2. Cell Cycle/DNA Damage Stem Cell/Wnt
  3. CDK β-catenin
  4. CDK8-IN-11

CDK8-IN-11 是一种有效的、选择性的 CDK8 抑制剂，IC50 值为 46 nM。CDK8-IN-11 可抑制 WNT/β-catenin 信号通路。CDK8-IN-11 可用于结肠癌的研究。

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CDK8-IN-11 Chemical Structure

CDK8-IN-11 Chemical Structure

CAS No. : 2839338-28-0

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Customer Review

Other Forms of CDK8-IN-11:

CDK8-IN-11 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer[1].

IC50 & Target[1]

CDK8

46 nM (IC50)

体外研究
(In Vitro)

CDK8-IN-11 (compound 29, 200 nM) shows inhibitory effects against CDK8 by 73.6% [1].
CDK8-IN-11 (0-50 μM, 48 h) inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells[1].
CDK8-IN-11 (0-4 μM, 48 h) inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM, 24 h) suppresses canonical WNT/β-catenin signaling pathways and deregulates β-catenin-mediated transcription in HCT-116 cells[1].
CDK8-IN-11 (0.5-2 μM, 48 h) increases the number of cells in the G1 phase in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM) reverses Sorafenib (HY-10201) resistance of HCT-116 cells[1].

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

CDK8-IN-11 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCT-116, HHT-29, SW480, CT-26, GES-1 cells
Concentration: 0.08, 0.4, 2, 10, and 50 μM
Incubation Time: 48 h
Result: Inhibited cell proliferation with IC50 values of 1.2, 0.7, 2.4, 5.5, 62.7 nM respectively.

Western Blot Analysis[1]

Cell Line: HCT-116 cell
Concentration: 0, 1, 2, 4 μM
Incubation Time: 48 h
Result: Inhibited the phosphorylation of STAT1 at Ser727 without affecting the JAK-regulated phosphorylation at Tyr701.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cell
Concentration: 0.5-2 μM
Incubation Time: 48 h
Result: Increased the number of cells in the G1 phase with an obvious decreased percentage of cells in the G2/M and S phase in HCT-116 cells.
体内研究
(In Vivo)

CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice[1].
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days[1].
CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10−6 cm/s[1].

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

Animal Model: CT-26 xenograft mice[1]
Dosage: 10 and 40 mg/kg
Administration: Oral adminstration (p.o.)
Result: Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor.
Animal Model: Rats (pharmacokinetic assay)[1]
Dosage: 10 mg/kg (p.o.), 2 mg/kg (i.v.)
Administration: Oral adminstration (p.o.) or intravenous injection (i.v.)
Result: Pharmacokinetic profile of CDK8-IN-11 (compound 29).
dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) F (%)
10 (p.o.) 1.1 0.8 453 31.7
2 (i.v.) 0.5 318
分子量

388.34

Formula

C19H15F3N4O2
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

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

DMSO 中的溶解度 : 250 mg/mL (643.77 mM; 超声助溶; 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 2.5751 mL 12.8753 mL 25.7506 mL
5 mM 0.5150 mL 2.5751 mL 5.1501 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

CDK8-IN-11 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 2.5751 mL 12.8753 mL 25.7506 mL 64.3766 mL
5 mM 0.5150 mL 2.5751 mL 5.1501 mL 12.8753 mL
10 mM 0.2575 mL 1.2875 mL 2.5751 mL 6.4377 mL
15 mM 0.1717 mL 0.8584 mL 1.7167 mL 4.2918 mL
20 mM 0.1288 mL 0.6438 mL 1.2875 mL 3.2188 mL
25 mM 0.1030 mL 0.5150 mL 1.0300 mL 2.5751 mL
30 mM 0.0858 mL 0.4292 mL 0.8584 mL 2.1459 mL
40 mM 0.0644 mL 0.3219 mL 0.6438 mL 1.6094 mL
50 mM 0.0515 mL 0.2575 mL 0.5150 mL 1.2875 mL
60 mM 0.0429 mL 0.2146 mL 0.4292 mL 1.0729 mL
80 mM 0.0322 mL 0.1609 mL 0.3219 mL 0.8047 mL
100 mM 0.0258 mL 0.1288 mL 0.2575 mL 0.6438 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:

CDK8-IN-112839338-28-0CDKβ-cateninCyclin dependent kinaseBeta cateninInhibitorinhibitorinhibit

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目录号：
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