E3 ligase

TAME is a small molecule anaphase-promoting complex/cyclosome (APC) inhibitor with an IC50 of 12 μM.

Thalidomide can directly inhibit angiogenesis induced by bFGF or VEGF in vivo.

SMER3 is a selective inhibitor of a yeast SCF family E3 ubiquitin ligase (SCFMet30) in vitro and in vivo. Induces the expression of MET genes; blocks cell proliferation.

HLI-98C, an analog, indeed inhibited Mdm2 E3 ligase activity.

SKPin C1 inhibits Skp2-mediated p27 degradation and it induces cell cycle arrest.

HLI 373 is an inhibitor of Hdm2 ubiquitin ligase (E3) which blocks Hdm2-mediated ubiquitylation, proteasomal degradation of p53 and activates p53-dependent transcription.

Avadomide(CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4CRBN.

cIAP1 ligand 2 is the LCL161 derivative based IAP ligand. cIAP1 ligand 2 can be connected to the ABL ligand for protein by a linker to form SNIPER.

cIAP1 ligand 1 is the LCL161 derivative based IAP ligand. cIAP1 ligand 1 can be connected to the ABL ligand for protein by a linker to form SNIPER.

NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.

SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation.

WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.

Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor.

CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD). CC-92480 shows high affinity to cereblon, resulting in potent antimyeloma activity.

BIO-2007817 is a positive allosteric modulator (PAM) of Parkin, an E3 ubiquitin ligase. It enhances the activity of wild-type Parkin by stimulating its autoubiquitination and promotes the monoubiquitination of Miro1, with an EC50 of 0.17 μM. BIO-2007817 is a valuable tool for studying Parkin-mediated mitophagy and neurodegenerative diseases such as Parkinson's disease.

CRBN-6-5-5-VHL is a potent and selective VHL-based PROTAC degrader targeting cereblon (CRBN), with a DC₅₀ of 1.5 nM. It selectively degrades CRBN without affecting neo-substrates IKZF1 and IKZF3.

RNF5-IN-1 is a selective RNF5 degrader that targets the RNF5 E3 ubiquitin ligase, inhibiting its activity and facilitating its proteasomal degradation via endoplasmic reticulum-associated degradation (ERAD). It demonstrates significant biological activity by inhibiting α-1-antitrypsin dislocation with an IC50 value of 2.7 μM. This compound is valuable for research into conditions such as cystic fibrosis, acute myeloid leukemia, and various viral infections.