UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.
Molecular Weight: 832.97
Chemical Name: (2S,4R)-1-((S)-2-(4-(4-(5-((Furan-2-ylmethyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)benzamido)butanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO 100 mg/mL (120.05 mM) Ethanol 100 mg/mL (120.05 mM)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
UNC6852 mediates PRC2 degradation. UNC6852 has no cytotoxicity when the concentration of HeLa cells is up to 30 μM. UNC6852 (10 μM; 1-72 hours) lead to a decrease in the levels of both EED and EZH2. UNC6852 facilitates PRC2 degradation via VHL recruitment. UNC6852 selectively degrades EED and EZH2.H3K27me3 levels and DLBCL cell proliferation reduced by UNC6852 .
- 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.
Products are for research use only. Not for human use.
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