Target Protein Ligand-Linker Conjugate

K-Ras ligand-Linker Conjugate 6 is a compound that combines a K-Ras-recruiting fragment ligand and a PROTAC linker to recruit E3 ligase for the synthesis of PROTAC K-Ras Degrader-1.

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride, a resorcinol di-Ph ether scaffold-based programmed cell death-1 (PD-1)/programmed cell death ligand 1 (PD-L1) inhibitor, inhibits the PD-1/PD-L1 interaction with an IC50 of 39.2 nM. It contains the target protein PD-1/PD-L1 ligand and PROTAC linker, which can be used to synthesize PROTAC PD-1/PD-L1 degrader-1 and has anticancer activity. Additionally, it serves as a diluent for the preparation of tablets for direct compression.

K-Ras ligand-Linker Conjugate 4 is a chemical compound combining a K-Ras recruiting ligand with a PROTAC linker, responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. It has the potential to be used in synthesizing PROTAC K-Ras Degrader-1, which shows a degradation efficacy of ≥70% in SW1573 cells[1].

ER ligand-9 is a conjugate of an estrogen receptor (Estrogen Receptor/ERR) ligand and a linker, utilized in the synthesis of PROTACs ERD-1233.

FKBP12 Ligand-Linker Conjugate 1 is a complex comprising a target protein ligand for FKBP12 and a linker, which is utilized in the synthesis of the PROTAC degrader MC-25B.

DDR1ligand 1-piperidine is a conjugate of a target protein ligand and linker, utilized in the synthesis of 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 is a BRD4 degrader that functions through an SKP1 and proteasome-dependent degradation pathway. It is utilized in the synthesis of proteolysis-targeting chimeras (PROTAC).

JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222 incorporates a BRD4 ligand and a PROTAC linker, and is used in the synthesis of PROTAC BRD4 Degrader-29.

K-Ras ligand-Linker Conjugate 5 is a chemical compound combining a K-Ras recruiting ligand with a PROTAC linker for E3 ligases, such as VHL, CRBN, MDM2, and IAP. This conjugate is crucial for synthesizing PROTAC K-Ras Degrader-1, displaying a degradation efficacy of ≥70% in SW1573 cells [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) is a conjugate of proteins/peptides that can combine with therapeutic, diagnostic, or labeling agents.

SMARCA2 ligand-12-3-methylazetidin is a target protein ligand-linker conjugate that includes a ligand for SMARCA2 and a PROTAC linker, capable of recruiting E3 ligase. It is utilized in the synthesis of PROTAC SMARCA2 degrader-25.

FLT3 Ligand-Linker Conjugate 1 consists of an FLT3 ligand and a PROTAC linker that can recruit E3 ligase VHL. This conjugate is useful for synthesizing PROTAC RSS0680, a bifunctional compound designed for targeted protein degradation of kinases.

MC-Val-Cit-PAB-Sunitinib is a conjugate composed of the payload Sunitinib and a linker. It is utilized in the synthesis of HR97-Sunitinib.

KDM4Ligand-Linker Conjugate 1 is a conjugate comprising a KDM4 target protein ligand and a linker, used in the synthesis of PROTACKDM4 degrader-1.

RET Ligand-Linker Conjugate-1 consists of a complex formed by a RET ligand and a linker, which can be utilized in the synthesis of 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) is a potent BRM (SMARCA2) degrader with a DC50 of less than 0.1 μM. It functions as a linker for E3 ubiquitin ligase, making it useful in cancer research, and is a conjugate of a target protein ligand and linker.

Ahx-DM1 (compound 2A) is a conjugate of proteins/peptides that can be combined with therapeutic, diagnostic, or labeling agents.

CYP51-IN-7 (compound 1g) is an analogue of Fluconazole and serves as an effective antifungal agent. It exhibits inhibitory activity against Microsporum gypseum and Candida albicans, with MIC80 values of 62.5 ng/mL and 250 ng/mL, respectively.

MS1262-C3-amide-C10-amine is an E3 Ligase Ligand-Linker conjugate. It includes a GLP ligand targeting the E3 ligase SPOP and a PROTAC linker. This compound can be utilized in designing PROTACs such as example [MS479].