Hsp70TAC BRD4 Degrader-1
Hsp70TAC BRD4 Degrader-1 is a degrader targeting BRD4, with a KD value of 0.22 μM. Hsp70TAC BRD4 Degrader-1 forms a ternary complex with Hsp70 (KD: 5.13 μM), and specifically and efficiently degrades intracellular BRD4 via the ubiquitin-proteasome pathway. Hsp70TAC BRD4 Degrader-1 exhibits potent anti-tumor proliferative activity. Hsp70TAC BRD4 Degrader-1 can be used in studies related to triple-negative breast cancer and glioblastoma multiforme. (Pink: BRD4 ligand (HY-78695); Blue: HSP70 ligand (HY-182979); Black: linker (HY-B0236)).
For research use only. We do not sell to patients.
- Formula: C50H56ClN9O3S2
- Molecular Weight:930.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
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All Hsp-targeting Chimeras Isoforms
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Biological Activity
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Hsp70TACs |
BRD4 |
HSP70 |
Hsp70TAC BRD4 Degrader-1 (compound SB-2) (0.01-10 μM; 8-24 h) induces proteasomal degradation of BRD4 in U-87 MG and MDA-MB-231 cells in a time-dependent, dose-dependent and Hsp70-dependent manner, with DC50 values of 0.55 μM and 0.67 μM in the two cell lines, respectively[1].
Hsp70TAC BRD4 Degrader-1 (0.1-12 μM; 48 h) inhibits the proliferation of U-87 MG cells, with an IC50 value of 0.32 μM[1].
Hsp70TAC BRD4 Degrader-1 (1-5 μM; 12 h) selectively degrades BRD4 in tumor cells with high Hsp70 expression, but exerts no such effect in cells with low Hsp70 expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T, MEF, MDA-MB-231, U-87 MG, TE-1, MCF-7, U937
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Concentration:1, 5 μM
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Incubation Time:12 h
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Result:Induced efficient BRD4 degradation in Hsp70-high expression tumor cells (MDA-MB-231, MCF-7, U-87 MG, U937), but caused negligible degradation in Hsp70-low expression cells (HEK293T, MEF, TE-1).
Showed degradation efficiency correlated with cellular Hsp70 expression levels.
Chemical Information
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Molecular Weight 930.62
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Formula C50H56ClN9O3S2
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SMILES
O=C1C(C#N)=C(C2=CC=C(C3=CC=CC1=C32)SC4CCCCC4)NCCN(C)CCNC(CCCCCNC(C[C@H]5C6=NN=C(N6C7=C(C(C8=CC=C(C=C8)Cl)=N5)C(C)=C(C)S7)C)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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