1. Epigenetics
  2. Epigenetic Reader Domain
  3. BRD4 Inhibitor-20

BRD4 Inhibitor-20 

目录号: HY-146208 纯度: 99.00%
COA 产品使用指南

BRD4 Inhibitor-20 是一种有效的溴结构域蛋白 4 (BRD4) 抑制剂,具有口服活性。 BRD4 Inhibitor-20 对 BRD4 (BD1) 和BRD4 (BD2) 具有抑制活性,IC50 值分别为 19 nM 和 28 nM。 BRD4 Inhibitor-20 在癌细胞系中也具有抗增殖活性。 BRD4 Inhibitor-20 可用于结肠癌等多种癌症的研究。

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BRD4 Inhibitor-20 Chemical Structure

BRD4 Inhibitor-20 Chemical Structure

CAS No. : 2490311-14-1

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5 mg ¥1900
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10 mg ¥3100
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer[1].

IC50 & Target[1]

BRD4 BD1

19 nM (IC50)

BRD4 BD2

28 nM (IC50)

BRD2 (BD1)

24 nM (IC50)

BRD2 (BD2)

18 nM (IC50)

体外研究
(In Vitro)

BRD4 Inhibitor-20 (compound 12j) exhibits excellent BRD4 inhibitory activities (BD1, IC50=19 nM; BD2, IC50=28 nM) and inhibitory activities against BRD2 (BD1, IC50=24 nM; BD2, IC50=18 nM)[1].
BRD4 Inhibitor-20 (0.5, 2.5, 5.0 μM; 24 h) reduces the expression of c-Myc[1].
BRD4 Inhibitor-20 (72 h) has anti-proliferation potency with IC50 values of 4.75 μM, 1.35 μM and 44.07 μM in HT-29, HL-60 and WI-38 cells, respectively[1].
BRD4 Inhibitor-20 (2.5, 5.0, 10.0 μM; 24 h) can arrest the cell-cycle progression of HT-29 cells into the G1 phase[1].

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

Western Blot Analysis[1]

Cell Line: HT-29 cells
Concentration: 0.5, 2.5, 5.0 μM
Incubation Time: 24 h
Result: Displayed profound inhibitory effects on c-Myc protein expression.

Cell Proliferation Assay[1]

Cell Line: HT-29, HL-60 and WI-38 cells
Concentration:
Incubation Time: 72 h
Result: Possessed strong anti-proliferative activity and weak toxicity.

Cell Cycle Analysis[1]

Cell Line: HT-29 cell lines
Concentration: 2.5, 5.0, 10.0 μM
Incubation Time: 24 h
Result: Arrested the cell-cycle progression of the cell line into the G1 phases and the percentage of cells in G1 phase after treatment under concentrations of 2.5, 5.0 and 10.0 μM were 85.98%, 86.49% and 86.05%, respectively.
体内研究
(In Vivo)

BRD4 Inhibitor-20 (compound 12j) (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie[1].

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

Animal Model: rats[1]
Dosage: 5 mg/kg, 15 mg/kg
Administration: intravenous dosing (iv) or oral dosing (po)
Result:
PK Parameters iv (5 mg/kg) po (15 mg/kg)
Cmax(μg/L) - 2175
Tmax(h) - 1.00
t1/2(h) 1.56 3.59
CLz/F (L/h/kg) 0.68 1.03
AUC0−t(μg/L*h) 7296 14384
AUC0−∞(μg/L*h) 7340 14600
F (%) - 66%
分子量

358.41

Formula

C18H18N2O4S

CAS 号
性状

固体

颜色

Brown to reddish brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (348.76 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7901 mL 13.9505 mL 27.9010 mL
5 mM 0.5580 mL 2.7901 mL 5.5802 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7901 mL 13.9505 mL 27.9010 mL 69.7525 mL
5 mM 0.5580 mL 2.7901 mL 5.5802 mL 13.9505 mL
10 mM 0.2790 mL 1.3951 mL 2.7901 mL 6.9753 mL
15 mM 0.1860 mL 0.9300 mL 1.8601 mL 4.6502 mL
20 mM 0.1395 mL 0.6975 mL 1.3951 mL 3.4876 mL
25 mM 0.1116 mL 0.5580 mL 1.1160 mL 2.7901 mL
30 mM 0.0930 mL 0.4650 mL 0.9300 mL 2.3251 mL
40 mM 0.0698 mL 0.3488 mL 0.6975 mL 1.7438 mL
50 mM 0.0558 mL 0.2790 mL 0.5580 mL 1.3951 mL
60 mM 0.0465 mL 0.2325 mL 0.4650 mL 1.1625 mL
80 mM 0.0349 mL 0.1744 mL 0.3488 mL 0.8719 mL
100 mM 0.0279 mL 0.1395 mL 0.2790 mL 0.6975 mL
Help & FAQs
  • 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:
BRD4 Inhibitor-20
目录号:
HY-146208
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