LP99

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LP99 是第一个有效且选择性的 BRD7/9 溴结构域抑制剂，对 BRD9 的 Kd 为 99 nM；以剂量依赖性方式抑制 THP-1 细胞分泌 IL-6。

LP99 is the first potent and selective BRD7/9 bromodomain inhibitor with Kd of 99 nM for BRD9; inhibits IL‐6 secretion from THP‐1 cells in a dose‐dependent manner; decreases 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 histones.

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.

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LP 99

Chromatin/Epigenetic

Bromodomain

Bromodomain

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1808951-93-0

516.05

C26H30ClN3O4S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (96.89 mM)

O=C(CC[C@H](NS(CC(C)C)(=O)=O)[C@H]1C2=CC=C(Cl)C=C2)N1C3=CC=C4C(N(C)C(C=C4C)=O)=C3

N-[(2R,3S)-2-(4-chlorophenyl)-1-(1,2-dihydro-1,4-dimethyl-2-oxo-7-quinolinyl)-6-oxo-3-piperidinyl]-2-methyl-1-propanesulfonamide

(-20℃)

With Ice Pack

≥ 2 years