THAL-SNS-032

製品コードS8979 バッチS897901

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₄₀H₅₂N₈O₁₀S₂
	分子量	869.02	CAS No.	2139287-33-3
Solubility (25°C)*	体外	DMSO	100 mg/mL (115.07 mM)
		Ethanol	30 mg/mL (34.52 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	THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
in vitro	THAL-SNS-032 is a selective CDK9 degrader consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative which binds the E3 ubiquitin ligase Cereblon (CRBN). THAL-SNS-032 induces rapid degradation of CDK9 without affecting the levels of other SNS-032 targets. The transcriptional changes elicited by THAL-SNS-032 are more like those caused by NVP-2 than those induced by SNS-032. Strikingly, compound washout does not significantly reduce levels of THAL-SNS-032-induced apoptosis, suggesting that CDK9 degradation had prolonged cytotoxic effects compared to CDK9 inhibition.^[1]

製品説明

THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).

in vitro

THAL-SNS-032 is a selective CDK9 degrader consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative which binds the E3 ubiquitin ligase Cereblon (CRBN). THAL-SNS-032 induces rapid degradation of CDK9 without affecting the levels of other SNS-032 targets. The transcriptional changes elicited by THAL-SNS-032 are more like those caused by NVP-2 than those induced by SNS-032. Strikingly, compound washout does not significantly reduce levels of THAL-SNS-032-induced apoptosis, suggesting that CDK9 degradation had prolonged cytotoxic effects compared to CDK9 inhibition.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Wildtype MOLT4 cells, CRBN−/− MOLT4 cells
	濃度	250nM
	反応時間	6 h, 72 h
	実験の流れ	Proliferation assays are performed by treating MOLT4 and CRBN−/− MOLT4 cells with THAL-SNS-032 at concentrations indicated for 72 hours. Anti-proliferative effects of compounds are assessed using Cell Titer Glo assay kit. IC50s are determined using Graphpad Prism non-linear regression curve fit. To determine the effect of washout, MOLT4 and CRBN−/− MOLT4 cells are treated with 250nM THAL-SNS-032. After 6 hours, compound is washed from cells by washing cells with media three times where indicated. Cells are allowed to grow for another 66 hours (72-hour total) and assayed for anti-proliferation using Cell Titer Glo assay kit.

参考

[1] Calla M Olson, et al. Nat Chem Biol. 2018 Feb;14(2):163-170.

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：

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3]	PubMed: 38262581

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3]

PubMed: 38262581

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。