Pharmacologically Active In Vivo Use of I-BET151

August 10, 2015

Harvard Medical School
Vaccine & Virology Research
Research Fellow

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Company:

Selleck Chemicals

Product Name:

I-BET151

Catalog Number:

S2780

I-BET151, a BET-inhibitor, is being explored in murine models as an HIV-1 latency reversing agent, activating the viral reservoirs in humanised mouse models. Its effect was investigated on alternate viral-vectors, in vivo. Transgene expression from viral vectors was assessed under the influence of BET inhibitors.

Experimental Design and Results Summary

Application

In vivo

Starting Material

I-BET151 powder

Protocol Overview

I-BET151 was solubilised in 30% DMSO, 70% PBS, prior to IP administration in BALB/c mice.

Tips

Mix thoroughly in DMSO prior to adding of PBS to avoid precipitation

Results Summary

I-BET151 significantly increased viral vector transgene expression over vehicle alone. This showed an in vivo pharmocological effect, at these concentrations when administered IP.

Additional Notes

None

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Summary

The Good

Availability, price, speed of delivery - a rare compound

The Bad

Has to be solubilised

The Bottom Line

Good availability for an uncommon epigenetic regulator, which has in vivo effects and is pharmacologically active in mice following IP administration. Would recommend this retailer and this drug for inhibiting BET proteins.

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