2. Epigenetics Stem Cell/Wnt Cell Cycle/DNA Damage Apoptosis Autophagy
  3. Epigenetic Reader Domain Casein Kinase Apoptosis Autophagy
  4. BRD4/CK2-IN-1

BRD4/CK2-IN-1 是一种首次高效、口服有效的 BRD4/CK2 (含溴结构域蛋白 4/酪蛋白激酶 2) 双靶点抑制剂。BRD4/CK2-IN-1 对 BRD4 和 CK2 的 IC50 值分别为 180 nM 和 230 nM。BRD4/CK2-IN-1具有很强的抗癌活性，且无明显毒性。BRD4/CK2-IN-1 在三阴性乳腺癌 (TNBC) 中诱导细胞凋亡和自噬相关的细胞死亡。

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BRD4/CK2-IN-1 Chemical Structure

BRD4/CK2-IN-1 Chemical Structure

CAS No. : 2756851-99-5

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2475
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1 mg ￥1022
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5 mg ￥2250
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10 mg ￥3420
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25 mg ￥6750
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Customer Review

BRD4/CK2-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Casein Kinase 亚型特异性产品:

查看所有亚型
CK1 CK2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)[1]

IC50 & Target[1]

BRD4

180 nM (IC50)

CK2

230 nM (IC50)

体外研究
(In Vitro)

BRD4/CK2-IN-1 (compound 44e) (0-25 μM; 24 hours) has anti-proliferation effect with IC50s of 2.66 and 3.52 μM in MDA-MB-231 and MDA-MB-468 cells, respectively[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently induces apoptosis of MDA-MB-231 and MDA-MB-468 cells[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently downregulates Bcl-2 but upregulates Bax and cleaved caspase-3[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) significantly downregulates the autophagy substrate p62 and up-regulated beclin-1 and LC3II in MDA-MB-231 and MDA-MB[1].

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

BRD4/CK2-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468 cells
Concentration: 0, 0.19, 0.39, 0.78, 1.56, 3.13, 6.25, 12.5, 25 μM
Incubation Time: 24 hours
Result: Showed anti-proliferative rates in MDA-MB-231 and MDA-MB-468 cells (IC50 = 2.66 and 3.52 μM, respectively).

Apoptosis Analysis[1]

Cell Line: MDA-MB-231, MDA-MB-468 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Dose-dependently induced apoptosis of MDA-MB-231 and MDA-MB-468 cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, MDA-MB-468 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Dose-dependently downregulated Bcl-2 but upregulated Bax and cleaved caspase-3.

Cell Line:
Concentration:
Incubation Time:
Result:
体内研究
(In Vivo)

BRD4/CK2-IN-1 (25 and 50 mg/kg; intragastric administration; daily for 19 days) inhibits tumor growth in TNBC xenograft models[1].
BRD4/CK2-IN-1 (25 and 50mg/kg; intragastric administration; daily for 19 days) shows weak toxicity measured by body weight loss in the MDA-MB-231 and MDA-MB-468 xenograft models[1].
Preliminary Assessment of Pharmacokinetics (PK) profile of BRD4/CK2-IN-1[1].

Parameter iv (1 mg/kg) po (10 mg/kg)
T1/2 (h) 4.21±0.57 5.14±0.71
Cmax (ng/mL) 237±11 206±6
AUC0-t (ng·h/mL) 579±49 2079±130
AUC0-∞ (ng·h/mL) 588±36 2090±146
VZ (L/kg) 21.1±2.6
CL ((mL/min)/kg) 57.4±1.3
F (%) 32.5

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

Animal Model: Female nude mice (BALB/c, 6-8 weeks, 20-22 g) bearing MDA-MB-231 cells[1]
Dosage: 25 and 50 mg/kg
Administration: Intragastric administration; daily for 19 days
Result: Had the most pronounced tumor growth inhibition (TGI) (63.8%) in the MDA-MB-231 xenograft tumor model at 50 mg/kg.
分子量

564.03

Formula

C29H30ClN5O5
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 20 mg/mL (35.46 mM; 超声助溶 (<60 ℃)；酸性条件溶解 (HCL 调节，pH=3) ; 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 1.7730 mL 8.8648 mL 17.7296 mL
5 mM 0.3546 mL 1.7730 mL 3.5459 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。-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

只
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

BRD4/CK2-IN-1 相关分类

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。-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 1.7730 mL 8.8648 mL 17.7296 mL 44.3239 mL
5 mM 0.3546 mL 1.7730 mL 3.5459 mL 8.8648 mL
10 mM 0.1773 mL 0.8865 mL 1.7730 mL 4.4324 mL
15 mM 0.1182 mL 0.5910 mL 1.1820 mL 2.9549 mL
20 mM 0.0886 mL 0.4432 mL 0.8865 mL 2.2162 mL
25 mM 0.0709 mL 0.3546 mL 0.7092 mL 1.7730 mL
30 mM 0.0591 mL 0.2955 mL 0.5910 mL 1.4775 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.

Keywords:

BRD4/CK2-IN-12756851-99-5Epigenetic Reader DomainCasein KinaseApoptosisAutophagyBRD4CK2anticanceranti-proliferationtumor growthtoxicityTNBCbreastMDA-MB-231MDA-MB-468Inhibitorinhibitorinhibit

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