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Cat. No. Product Name CAS No. Information
PC-43439

MG-132

133407-82-6

MG-132 (Z-Leu-leu-leu-al, Zlllal) is a potent, reversible, and cell-permeable proteasome inhibitor with IC50 of 0.1 and 1.2 μM for the inhibition of proteasome and calpain, respectively; induces neurite outgrowth in PC12 cells with optimal concentrations of 20 nM, inhibits autolytic activation of calpain in rabbit erythrocytes at 100 uM; demonstrates in vivo antitumor activity.

PC-61352

O-phenanthroline

66-71-7

A selective inhibitor of 26S proteasome subunit Rpn11 with IC50 of 10±2 uM; shows no activity for other DUBs (USP1/USP2/USP4/USP5/USP7/USP8/USP20/UCH37, IC50>50 uM); blocks cellular proteasome function, induces apoptosis in MM cells and overcomes resistance to proteasome inhibitor bortezomib, activates caspase cascade and endoplasmic stress response signaling; reduces progression of tumor growth and prolongs survival in mice MM xenograft model.

PC-61193

CSN5i-3

CSN5i-3 (CSN5 inhibitor 3) is a potent, selective and orally available inhibitor of CSN5 with IC50 of 5.8 nM, the proteolytic subunit of COP9 signalosome (CSN); displays >1,000-fold selectivity over JAMM domain proteases (Rpn11 and AMSHLP) and other metalloproteinases; inhibits CSN-catalysed Cul1 deneddylation with IC50 of 5.8 nM, traps the cullin-RING E3 ubiquitin ligases (CRLs) in the neddylated state, and results in the inactivation of a subset of CRLs and the stabilization of their substrates; exhibits a differentiating effect on the viability of cancer cells, inhibits growth of a human xenograft in vivo.

PC-61132

Rpn11 inhibitor 35

2084868-04-0

Rpn11 inhibitor 35 is a potent, small molecule inhibitor of the proteasome subunit Rpn11 with IC50 of 400 nM,100-fold selectivity over Csn5 and 10-fold selectivity over AMSH; inhibits 293T and A549 cells proliferation with IC50 of 2.1 and 3.8 uM, respectively.

PC-60969

NC-001

1237540-68-9

NC-001 (NC 001, NC001, az-NC-001) is a potent, specific, cell-permeable inhibitor of immunoproteasome caspase-like sites (β1i and β1), does not correlate with inhibition of chymotrypsin-like sites.

PC-60962

KZR-504

1629052-78-3

KZR-504 (KZR504) is a potent, highly selective inhibitor of immunoproteasome low molecular polypeptide-2 (LMP-2) subunit with IC50 of 51 nM; displays >100-fold selectivity over β1, LMP7, β5, MECL1 and β2 subunits; shows little to no effect on cytokine production in human peripheral blood mononuclear cells (PBMCs) stimulated with LPS, and can be administered at a selective dose in vivo.

PC-35758

KZR-616

1629677-75-3 KZR-616 (KZR616) is a potent, selective dual immunoproteasome subunit LMP7/LMP2 inhibitor with IC50 of 39 nM/139 nM, weakly inhibits β5, MECL-1 and no acitivty against β1 subunit; shows no inhibition at 10 uM against a broad selectivity panel of 20 serine, metallo-, cysteine and aspartyl proteases and 11 hydrolases; demonstrates efficacy in the anti-collagen antibody induced arthritis (CAIA) models.

Other Indication

Phase 2 Clinical

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