lmp 7

LMP7-IN-2 is an inhibitor of LMP7 and may be utilized in the treatment of associated inflammatory diseases and disorders [1].

LMP7/LMP2-IN-1 (Compound 19) is an orally effective inhibitor targeting the immunoproteasome subunits LMP7 and LMP2, with respective IC50 values of 257 and 10 nM. This compound reduces the production of antibodies and downregulates the B cells in the germinal centers of the spleen and plasma cells in NP-OVA immunized mice. It has potential applications in the study of autoimmune diseases.

LMP7-IN-1 may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer, is an inhibitor of immunoproteasome (LMP7).

PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.

KZR-504 is a selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2) (IC50s: 51 nM, 4.274 μM for LMP2 and LMP7, respectively).

ML604440 is a cell permeable proteasome β1i (LMP2) subunit inhibitor.

Oprozomib (PR-047) (ONX 0912) , an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM)/LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has potential antineoplastic activity.

LMP744 is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.

LMP744 hydrochloride (NSC-706744 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity. 

IndiMitecan (LMP776) is an inhibitor of topoisomerase I (Top1) with anticancer activities [1].

Indotecan (LMP-400) is an effective inhibitor of topoisomerase 1(Top1) (IC50: 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively).