Activators & Inhibitors

Palbociclib-propargyl, a PROTAC ligand targeting the protein CDK6, connects to the CRBN ligand through a PEG linker to form PROTAC CP-10. CP-10 exhibits a potent DC50 value of 2.1 nM against CDK6[1].

PDP-Pfp is a reducible ADC linker primarily utilized for targeting agents aimed at the extracellular loop 1 (ECL1) of TM4SF1, a member of the transmembrane 4 L6 family, as supported by reference [1].

Phe-Lys(Fmoc)-PAB is a cathepsin cleavable ADC linker employed in the conjugation of antibody-drug conjugates (ADCs)[1].

(+)-Biotin-SLC is an alkyl chain-based PROTAC linker employed for the synthesis of PROTACs [1].

Pomalidomide-amido-C1-Br is a synthesized conjugate consisting of the Pomalidomide-based cereblon ligand and a linker, functioning as an E3 ligase ligand-linker. This compound serves as a tool for designing a B-Raf PROTAC degrader, specifically PROTAC B-Raf degrader 1, which exhibits anti-cancer activity[1].

PPC-NB is a glutathione cleavable linker used for the antibody-drug conjugate (ADC)[1].

PPC-NHS ester is a cleavable linker vital in ADC synthesis. PPC-NHS ester joins cytotoxic drugs to antibodies, enabling precise delivery to cells or proteins. The cleavable nature ensures controlled drug release, optimizing ADC effectiveness.

AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG molecules[1].

S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate, an ADC linker, is a glutathione cleavable compound used for the attachment of monoclonal antibodies (mAb) in antibody-drug conjugates (ADCs). It specifically refers to the Alkyl-Chain composition of the linker portion of these molecules [1].