1. Epigenetics
  2. Epigenetic Reader Domain
  3. LP99

LP99 

Cat. No.: HY-19553
Handling Instructions

LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells.

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

LP99 Chemical Structure

LP99 Chemical Structure

CAS No. : 1808951-93-0

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Description

LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells[1].

IC50 & Target

Kd: 99 nM (BRD9)[1]

In Vitro

LP99 disrupts BRD9 interactions with chromatin at a concentration of 0.8 μM. BRD7- and BRD9-NanoLuc luciferase fusion proteins and fluorescently labelled histone H3.3- and H4-HaloTag fusions were expressed in HEK293 cells. The addition of LP99 decreased BRET for both BRD7 and BRD9 in both the H3.3 and H4 systems in a dose-dependent manner, with cellular IC50 values in the low micromolar range for both histone. Cytotoxicity tests in U2OS cells for 24 and 72 hours shows the inhibitor to be non-toxic at concentrations of <33 μM. LP99 inhibits IL-6 secretion from THP-1 cells in a dose-dependent manner[1].

Molecular Weight

516.05

Formula

C₂₆H₃₀ClN₃O₄S

CAS No.

1808951-93-0

SMILES

O=C1N(C2=CC(N(C)C(C=C3C)=O)=C3C=C2)[[email protected]](C4=CC=C(Cl)C=C4)[[email protected]@H](NS(CC(C)C)(=O)=O)CC1

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Storage

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

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Keywords:

LP99LP 99LP-99Epigenetic Reader Domainbromodomainepigeneticsorganocatalysisselectiveprobehistonespro-inflammatorycytokinesecretionInhibitorinhibitorinhibit

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