e3 ligase ligand 14

E3 ligase Ligand 14 binds to E3 ubiquitin ligase and, when conjugated to a protein ligand via a linker, forms PROTACs that facilitate the ubiquitination-mediated degradation of cancer-promoting proteins[1].

VH032-thiol-C6-NH2, also known as VHL Ligand-Linker Conjugates 14, is a synthesized compound that functions as an E3 ligase ligand-linker conjugate. This compound combines the VH032 based VHL ligand with a linker commonly utilized in PROTAC technology.

PROTAC ER Degrader-14 (compound 86) is a PROTAC-type estrogen receptor ERR degrader. It comprises an E3 ubiquitin ligase ligand (blue part) (S)-Deoxy-thalidomide, a PROTAC linker (black part) N-Boc-piperazine, and a target protein ligand (red part) ER ligand-6. The combination of the E3 ligase and linker forms tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate.

SMD-3236 is a PRAOTAC degrader targeting SMARCA2, designed using SMARCA ligand and VHL-1 ligand, and exhibits prolonged anti-tumor activity in vivo. SMARCA2 acts as a synthetic lethal target in cancer cells lacking SMARCA4, with SMD-3236 showing 2000-fold selectivity for SMARCA2 over SMARCA4, having a DC50 of less than 1 nM and a Dmax of over 95%. In the human cancer xenograft models deficient in SMARCA4, notably the H838 model, SMD-3236 effectively induces loss of SMARCA2 in tumor tissue while sparing the SMARCA4 protein, thereby inhibiting tumor growth. The compound consists of a target protein ligand (red part) SMI-1074, a PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate, and an E3 ligase ligand (blue part) SMARCA2 ligand-14, forming the E3LigaseLigand-linker Conjugate 159.

Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a chemically synthesized E3 ligase ligand-linker conjugate, incorporating the cereblon ligand from Pomalidomide and a linker used in PROTAC technology. It facilitates targeted protein degradation by modulating E3 ligase activity, thereby enabling the selective elimination of specific proteins of interest.

Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is an E3 ligase ligand-linker conjugate developed using a Thalidomide-based cereblon ligand and a 3-unit PEG linker, synthesized specifically for use in PROTAC technology.

Thalidomide-O-amido-PEG3-C2-NH2 TFA (Cereblon Ligand-Linker Conjugates 3 (TFA)) is a synthesized E3 ligase ligand-linker conjugate incorporating a Thalidomide-based cereblon ligand and a 3-unit PEG linker, used in PROTAC technology.

PROTAC HDAC6 degrader4 (Compound 17c) is a PROTAC that targets and degrades HDAC6, with a DC50 of 14 nM. It exhibits inhibitory activity against HDAC1, HDAC2, HDAC3, and HDAC6, with IC50 values of 2.2, 2.37, 0.61, and 0.295 μM, respectively. [Pink: ligand for target protein HDAC6 ligand-3; Black: linker; Blue: ligand for cereblon E3 ligase]

cIAP1 Ligand-Linker Conjugates 2 Hydrochloride is a chemical compound that combines an IAP ligand, targeting the E3 ubiquitin ligase, with a PROTAC linker and is utilized in the creation of SNIPERs[1].

CRBN ligand-14 is a CRBN-type E3 ubiquitin ligase ligand, suitable for the synthesis of PROTAC.

cIAP1 Ligand-Linker Conjugates 14 consist of an IAP ligand that targets the E3 ubiquitin ligase and a PROTAC linker. These conjugates, known as cIAP1 Ligand-Linker Conjugates 14, are used in the development of SNIPERs[1].

(S,R,S)-AHPC-CO-C-cyclohexane serves as an E3 Ligase Ligand-Linker Conjugate. This chemical compound is utilized in the synthesis of PROTAC SMARCA2 4-degrader-14.

E3 Ligase Ligand-linker Conjugate 137 serves as both a linker and an E3 ligase ligand for PROTAC METTL3-14 degrader 1, employed in the study of acute myeloid leukemia.