Ubiquitination/ Proteasome

Clematichinenoside AR is a major active ingredient that could be extracted from the traditional Chinese herb Clematis chinensis and has potent pharmacological effects on various diseases, including atherosclerosis (AS).

Dazcapistat is a potent calpain inhibitor, with IC50s of <3 μM for calpain 1, calpain 2 and calpain 9, respectively (patent WO2018064119A1, compound 405).

UPCDC-30245 is an allosteric p97 inhibitor with an IC50 of approximately 27 nM. UPCDC-30245 inhibits the p97 mutant N660K similar to wild type (WT; IC50=300 nM) and shows 3-fold resistance for p97 mutant T688A. UPCDC-30245 can be used in the research of cancer.

Apostatin-1 (Apt-1) is a potent TRADD inhibitor.

Bortezomib-d8 (PS-341-d8) is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.

mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.

DC-LC3in-D5 acts as an autophagy inhibitor by attenuating LC3B lipidation.

MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.

S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 ?M. S130 suppresses autophagy flux.

BOLD-100 is a ruthenium-based anticancer agent.

IZCZ-3 is a potent c-MYC transcription inhibitor with antitumor activity.

Trimetazidine-d8 dihydrochloride is the deuterium labeled Trimetazidine dihydrochloride.

LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5??M and a Kd of 16??M. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.

eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM.

(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD).

Cabazitaxel-d6 (XRP6258-d6) is the deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.

5-Amino-8-hydroxyquinoline (5A8HQ), a potential anticancer candidate, has promising proteasome inhibitory activity.

Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor, with IC50s ranging from 0.1 μM to 1 μM. Thrombin inhibitor 5 can be used for research of venous thromboembolism.

20S Proteasome activator 1 is an effective activator of the 20S protease, with IC50 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like sites, chymotrypsin-like sites and caspase-like sites respectively. It can be translated in cellular systems to prevent accumulation of pathogenic A53T mutant alpha-synuclein. 20S Proteasome activator 1 can be used for research on neurodegenerative diseases.