PROTAC EED degrader-2
Modify Date: 2024-01-09 17:25:54
PROTAC EED degrader-2 structure
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Common Name | PROTAC EED degrader-2 | ||
|---|---|---|---|---|
| CAS Number | 2639882-69-0 | Molecular Weight | 960.13 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C50H58FN11O6S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of PROTAC EED degrader-2PROTAC 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]. |
| Name | PROTAC EED degrader-2 |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
VHL |
| In Vitro | 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]. Cell Proliferation Assay[1] Cell Line: Karpas422 cells Concentration: 0.01, 0.1, 1, 10, 100 μM Incubation Time: 4, 8, 12, 14 days Result: Reduced proliferation. GI50=0.057 μM (Day 14). Western Blot Analysis[1] Cell Line: Karpas422 cells Concentration: 0.1, 1, and 3 μM Incubation Time: 48 hours Result: The protein levels of EED, EZH2, H3K27me3 was reduced. Western Blot Analysis[1] Cell Line: Karpas422 cells Concentration: 1 μM Incubation Time: 1, 2, 4, 6, 8, 24 hours Result: EED protein levels decreased within 1-2 h of treatment. |
| References |
| Molecular Formula | C50H58FN11O6S |
|---|---|
| Molecular Weight | 960.13 |
| Storage condition | -20°C |