ligase

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 18 is a small molecule ligand that specifically binds to E3 ubiquitin ligase, and E3 ligase Ligand 18 can be chemically linked to a protein-targeting ligand through a molecular linker to construct proteolysis-targeting chimeras (PROTACs), which subsequently induce ubiquitination-mediated degradation of disease-related proteins such as oncogenic factors, thereby supporting the study of targeted protein degradation in cancer biology.

Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.

Lenalidomide-Br (Compound 41), a derivative of Lenalidomide, acts as a ligand for cereblon (CRBN) - an E3 ubiquitin ligase involved in protein recruitment. This compound can be conjugated to a protein ligand via a linker to create PROTACs, such as the PROTAC STAT3 degrader SD-36.

Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor.

Lenalidomide hemihydrate is a derivative of Thalidomide, an orally active immunomodulator that acts as a molecular gel. It is a ligand for the ubiquitin E3 ligase cereblon, which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase.

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.

Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).

Apcin is a potent and competitive inhibitor of anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. It acts by blockin

BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specifically disrupts the HECTD2/PIAS1 interaction(IC50 of 5 nM).

HaloPROTAC3 (HaloPROTAC-3) is a conjugate of ligands for E3 and 16-atom-length linker and a degrader of HaloTag fusion proteins.

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.

Mezigdomide (CC-92480) is a potent, novel, selective and active cereblon E3 ubiquitin ligase modulator (CELMoD) that acts as a molecular glue. Mezigdomide has anti-myeloma activity. [1]

VH032 commonly used as a precursor to a PROTAC that hijacks VHL as the E3 ubiquitin ligase component.VH032 is a VHL/HIF-1α interaction inhibitor with a KdPROTACs, which can recruit von Hippel-Lindau (VHL) proteins as a ligand of VHL.

Pomalidomide-peg1-co2H is a synthetic E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand and a 2-unit PEG linker.

L82 is a DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM) that is selective and non-competitive.L82 expresses anti-proliferative activity against breast cancer cells.

NRX-252262 is a potent enhancer of the interaction between β-Catenin and its cognate E3 ligase, SCFβ-TrCP, inducing mutant β-Catenin degradation (EC50: 3.8 nM).

dCeMM3 (2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide) is a glue degrader. dCeMM3 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, result in inducing ubiquitination and degradation of cyclin K.