MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.

Foldamer 33 is a small molecule HSP110 inhibitor, directly binds to the nucleotide-binding domain (NBD) of HSP110, blocks HSP110 chaperone function and colorectal cancer growth.Foldamer 33 significantly inhibit HSP110 anti-aggregating activity with IC50 of 87.8 uM.Foldamer 33 disrupts HSP110-STAT3 interaction with IC50 of 35.9 uM in competitive BLI assays.Foldamer 33 inhibits SW480 colorectal cancer cell proliferation, and (5 mg/kg) Foldamer 33 displays an anti-tumor effect (TGI of 40% and 60%) in mice bearing a colorectal cancer.

MF-094 (MF094) is a potent, highly selective inhibitor of ubiquitin specific protease 30 (USP30) with IC50 of 0.12 uM, demonstrates <30% inhibitory activity for a panel of 22 USPs assays at 10 uM.

Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83 μM.

p97-IN-1 is a potent p97 inhibitor with an IC50 <30 nM (WO2015109285A1, compound FF07).

Usp22i-S02(USP22-IN-1, compound S02) is a potent inhibitor of ubiquitin specific peptidase 22 (USP22). It showed anticancer activity by suppressing Foxp3 expression in T-regulatory cells.

M435-1279 is a UBE2T inhibitor. M435-1279 acts inhibit the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.

M3258 (M 3258) is a potent, reversible, highly selective and orally acitve LMP7 inhibitor with ceullar IC50 of 4.1 nM.M3258 does not inhibit other constitutive proteasome and immunoproteasome subunits (IC50>2.5 uM).M3258 demonstrated strong antitumor efficacy in multiple myeloma xenograft models.M3258 treatment led to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells both in vitro and in vivo.M3258 showed superior antitumor efficacy in selected multiple myeloma and mantle cell lymphoma xenograft models compared with the approved nonselective proteasome inhibitors bortezomib and ixazomib.

NPX-800 is a potent, selective, oral heat shock factor 1 (HSF1) pathway inhibitor.

NJH-2-075 is an alkyne-functionalized probe of EN523, retains binding to OTUB1 in vitro.

XL888 is an orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.

VR-23 is a Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E–Mediated Centrosome Amplification

Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.

PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 uM, with no or little activity at E2.

PRT4165 is a potent inhibitor of PRC1 (Polycomb-repressive complex 1)-mediated H2A ubiquitylation.

PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome.

PF-04929113 (SNX-5422) is a potent and selective Hsp90 inhibitor (Kd of 41 nM). PF-04929113 also inhibits Her-2 degradation (IC50 of 37 nM).

PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor (Ki values for ν and m-calpains are 0.21 and 0.37 μM respectively).

Oprozomib (ONX 0912) selectively inhibits CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.

MLN-9708 is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.

MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM.

ML364 is an USP2 inhibitor.xtracted from patent WO 2016134026 A1, compound example 10G.

ML346 is a novel activator of Hsp70 with EC50 of 4600 nM in HeLa cell toxicity assay.

ML323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay and 174 nM and 820 nM in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) and monoubiquitinated PCNA (Ub-PCNA) as substrates, respectively.

MG-132 is an inhibitor of proteasome with IC50 of 100 nM, and also inhibits calpain with IC50 of 1.2 μM.

LDN-57444 is a reversible, competitive proteasome inhibitor for Uch-L1 with IC50 of 0.88 μM, 28-fold selectivity over isoform Uch-L3.

KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.

HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.

Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.

Debio 0932 ( CUDC-305 ) is a novel heat shock protein 90 (HSP90) inhibitor trong affinity for HSP90 alpha/beta, high oral bioavailability and potent anti-proliferative activity against a broad range of cancer cell lines (with a mean IC50 of 220 nmol/L) .