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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C28H30N4O4
- Molecular Weight:486.56
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
CRBN 14 nM (IC50) |
In Vitro
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.
Chemical Information
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Molecular Weight 486.56
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Lösungsmittel & Löslichkeit
In Vitro:
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)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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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.
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
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 |