2. PROTAC Epigenetics
  3. LYTACs Epigenetic Reader Domain
  4. 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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MrTAC-8

MrTAC-8 Chemical Structure

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MrTAC-8 Related Antibodies

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Description

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[1].

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.

MrTAC-8 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293, HeLa, U87 human cancer cells
Concentration: 0.01 nM; 0.1 nM; 1 nM; 10 nM; 100 nM; 1 μM; 10 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: HeLa human cervical cancer cells
Concentration: 1 μM plus 500 nM bafilomycin and 10 μM Chloroquine
Incubation Time: 2 h
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.
Molecular Weight

1017.68

Formula

C54H65ClN10O6S
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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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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MrTAC-8 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MrTAC-8MrTAC8MrTAC 8LYTACsEpigenetic Reader DomainLysosome-targeting chimerasPRMT1PRMT4PRMT5glioblastomaPRMT7arginine methylationPRMT3cervical cancerlysosomal degradationHeLa cellsInhibitorinhibitorinhibit

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