| Cat. No. |
Product Name |
CAS No. |
Information |
| H9372 |
Subasumstat
|
1858276-04-6 |
Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities. |
| H7309 |
UBE2M-DCN1 inhibitor 52
|
2089293-14-9 |
UBE2M-DCN1 inhibitor 52 is a highly potent inhibitor of DCN1-UBE2M protein-protein interaction with IC50 of 60 nM, inhibits cullin neddylation in pulse-chase NEDD8 transfer assay with EC50 of 80 nM; binds to DCN1 and selectively reduce steady-state levels of neddylated CUL1 and CUL3 in a squamous cell carcinoma cell line, inhibits DCN1 but not DCN3 stimulated NEDD8 transfer from UBE2F to the cullins. |
| H7308 |
TZ9
|
1002789-86-7 |
A novel selective inhibitor of Rad6 ubiquitin conjugating enzyme; inhibits Rad6B-ubiquitin thioester formation and subsequent ubiquitin transfer to histone H2A, with no activity for UbcH5; potently inhibits proliferation, colony formation, and migration and induces MDA-MB-231 breast cancer cell G2-M arrest and apoptosis. |
| H7307 |
NSC697923
|
343351-67-7 |
NSC697923 (NSC 697923) is a small molecule that specifically inhibits the activity of the ubiquitin-conjugating (E2) enzyme Ubc13 (UBE2N)-Uev1A; NSC697923 impedes the formation of the Ubc13 and ubiquitin thioester conjugate and suppresses constitutive NF-κB activity in ABC-DLBCL cells, inhibits NF-κB activation induced by PMA, but not by TNFα; specifically inhibits Ubc13-mediated polyubiquitin chain synthesis in vitro, does not inhibits UbcH5c-mediated polyubiquitin chain formation; inhibits the proliferation and survival of ABC-DLBCL cells and GCB-DLBCL cells. |
| H7306 |
NAcM-OPT
|
2089293-61-6 |
NAcM-OPT is a specific, reversible small molecule inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 with IC50 of 79 nM in TR-FRET assays; also inhibits DCN2, but has no activity against DCN3, DCN4, or DCN5; inhibits NEDD8 ligation in vitro and in cells, and suppress anchorage-independent growth of a cell line with DCN1 amplification. |
| H7305 |
NAcM-COV
|
2089293-81-0 |
NAcM-COV is a specific, irreversible small molecule inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 with IC50 of 28 nM in TR-FRET assays; shows highly selectivity with respect to other protein acetyl-amide-binding sites; inhibits NEDD8 ligation in vitro and in cells, and suppress anchorage-independent growth of a cell line with DCN1 amplification. |
| H7304 |
GSK145A
|
1609945-27-8 |
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. |
| H7303 |
DI-591
|
2245887-38-9 |
DI-591 (DI591)?is a potent, selective, cell-permeable inhibitor of the DCN1-UBC12 interaction with Ki of 10-12 nM for human DCN1 and DCN2; displays no affinity against DCN3/4/5 (Ki>10 uM); selectively inhibits neddylation of cullin 3 but has no or minimal effect on neddylation of other cullin family members; accumulates NRF2 protein and its transcriptional activation in cells. |
| H7302 |
DI-404
|
2187412-79-7 |
DI-404 is a highly potent, peptidomimetic inhibitor of DCN1-UBC12 protein-protein interaction that bind to DCN1 protein with Kd of 6.9 nM, selectively inhibits the neddylation of cullin 3 over other cullin members; effectively enhances the thermal stability of cellular DCN1 protein at 0.3 uM in H2170 cells, decreases the association of cellular DCN1 protein with cellular UBC12 protein in a dose-dependent manner; effectively increases the level of NRF2 protein, a substrate of cullin 3 CRL (CRL3), but has no effect on CDT1, a substrate of cullin 4A CRL (CRL4A). |
| H7301 |
C25-140
|
1358099-18-9 |
C25-140 is a specific, first-in-class small molecule inhibitor of the TRAF6-Ubc13 interaction, binds TRAF6, inhibits TRAF6-Ubc13 interaction and TRAF6 activity; C25-140 effectively reduced TRAF6-mediated ubiquitin chain formation in vitro, impedes NF-κB activation in various immune and inflammatory signaling pathways also in primary human and murine cells; does not effect other E3 ligases (MDM2, TRIM63, ITCH, E6AP and RNF4), also does inhibit E1/E2 reactions. |
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