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    Epigenetic Reader Domain

A1874 

目录号: HY-114305
产品使用指南

A1874 是一种以nutlin 为基础的、BRD4-降解的 PROTACDC50 值为 32 nM (诱导细胞内的BRD4降解)。有效抑制多种癌细胞增殖。

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A1874 Chemical Structure

A1874 Chemical Structure

CAS No. : 2064292-12-0

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Description

A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation[1].

IC50 & Target[1]

BRD4

 

In Vitro

Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) induces a dose-dependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nmol/L and a maximum degradation (Dmax) of BRD4 of 98% of the levels in control (0.1% DMSO-treated) cells[1].
Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) increases p53 levels in the HCT116 cells and showed dose-dependent p53 stabilization[1].

Western Blot Analysis[1]

Cell Line: HCT116 cells.
Concentration: 0-10 μM.
Incubation Time: 24 hours.
Result: Induced a dosedependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nM.
References
Molecular Weight

1173.59

Formula

C₅₈H₆₂Cl₃F₂N₉O₇S

CAS No.

2064292-12-0

SMILES

ClC(C=C1)=CC=C1C2=N[C@H](C3=NN=C(C)N3C4=C2C(C)=C(C)S4)CC(NCCOCCOCCOCCNC(C5=CC(OC)=C(NC([C@H]6[C@H](C7=C(F)C(Cl)=CC=C7)[C@](C8=CC=C(Cl)C=C8F)(C#N)[C@H](CC(C)(C)C)N6)=O)C=C5)=O)=O

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
A1874
目录号:
HY-114305
需求量:

A1874

Cat. No.: HY-114305