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.

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.

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].

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].

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.

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].

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.

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.

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].

BMS-1166-N-piperidine-CO-N-piperazine is a chemical compound containing a PD-1 PD-L1 immune checkpoint ligand and a PROTAC linker. It is used in synthesizing [PROTAC PD-1 PD-L1 degrader-1], which effectively inhibits the PD-1 PD-L1 interaction with an IC50 value of 39.2 nM.

K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in synthesizing PROTAC K-Ras Degrader-1, a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1].

K-Ras ligand-Linker Conjugate 3 (Compound 001371) is a chemical compound comprising a ligand for the K-Ras recruiting moiety and a PROTAC linker, responsible for recruiting E3 ligases (e.g., VHL, CRBN, MDM2, and IAP). This compound is essential for synthesizing PROTAC K-Ras Degrader-1, a potent degrader with a degradation efficacy of ≥70% in SW1573 cells[1].

ERRα Ligand-Linker Conjugates 1 refers to a chemical compound that consists of a ligand targeting estrogen-related receptor alpha (ERRα), and a PROTAC linker that facilitates the recruitment of E3 ligases MDM2. It finds utility in the synthesis of a range of PROTACs, including one known as PROTAC ERRalpha Degrader-1. With its capability to induce degradation of ERRα, PROTAC ERRalpha Degrader-1 functions as an ERRα degrader[1].

RNA recruiter-linker 1 is part of the RNA ligand-linker in RNAse L RIBOTAC, which is an RNA-degrading chimera designed to bind the four-stranded RNA helix SL5 within the 5' untranslated region of the SARS-CoV-2 RNA genome. This binding inhibits the replication of the virus in lung epithelial carcinoma cells. RNA recruiter-linker 1 is also useful in RIBOTAC synthesis.

FKBP12 Ligand-Linker Conjugate 2 is a conjugate composed of an FKBP12 target protein ligand and a linker. It is utilized in the synthesis of FKBP12PROTACFM4.