-C3-NH2 TFA (Cereblon Ligand-Linker Conjugates 16 TFA) 包含基于 Thalidomide 的 cereblon 配体和 1 个 linker，是一种合成的 E3 连接酶配体-linker 偶联物，。

Thalidomide-NH-C2-PEG3-OH (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethyl]amino]-) 包含基于 Thalidomide 的 cereblon 配体和 1 个 linker，是 E3 连接酶配体-linker 偶联物，可用于合成 PROTAC BCL-XL 降解剂 XZ739。

MAK683-CH2CH2COOH 与 EED (胚胎外胚层发育蛋白) 结合。基于MAK683-CH2CH2COOH 和 E3 泛素连接酶的 VHL 配体，设计了靶向EED 的PROTACs， PROTAC EED degrader-1 和 PROTAC EED degrader-2 。

PROTAC IRAK4 degrader-1 (compound I-210) 是一种基于 Cereblon 的PROTAC，由 IRAK4 配体PROTAC IRAK4 ligand-1，E3 连接酶配体Pomalidomide和PROTAC linker AM-Imidazole-PA-Boc组成。

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。

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1 Sirt3 (IC50s > 100 μM)[1].

VH032-PEG3-acetylene is a synthesized conjugate compound consisting of a VH032-based VHL ligand and a linker, designed for use in PROTAC technology as an E3 ligase ligand-linker conjugate[1].

Pomalidomide-PEG4-C-COOH (E3 Ligase Ligand-Linker Conjugates 1) 包含基于 Pomalidomide 的 cereblon 配体和 4 个单元 PEG linker，是一种合成的 E3 连接酶配体-linker 偶联物。

7-Octynoic acid (compound 42) serves as a PROTAC linker for synthesizing various PROTACs, which are composed of two distinct ligands joined by this linker. One ligand interacts with an E3 ubiquitin ligase, while the other binds to the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs selectively degrade target proteins[1].

β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) serves as an AhR E3 ligase ligand, forming chimeric molecules when connected to a protein ligand through a linker, resulting in PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1). These chimeric molecules recruit the AhR E3 ligase complex by incorporating AhR ligands. By inducing ubiquitination-mediated degradation, PROTACs effectively target and degrade cancer-promoting proteins [1].

AhR Ligand-Linker Conjugates 1, also known as E3 Ligase Ligand-Linker Conjugates 57, is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a SNIPER linker. It is specifically designed to be used in the development of SNIPER[1].

Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PEG-based PROTAC linker employed in the synthesis of various PROTACs, including PROTAC SGK3 degrader-1. PROTACs are composed of two distinct ligands connected by a linker; one ligand binds to an E3 ubiquitin ligase, while the other specifically interacts with the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs can selectively degrade target proteins[1].

Boc-C1-PEG3-C4-OH is an Alkyl ether-based PROTAC linker utilized in the synthesis of PROTACs, which are characterized by their structure comprising two distinct ligands tethered by a linker. One ligand of PROTACs binds to an E3 ubiquitin ligase, while the other binds to the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs facilitate the targeted degradation of specific proteins[1].