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  2. Drug Derivative HIV Epigenetic Reader Domain
  3. XQ2

XQ2 is a resveratrol (HY-16561) derivative and latency-reversing agent. XQ2 releases positive transcription elongation factor b (P-TEFb) from BRD4, thereby promoting Tat-dependent viral transcription. XQ2 reactivates latent HIV-1 via activating P-TEFb.

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XQ2

XQ2 Chemical Structure

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Description

XQ2 is a resveratrol (HY-16561) derivative and latency-reversing agent. XQ2 releases positive transcription elongation factor b (P-TEFb) from BRD4, thereby promoting Tat-dependent viral transcription. XQ2 reactivates latent HIV-1 via activating P-TEFb[1].

IC50 & Target[1]

HIV-1

 

BRD4

 

In Vitro

XQ2 (10-80 μM; 24-72 h) dose- and time-dependently reactivates latent HIV-1 in J-Lat 10.6 cells[1].
XQ2 (10-80 μM; 24-72 h) dose-dependently and time-dependently activates latent HIV-1 in J-Lat A2 cells[1].
XQ2 (40 μM; 48 h) downregulates the cell surface expression levels of HIV-1 receptor CD4 and coreceptors CXCR4 and CCR5 in human peripheral blood mononuclear cells (PBMCs)[1].

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

ELISA Assay[1]

Cell Line: ACH2 cells
Concentration: 10-100 μM (48 h dose-response); 40 μM (24-72 h time-response)
Incubation Time: 48 h (10-100 μM dose-response); 24, 48, 72 h (40 μM time-response)
Result: Dose-dependently increased supernatant p24 levels at 10, 20, 40, 60, 100 μM for 48 h, with highly significant increases at all tested concentrations compared to resveratrol.
Time-dependently increased supernatant p24 levels at 40 μM for 24, 48, 72 h, with a dramatic increase observed at 72 h compared to resveratrol.

Real Time qPCR[1]

Cell Line: ACH2 cells
Concentration: 5-40 μM (48 h dose-response); 40 μM (24-72 h time-response)
Incubation Time: 48 h (5-40 μM dose-response); 24, 48, 72 h (40 μM time-response)
Result: Dose-dependently increased mRNA expression of HIV-1 genes LTR, Vpr, Vif, Tat, and Gag at 5, 10, 20, 40 μM for 48 h, with significant increases at all tested concentrations compared to the blank control.
Time-dependently increased mRNA expression of all tested HIV-1 genes at 40 μM for 24, 48, 72 h, with significant increases observed at 24, 48, 72 h compared to the 0 h control.

Western Blot Analysis[1]

Cell Line: ACH2 cells
Concentration: 5-100 μM
Incubation Time: 48 h
Result: Weakly increased acetyl-H3K9 and acetyl-H3K14 levels at 5-100 μM for 48 h.
Reduced p-HSF1 (Ser320) levels in a dose-dependent manner at 5-100 μM for 48 h.
Molecular Weight

330.34

Formula

C17H18N2O5

SMILES

O=C1NC(C2=CC=C(COCC)O2)=NC3=C1C(OC)=CC(OC)=C3

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
References
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  • 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:
XQ2
Cat. No.:
HY-181831
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