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Home > Inhibitors & Agonists > Proteasome/Ubiquitin

Proteasome/Ubiquitin

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Cat. No. Product Name Field of Application Chemical Structure
DC74311 HLQ2H Featured
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.
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DC8747 PD 151746 Featured
PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.
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DC8576 ML-240 Featured
ML-240 functions as a potent ATP-competitive inhibitor targeting the p97 ATPase, demonstrating inhibitory activity with an IC50 value of 110 nM.
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DC71617 Suc-Gly-Gly-Phe-pNA(chymotrypsin substrate) Featured
The synthetic peptide Suc-Gly-Gly-Phe-pNA serves as a specific substrate for the enzyme chymotrypsin, demonstrating a Michaelis constant (Km) of 1.6 mM. This value reflects the substrate concentration at which the enzyme achieves half of its maximum reaction rate, indicating its affinity for the peptide.
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DC9482 17-AAG Featured
17-AAG (17-N-Allylamino-17-demethoxygeldanamycin), also known by its NSC number 330507 and CP number 127374, is a well-studied inhibitor of Heat Shock Protein 90 (HSP90). HSP90 is a molecular chaperone that plays a critical role in the stabilization and activation of a wide range of client proteins, many of which are involved in oncogenic processes. By inhibiting HSP90, 17-AAG disrupts the function of these client proteins, leading to the degradation of oncogenic proteins and ultimately inhibiting cancer cell growth and survival.
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DC74313 PLIHZ Featured
PLIHZ is a small molecule inhibitor that targets DNAJA1, a member of the heat shock protein 40 (Hsp40) family. Derived from the natural compound plumbagin, PLIHZ specifically binds to the J domain of DNAJA1, which is crucial for its co-chaperone activity with Hsp70. By inhibiting DNAJA1, PLIHZ effectively reduces the levels of DNAJA1 and several conformational mutant p53 (mutp53) proteins, which are often stabilized in cancer cells and contribute to tumorigenesis.
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DC10304 RA190 Featured
RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
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DC70072 ML-241 hydrochloride Featured
ML241 Hcl is a potent, selective and reversible AAA ATPase p97 inhibitor (IC50=100 nM).
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DC44512 Conglobatin Featured
Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo.
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DC8840 CB-5083 Featured
CB-5083 is a novel first in class, potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models .
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DC74330 HA-9104 Featured
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.
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DC74301 NX-1607 Featured
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.
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DC11970 KU675 Featured
A novel, second-generation C-terminal Hsp90 inhibitor with Kd of 191 and 726 uM for Hsp90α and Hsp90β, respectively.
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DC74320 OSSL_325096 Featured
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).
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DC9431 TZ9 Featured
TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.
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DC8142 TAS-116 Featured
TAS-116 is a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models.
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DC7806 Geldanamycin (NSC122750)
Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.
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DC70103 MS.001 Featured
MS.001 is a small molecule that inhibits both the chaperone binding and ubiquitin ligase activity of C-terminus of Hsc70 interacting protein (CHIP) at low micromolar concentrations (IC50=3.3 uM).
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DC74331 UM130646
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.
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DC74329 ETC-6152
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.
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DC74328 WZ-1831
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).
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DC74327 TXS-8
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.
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DC74326 TCL-Ester
TCL-Ester is the cell-permeable derivative of TCL-1, a non-covalent ligand targeting the Pru domain of Rpn-13.
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DC74325 TCL-1
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.
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DC74324 KDT-11
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.
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DC74323 BT317
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.
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DC74322 VCP Activator 1
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).
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DC74321 UPCDC-30766
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.
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DC74319 NW1030
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.
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DC74318 NW1028
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.
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