2. PROTAC Epigenetics Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Hsp-targeting Chimeras Epigenetic Reader Domain HSP
  4. 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.

Hsp70TAC BRD4 Degrader-1

Hsp70TAC BRD4 Degrader-1 Chemical Structure

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Hsp70TAC BRD4 Degrader-1 Related Antibodies

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Description

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))[1].

IC50 & Target[1]

Hsp70TACs

 

BRD4

 

HSP70

 

In Vitro

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.

Hsp70TAC BRD4 Degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293T, MEF, MDA-MB-231, U-87 MG, TE-1, MCF-7, U937
Concentration: 1, 5 μM
Incubation Time: 12 h
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.
Molecular Weight

930.62

Formula

C50H56ClN9O3S2
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Hsp70TAC BRD4 Degrader-1 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:

Hsp70TAC BRD4 Degrader-1Hsp-targeting ChimerasEpigenetic Reader DomainHSPHspTACsHeat shock proteinsMycPARPtriple-negative breast cancerHsp70MDA-MB-231 cellsU-87 MG cellsubiquitin-proteasome systemBcl-2glioblastoma multiformeBRD4Inhibitorinhibitorinhibit

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