[CAS NO. 2688842-08-0] UNC6852
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PRODUCTS SPECIFICATIONS [2688842-08-0]
Store
Catalog
SLK-S9659
Brand
Selleck
CAS
2688842-08-0
DESCRIPTION [2688842-08-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 832.97 |
| Molecular Formula | C43H48N10O6S |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2005 mL | 6.0026 mL | 12.0052 mL |
| 5 mM | 0.2401 mL | 1.2005 mL | 2.4010 mL |
| 10 mM | 0.1201 mL | 0.6003 mL | 1.2005 mL |
| 50 mM | 0.0240 mL | 0.1201 mL | 0.2401 mL |
Description
UNC6852 is a selective degrader that targets with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.
Targets
| EED [1] (Cell-free assay) |
| 247 nM |
In vitro
UNC6852 contains an EED226-derived ligand and a ligand for VHL which bind to the WD40 aromatic cage of EED and CRL2VHL, respectively, to induce proteasomal degradation of PRC2 components, EED, EZH2, and SUZ12. Degradation of PRC2 with UNC6852 blocks the histone methyltransferase activity of EZH2, decreasing H3K27me3 levels in HeLa cells and diffuse large B cell lymphoma (DLBCL) cells containing EZH2 gain-of-function mutations. UNC6852 degrades both wild-type and mutant EZH2, and additionally displays anti-proliferative effects in this cancer model system.
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