e3 ligase ligand 10

E3 ligase Ligand 10 serves as a ligand for E3 ubiquitin ligase and can be conjugated to a protein ligand through a linker, resulting in the formation of PROTACs. These PROTACs act as inducers of ubiquitination-mediated degradation, specifically targeting cancer-promoting proteins[1].

MS 39 is a potent Proteolysis Targeting Chimera (PROTAC) designed to degrade the Epidermal Growth Factor Receptor (EGFR). The molecule is composed of three structural motifs: an EGFR target ligand (red part), a VHL E3 ligase ligand (S,R,S)-AHPC (blue part), and an undecanedioic acid linker (black part). By facilitating the formation of a ternary complex between EGFR and the VHL E3 ubiquitin ligase, MS 39 triggers the polyubiquitination and subsequent proteasomal degradation of the receptor. MS 39 effectively reduces EGFR protein levels and inhibits downstream oncogenic signaling in HCC-827 and H3255 cell lines, leading to significant suppression of H3255 cancer cell proliferation.

(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate, comprising an (S,R,S)-AHPC-based VHL ligand and a linker, designed for BET-targeted PROTAC applications.

cIAP1 Ligand-Linker Conjugates 10 comprise of an IAP ligand and a PROTAC linker, which facilitates the design of SNIPERs. These conjugates incorporate an IAP ligand that interacts with the E3 ubiquitin ligase, and a PROTAC linker. SNIPERs can be developed using cIAP1 Ligand-Linker Conjugates 10.

Pomalidomide-PEG1-C2-N3, a conjugate of an E3 ligase ligand-linker, incorporates the cereblon ligand based on Pomalidomide and a 1-unit PEG linker, commonly used in PROTAC technology. This compound enables the design of the selective CDK6 PROTAC degrader CP-10, which effectively induces CDK6 degradation with a DC50 value of 2.1 nM[1].

(S,R,S)-AHPC-PEG2-C4-Cl is a small molecule HaloPROTAC, comprising the (S,R,S)-AHPC based VHL ligand and a 2-unit PEG linker, that induces the degradation of GFP-HaloTag7 in cell-based assays[1].

Thalidomide-O-amido-PEG2-C2-NH2 TFA (E3 Ligase Ligand-Linker Conjugates 24 TFA) is a synthesized E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and a 2-unit PEG linker, utilized in PROTAC technology.

(S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC comprising the (S,R,S)-AHPC based VHL ligand and a 6-unit PEG linker, capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

(S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-linker 10) is a synthesized E3 ligase ligand-linker conjugate, incorporating an (S,R,S)-AHPC-based VHL ligand and a linker[1].

(S,R,S)-AHPC-Me-C10-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating a VHL ligand and a linker.

E3 Ligase Ligand-linker Conjugate 112, a type of E3 ubiquitinase ligand-linker conjugate, serves as a precursor for the synthesis of SMARCA2 degrader-10.

E3 Ligase Ligand-linker Conjugate 134 is a crucial intermediary in synthesizing the complete PROTAC molecule STING-IN-10. It consists of a conjugate of an E3 Ligase Ligand and a linker, which facilitates the assembly of the target molecule.

Acepromazine-1-Piperazinepropanamine (compound 10) is an E3 ligase ligand-linker conjugate (E3 Ligase Ligand-Linker Conjugate) consisting of a cereblon ligand and a linker. This compound can target protein ligands to form the PROTAC molecule, TrimTAC1.

PROTAC BTK Degrader-10 (Example 1P) is a PROTAC compound that targets BTK for degradation. It is applicable in the research of chronic lymphocytic leukemia (CLL). [Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase Cereblon].

E3 Ligase Ligand 50 acts as a ligand for the E3 ligase Cereblon. It is utilized in synthesizing PROTAC BTK Degrader-10.

CRBN ligand-10 (compound 18) is a CRBN-based E3 ubiquitin ligase ligand suitable for the preparation of PROTAC.

2-Methoxyphenyl dihydrouracil-azaspiro[5.5]undecane-C-PIP is an E3 ligase ligand-linker conjugate designed for the synthesis of PROTACSOS1 degrader-10.

(S,R,S)-AHPC-Me-10-bromodecanoic acid is an E3 ligase ligand-linker conjugate composed of VHL ligand 2 and the linker 10-bromoheptanoic acid. This compound can be utilized in the synthesis of PROTACPI3Kδ degrader-1.

Thalidomide-C-amide-C5-amine serves as an E3 ligase ligand (E3 ligase Ligand) and can be utilized in the synthesis of PROTAC BET Degrader-10.

VHL Ligand 38 (Compound 1) is a competitive inhibitor of the E3 ubiquitin ligase VHL, demonstrating IC50 values of 4.1 μM and 7.0 μM in 1% and 10% DMSO solutions, respectively. It features a hydroxyproline residue and an isoxazole acetamide moiety, and effectively inhibits the binding of the fluorescence peptide derived from HIF1α (FAM-DEALA-Hyp-YIPD) to VHL.

Acepromazine-1-piperazinepropanamine dihydrochloride (compound 10) is an E3 ligase ligand-linker conjugate, incorporating a TRIM21 ligand and a linker. It can bind to target protein ligands, forming the PROTAC molecule known as TrimTAC1.