PROTAC SGK3 degrader-1

製品コードS9672 バッチS967201

化学情報

	Synonyms	SGK3-PROTAC1	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₅₇H₇₃FN₁₀O₁₁S₂
	分子量	1157.38	CAS No.	2381320-35-8
Solubility (25°C)*	体外	DMSO	100 mg/mL (86.4 mM)
		Ethanol	100 mg/mL (86.4 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	PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3 (Serum/Glucocorticoid Regulated Kinase Family Member 3) for degradation.
in vitro	SGK3-PROTAC1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 h, with maximal 80% degradation observed within 8 h, accompanied by a loss of phosphorylation of NDRG1, an SGK3 substrate. Low doses of SGK3-PROTAC1 (0.1−0.3 μM) restores sensitivity of SGK3 dependent ZR-75-1 and CAMA-1 breast cancer cells to Akt and PI3K inhibitors, whereas the cis epimer analogue incapable of binding to the VHL E3 ligase has no impact. SGK3-PROTAC1 suppresses proliferation of ZR-75-1 and CAMA-1 cancer cell lines treated with a PI3K inhibitor more effectively than could be achieved by a conventional SGK isoform inhibitor.^[1]

製品説明

PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3 (Serum/Glucocorticoid Regulated Kinase Family Member 3) for degradation.

in vitro

SGK3-PROTAC1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 h, with maximal 80% degradation observed within 8 h, accompanied by a loss of phosphorylation of NDRG1, an SGK3 substrate. Low doses of SGK3-PROTAC1 (0.1−0.3 μM) restores sensitivity of SGK3 dependent ZR-75-1 and CAMA-1 breast cancer cells to Akt and PI3K inhibitors, whereas the cis epimer analogue incapable of binding to the VHL E3 ligase has no impact. SGK3-PROTAC1 suppresses proliferation of ZR-75-1 and CAMA-1 cancer cell lines treated with a PI3K inhibitor more effectively than could be achieved by a conventional SGK isoform inhibitor.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	CAMA-1, HEK293 cells
	濃度	0.3 μM
	反応時間	8 h
	実験の流れ	Cells are treated with DMSO (control), SGK3-PROTAC1 (0.3 μM), or cisSGK3-PROTAC1 (0.3 μM) for 8 h and lysed. Lysates are subjected to immunoblot analysis with the indicated antibodies.

参考

[1] Hannah Tovell, et al. ACS Chem Biol. 2019 Sep 20;14(9):2024-2034.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The role of the SGK3/TOPK signaling pathway in the transition from acute kidney injury to chronic kidney disease [ Front Pharmacol, 2023, 14:1169054]	PubMed: 37361201
The role of the SGK3/TOPK signaling pathway in the transition from acute kidney injury to chronic kidney disease [ Front Pharmacol, 2023, 14:1169054]	PubMed: 37361201

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。