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PRT4165 is a potent inhibitor of PRC1 (polycomb-repressive complex 1)-mediated histone H2A ubiquitylation in vivo and in vitro. PRT4165 inhibits the in vitro histone H2A E3 ubiquitin ligase activity of PRC1 components RING1, RNF2, and a BMI1/RNF2 complex. PRT4165 also inhibits DNA double-strand breaks induced ubiquitylation of histone H2AX.
| Molecular Weight | 235.24 |
| Formula | C15H9NO2 |
| CAS Number | 31083-55-3 |
| Form | Solid |
| Solubility (25°C) | DMSO: 20 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
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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