For research use only. Not for therapeutic Use.
UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC50 of 247 nM for EED[1].
UNC6852 mediates PRC2 degradation[1].?
UNC6852 displays no cellular toxicity at concentrations up to 30 μM for HeLa Cells[1].?
UNC6852 (10 μM; 1-72 hours) results in a decrease in the levels of both EED and EZH2[1].?
UNC6852 facilitates PRC2 degradation via VHL recruitment[1].?
UNC6852 selectively degrades EED and EZH2[1].?
UNC6852 reduces H3K27me3 levels and DLBCL cell proliferation[1].
| Catalog Number | I045987 |
| CAS Number | 2688842-08-0 |
| Synonyms | (2S,4R)-1-[(2S)-2-[4-[[4-[5-(furan-2-ylmethylamino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl]benzoyl]amino]butanoylamino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide |
| Molecular Formula | C43H48N10O6S |
| Purity | ≥95% |
| InChI | InChI=1S/C43H48N10O6S/c1-26-36(60-25-48-26)29-11-9-27(10-12-29)20-45-40(57)34-19-31(54)23-52(34)41(58)37(43(2,3)4)50-35(55)8-5-17-44-39(56)30-15-13-28(14-16-30)33-22-47-42(53-24-49-51-38(33)53)46-21-32-7-6-18-59-32/h6-7,9-16,18,22,24-25,31,34,37,54H,5,8,17,19-21,23H2,1-4H3,(H,44,56)(H,45,57)(H,46,47)(H,50,55)/t31-,34+,37-/m1/s1 |
| InChIKey | PPNNFXIBKLCMTI-WXEAQWFJSA-N |
| SMILES | CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)CCCNC(=O)C4=CC=C(C=C4)C5=CN=C(N6C5=NN=C6)NCC7=CC=CO7)O |
| Reference | [1]. Potjewyd F, et al. Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15. |
