vhl

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。

VHL Ligand-Linker Conjugates 15 is a chemical compound that combines a VHL ligand, which targets the E3 ubiquitin ligase, with a PROTAC linker. It is specifically designed for the creation of PROTACs[1].

VHL Ligand-Linker Conjugates 17 are chemical compounds that consist of a VHL ligand specialized for the E3 ubiquitin ligase, as well as a PROTAC linker. These conjugates are utilized in the synthesis of various PROTACs, including the notable ARD-266. ARD-266 is an exceptionally effective androgen receptor (AR) PROTAC degrader[1].

Homo-PROTAC pVHL30 degrader 1 是一种基于 PROTAC 的 pVHL30 降解剂。

Navitoclax-piperazine (ABT-263-piperazine) 是一种特大型 B 细胞淋巴瘤(BCL-XL)抑制剂。它和 E3 泛素连接酶的 VHL 配体可用来合成 PROTAC DT2216。

(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。

GNE-987 is a highly active chimeric BET degrader. GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50: 4.7 and 4.4 nM, respectively). GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03

PROTAC EED degrader-1, a PROTAC targeting EED (pKD = 9.02), is an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.17.

PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27) and an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.11.

ARD-266 是一种基于 von Hippe-Lindau E3 连接酶的 PROTAC 降解剂，可诱导 AR 蛋白的降解，可用于研究前列腺癌。

(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.

PROTAC ER Degrader-4 is a PROTAC degrader of the estrogen receptor (ER) with an IC50 of 0.8 nM.

PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.

(S,S,S)-AHPC hydrochloride 是 von Hippel-Lindau (VHL) 氨基砌块。(S,S,S)-AHPC (Compound 27) 常作为 (S,R,S)-AHPC 的阴性对照。(S,R,S)-AHPC 是基于 VH032 的 VHL 配体，可用于募集 VHL 蛋白。

ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide and it is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy[1].

(S, R, S)-AHPC-PEG4-NH2 hydrochloride is a chemically synthesized conjugate consisting of an E3 ligase ligand-linker, incorporating the VHL ligand based on (S, R, S)-AHPC, and a 4-unit PEG linker, which are specifically designed for use in PROTAC technology.

(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) 包含基于 (S,R,S)-AHPC 的VHL 配体和 1 个 linker，是一种合成的 E3 连接酶配体-linker 偶联物 (E3 ligase ligand-linker conjugate)。用于 BET 的靶向 PROTAC 的合成。

(S,R,S)-AHPC-PEG1-OTs is a chemically synthesized conjugate, functioning as an ligase ligand-linker for E3 ligase. It incorporates the VHL ligand derived from (S,R,S)-AHPC and a 1-unit PEG linker. This synthesized compound is commonly employed in PROTAC technology.

(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-PEG2-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

(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].

(S,R,S)-AHPC-(C3-PEG)2-C6-Cl is a small molecule HaloPROTAC incorporating the (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker, capable of inducing degradation of GFP-HaloTag7 in cell-based assays [1].

(S,R,S)-AHPC-PEG1-N3 (E3 ligase Ligand-Linker Conjugates 3) 是 E3 连接酶配体和linker 连接得到的 偶联物，包含基于 (S,R,S)-AHPC 的 VHL 配体和 1 个单元 PEG linker。

(S,R,S)-AHPC-PEG3-NH2 is a synthetic conjugate of an E3 ligase ligand-linker, incorporating the (S,R,S)-AHPC VHL ligand and a 3-unit PEG linker, which are utilized in PROTAC technology.