UNC6852

Catalog No.S9659 Batch:S965901

Technical Data

Formula	C₄₃H₄₈N₁₀O₆S
Molecular Weight	832.97	CAS No.	2688842-08-0
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (120.05 mM)
		Ethanol	100 mg/mL (120.05 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

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.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Hela cells Concentrations 0.1 μM, 0.5 μM, 1 μM, 3 μM, 5 μM, 10 μM, 20 μM, 30 μM Incubation Time 2 h, 4 h, 8 h, 10 h, 16 h, 20 h, 24 h, 48 h, 72 h Method Jess Protein Simple is used according to product guideline instructions. HeLa cells are treated with bivalent degraders UNC6852 at 5 μM for 4 hrs, 24 hrs, and 48 hrs, and cell lysates are generated using a modified RIPA buffer. Cell lysates are used at 1 mg/mL. The primary antibodies used are: anti-EED, anti-EZH2. The secondary antibodies used are: anti-sheep HRP secondary antibody, anti-rabbit secondary IR antibody.

Cell Assay:^{^[1]}

Cell lines
Hela cells
Concentrations
0.1 μM, 0.5 μM, 1 μM, 3 μM, 5 μM, 10 μM, 20 μM, 30 μM
Incubation Time
2 h, 4 h, 8 h, 10 h, 16 h, 20 h, 24 h, 48 h, 72 h
Method
Jess Protein Simple is used according to product guideline instructions. HeLa cells are treated with bivalent degraders UNC6852 at 5 μM for 4 hrs, 24 hrs, and 48 hrs, and cell lysates are generated using a modified RIPA buffer. Cell lysates are used at 1 mg/mL. The primary antibodies used are: anti-EED, anti-EZH2. The secondary antibodies used are: anti-sheep HRP secondary antibody, anti-rabbit secondary IR antibody.

References

[1] Frances Potjewyd, et al. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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