| Cat. No. |
Product Name |
CAS No. |
Information |
| H7300 |
UbcH5c-IN-6d
|
2123480-72-6 |
A potent, specific, orally bioactive small-molecule inhibitor of ubiquitin-conjugating enzyme UbcH5c with Kd of 283 nM; suppresses the activation of the NF-κB signaling pathway by selectively covalently binding to the Cys85 residue of UbcH5c; exhibits potent anti-inflammatory activity against complete Freund’s adjuvant-induced adjuvant arthritis in vivo. |
| H7299 |
TAK-243
|
1450833-55-2 |
TAK-243 (MLN-7243, AOB87172) is a small-molecule, cell-permeable inhibitor of ubiquitin-activating enzyme E1 (UAE1); blocks ssential monoubiquitination events within the translesion synthesis, and homologous recombination (HR) pathways; shows synergistic and additive anti-tumor combination benefits in vivo combined with carboplatin and docetaxel.
|
| H7298 |
PYZD-4409
|
423148-78-1 |
PYZD-4409 is a specific inhibitor of ubiquitin-activating enzyme (E1) with IC50 of 20 uM, inhibits the ATP-dependent activation of ubiquitin and subsequent transfer of the activated ubiquitin from the E1 to the common human E2 enzyme UBE2E2; blockes the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc3, induces cell death in hematologic malignant cell lines and primary patient samples preferentially over normal hematopoietic cells; decreases tumor weight and volume without untoward toxicity in vivo. |
| H7297 |
PYR-41
|
418805-02-4 |
PYR-41 is a selective, cell-permeable inhibitor of ubiquitin-activating enzyme (E1), blocks loading of immobilized His6-tagged E1 with ubiquitin with IC50 of
|
| H7296 |
NEDD8 inhibitor M22
|
864420-54-2 |
NEDD8 inhibitor M22 is a novel, potent, selective reversible NEDD8 activating enzyme (NAE) inhibitor; inhibit A549 cell proliferation completely at 30 uM (GI50=5.5 uM and GI90=19.3 uM); produces tumor inhibition in AGS xenografts in nude mice and low acute toxicity in zebrafish model; exhibts different binding mode compared with MLN4924. |
| H7295 |
ML 792
|
1644342-14-2 |
ML 792 is a potent, seletive SUMO-activating enzyme (SAE) inhibitor with IC50 of 3 nM and 11 nM for SAE/SUMO1 and SAE/SUMO2, respectively; shows no significant inhibition for closely related E1 enzymes NAE (IC50=32 uM) and ubiquitin-activating enzyme (UAE) (IC50 >100 uM), as well as a panel of 366 ATP-using enzymes; dose-dependently decreases global SUMOylation in HCT116 cells (EC50=19 nM), demonstrates potent antiproliferative effect in HCT116 cells and MDA-MB-231 cells with EC50 of 0.04 and 0.11 uM, respectively. |
| H7294 |
IJ-5
|
68776-47-6 |
A potent, covalent inhibitor of ubiquitin-conjugating enzyme UbcH5 with Kd of 5.189 uM, 3.578 uM, and 2.577 uM for UbcH5a, UbcH5b, and UbcH5c, respectively; shows weak affinity for Ubc13 (Kd=13.37 uM); inhibits TNFα-induced NF-kB pathway activation and inflammatory gene expression in 293T cells, exhibites potent anti-inflammatory activity against TNF-α- and D-galactosamine-induced hepatitis and collagen-induced arthritis in preclinical models. |
| H7293 |
COH000
|
1534358-79-6 |
COH000 (COH-000) is a highly selective, first-in-class, irreversible, allosteric, covalent inhibitor of SUMO-Activating Enzyme E1, inhibits SUMOylation in vitro with IC50 of 0.2 uM, displays >500-fold selectivity for SUMOylation over ubiquitylation; increased the degradation of SAE2, increases the expression of miR-34b and reduces c-Myc levels in lymphoma and colorectal cancer cell lines and a colorectal cancer xenograft mouse model. |
| H7292 |
ABP-A3
|
|
ABP-A3(ABP A3) is an inhibitor of ubiquitin conjugation that targets ubiquitin and Nedd8 E1 enzymes; inhibits conjugation of ubiquitin to intracellular proteins and prevents the formation of cytoprotective aggresomes; induces activation of the unfolded protein response (UPR) and apoptosis, displays IC50 of 2.5 uM in cell viability assays in A549 cells. |
| H7291 |
ABP 1
|
1482293-92-4 |
A nonselective inhibitor of UBL protein-activating E1 enzymes that forms covalent adducts with UBL proteins SUMO1, ubiquitin, Nedd8, ISG15, and GABARAP in the presence of ATP and E1 enzymes in vitro; covalently labels not only for canonical E1s (UBE1, SAE1/SAE2, NAE1/UBA3, UBE1L, and UBA6) but also for noncanonical E1s (UBA5 and ATG7).
|
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