EC Number   |
Inhibitors |
Structure |
|---|
   6.2.1.45 | (3E)-4-[(5R,8S)-5-methyl-6,9,13-trioxo-8-(propan-2-yl)-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-trien-11-yl]but-3-en-1-yl octanoate |
- |
   |
| 6.2.1.45 | (5R,8S)-11-ethenyl-5-methyl-8-(propan-2-yl)-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-triene-6,9,13-trione |
- |
|
| 6.2.1.45 | (5R,8S)-5-methyl-11-[(1E)-6-oxotridec-1-en-1-yl]-8-(propan-2-yl)-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-triene-6,9,13-trione |
- |
|
| 6.2.1.45 | (5R,8S)-5-methyl-8-(propan-2-yl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-triene-6,9,13-trione |
- |
|
| 6.2.1.45 | 1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furyl)methylene]-3,5-pyrazolidinedione |
i.e. PYZD-4409, small molecule inhibitor. PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells compared with normal hematopoietic cells |
|
| 6.2.1.45 | 1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furyl)methylene]-3,5-pyrazolidinedione |
i.e. PYZD-4409. In a mouse model of leukemia, intraperitoneal administration of PYZD-4409 decreases tumor weight and volume compared with control without untoward toxicity |
|
| 6.2.1.45 | 4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester |
i.e. Pyr-41. Inhibitor blocks loading of immobilized His6-tagged E1 with ubiquitin. PYR-41 does not affect the transfer of ubiquitin to E2 from E1 that is preloaded with ubiquitin, it directly inhibits E1, but not E2 enzymes. In addition to blocking ubiquitylation, PYR-41 increases total sumoylation in cells. PYR-41 attenuates cytokine-mediated nuclear factor-kappaB activation. This correlates with inhibition of nonproteasomal Lys63 ubiquitylation of TRAF6, which is essential to IkappaB kinase activation |
|
| 6.2.1.45 | 4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester |
i.e. PYR-41, potential of the inhibitor as therapeutic in cancer |
|
| 6.2.1.45 | 4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester |
i.e. PYR-41 |
|
| 6.2.1.45 | 5'-[[(L-cysteinylglycylglycyl)sulfamoyl]amino]-5'-deoxyadenosine |
inhibits Uba1-S-Ub thioester formation in a dose-dependent manner. The inhibitor is highly selective for its cognate E1 enzyme and does not inhibit the corresponding non-cognate E1s |
|
