UNC6852

製品コードS9659 バッチS965901

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₄₃H₄₈N₁₀O₆S
	分子量	832.97	CAS No.	2688842-08-0
Solubility (25°C)*	体外	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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]

製品説明

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.

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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Hela cells
	濃度	0.1 μM, 0.5 μM, 1 μM, 3 μM, 5 μM, 10 μM, 20 μM, 30 μM
	反応時間	2 h, 4 h, 8 h, 10 h, 16 h, 20 h, 24 h, 48 h, 72 h
	実験の流れ	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.

参考

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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