1. Epigenetics
  2. Epigenetic Reader Domain
  3. PBRM1-BD2-IN-1

PBRM1-BD2-IN-1 是一种选择性和细胞活性的 PBRM1 溴化域抑制剂。PBRM1-BD2-IN-1 对 PBRM1-BD2 具有结合亲和力和抑制活性,KdIC50 值分别为 0.7 μM 和 0.2 μM。PBRM1-BD2-IN-1 可用于癌症的研究。

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PBRM1-BD2-IN-1 Chemical Structure

PBRM1-BD2-IN-1 Chemical Structure

CAS No. : 1915012-21-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer[1].

IC50 & Target

Kd: 0.7 μM (PBRM1-BD2), 0.35 μM (PBRM1-BD5), 8.1 μM (SMARCA2B), 5.0 μM (SMARCA4) [1].
IC50: 0.2 μM (PBRM1-BD2)[1].

体外研究
(In Vitro)

PBRM1-BD2-IN-1 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibit growth of a PBRM1-dependent prostate cancer cell line[1].
PBRM1-BD2-IN-1 has binding affinity for PBRM1-BD2, PBRM1-BD5, SMARCA2B amd SMARCA4 with Kd values of 0.7 μM, 0.35 μM, 8.1 μM and 5.0 μM, respectively[1].
PBRM1-BD2-IN-1 has inhibitory activity for PBRM1-BD2 with IC50 value of 0.2 μM[1].

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

Cell Viability Assay[1]

Cell Line: Human prostate cell lines LNCaP, PC3, and RWPE-1
Concentration: 0, 0.1, 1, and 10 μM
Incubation Time: 5 days
Result: Inhibited LNCaP growth at higher concentrations.
分子量

302.80

Formula

C17H19ClN2O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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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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产品名称:
PBRM1-BD2-IN-1
目录号:
HY-151528
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