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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
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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DC74317 STA-1474
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).
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DC74316 SOMCL-16-175
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.
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DC74315 SL-145
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.
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DC74314 PLTFBH
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.
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DC74312 KUNG65
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.
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DC74310 Foldlin
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.
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DC74309 DCEM1
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.
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DC74308 BX-2819
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.
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DC74307 17-AAG hydrochloride
A potent Hsp90 inhibitor with IC50 of 5 nM in cell-free assays.
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DC74306 T0467
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.
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DC74305 Skp2-2
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.
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DC74303 MN714
MN714 is a cell-premeable prodrug of MN551 containing a pivaloyloxymethyl (POM) and covalent inhibitor of E3 ligase suppressor of cytokine signaling 2 (SOCS2).
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DC74302 MN551
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.
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DC74297 AAA237
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.
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DC74296 YCH2823
YCH2823 is a potent, selective USP7 inhibitor with IC50 of 49.6 nM, ITC Kd of 117 nM.
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DC74295 XL-9872-106C
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.
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DC74294 USP7-797
USP7-797 is a novel potent selective inhibitor of USP7 with IC50 of 0.44 nM.
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DC74293 TG2-179-1
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.
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