1. PROTAC Epigenetics Anti-infection
  2. PROTACs Epigenetic Reader Domain HIV
  3. PROTAC BRD4 Degrader-43

PROTAC BRD4 Degrader-43 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-43 recruits the DCAF1-DDB1-Cul4A E3 ligase complex via a Vpr-derived peptide moiety to induce BRD4 ubiquitination and degradation through the ubiquitin-proteasome system. PROTAC BRD4 Degrader-43 exhibits potent HIV latency-reversing activity. PROTAC BRD4 Degrader-43 can be used for the research of HIV-1 latent infection. (Pink: BRD4 ligand (HY-13030); Blue: Cul4A-DDB1-DCAF1 ligand (HY-P11640); Black: conjugate of PEG linker + cell-penetrating peptide (HY-P2483))

For research use only. We do not sell to patients.

PROTAC BRD4 Degrader-43

PROTAC BRD4 Degrader-43 Chemical Structure

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Description

PROTAC BRD4 Degrader-43 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-43 recruits the DCAF1-DDB1-Cul4A E3 ligase complex via a Vpr-derived peptide moiety to induce BRD4 ubiquitination and degradation through the ubiquitin-proteasome system. PROTAC BRD4 Degrader-43 exhibits potent HIV latency-reversing activity. PROTAC BRD4 Degrader-43 can be used for the research of HIV-1 latent infection[1]. (Pink: BRD4 ligand (HY-13030); Blue: Cul4A-DDB1-DCAF1 ligand (HY-P11640); Black: conjugate of PEG linker + cell-penetrating peptide (HY-P2483))

IC50 & Target[1]

BRD4

 

In Vitro

PROTAC BRD4 Degrader-43 (Compound 11) (1-30 μM) degrades BRD4 in MCF-7 cells[1].
PROTAC BRD4 Degrader-43 has low cytotoxicity in MCF-7, J-Lat 10.6, and THP-1 NLuc#225 cells, with CC50 values ≥45 μM[1].
PROTAC BRD4 Degrader-43 (20-50 μM) exhibits potent HIV latency-reversing activity in J-Lat 10.6 and THP-1 NLuc#225 cells, with stronger activity in THP-1 NLuc#225 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

3662.57

Formula

C151H251ClN60O41S2

SMILES

O=C([C@@H](NC(COCCOCCN[C@@H](CCCCNC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](N)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)C(COCCOCCOCCNC(C[C@H]1C2=NN=C(N2C3=C(C(C4=CC=C(C=C4)Cl)=N1)C(C)=C(S3)C)C)=O)=O)=O)CCSC)N[C@H](C(N[C@H](C(N[C@H](C(N5[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N6[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N7[C@H](C(N)=O)CCC7)=O)CCC(O)=O)=O)CCCNC(N)=N)=O)CCC(N)=O)=O)CCC6)=O)=O)CCC(N)=O)=O)CC(O)=O)=O)CCC(O)=O)=O)CCC5)=O)C)=O)CCC(N)=O)=O)CCC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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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.

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Product Name:
PROTAC BRD4 Degrader-43
Cat. No.:
HY-181164
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