| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2639882-69-0 | [Synonyms]
| [Molecular Formula]
C50H58FN11O6S | [Molecular Weight]
960.13 |
| Chemical Properties | Back Directory | [density ]
1.40±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 100 mg/mL (104.15 mM; Need ultrasonic) | [form ]
Solid | [pka]
14.08±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
PROTAC EED degrader-2 is a PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit[1].
PROTAC EED degrader-2 (Compound PROTAC 1) binds to EED with a pKD of 9.27±0.05 and inhibits PRC2 function with a pIC50 of 8.11±0.09[1]. PROTAC EED degrader-2 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422[1]. PROTAC EED degrader-2 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells[1].PROTAC EED degrader-2 (1 μM ; 1-24 h) promotes degradation of EED, EZH2, and SUZ12 in Karpas422 cells[1]. | [References]
[1]. Hsu JH, et al. EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex. Cell Chem Biol. 2019 Nov 26. pii: S2451-9456(19)30362-9. |
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