1. Apoptosis Cell Cycle/DNA Damage
  2. Apoptosis CDK
  3. CDK8-IN-13

CDK8-IN-13 is a potent, selective and orally active CDK8 inhibitor with an IC50 value of 51.9 nM. CDK8-IN-13 induces Apoptosis. CDK8-IN-13 decreases the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 shows antitumor activity.

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CDK8-IN-13 Chemical Structure

CDK8-IN-13 Chemical Structure

CAS No. : 918523-75-8

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK8-IN-13 is a potent, selective and orally active CDK8 inhibitor with an IC50 value of 51.9 nM. CDK8-IN-13 induces Apoptosis. CDK8-IN-13 decreases the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 shows antitumor activity[1].

IC50 & Target[1]

CDK8

51.9 nM (IC50)

体外研究
(In Vitro)

CDK8-IN-13 (compound 43; 1, 2.5, 5, 10 µM; 12 h) 以剂量依赖性方式降低 HCT-116 细胞中 p-STAT1 S727 和 p-STAT5 S726 的表达[1] .
CDK8-IN-13 (0, 1, 5, 10 µM; 48 h) 以剂量依赖的方式诱导细胞凋亡
[1]

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

Cell Proliferation Assay[1]

Cell Line: molm-13, HL-60, MV4-11, MGC-803, MDA-MB-231, A375, A549 cells
Concentration: 0-50 µM
Incubation Time:
Result: Showed antiproliferative activity with GC50s of 1.57, 1.00, 4.61, >50, >50, >50, >50 µM, respectively.

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 1, 2.5, 5, 10 µM
Incubation Time: 12 h
Result: Decreased the expression of p-STAT1 S727 and p-STAT5 S726, and suppressed the phosphorylation of STAT1 S727 induced by IFN-γ (10 ng/mL) in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: HL-60 cells
Concentration: 0, 1, 5, 10 µM
Incubation Time: 48 h
Result: Induced approximately 7% and 36% apoptotic at concentrations of 5 and 10 μM, respectively.
体内研究
(In Vivo)

CDK8-IN-13 (40、80 mg/kg;口服;持续 15 天) 在小鼠体内以剂量依赖性方式抑制肿瘤生长[1]

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

Animal Model: 6-week-old Balb/C mice (C1498 cells)[1]
Dosage: 40, 80 mg/kg
Administration: P.o.; for 15 days
Result: Decreased the tumor growth with no significant weight loss, the expression of Ki67 decreased in a dose-dependent manner, the level of phosphorylation of STAT1 S727 in tumor tissues was downregulated.
分子量

237.26

Formula

C14H11N3O

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 : 125 mg/mL (526.85 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 4.2148 mL 21.0739 mL 42.1479 mL
5 mM 0.8430 mL 4.2148 mL 8.4296 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

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-13 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 4.2148 mL 21.0739 mL 42.1479 mL 105.3696 mL
5 mM 0.8430 mL 4.2148 mL 8.4296 mL 21.0739 mL
10 mM 0.4215 mL 2.1074 mL 4.2148 mL 10.5370 mL
15 mM 0.2810 mL 1.4049 mL 2.8099 mL 7.0246 mL
20 mM 0.2107 mL 1.0537 mL 2.1074 mL 5.2685 mL
25 mM 0.1686 mL 0.8430 mL 1.6859 mL 4.2148 mL
30 mM 0.1405 mL 0.7025 mL 1.4049 mL 3.5123 mL
40 mM 0.1054 mL 0.5268 mL 1.0537 mL 2.6342 mL
50 mM 0.0843 mL 0.4215 mL 0.8430 mL 2.1074 mL
60 mM 0.0702 mL 0.3512 mL 0.7025 mL 1.7562 mL
80 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3171 mL
100 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0537 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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