2639882-72-5
2639882-72-5 structure
- Name: PROTAC EED degrader-1
- Chemical Name: PROTAC EED degrader-1
- CAS Number: 2639882-72-5
- Molecular Formula: C55H60FN11O8S
- Molecular Weight: 1054.20
- Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
- Create Date: 2021-09-11 08:38:34
- Modify Date: 2024-01-09 20:57:14
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PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit[1].
| Name | PROTAC EED degrader-1 |
|---|
| Description | PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit[1]. |
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| Related Catalog | |
| Target |
VHL |
| In Vitro | PROTAC EED degrader-1 (Compound PROTAC 2) binds to EED with a pKD of 9.02±0.09 and inhibits PRC2 function with a pIC50 of 8.17±0.24[1]. PROTAC EED degrader-1 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422[1]. PROTAC EED degrader-1 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells[1]. PROTAC EED degrader-1 (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, 100μM Incubation Time: 4, 8, 12, 14 days Result: Reduced proliferation. GI50=0.045 uM (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 | C55H60FN11O8S |
|---|---|
| Molecular Weight | 1054.20 |
| Storage condition | -20°C |