Target Protein Ligand-Linker Conjugate

K-Ras ligand-Linker Conjugate 6 是一种结合 K-Ras 招募片段配体和PROTAC连接子的化合物,可募集 E3 连接酶,合成 PROTAC K-Ras Degrader-1.

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride 是一种基于间苯二酚二Ph醚支架的程序性细胞死亡-1（PD-1）/程序性细胞死亡配体1（PD-L1）抑制剂, 抑制 PD-1/PD-L1 相互作用，IC50 值为 39.2 nM.BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride 包含靶蛋白 PD-1/PD-L1 配体和 PROTAC linker。BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride 可用于合成 PROTAC PD-1/PD-L1 degrader-1。BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride 具有抗癌活性。BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride 可作为稀释剂，用于用于直接压缩制备片剂。

K-Ras ligand-Linker Conjugate 4 is a chemical compound that combines a ligand for K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The compound has the potential to be used in the synthesis of PROTAC K-Ras Degrader-1, a powerful degrader of K-Ras that has been shown to exhibit a degradation efficacy of ≥70% in SW1573 cells[1].

ER ligand-9 是一种结合了雌激素受体 (Estrogen Receptor/ERR) 配体和 Linker 的化合物，可用于合成PROTACsERD-1233。

FKBP12 Ligand-Linker Conjugate 1 是一种由FKBP12的靶蛋白配体与连接子构成的复合物，用于合成PROTAC降解剂MC-25B。

DDR1ligand 1-piperidine 是一种靶蛋白配体与连接子的复合物，适用于合成PROTAC DDR1 degrader-1。

Desmorpholinyl Quizartinib-PEG2-COOH is a compound featuring an FLT-3 ligand and a PEG-based PROTAC linker. It is employed in the synthesis of PROTAC FLT-3 degrader 1, which serves as a degrader for the FLT-3 internal tandem duplication (ITD) through PROTAC technology. The degrader exhibits an IC50 of 0.6 nM.

EN884 是一个 BRD4 降解剂，通过依赖于 SKP1 和蛋白酶体的途径进行降解。EN884 适用于合成蛋白水解靶向嵌合体 (PROTAC)。

JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222 是一种包含BRD4的配体与PROTAC接头的化合物，可用于合成PROTACBRD4 Degrader-29。

K-Ras ligand-Linker Conjugate 5 is a chemical compound that combines a ligand for the K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The K-Ras ligand-Linker Conjugate 5 plays a crucial role in the synthesis of PROTAC K-Ras Degrader-1, a highly potent K-Ras degrader. In SW1573 cells, this degrader exhibits an impressive degradation efficacy of ≥70% [1].

FAK ligand-Linker Conjugate 1 is a chemical compound designed to facilitate PROTAC-mediated protein degradation. This compound consists of a ligand specifically targeting FAK and a PROTAC linker module, which acts as a recruitment agent for E3 ligases including VHL, CRBN, MDM2, and IAP[1].

MRTX849 ethoxypropanoic acid is a compound that contains a ligand for KRAS G12C and a PROTAC linker. It is commonly employed in the synthesis of PROTAC LC-2, which is a highly effective and innovative PROTAC. LC-2 has been proven to degrade endogenous KRAS G12C with remarkable potency, exhibiting DC50 values ranging from 0.25 to 0.76 μM.

Ahx-DM1 (TFA) (compound 2A) 是一种用于与治疗、诊断或标记剂结合的蛋白质/肽偶联物。

FLT3 Ligand-Linker Conjugate 1 包括FLT3配体和PROTAC linker，能够招募E3连接酶VHL。这种化合物用于合成PROTAC RSS0680。PROTAC RSS0680是一种双功能化合物，用于靶向蛋白激酶的降解。

MC-Val-Cit-PAB-Sunitinib 是由有效载荷Sunitinib与连接子组成的化合物。MC-Val-Cit-PAB-Sunitinib 适用于合成 HR97-Sunitinib。

KDM4Ligand-Linker Conjugate 1 是一种结合了KDM4靶蛋白配体和连接子的化合物，用于合成PROTAC KDM4 degrader-1。

RET Ligand-Linker Conjugate-1 是一种由RET配体和连接子构成的化合物，可用于合成QZ2135。

K-Ras ligand-Linker Conjugate 1 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, facilitating the recruitment of E3 ligases VHL, CRBN, MDM2, and IAP. It can be utilized in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells[1].

BRD4 Ligand-Linker Conjugate 1 is a compound consisting of a ligand and a linker, specifically designed to bind to the target protein BRD4. This conjugate serves as a valuable tool for synthesizing PROTACs, molecules utilized for targeted protein degradation.

PROTACSMARCA2 degrader-1 (compound ex7) 是一种BRM(SMARCA2) 降解剂，具有DC50小于0.1 μM的特性。它也是癌症研究中用于E3泛素连接酶的连接子，并作为靶蛋白配体-连接物缀合物。

Ahx-DM1 (compound 2A) 是一种与治疗、诊断或标记剂结合的蛋白质/肽偶联物。

MS1262-C3-amide-C10-amine 是一种 E3 Ligase Ligand-Linker Conjugates。它由一个靶向E3连接酶SPOP的GLP配体和一个PROTAC连接子组成。可用于设计PROTAC，例如MS479。

BMS-1166-N-piperidine-CO-N-piperazine is a chemical compound that contains a PD-1/PD-L1 immune checkpoint ligand and a PROTAC linker. It can be utilized in the synthesis of PROTAC PD-1/PD-L1 degrader-1, which effectively inhibits the PD-1/PD-L1 interaction, demonstrating an IC50 value of 39.2 nM.

(Rac)-PROTAC PARP/EGFR ligand 1 包含用来结合PARP和EGFR的配体，以及用于募集E3连接酶（诸如VHL、CRBN、MDM2和IAP）的PROTAC linker。(Rac)-PROTAC PARP/EGFR ligand 1 可用于合成PROTAC DP-C-4，DP-C-4 是一种基于CRBN的双PROTAC，可同时降解EGFR和PARP。