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TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM. IC50 value: 6 uM Target: Rad6 inhibitor The bulk of MDA-MB-231 cells treated with 10 μmol/L or more SMI #9 displayed a round morphology compared with controls and less than 5 μmol/L doses of SMI #9. Simultaneous comparison of SMIs #8 and 9 confirmed SMI #9 inhibits Matrigel-induced migration of MDA-MB-231 cells in a dose-dependent manner compared with SMI #8. 5 μmol/L SMI #9 treatment triggered morphologic changes consistent with apoptosis in a time-dependent manner. 5 μmol/L SMI #9 treatment of MDA-MB-231 cells for 24 hours increased the proportion of G2–M-arrested cells by 2-fold and was accompanied by a proportional decrease in S-phase cells. SMIs #8 or 9 treatments dramatically reduced β-catenin staining as visualized by reduced merged Rad6/β-catenin yellow fluorescence.
| Molecular Weight | 366.33 |
| CAS Number | 1002789-86-7 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| 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 |
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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. |
| CC0651
CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme and inhibited the ubiquitination of p27Kip1 with IC50 value of 1.72 μM. |
| 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. |
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