UC-764864 (UC764864) is a small-molecule inhibitor that targeted ubiquitin-conjugating enzyme UBE2N active site.UC-764864 blocks ubiquitination of innate immune- and inflammatory-related substrates in human AML cell lines.Inhibition of UBE2N function disrupted oncogenic immune signaling by promoting cell death of leukemic HSPCs while sparing normal HSPCs in vitro.

UC-764865 (UC764865) is a small-molecule inhibitor that targeted ubiquitin-conjugating enzyme UBE2N active site.UC-764865 blocks ubiquitination of innate immune- and inflammatory-related substrates in human AML cell lines.Inhibition of UBE2N function disrupted oncogenic immune signaling by promoting cell death of leukemic HSPCs while sparing normal HSPCs in vitro.

UCHL1 inhibitor 27 is a potent, selective, covalent UCHL1 inhibitor with IC50 of 90 nM.UCHL1 inhibitor 27 demonstrated exquisite selectivity in a cross-screening against 20 DUBs.UCHL1 inhibitor 27 demonstrated >50% fibroblast–myofibroblast transition (FMT) inhibition (IC50=100 nM) in idiopathic pulmonary fibrosis (IPF), as well as αSMA inhibition.UCHL1 inhibitor 27 is a powerful and selective probe to explore UCHL1 activity with potential application to substrate identification, mode of action studies, and cellular target profiling.

USP inhibitor 1 is an irreversible USP inhibitor with submicromolar IC50 of USP4 and its phylogenetic relative USP11, also functionally inhibits USP33, leading to CP110 instability and synergy with ATR inhibition in U2OS cells.

USP inhibitor 2 is a broad DUB inhibitor with IC50 of 0.04 and 0.21 uM for USP4 and USP11, also inhibits USP10/16/15/19 with submicromolar potency, forms a covalent adduct with USP11. USP inhibitor 2 does not inhibit USP5 (IC50>100 uM).

USP10 inhibitor Wu-5 (Wu-5) is a novel small molecule USP10 inhibitor inducing the degradation of FLT3-mutated protein, directly interacts and inactivates USP10, the deubiquitinase for FLT3-ITD in vitro (IC50=8.3 uM) and in FLT3-ITD-positive AML cells.Wu-5 selectively inhibited the viability of FLT3 inhibitor-sensitive (MV4-11, Molm13) and -resistant (MV4-11R) FLT3-ITD-positive AML cells with IC50 of 3.794, 5.056, and 8.386 uM, respectively.Wu-5 (1-10 μM) dose-dependently induced apoptosis of MV4-11, Molm13, and MV4-11R cells through the proteasome-mediated degradation of FLT3-ITD.Combined treatment of Wu-5 and crenolanib produced synergistic cell death in FLT3-ITD-positive cells via the reduction of both FLT3 and AMPKα proteins.

USP30 inhibitor Q14 peptide is a peptide derived from the transmembrane (TM) domain of USP30 that can target mitochondrial-anchored USP30 directly and increase mitophagy.

USP30Inh-1 is a potent, selective small molecule USP30 inhibitor with IC50 of 15-30 nM (inhibition of USP30-mediated cleavage of Ub-Rho110).USP30Inh-1 is anticipated to form a covalent linkage with the catalytic cysteine within the USP30 active site.USP30Inh-1 demonstrated good selectivity against >40 known DUB enzymes at 1 uM. USP30Inh-1 (1-10 uM) enhances mitoKeima signal in SHSY5Y cell, increases p-Ser65-Ub in dopaminergic neurones and astrocytes, as well as in Parkin heterozygote fibroblasts.

USP5 inhibitor 64 is a selective chemical probe (inhibitor) against USP5 deubiquitinase, binds to the USP5 ZnF-UBD (zinc-finger ubiquitin binding domain) with KD of 2.8 uM.USP5 inhibitor 64 is selective over nine proteins containing structurally similar ZnF-UBD domains.USP5 inhibitor 64 inhibits the USP5 catalytic cleavage of a di-ubiquitin substrate in an in vitro assay.

