Activators & Inhibitors

Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a chemically synthesized compound, designed as an E3 ligase ligand-linker conjugate, integrating the cereblon ligand derived from Pomalidomide and a linker employed in PROTAC technology. This compound serves to facilitate targeted protein degradation through the modulation of E3 ligase activity, enabling the selective elimination of specific proteins of interest.

Thalidomide-O-amido-C3-COOH is a synthesized conjugate of an E3 ligase ligand-linker compound that combines a cereblon ligand derived from Thalidomide with a linker commonly employed in PROTAC technology.

Fmoc-Phe-Lys(Trt)-PAB-PNP is a cleavable linker for antibody-drug conjugate (ADC) synthesis, specifically designed for use in ADC synthesis.

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].

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].

K-Ras ligand-Linker Conjugate 6 is a chemical compound that combines a ligand for K-Ras recruiting moiety and a PROTAC linker. This compound can recruit E3 ligases, including VHL, CRBN, MDM2, and IAP. K-Ras ligand-Linker Conjugate 6 is particularly useful in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells[1].

Lenalidomide-acetylene-C5-COOH (compound 43; Cereblon ligand-linker Conjugate) serves as a Lenalidomide-based Cereblon ligand that facilitates the recruitment of the CRBN protein. This compound can be connected to the protein's ligand through a linker, resulting in the formation of PROTAC[1].

MAC glucuronide linker-1 is a nonclaevable ADC linker for antibody-drug-conjugations (ADCs).

Mal-C2-NHS ester is a noncleavable linker compound commonly employed for the synthesis of antibody-drug conjugates (ADCs)[1].