| 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. |
|
| DC74333 |
BAY-405
Featured
|
BAY-405 is a potent and selective MAP4K1 inhibitor with IC50 of 6 nM. BAY-405 potentiates in vitro and in vivo antitumor T-cell reactivity which overcomes the suppression by TGFβ and PGE2. |
|
| DC74334 |
F389-0746 |
F389-0746 is a potent, selective and orally active MAP4K4 inhibitor with IC50 of 120.7 nM. |
|
| DC74335 |
MMI-0100 |
MMI-0100 is a cell-permeant peptide inhibitor of MAPKAP kinase 2 (MK2), inhibits MK2 and downstream fibrosis and inflammation. |
|
| DC74336 |
Darizmetinib
Featured
|
Darizmetinib (HRX-0215, HRX0215) is a potent, selective inhibitor of MKK4 (MAP2K4/SEK1), shows potential for promoting liver regeneration or reducing or preventing hepatocyte death. |
|
| DC74337 |
DK2403 |
DK2403 (DK-2403) is a highly potent, selective and covalent MAP2K7 (MEK7) inhibitor with IC50 of 10 nM, covalently engages the unique Cys218 residue within the active site. |
|
| DC74338 |
DS03090629 |
DS03090629 is a potent, selective, ATP-competitive and orally available MEK1/2 inhibitor, shows high affinity for the MEK protein regardless of its phosphorylation status (npMEK (inactive) Kd=0.11 nM, and pMEK (active) Kd=0.15 nM). |
|
| DC74339 |
HRX-0233
Featured
|
HRX-0233 (HRX0233) is a potent, selective MAP2K4 (MKK4) inhibitor, HRX-0233 is synergistic with RAS inhibitors in KRAS-mutant cancers. |
|
| DC74340 |
KZ-001 |
KZ-001 is a highly potent and selective MEK 1/2 inhibitor with IC50 values of 7.4/64 nM, respectively, exhibits greater inhibition against BRAF- and KRAS-mutant tumor cells than AZD6244. |
|
| DC74341 |
NFX-179
Featured
|
NFX-179 (Nedometinib, NFX179) is a potent, specific, topical, metabolically labile MEK1/2 inhibitor with biochemical IC50 of 135 nM (MEK1). |
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|
| DC74342 |
IACS-52825 |
IACS-52825 is a potent, selective dual leucine zipper kinase (DLK, MAP3K12) inhibitor with binding Kd of 1.3 nM, and IC50 of 107 nM in p-c-Jun cell assays. |
|
| DC74343 |
IKAM-1 |
IKAM-1 (Compound 39-100) is an orally bioavailable, small-molecule IKKβ activation modulator (IKAM) that selectively targets MAP3K1, inhibits TNF-α-induced IKKβ-mediated NF-κB activation in A549 cells with IC50 of 4.7 uM. |
|
| DC74344 |
KC-130 |
KC-130 (KC130, ZAK inhibitor 8) is a potent, selective and covalent leucine-zipper and sterile-α motif kinase (ZAK) inhibitor with IC50 of 11.5 nM. |
|
| DC74345 |
TC13172 |
TC13172 (TC 13172) is a highly potent necroptosis inhibitor targeting the mixed lineage kinase domain-like protein (MLKL), inhibits necroptosis with IC50 of 2 nM in TSZ-induced necroptosis assays in HT-29 cells. |
|
| DC74346 |
DCZ19931 |
DCZ19931 is a novel multi-targeting kinase inhibitor, exhibits anti-angiogenic effects in vitro and inhibits ocular neovascularization in vivo. |
|
| DC74347 |
NC-p38i NC-37
Featured
|
Non-canonical p38α inhibitor NC-37 (NC-p38i NC-37) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM. |
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