USP7-866 is a novel potent selective inhibitor of USP7 with IC50 of 0.18 nM; USP7-866 inhibited the growth of p53-mutant small cell lung cancer cell line H526 at a CC50 of 42 nM.

EC144 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with an IC50 of 1.1 nM. EC144 inhibits tumor growth and causes partial tumor regressions. EC144 has the potential for the research of cancer diseases.

FT709 is a potent and selective USP9X inhibitor, an IC50 of 82 nM. USP9X has been linked with centrosome function, chromosome alignment during mitosis, EGF receptor degradation, chemo-sensitization, and circadian rhythms.

MG-262 is a reversible proteasome inhibitor with diverse biological activities.

Macbecin is a stable HSP90 inhibitor by binding to the ATP-binding site with an IC50 of 2 μM and a Kd of 0.24 μM. Macbecin exhibits antitumor and cytocidal activities.

Suc-Gly-Gly-Phe-pNA is the chymotrypsin substrate with an Km value of 1.6 mM.

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

20S Proteasome activator 1 is a potent 20S proteasome activator with EC200 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases.

Ac-PAL-AMC is a fluorogenic substrate specific for 20S proteasome LMP2/β1i activity.

Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate.

NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.

Teslexivir (BTA074) hydrochloride is a potent antiviral agent. Teslexivir hydrochloride is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir hydrochloride can be used for condyloma research.

KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research.

8RK64 is a covalent UCHL1 inhibitor (IC50: 0.32 μM).

Brigimadlin is an E3 ubiquitin-protein ligase MDM-2 inhibitor. Brigimadlin serves as an antineoplastic agent.

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.

BAY-728 (NAY728) is a less potent enantiomer and negative control compound of BAY-805.

BK50118-C is a potent small molecule inhibitor of ubiquitin-specific protease-13 (USP13) with IC50 of 0.42 nM.

BML-260 (BML260) is a potent inhibitor of dual-specific phosphatase JSP-1 (JNK Stimulatory Phosphatase-1, DUSP22) and stimulator of uncoupling protein 1 (UCP-1) expression in adipocytes.

C598-0556 is a selective, small molecule inhibitor of USP10, inhibits USP10 comparably to HBX19818 (IC50=10 uM), with no inhibition against USP7 (IC50>100 uM).

C673-0105 is a selective, small molecule inhibitor of USP10, inhibits USP10 comparably to HBX19818 (IC50=10 uM), with no inhibition against USP7 (IC50>100 uM.

CAS-12290-201 is a potent and selective inhibitor of deubiquitinating enzyme (DUB) VCPIP1 with IC50 of 70 nM, covalently and specificly targets the catalytic cysteine of VCPIP1 with little to no activity toward other cellular DUBs.

DC-U4106 is a potent, selective small molecule inhibitor of Ubiquitin-specific protease 8 (USP8) with binding KD value of 4.7 uM, DC-U4106 is selective over USP2 and USP7.

FT206 (FT-206, FT3951206, CRT0511973) is a potent, selectivel inhibitor of USP28 with a remarkable USP28/25 selectivity.

FT385 (FT3967385) is a potent, selective USP30 inhibitor with biochemical IC50 of 1.5 nM.

GK13S is a highly potent, specific and covalent inhibitor of deubiquitinase UCHL1 with IC50 of 87 nM, displays exquisite specificity for UCHL1 over the other UCH family members (IC50>10 uM).

HY041004 is the first small molecule inhibitor of deubiquitinase Josephin Domain-containing protein 2 (JOSD2) with IC50 of 0.26 uM for JOSD2 catalytic activity inhibition.

I-138 (I 138) is a potent, specific small molecule USP1-UAF1 inhibitor with IC50 of 4.1 nM, binds to USP1-UAF1 at an allosteric pocket synergistically with ubiquitin.

IMP-2373 is a highly targeted cyanopyrrolidine (CNPy) probe for pan-DUB to monitor DUB activity in physiologically relevant live cells.

IU1-206 is a IU1 derivative with more potent activity against USP14, 10-fold more potent than IU1 and is comparable to the IU1-47.

IU2-6 is a small molecule USP14 inhibitor, shows 74% inhibition at 8 uM.

