mac glucuronide linker 1

MAC glucuronide linker-1 is a noncleavable ADC linker used in antibody-drug conjugations (ADCs).

MAC glucuronide phenol-linked SN-38, a pH-sensitive lactone and DNA topoisomerase I inhibitor drug linker, exhibits cytotoxicity in L540cy and Ramos cells, with IC50 values of 113 ng/mL and 67 ng/mL, respectively[1].

MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a cytotoxic drug linker that maintains a stabilized lactone form, demonstrating efficacy against L540cy and Ramos cells with IC50 values of 99 and 105 ng mL, respectively[1].

MAC glucuronide linker-2 is an ADC linker employed in the synthesis of ADCs, offering cleavability [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.

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].

CCK2R Ligand-Linker Conjugate 1 is a hydrophilic peptide linker that conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) as ligand-linker conjugates[1].

TSPO Ligand-Linker Conjugates 1, comprising a translocator protein (TSPO) ligand and a linker, is instrumental in synthesizing mitochondria-targeting autophagy-targeting chimera (AUTAC). This compound binds TSPO on the outer mitochondrial membrane (OMM), facilitating the degradation of malfunctioning mitochondria and proteins through mitophagy, thereby enhancing mitochondrial function. It holds potential applications in research related to mitochondrial dysfunction, encompassing neurodegenerative diseases, cancer, and diabetes [1].

cIAP1 Ligand-Linker Conjugates 1 is composed of an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 1, is particularly useful in the development of SNIPERs[1].

AhR Ligand-Linker Conjugates 1, also known as E3 Ligase Ligand-Linker Conjugates 57, is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a SNIPER linker. It is specifically designed to be used in the development of SNIPER[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].

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

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].