1. Epigenetics
  2. Epigenetic Reader Domain
  3. TRIM24/BRPF1-IN-2

TRIM24/BRPF1-IN-2 (compound 20l) 是一种有效的 TRIM24/BRPF1 双重抑制剂,IC50 值分别为 0.98 和 1.16 μM。 TRIM24/BRPF1-IN-2 显示出 TRIM24/BRPF1 溴结构域结合亲和力。 TRIM24/BRPF1-IN-2 可用于前列腺癌研究。

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TRIM24/BRPF1-IN-2 Chemical Structure

TRIM24/BRPF1-IN-2 Chemical Structure

CAS No. : 3033288-68-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate cancer research[1].

IC50 & Target

BRPF1

1.16 μM (IC50)

体外研究
(In Vitro)

TRIM24/BRPF1-IN-2 (compound 20l) (0-10 μM, 48 h) 抑制前列腺细胞系 (C4-2B、LNCaP 和 22Rv1) 的生长,IC50 值 分别为 0.78±0.15、1.07±0.47 和 0.82±0.26 μM[1]
TRIM24/BRPF1-IN-2抑制前列腺癌细胞基因和蛋白表达[1]
TRIM24/BRPF1-IN-2 表现出合理的 Caco-2 渗透性[1]

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

RT-PCR[1]

Cell Line: 22Rv1 cell, LNCaP cells
Concentration: 0.4, 2, 5, and 10 μM
Incubation Time: 48 h
Result: Decreased the mRNA expression of full-length AR, AR-V7 and AR-regulated genes PSA, KLK2 and TMPRSS2. inhibited the mRNA level of C-MYC.
体内研究
(In Vivo)

TRIM24/BRPF1-IN-2 (compound 20l) (50 mg/kg,腹腔注射,每日1次,连用21天)可抑制肿瘤生长 (TGI = 53%) 而没有表现出明显的毒性[1]

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

Animal Model: Mice (n = 5-7 per dose group, Four-week-old, male, non-obese diabetic server combined immune-deficiency (NOD SCID), 22Rv1 xenograft model)[1]
Dosage: 50 mg/kg
Administration: IP, once daily for 21 days
Result: Inhibited the progression of the tumors significantly (53% tumor growth inhibition) without body weight loss.
分子量

386.46

Formula

C20H22N2O4S

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:
TRIM24/BRPF1-IN-2
目录号:
HY-143332
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