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CC0651 selectively inhibits hCdc34. Structure determination revealed that CC0651 inserts into a cryptic binding pocket on hCdc34 distant from the catalytic site, causing subtle but wholesale displacement of E2 secondary structural elements. CC0651 analogs inhibited proliferation of human cancer cell lines and caused accumulation of the SCF(Skp2) substrate p27(Kip1). CC0651 does not affect hCdc34 interactions with E1 or E3 enzymes or the formation of the ubiquitin thioester but instead interferes with the discharge of ubiquitin to acceptor lysine residues.
| Molecular Weight | 442.29 |
| Formula | C20H21Cl2NO6 |
| CAS Number | 1319207-44-7 |
| Form | Solid |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related E1/E2/E3 Enzyme Products |
|---|
| NSC697923
NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A. |
| PYR-41
PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2. |
| Iberdomide
Iberdomide (CC-220) is an orally effective cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 for cereblon binding affinity of approximately 150 nM. Iberdomide (CC-220) binds CRBN with higher affinity than lenalidomide and pomalidomide and has enhanced degradation of IKZF1 and IKZF3 with enhanced degradation. |
| Ginkgolic Acid
Ginkgolic Acid is a inhibits SUMOylation by binding E1. |
| Heclin
Heclin is a hECT E3 ubiquitin ligase inhibitor. |
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