MrTAC-8
MrTAC-8, methylarginine-targeting chimera (MrTAC), is a BRD4 degrader with DC50 values of 46 nM in HeLa cells. MrTAC-8 recruits PRMT1, PRMT3, PRMT4, PRMT5, and PRMT7 to target proteins, inducing arginine methylation that triggers lysosomal degradation. MrTAC-8 degrades proteins across diverse subcellular localizations and independent of native proteolytic routes. MrTAC-8 can be used for the research of cervical cancer, glioblastoma.
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- Formel: C54H65ClN10O6S
- Molecular Weight:1017.68
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
BRD4 |
In Vitro
MrTAC-8 (0.01 nM-10 μM; 24 h) potently induces lysosomal degradation of endogenous BRD4 via catalytically active PRMT5 recruitment, with DC50 values of 46 nM in HeLa cells, 67 nM in U87 cells, and 4.8 μM in HEK293 cells[1].
MrTAC-8 (1 μM; 2 h) blocks BRD4 degradation in HeLa cells when pre-treated with lysosomal inhibitors bafilomycin and Chloroquine (HY-17589A), restoring BRD4 levels to 110% of DMSO control[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HEK293, HeLa, U87 human cancer cells
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Concentration:0.01 nM; 0.1 nM; 1 nM; 10 nM; 100 nM; 1 μM; 10 μM
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Incubation Time:24 h
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Result:Reduced BRD4 levels to 39% of DMSO control in HEK293 cells at 1 μM.
Reduced BRD4 levels to 13% of DMSO control in HEK293 cells at 10 μM.
Demonstrated cell line-specific potency, with DC50 values of 46 nM in HeLa cells, 67 nM in U87 cells, and 4.8 μM in HEK293 cells.
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Cell Line:HeLa human cervical cancer cells
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Concentration:1 μM plus 500 nM bafilomycin and 10 μM Chloroquine
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Incubation Time:2 h
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Result:Blocked BRD4 degradation when pre-treated with lysosomal inhibitors bafilomycin and Chloroquine, restoring BRD4 levels to 110% of DMSO control.
Reduced BRD4 levels to 100% of DMSO control in cells expressing catalytically dead (E444Q) PRMT5 at 1 μM, compared to 15% reduction in cells expressing wild-type PRMT5.
Enriched BRD4 in SDMA-positive fractions after treatment, confirming proximity-induced arginine methylation.
Chemical Information
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Molecular Weight 1017.68
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Formel C54H65ClN10O6S
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SMILES
O=C(NCCC1CCN(CC(C(NCCOCCNC(C[C@@H]2N=C(C3=CC=C(Cl)C=C3)C4=C(SC(C)=C4C)N5C(C)=NN=C25)=O)=O)=C)CC1)C6=CC=C(C(NC[C@H](O)CN7CCC8=CC=CC=C8C7)=O)C=C6
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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.
Protokoll
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MrTAC-8 Related Classifications
HY-183061 Related Classifications
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