1. Anti-infection
    Epigenetics
  2. HIV
    Epigenetic Reader Domain
  3. ZL0580

ZL0580 

Cat. No.: HY-126428
Handling Instructions

ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter.

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ZL0580 Chemical Structure

ZL0580 Chemical Structure

CAS No. : 2377151-10-3

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Description

ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter[1][2][3].

IC50 & Target

BRD4 (BD1)

 

In Vitro

ZL0580 (8 μM, 2 days, PBMCs of viremic HIV-infected individuals) induces HIV transcriptional suppression with low toxicity[1].
ZL0580 treatment (10 μM) suppresses both PMA-stimulated and basal HIV transcription[1].

Cell Viability Assay[1]

Cell Line: HIV-infected human CD4+ T cells.
Concentration: 0-8 μM.
Incubation Time: 2 days.
Result: Suppress HIV in primary CD4+ T cell.
Single treatment (8 μM) led to almost completed loss of productive HIV infection in CD4+ T cells.

RT-PCR[1]

Cell Line: PBMCs of viremic HIV-infected individuals.
Concentration: 8 μM.
Incubation Time: 2 days.
Result: Suppresses HIV transcription ex vivo in PBMCs of viremic HIV-infected individuals.

Cell Cytotoxicity Assay[1]

Cell Line: J-Lat cells.
Concentration: 0-80 μM.
Incubation Time: 1 and 3 days.
Result: Did not cause significant cell death at concentrations below 40 μM.
Treatment of J-Lat cells with ZL0580 (10 μM) also did not cause significant cell death on days 2, 7, and 14 compared with NC in both PMA-activated and unstimulated cells.
Molecular Weight

532.53

Formula

C₂₅H₂₃F₃N₄O₄S

CAS No.

2377151-10-3

SMILES

O=C(NC1=CC=C(S(N2CCC[[email protected]]2C(NC3=CC=CC=C3)=O)(=O)=O)C=C1)NC4=CC=C(C(F)(F)F)C=C4

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Storage

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

References
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Keywords:

ZL0580ZL 0580ZL-0580HIVEpigenetic Reader DomainHuman immunodeficiency viruslowtoxicityPBMCInhibitorinhibitorinhibit

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ZL0580
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HY-126428
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