LN5P45 is a selective, covalent, irreversible inhibitor of ubiquitin thioesterase OTUB2 with IC50 of 2.3 uM, strongly induces monoubiquitination of OTUB2 on Lys31.

MS102 is a small molecule, orally available USP2 inhibitor with IC50 of 5.46 uM, induces transient degradation of ACE2 protein and inhibits ACE2-dependent coronavirus infection.

MTX115325 is a potent, selective, brain-penetrant USP30 inhibitor with IC50 of 12 nM in biochemical fluorescence polarization assays.

NCI677397 is a specific small molecule inhibitor of USP24, inhibits chemotherapy-induced drug resistance in vitro and in vivo.

OTUDin3 (OTUD3 inhibitor) is a specific, small molecule inhibitor of deubiquitylase OTUD3, binds to OTUD3 (KD=0.32 uM) and inhibits the deubiquitinating activity of OTUD3 by interfering with Ub binding to OTUD3.

SB1-F-70 is a potent, selective inhibitor of the deubiquitinase (DUB) JOSD1/USP30/UCHL1 with IC50 of 324/400/400 nM, respectively.

TG2-179-1 is a potent, selective and covalently inhibitor of deubiquitinase (DUB) BRCA1-associated protein-1 (BAP1), covalently binds to the active site of BAP1 (Cys91), exhibits potent cytotoxic activity against colon cancer cells.

USP7-797 is a novel potent selective inhibitor of USP7 with IC50 of 0.44 nM.

XL-9872-106C (XL-106C) is a potent, selective inhibitor of the deubiquitinase (DUB) JOSD1/USP30/UCHL1 with IC50 of 134/390/166 nM, respectively.

YCH2823 is a potent, selective USP7 inhibitor with IC50 of 49.6 nM, ITC Kd of 117 nM.

AAA-237 (AAA237) is a small molecule Skp2 E3 ligase inhibitor, binds to Skp2 protein (KD=28.77 uM) and inhibits the degradation of Skp2 substrates, inhibits the proliferation of the NSCLC cells.

BC18630 (BC 18630) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 39 nM in cell-based assays.

BC18630 free base (BC 18630) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 39 nM in cell-based assays.

BC18813 (BC 18813) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 48 nM in cell-based assays.

NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research.

MN551 is a Cys111-specific, covalent ligand targeting the E3 ligase SOCS2 with ITC Ki value of 2.2 uM, blocks recruitment of cellular SOCS2 protein to its native substrate.

MN714 is a cell-premeable prodrug of MN551 containing a pivaloyloxymethyl (POM) and covalent inhibitor of E3 ligase suppressor of cytokine signaling 2 (SOCS2).

Skp2-2 is a small molecule inhibitor of Skp2-Cks1 interaction with IC50 of 27.8 uM, significantly and dose-dependently reduces the protein expression of Skp2 in cancer cells.

T0467 is a small molecule activator of PINK1-Parkin signaling, activates Parkin mitochondrial translocation in dopaminergic neurons and myoblasts (20 uM, 3h), does not induce mitochondrial accumulation of PINK1.

A potent Hsp90 inhibitor with IC50 of 5 nM in cell-free assays.

BX-2819 is a potent, selective Hsp90 inhibitor with KD of 16.4 nM for human Hsp90α, also is a potent B. burgdorferi high-temperature protein G (Bb HtpG) with KD of 12 nM.

DCEM1 is a mitochondrial unfolded protein response (UPRmt) inhibitor, specifically disrupts HSP60-ClpP interaction in PCa cells and in vitro, suppresses prostate cancer growth in vivo.

Foldlin is a small-molecule tool compound that reduces the protein levels of misfolded/aggregated mutant p53, without effect on contact mutants or wild-type p53, Foldlin is small-molecule HSF-1 activator.

HLQ2H (Msi3 inhibitor 2H) is a first-in-class, specific inhibitor of fungal Hsp110 molecular chaperone Msi3, inhibits the holdase activity of Msi3 (IC50=5.02 uM) as well as the growth and viability of C. albicans.

