MRT-31619
MRT-31619 is a selective CRBN Molecular glue degrader, with an IC50 of 14 nM and an EC50 of 72 nM. MRT-31619 triggers ubiquitination and proteasomal degradation of CRBN. MRT-31619 serves as a chemical knockout tool for CRBN depletion to evaluate the dependence of other molecular glues on CRBN. MRT-31619 is applicable to the research of CRBN-related disease models.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C28H30N4O4
- 分子量:486.56
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
CRBN 14 nM (IC50) |
体外実験
MRT-31619 (1-10 μM; 1-24 h) potently and selectively degrades CRBN in Jurkat cells: this effect occurs after treatment at 1 μM for 1 h, 3 h and 24 h, as well as after treatment at 10 μM for 24 h, without affecting the level of DDB1[1].
Incubation of purified recombinant CRBN-DDB1 complex with MRT-31619 (10 μM; 60 min) induces the formation of CRBN-DDB1 dimeric complex[1].
MRT-31619 induces the formation of CRBN ternary complex, with an EC50 of 72 nM as determined by FIDA assay using purified recombinant CRBN-DDB1 complex[1].
MRT-31619 efficiently and selectively degrades CRBN via a self-targeting mechanism involving CRBN homodimerization, with a CRBN-binding IC50 of 14 nM and a complex-formation EC50 of 72 nM in Jurkat cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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分子量 486.56
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分子式 C28H30N4O4
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SMILES
O=C1CCC(C(N1)=O)N2CC3=C(C2=O)C=C(C=C3)N4CCC5(C4)CCN(CC5)C(C6=CC=CC=C6)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
溶剤 & 溶解度
体外:
DMSO : 1.25 mg/mL (2.57 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Gene Editing
Gene editing modify specific sites within the genome through gene deletions, insertions or conversions to study functionally unknown genes or conduct gene therapy. It is also used to change the biological traits of organisms to establish new varieties. Gene editing techniques include zinc finger nuclease (ZFN), transcription activator-like effector nuclease (TALEN), and clustered regularly interspaced short palindromic repeats (CRISPR)/CRISPR-associated protein 9 (Cas 9) (CRISPR/Cas9).
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
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データシート (273 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0552 mL | 10.2762 mL | 20.5524 mL | 51.3811 mL |