E3 Ligase Ligand-Linker Conjugate

A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to be degraded via the ubiquitin-proteasome system. The advent of nonpeptidic small-molecule E3 ligase ligands, notably for von Hippel-Lindau (VHL) and cereblon (CRBN), revolutionized the field and ushered in the design of drug-like PROTACs with potent and selective degradation activity. Enabled by the discoveries of high-quality, crystallographically defined ligands for the E3 ligases VHL and CRBN, PROTACs have had a meteoric resurgence in the limelight, a remarkable development that has culminated in the first PROTAC degraders being demonstrated as safe and efficacious in the clinic.

产品编号	产品名称
T18662	(S,R,S)-AHPC-C2-PEG4-N3	(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate combining the (S,R,S)-AHPC-based VHL ligand with a 4-unit polyethylene glycol (PEG) linker, employed in PROteolysis TAgeting Chimera (PROTAC) technology. This compound facilitates the creation of vRucaparib-TP4, a potent PARP1 degrader demonstrating a half-maximal degrading concentration (DC50) of 82 nM[1].
T18872	(S,R,S)-AHPC-PEG5-COOH	(S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) is a synthetic E3 ligase ligand-linker conjugate developed for use in PROTAC technology. It consists of the (S,R,S)-AHPC based VHL ligand and a 5-unit PEG linker [1].
T18824	Thalidomide-O-C6-NH2 TFA	Thalidomide-O-C6-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12F36V and BET[1].
T18817	Thalidomide-O-amido-C8-NH2 hydrochloride	Thalidomide-O-amido-C8-NH2 hydrochloride is a synthetic conjugate of an E3 ligase ligand-linker, which combines a cereblon ligand derived from Thalidomide and a linker. It can be utilized in the synthesis of PROTACs[1].
T18812	Thalidomide-PEG2-C2-NH2 TFA	Thalidomide-O-amido-PEG3-C2-NH2 TFA, a synthesized E3 ligase ligand-linker conjugate, combines the cereblon ligand based on Thalidomide and a 2-unit PEG linker for use in PROTAC technology[1].
T18671	(S,R,S)-AHPC-Me-C7 ester	(S,R,S)-AHPC-Me-C7 ester is an E3 ligase ligand-linker conjugate used to synthesize BCL-XL PROTAC degraders[1].
T18669	(S,R,S)-AHPC-Me-C10-NH2	(S,R,S)-AHPC-Me-C10-NH2 is a chemical compound consisting of a synthesized E3 ligase ligand-linker conjugate that incorporates both a VHL ligand and a linker. This compound, (S,R,S)-AHPC-Me-C10-NH2, finds application in PROTAC MS432[1].
T18666	(S,R,S)-AHPC-C4-NH2	(S,R,S)-AHPC-C4-NH2 is a custom-synthesized conjugate of an E3 ligase ligand-linker, which combines the VHL ligand based on (S,R,S)-AHPC and a linker specifically designed for EED-Targeted PROTAC[1].
T18820	Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride	Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride is a chemical compound that has been synthesized as an E3 ligase ligand-linker conjugate. This compound incorporates a cereblon ligand derived from Thalidomide and a 3-unit PEG linker. It is specifically designed for use in PROTAC technology, which utilizes small molecules to induce protein degradation [1].
T18664	(S,R,S)-AHPC-C3-NH2	(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized conjugate consisting of an E3 ligase ligand-linker and the VH032 based VHL ligand, which is commonly used in PROTAC technology. This compound serves as a key component in the synthesis of various PROTACs, including UNC6852. UNC6852 is a bivalent chemical degrader specifically targeting EED [1].
T18668	(S,R,S)-AHPC-Me-C10-Br	(S,R,S)-AHPC-Me-C10-Br is a chemically synthesized conjugate that functions as a ligand-linker for E3 ligases. This compound incorporates a VHL E3 ligase linker and MS432, derived from the MEK1/2 inhibitor PD0325901[1].
T18806	Thalidomide-NH-C10-COOH	Thalidomide-NH-C10-COOH (compound 6b) is a synthetic E3 ligase ligand-linker conjugate. This compound combines the Thalidomide-based von Hippel-Lindau (VHL) ligand with a linker commonly employed in PROTAC technology. [1]
T13671L	(S,R,S)-AHPC-Me dihydrochloride	(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.
T18826	Thalidomide-O-PEG2-propargyl	Thalidomide-O-PEG2-propargyl (E3 Ligase Ligand-Linker Conjugates 32) is a chemical compound that has been synthesized as a conjugate of an E3 ligase ligand and a linker. It incorporates the cereblon ligand based on Thalidomide, along with a 2-unit PEG linker. This compound is specifically designed for use in PROTAC technology, which utilizes ligand-induced protein degradation [1].
T5102	TGN-020	TGN-020 是一种属于 alkyl chain 类的 PROTAC linker，可用于 PROTAC 的合成分子。TGN020 是一种选择性水通道蛋白 4 (AQP4) 抑制剂，IC50为 3.1 μM。TGN020 减轻大鼠脊髓压迫损伤后的水肿并抑制神经胶质瘢痕的形成。
T7752	(S,R,S)-AHPC-Me	(S,R,S)-AHPC-Me是基于 (S,R,S)-AHPC 的的 VHL 配体，可用于募集 von Hippel-Lindau (VHL) 蛋白。它可有效降解去势抵抗性前列腺癌细胞中的 BET 蛋白，DC50<1 nM。它可用于合成 ARV-771。
T8412	(S,R,S)-AHPC	(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。
T40002	Pomalidomide-C3-NH2 hydrochloride	Pomalidomide-C3-NH2 hydrochloride 包含基于 Pomalidomide 的 cereblon 配体和 1 个 linker，是合成的 E3 连接酶配体-linker 偶联物，可用于 PROTAC 的合成。
T40001	Pomalidomide-C6-COOH	Pomalidomide-C6-COOH 是一种合成的 E3 连接酶配体-接头偶联物，它结合了 PROTAC 技术中使用的基于 Pomalidomide 的 CRBN 配体和接头。
T40008	Pomalidomide-C6-I TFA	Pomalidomide-C6-I TFA 是一种合成的 E3 连接酶配体-接头偶联物，它结合了 PROTAC 技术中使用的基于 Pomalidomide 的 CRBN 配体和接头。

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E3 Ligase Ligand-Linker Conjugate