e3 ligase ligand 14

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].

cIAP1 Ligand-Linker Conjugates 14 consist of an IAP ligand that targets the E3 ubiquitin ligase and a PROTAC linker. These conjugates, known as cIAP1 Ligand-Linker Conjugates 14, are used in the development of SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 2 Hydrochloride is a chemical compound that combines an IAP ligand, which targets the E3 ubiquitin ligase, with a PROTAC linker. It is utilized in the creation of SNIPERs[1].

Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a chemically synthesized compound, designed as an E3 ligase ligand-linker conjugate, integrating the cereblon ligand derived from Pomalidomide and a linker employed in PROTAC technology. This compound serves to facilitate targeted protein degradation through the modulation of E3 ligase activity, enabling the selective elimination of specific proteins of interest.

Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is an E3 ligase ligand-linker conjugate which is designed using Thalidomide-based cereblon ligand and a 3-unit PEG linker. This compound is synthesized specifically for utilization in PROTAC technology.

VH032-thiol-C6-NH2, also known as VHL Ligand-Linker Conjugates 14, is a synthesized compound that functions as an E3 ligase ligand-linker conjugate. This compound combines the VH032 based VHL ligand with a linker commonly utilized in PROTAC technology.

(S,R,S)-AHPC-CO-C-cyclohexane 作为一种 E3 泛素酶配体+连接子偶联物 (E3 Ligase Ligand-Linker Conjugates)，它用于制备 PROTAC SMARCA2 4-degrader-14。

E3 Ligase Ligand-linker Conjugate 137 作为PROTAC METTL3-14 degrader 1的连接子和E3连接酶配体，主要用于急性髓性白血病的研究。

PROTAC ER Degrader-14 (compound 86) 是一种 PROTAC 类型的 Estrogen Receptor ERR 降解剂，由以下部分组成：E3 泛素连接酶配体 (blue part)(S)-Deoxy-thalidomide、PROTAC Linker (black part) N-Boc-piperazine，以及靶蛋白配体 (red part) ER ligand-6。E3 连接酶加上 Linker 共同构成了 tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate。

SMD-3236是一种基于SMARCA配体和VHL-1配体设计的PRAOTAC降解剂，专门针对SMARCA2，展示了体内的长效抗肿瘤活性。SMARCA2是SMARCA4缺陷癌细胞中的合成致死靶点，SMD-3236对SMARCA2的降解选择性是SMARCA4的2000倍，DC50< 1 nM，Dmax>95%。SMD-3236可诱导肿瘤组织的SMARCA2缺失，同时保留SMARCA4蛋白，并在H838 smarca4缺陷人类癌症异种移植模型中抑制肿瘤生长。SMD-3236由靶蛋白配体(red part) SMI-1074、 PROTAC linker (black part) (trans-4-Ethynylcyclohexyl) methyl methanesulfonate 和E3连接酶配体(blue part)SMARCA2 ligand-14组成，其中E3连接酶配体和linker构成偶联物E3LigaseLigand-linker Conjugate 159。

CRBN ligand-14 是一种 CRBN 型 E3 泛素连接酶的配体，可用于 PROTAC 的制备。

PROTAC HDAC6 degrader4 (Compound 17c) 是一种选择性降解剂，专门作用于HDAC6，DC50为14 nM。它对HDAC1、HDAC2、HDAC3和HDAC6表现出抑制活性，其IC50分别为2.2、2.37、0.61和0.295 μM。(Pink: ligand for target protein HDAC6 ligand-3; Black: linker; Blue: ligand for cereblon E3 ligase)

Thalidomide-O-amido-PEG3-C2-NH2 TFA (Cereblon Ligand-Linker Conjugates 3 (TFA)) 包含基于 Thalidomide 的 cereblon 配体和 3 个单元的 PEG linker，是一种合成的 E3 连接酶配体-linker 偶联物。