| 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. |
|
| 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). |
|
| 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. |
|
| 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. |
|
| DC74307 |
17-AAG hydrochloride |
A potent Hsp90 inhibitor with IC50 of 5 nM in cell-free assays. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| DC74311 |
HLQ2H |
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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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). |
|
| 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. |
|
| 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. |
|
| 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). |
|
| 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. |
|
| 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). |
|
| 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. |
|
| 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. |
|
| 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. |
|
| DC74326 |
TCL-Ester |
TCL-Ester is the cell-permeable derivative of TCL-1, a non-covalent ligand targeting the Pru domain of Rpn-13. |
|
| 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. |
|
| 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). |
|
| 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. |
|
| 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. |
|
| 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. |
|
| DC74332 |
YL5084 |
YL5084 (YL 5084) is a potent, selective and covalent JNK2/3 inhibitor with IC50 of 70 nM (JNK2), displays selectivity (>30-fold) for JNK2 over JNK1. |
|
