KL4-219A
Based on 1 Customer Validation
KL4‑219A is a more durable MYC degrader derived from structural optimization of KL2‑236, with its inactive diastereomer being KL4‑219B. KL4‑219A induces destabilization and degradation of MYC protein in a proteasome-dependent manner. KL4‑219A is applicable to the research of pancreatic cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.85%
- Fòrmula: C20H22N2O3S
- Peso molecular:370.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
KL4-219A (50 μM; 0-24 h) induces potent, persistent proteasome-dependent MYC degradation in MYC-amplified PSN-1 pancreatic cancer cells, with sustained loss of MYC expression observed 24 h later[1].
KL4-219A-mediated MYC degradation in cancer cells is dependent on the proteasome; it exhibits whole-proteome selectivity for MYC degradation in cancer cells[1].
KL4-219A exhibits relatively selective cellular binding to MYC, which is evidenced by its ability to competitively inhibit the binding enrichment of KL2-236 to MYC in chemoproteomic analysis[1].
KL4-219A inhibits the transcriptional activity of MYC in HEK293T cells, and exhibits superior activity over its diastereomer KL4-219B[1].
KL4‑219A displayed an in vitro GSH half‑life of 19.3 minutes, which was shorter than that of the parent compound KL2‑236, and it exhibited sustained MYC degradation independent of warhead stability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:PSN1 cells
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Concentration:50 μM
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Incubation Time:0, 4, 8, 16, 24 h
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Result:Induced potent, persistent proteasome-dependent MYC degradation in MYC-amplified PSN-1 pancreatic cancer cells, with sustained loss of MYC expression observed 24 h later.
Chemical Information
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Appearance Solid
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Peso molecular 370.47
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Fòrmula C20H22N2O3S
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Color Off-white to light yellow
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SMILES
COC1=CC=C(C=C1)N2C([C@]3(C4=CC=CC=C42)CN3[S@](C(C)(C)C)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 23.33 mg/mL (62.97 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)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (291 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6993 mL | 13.4964 mL | 26.9927 mL | 67.4818 mL |
| 5 mM | 0.5399 mL | 2.6993 mL | 5.3985 mL | 13.4964 mL | |
| 10 mM | 0.2699 mL | 1.3496 mL | 2.6993 mL | 6.7482 mL | |
| 15 mM | 0.1800 mL | 0.8998 mL | 1.7995 mL | 4.4988 mL | |
| 20 mM | 0.1350 mL | 0.6748 mL | 1.3496 mL | 3.3741 mL | |
| 25 mM | 0.1080 mL | 0.5399 mL | 1.0797 mL | 2.6993 mL | |
| 30 mM | 0.0900 mL | 0.4499 mL | 0.8998 mL | 2.2494 mL | |
| 40 mM | 0.0675 mL | 0.3374 mL | 0.6748 mL | 1.6870 mL | |
| 50 mM | 0.0540 mL | 0.2699 mL | 0.5399 mL | 1.3496 mL | |
| 60 mM | 0.0450 mL | 0.2249 mL | 0.4499 mL | 1.1247 mL |
KL4-219A Related Classifications
HY-172825 Related Classifications
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