e3 ligase

Vepdegestrant (ARV-471) is a selective and highly potent estrogen receptor (ER, ESR1) PROTAC degrader with strong degrading activity against the ER protein. By directly degrading the ER protein rather than merely antagonizing its activity, vepdegestrant effectively inhibits the ER signaling pathway and demonstrates significant antitumor activity in ER-positive (ER⁺) breast cancer, with a DC50 value of approximately 2 nM. It is particularly effective against tumors harboring ESR1 mutations.

LS-102 is a selective inhibitor of the E3 ligase synoviolin (Syvn1), an astragaloside IV derivative, which attenuates myocardial ischemia/reperfusion injury by inhibiting mitochondrial fission.LS-102 inhibits Syvn1 auto-ubiquitylation, which ameliorates amyloidazole-induced slowing of the heart rate, and is useful for studying cardiovascular diseases.

SMER3 is an inhibitor of the Skp1-Cullin-F-box (SCF)(Met30) ubiquitin ligase, a member of the SCF E3-ligase family, which regulates diverse cellular processes including transcription, cell-cycle control and immune response.

Avadomide (CC 122) is an orally available pleiotropic pathway modulator with potential antineoplastic activity.

Pomalidomide-amino-PEG3-NH2 hydrochloride is an E3 ligase ligand-linker conjugate containing a pomalidomide-based cereblon ligand and a linker, which can be used to synthesize PROTACs.

Thalidomide-5-NH2-CH2-COOH (compound 114) is a selective inhibitor of the protomyosin receptor kinase and a ligand for E3 ligase, offering potential for studying various diseases.

Golcadomide (CC-99282) is a orally active CRBN E3 ligase modulator that induces interactions between CRBN and its neo-substrate, recruiting the target disease-causing proteins and the E3 ubiquitin ligase.Golcadomide is used in the study of hematologic malignancies.

E3 ligase Ligand 23 is a cereblon binding agent that degrades Ikaros or Aiolos via the ubiquitin proteasome.

E3 ligase Ligand 8, a ligand for E3 ubiquitin ligase, can be connected to protein ligands through linkers to form PROTACs, which induce ubiquitination-mediated degradation of cancer-promoting proteins.

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].

E3 ligase Ligand 13 is an E3 ubiquitin ligase ligand that can be employed to create PROTACs, which are connected to the ligand for the protein through a linker. PROTACs serve as inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].

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].

E3 ligase Ligand 9 is a compound that acts as a ligand for E3 ubiquitin ligase and can be attached to a protein ligand via a linker to form PROTACs or SNIPERs, which degrade cancer-promoting proteins through ubiquitination-mediated mechanisms[1].

E3 Ligase Ligand-linker Conjugate 114, a conjugate of an E3 ubiquitinase ligand and linker, facilitates the synthesis of PTOTAC HSD17B13 degrader 1.

E3 Ligase Ligand-linker Conjugate 116, an E3 ubiquitinase ligand plus linker conjugate (E3 Ligase Ligand-Linker Conjugates), facilitates the synthesis of PROTAC SMARCA2/4-degrader-28.

E3 Ligase Ligand-linker Conjugate 118, an E3 ubiquitinase ligand plus linker conjugate (E3 Ligase Ligand-Linker Conjugates), serves as a precursor for synthesizing PROTAC SMARCA2/4-degrader-30.

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 136 is an E3 ubiquitin ligase ligand-linker conjugate (E3 Ligase Ligand-linker conjugate) used for the synthesis of c-Myc inhibitor7.

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.

E3 Ligase Ligand-linker Conjugate 139 is an E3 ubiquitin ligase ligand and linker for PROTACKB03-SLF, used in cancer research.

E3 Ligase Ligand-linker Conjugate 133 is a critical intermediate in the synthesis of the complete PROTAC molecule CPD-39, comprising a conjugate (conjugate of E3 ligase Ligand and linker) that connects the E3 ligase ligand with a linker.

E3 Ligase Ligand-linker Conjugate 131 serves as a crucial intermediate in the synthesis of the complete PROTAC molecule CPD-39; it represents a (conjugate of E3 ligase Ligand and linker). This compound is vital for bridging the components necessary for forming the active PROTAC structure.

E3 Ligase Ligand 41 (Compound SI-13) serves as a ligand for the E3 ubiquitin ligase DCAF16. It is designed to connect with SLF through a linker, enabling the formation of KB03-SLF.

E3 Ligase Ligand-linker Conjugate 126 is an E3 ligase ligand-linker conjugate designed for the synthesis of PROTACs, such as PROTAC BRM/BRG1 degrader-1.