Ubiquitin

BI-8626 is a specific inhibitor of the HUWE1 ubiquitin ligase with an IC50 of 0.9 μM.

MSC1094308 is a reversible and allosteric inhibitor of the type II AAA ATPase human ubiquitin-directed unfoldase (VCP)/p97 and the type I AAA ATPase VPS4B, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively.

FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor (Ki=4.2 ?M). FT827 binds to the USP7 catalytic domain (USP7CD; residues 208-560) with an apparent Kd value of 7.8 ?M.

MF-094 is a potent and selective USP30 inhibitor with an IC50 of 120 nM. MF-094 increases protein ubiquitination and accelerates mitophagy.

GNE-6776 is a selective USP7 inhibitor.

FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.

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.

Vialinin A is a terphenyl compound originally isolated from the fungi T. terrestris and T. vialis.

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

COH000 is a highly specific covalent allosteric SUMO E1 inhibitor with an IC50 of 0.2 μM for SUMOylation in vitro.

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.

PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay).

NMS-859 is a potent, covalent VCP (p97) inhibitor, with IC50s of 0.37 and 0.36 μM for wild-type VCP in the presence of 60 μM and 1 mM ATP in cells, respectively.

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

RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity.

XL177A is a potent USP7 inhibitor that irreversibly inhibits USP7 with sub-nM potency and selectivity across the human proteome.

TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective inhibitor of neuronal ubiquitin C-terminal hydrolase UCH-L3, with an IC50 of 0.6 μM. It reduces ubiquitination of the glycine transporter GlyT2 in primary neurons from the brainstem and spinal cord, making it a valuable tool for studying neuronal ubiquitin regulation and glycinergic neurotransmission.

DUB-IN-7 is a potent deubiquitinating enzyme (DUB) inhibitor. This compound selectively targets DUBs, facilitating the investigation of their role in various biological processes. DUB-IN-7 is particularly relevant for research into diseases associated with dysregulated JAK2 activity, including leukemia.