Homo-PROTAC cereblon degrader 1

製品コードS2881 バッチS288101

印刷

化学情報

Synonyms

OUN20985

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₃₂H₃₂N₆O₁₀

分子量

660.63

CAS No.

2244520-98-5

Solubility (25°C)*

体外

DMSO

100 mg/mL (151.37 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.500mg/ml (3.78mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.
in vitro	Homo-PROTAC cereblon degrader 1 (OUN20985), a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on pomalidomide neosubstrates IKZF1 and IKZF3, has no effects on proliferation of different cell lines, prevents pomalidomide-induced degradation of IKZF1 and IKZF3, and antagonizes the effects of pomalidomide on multiple myeloma cellslidomide resistance in different multiple myeloma cells.^[1]

製品説明

Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.

in vitro

Homo-PROTAC cereblon degrader 1 (OUN20985), a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on pomalidomide neosubstrates IKZF1 and IKZF3, has no effects on proliferation of different cell lines, prevents pomalidomide-induced degradation of IKZF1 and IKZF3, and antagonizes the effects of pomalidomide on multiple myeloma cellslidomide resistance in different multiple myeloma cells.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Multiple myeloma cell line NCI-H929, MM1S, HEK293T
	濃度	0.1 µM
	反応時間	3 h
	実験の流れ	HEK293T cells were transfected with a FLAG-CRBN-expressing plasmid. Forty-eight hours after transfection, cells were treated with DMSO or compound 15a for 3 h. Cells were then washed twice with ice-cold phosphate-buffered saline (PBS), lysed under denaturing conditions using 2% sodium dodecyl sulfate (SDS)-containing lysis buffer, and boiled for 10 min at 95 ℃. The SDS was diluted via the addition of 10×IP lysis buffer (Pierce) containing HALT Protease and Phosphatase Inhibitor Cocktail, MG132 (10 μM), and PR619 (50 nM) and incubated at 4 ℃ for 30 min. Immunoprecipitation was performed using anti-FLAG M2 Affinity Gel according to the manufacturer's protocol, and protein was eluted with FLAG peptide. CRBN was detected by a FLAG-specific antibody, and ubiquitinated CRBN by the FK2 antibody.

参考

https://pubmed.ncbi.nlm.nih.gov/30118587/

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：

LDC000067, a CDK9 inhibitor, unveils promising results in suppressing influenza virus infections in vitro and in vivo [ Antimicrob Agents Chemother, 2025, 69(1):e0117224]	PubMed: 39565117
Cereblon regulates NK cell cytotoxicity and migration via Rac1 activation [ Eur J Immunol, 2021, 10.1002/eji.202149269]	PubMed: 34392531

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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