| DC74330 |
HA-9104
|
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. |
| DC70862 |
UC-764865
|
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. |
| DC70861 |
UC-764864
|
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. |
| DC70605 |
ML307
|
ML307 is a potent, sub-micromolar (IC50=781 nM), first-in-class, small molecule inhibitor of Ubc13 enzyme activity, >128-fold selective against Caspase-3 and Bfl-1. |
| DC47678 |
M435-1279
|
M435-1279 is a UBE2T inhibitor. M435-1279 acts inhibit the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1. |
| 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. |
| 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. |
| DC70859 |
UbcH5c inhibitor DHPO
|
UbcH5c inhibitor DHPO is a small molecule UbcH5c inhibitor, directly targets UbcH5c with KD of 37.5 uM.DHPO effectively engaged by the UbcH5c protein in both Panc1 and SW1990 cells.DHPO exerts significant growth inhibition in pancreatic cancer cells in vitro (IC50=2.3-8.5 uM), prevents the migration and invasion of both Panc1 and SW1990 cells.DHPO inhibits pancreatic cancer cell growth and metastasis by inhibiting the NF-κB pathway.DHPO suppresses orthotopic pancreatic tumor growth in vivo, without causing significant host toxicity.DHPO prevents metastasis of pancreatic cancer in vivo. |
| DC70836 |
TG-6304
|
TG-6304 (TG6304) is a first-in-class, potent, highly selective, cell-permeable DCN3 inhibitor with Ki of 35 nM, does not bind to DCN1 at 30 uM.TC-6304 engages DCN3 in cells in a dose-dependent manner but does not affect the neddylation of any of the cullins.TC-6304 effectively enhances the thermal stability of cellular DCN3 protein in a dose-dependent manner and has no significant effect on the thermal stability of cellular DCN1 protein (10-1000 nM). |
| DC70448 |
GSK145A
|
GSK145A is a small molecule inhibitor of SUMO-conjugating enzyme E2 with IC50 of 12.5 uM, GSK145A is competitive with the sumoylation of the TRPS1 peptide substrates. |