KUNG65 is a potent, selective glucose regulated protein 94 (Grp94) inhibitor with Kd value of 540 nM in fluorescence polarization assays, 73-fold selectivity over Hsp90α.

PLIHZ is a small molecule inhibitor of DNAJA1 derived from the natural compound plumbagin, binds to J domain of DNAJA1 and efficiently reduces the levels of DNAJA1 and several conformational mutp53 with minimal impact on DNA contact mutp53 and wild-type p

PLTFBH is a cell-active small molecule inhibitor of DNAJA1, binds to and reduces protein levels of DNAJA1 and several other HSP40/J-domain proteins (JDPs), specifically reduces conformational mutp53 levels similar to PLIHZ.

SL-145 is a novel C-terminal HSP90 inhibitor, induces apoptosis in TNBC cells via the suppression of oncogenic AKT, MEK/ERK, and JAK2/STAT3 signaling.

SOMCL-16-175 is a non-covalent, allosteric modulator targeting Hsp90α’s middle domain (Hsp90M) with binding Kd of 804 uM, inhibits breast cancer cell growth and proliferation.

STA-1474 is a water soluble prodrug of Ganetespib (STA 9090), which is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).

NW1028 is a small molecule that target the regulatory domain of VCP/p97, inhibits the degradation of a p97-dependent reporter, does not affect the main catalytic domain of p97.

NW1030 is a small molecule that target the regulatory domain of VCP/p97, increases the degradation of a p97-dependent reporter, does not affect the main catalytic domain of p97.

OSSL_325096 is a novel potent small mlolecule p97/VCP inhibitor, suppresses cell proliferation and induces ER stress and apoptotic cell death in MM cell lines (IC50=0.1-0.5 uM).

UPCDC-30766 (UPCDC 30766) is a potent, allosteric inhibitor of AAA+ ATPase p97 (valosin-containing protein, VCP) with biochemical IC50 of 12 nM, EC50 of 226 nM in cellular UbG76V-GFP accumulation assays.

VCP Activator 1 (VA1) is a small molecule allosteric activator of valosin-containing protein (VCP)/p97, dose-dependently stimulates VCP ATPase activity up to 3-fold (EC50= 4 uM).

BT317 is a small molecule dual inhibitor of mitochondrial Lon Peptidase 1 (LonP1) and CT-L proteasome, subsequently induces ROS accumulation and autophagy-dependent cell death in high-grade IDH1 mutated astrocytoma lines.

KDT-11 is a specific, reversible peptidomimetic binder inhibitor of Rpn-13 with binding KD of 3 uM, selectively inhibit proliferation of a broad range of cancer cell lines (NCI60, IC50=5 uM), but not non-malignant cells.

TCL-1 is a non-covalent ligand targeting the Pru domain of Rpn-13, TCL-1 binds to the Pru domain at the Rpn-2 docking site, affects proteasome-mediated proteolysis.

TCL-Ester is the cell-permeable derivative of TCL-1, a non-covalent ligand targeting the Pru domain of Rpn-13.

TXS-8 is a specific, small molecule binder of Rpn-6 with KD of 14 uM, Rpn-6 is a subunit of the 19S regulatory particle (RP) of 26s proteasome.

WZ-1831 is a potent and highly selective inhibitor of human constitutive proteasome chymotryptic activity (β5c) with IC50 of 10 nM, >500-fold selectivity over β5i (IC50=7.1 uM).

ETC-6152 is a potent, specific and covalent E2 ubiquitin ligase UBE2T inhibitor with IC50 of 0.22 uM, targets Cys86 of UBE2T and shows selectivity on UBE2T over UBE2K.

HA-9104 is a specific small molecule inhibitor of E2 conjugating enzyme UBE2F with IC50 of 33.29 uM for inhibition of cullin-5 neddylation, abrogates UBE2F-NEDD8 thioester formation and inhibits cullin-5 neddylation.

UM130646 (UM 130646) is a specific small molecule E2 enzyme UBCH10 inhibitor with IC50 of 20.3 uM in TR-FRET UBCH10 autoubiquitination assays, inhibits UBCH10 E2 activity and antagonizes APC/C-mediated substrate degradation.