For research use only. Not for therapeutic Use.
PROTAC EED degrader-2 is a von Hippel-Lindau-based 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].
| Catalog Number | I046011 |
| CAS Number | 2639882-69-0 |
| Synonyms | (2S,4R)-1-[(2S)-2-[5-[3-[5-[5-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methylamino]-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl]-6-methylpyridin-2-yl]propanoylamino]pentanoylamino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide |
| Molecular Formula | C50H58FN11O6S |
| Purity | ≥95% |
| InChI | InChI=1S/C50H58FN11O6S/c1-29-35(38-25-55-49(62-27-57-60-46(38)62)54-24-37-36-19-21-68-41(36)17-16-39(37)51)15-13-33(58-29)14-18-42(64)52-20-7-6-8-43(65)59-45(50(3,4)5)48(67)61-26-34(63)22-40(61)47(66)53-23-31-9-11-32(12-10-31)44-30(2)56-28-69-44/h9-13,15-17,25,27-28,34,40,45,63H,6-8,14,18-24,26H2,1-5H3,(H,52,64)(H,53,66)(H,54,55)(H,59,65)/t34-,40+,45-/m1/s1 |
| InChIKey | CQSOTYMFUWTIIR-HUSBZTEESA-N |
| SMILES | CC1=C(C=CC(=N1)CCC(=O)NCCCCC(=O)NC(C(=O)N2CC(CC2C(=O)NCC3=CC=C(C=C3)C4=C(N=CS4)C)O)C(C)(C)C)C5=CN=C(N6C5=NN=C6)NCC7=C(C=CC8=C7CCO8)F |
| Reference | [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. |
